Lec 4- Semisolid Dosage Forms
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Questions and Answers

What is a key characteristic of semisolid dosage forms at room temperature?

  • Maintains a rigid shape
  • Conforms to the shape of its container (correct)
  • Easily shatters upon impact
  • Becomes a liquid

What is the primary purpose of topical dosage forms?

  • Delivering drugs into the bloodstream
  • Treating skin disorders by delivering drugs into the skin (correct)
  • Providing systemic effects through the skin
  • Bypassing the skin to reach deeper tissues

Which of the following is NOT a typical function of topical dosage forms?

  • Protecting injured skin
  • Delivering medication for a specific effect
  • Providing skin hydration
  • Inducing a systemic effect (correct)

What type of dosage form delivers drugs through the skin for systemic effects?

<p>Ointment (B)</p> Signup and view all the answers

Which of the following is an example of a semisolid dosage form?

<p>Solution (C)</p> Signup and view all the answers

The volume of drug that penetrates the skin from a semisolid is NOT determined by

<p>The surface area covered (C)</p> Signup and view all the answers

What effect does increased skin hydration typically have on percutaneous absorption?

<p>Prevents absorption (C)</p> Signup and view all the answers

What is the effect of vasodilation on drug absorption?

<p>Has no effect on drug absorption (B)</p> Signup and view all the answers

When selecting a base for a semisolid, what is a key consideration?

<p>The cost of the base (B)</p> Signup and view all the answers

Which property is characteristic of oleaginous bases?

<p>Occlusive (B)</p> Signup and view all the answers

What is a disadvantage of using oleaginous bases?

<p>Poor water absorption (C)</p> Signup and view all the answers

Anhydrous absorption bases can form what type of emulsion when water is added?

<p>Oil-in-oil (B)</p> Signup and view all the answers

What is an advantage of using water-removable bases?

<p>Highly protective (C)</p> Signup and view all the answers

What is a potential disadvantage of water-soluble bases?

<p>They are difficult to remove. (C)</p> Signup and view all the answers

According to the content, what should be the focus during the pre-formulation stage of compounding?

<p>Solubility and stability (B)</p> Signup and view all the answers

What is the role of excipients in a dosage form?

<p>They determine the dosage amount. (C)</p> Signup and view all the answers

Which of these is a commonly compounded semisolid?

<p>Capsules (C)</p> Signup and view all the answers

What is the purpose of stiffening agents in semisolids?

<p>To enhance viscosity (B)</p> Signup and view all the answers

When is a preservative typically needed in a semisolid formulation?

<p>Always (C)</p> Signup and view all the answers

What is the primary use of ointments?

<p>External application to the skin (B)</p> Signup and view all the answers

Ointments are best suited for which type of skin lesions?

<p>Dry, scaly (C)</p> Signup and view all the answers

What is the purpose of levigating a solid material when preparing an ointment?

<p>To add color (B)</p> Signup and view all the answers

In the fusion method of ointment preparation, when are materials with the lowest melting points typically added?

<p>After the mixture is congealed (B)</p> Signup and view all the answers

Creams are best applied to what type of lesions?

<p>Hardened (B)</p> Signup and view all the answers

What characterizes gels as a semisolid system?

<p>Dispersions of small or large molecules in an aqueous liquid (B)</p> Signup and view all the answers

What determines the preparation technique for gels?

<p>Color of the gel (B)</p> Signup and view all the answers

What happens to suppositories after insertion into body orifices?

<p>They melt, soften, or dissolve (B)</p> Signup and view all the answers

What is a local effect that suppositories can provide?

<p>Relieving constipation (B)</p> Signup and view all the answers

What is a key advantage of using suppositories?

<p>Administering smaller doses of drugs (A)</p> Signup and view all the answers

What is a desirable property of suppository bases?

<p>Remaining solid at room temperature (D)</p> Signup and view all the answers

Which of the following describes cocoa butter when used as a suppository base?

<p>Brittle solid (B)</p> Signup and view all the answers

Why are commercial suppository products sometimes preferred over cocoa butter?

<p>Difficult to work with (C)</p> Signup and view all the answers

What happens to glycerinated gelatin suppositories?

<p>Must be stored at high temperature. (B)</p> Signup and view all the answers

What is an important consideration for glycerinated gelatin suppositories?

<p>Protect from moisture (B)</p> Signup and view all the answers

When preparing suppositories by hand molding, which base is generally used?

<p>Cocoa butter (B)</p> Signup and view all the answers

What should you ensure when preparing a mold for suppositories?

<p>Make sure the mold is warmed up (B)</p> Signup and view all the answers

How is the active drug prepared before incorporating it into a suppository base?

<p>Evaporated to dryness (D)</p> Signup and view all the answers

What is the final step in suppository preparation?

<p>Re-melting the mixture (B)</p> Signup and view all the answers

Cold compression molding is suitable for which type of suppository bases?

<p>Formed with water (B)</p> Signup and view all the answers

What are troches intended to do?

<p>Injected (B)</p> Signup and view all the answers

What is a potential disadvantage of troches?

<p>Mistaken for candy (D)</p> Signup and view all the answers

What is a key characteristic of hard troches?

<p>Soft surface texture (D)</p> Signup and view all the answers

What are chewable troches formulated with?

<p>Sugar (C)</p> Signup and view all the answers

What is the term for bases that contain an emulsifier and form water-in-oil emulsions when water is added?

<p>Water-removable bases (B)</p> Signup and view all the answers

Which type of base is known for being non-greasy and easily removable from the skin by washing?

<p>Water-removable bases (C)</p> Signup and view all the answers

Which ingredient is used to keep ingredients from sticking to each other during the compounding process?

<p>Antioxidant (C)</p> Signup and view all the answers

Which of the following ointment bases is best suited for incorporating aqueous solutions?

<p>Anhydrous absorption bases (B)</p> Signup and view all the answers

What is a key characteristic of oleaginous ointment bases?

<p>They are non-irritating and water-soluble. (B)</p> Signup and view all the answers

What is the definition of a semisolid dosage form?

<p>A solid that maintains its shape under pressure. (C)</p> Signup and view all the answers

What is the purpose of transdermal dosage forms?

<p>To provide a local anesthetic effect. (B)</p> Signup and view all the answers

Which factor affects the volume of drug that penetrates the skin from a semisolid?

<p>The color of the semisolid. (B)</p> Signup and view all the answers

What effect does increased skin hydration have on percutaneous absorption?

<p>Causes irritation (C)</p> Signup and view all the answers

What is a key advantage of oleaginous bases?

<p>They are non-greasy. (B)</p> Signup and view all the answers

What type of emulsion do anhydrous absorption bases form when water is added?

<p>Water-in-oil emulsions (B)</p> Signup and view all the answers

What characterizes water-removable bases?

<p>Anhydrous (C)</p> Signup and view all the answers

What is a disadvantage of water-soluble bases?

<p>They cannot absorb water. (C)</p> Signup and view all the answers

What is the focus during the pre-formulation stage of compounding?

<p>Drug marketing strategies (B)</p> Signup and view all the answers

What is the primary role of excipients in a dosage form?

<p>To cause adverse effects (B)</p> Signup and view all the answers

What is the purpose of using stiffening agents in semisolids?

<p>To prevent microbial growth (C)</p> Signup and view all the answers

When is a preservative needed in a semisolid formulation?

<p>Only in anhydrous formulations (C)</p> Signup and view all the answers

Ointments are generally used for which type of skin lesions?

<p>All types of lesions (B)</p> Signup and view all the answers

When are materials with the lowest melting points typically added in the fusion method of ointment preparation?

<p>At the beginning (B)</p> Signup and view all the answers

Creams are best suited for which type of lesions?

<p>Moist, weeping lesions (B)</p> Signup and view all the answers

After insertion, what do suppositories do?

<p>Vaporize (B)</p> Signup and view all the answers

What effects can suppositories provide?

<p>No therapeutic effects (C)</p> Signup and view all the answers

What is an advantage of using suppositories over oral medications?

<p>They always have a faster onset of action. (B)</p> Signup and view all the answers

When preparing suppositories through hand molding, which base is generally used?

<p>Cocoa butter (B)</p> Signup and view all the answers

What is the first priority when preparing a mold for suppositories?

<p>Lubricating it with a similar base type as the suppository (B)</p> Signup and view all the answers

How is the active drug generally prepared before incorporating it into a suppository base?

<p>By mixing it with a preservative (B)</p> Signup and view all the answers

Chewable troches are formulated with what?

<p>Mineral oil (B)</p> Signup and view all the answers

What substance is added to semi-solids to reduce the evaporation rate of water?

<p>Absorption Enhancers (A)</p> Signup and view all the answers

What is the MOST important consideration when choosing a base?

<p>Occlusion ability (B)</p> Signup and view all the answers

Which base is used to incorporate an aqueous solution?

<p>Absorption (D)</p> Signup and view all the answers

A high HLB surfactant, Glycerin, and Propylene Glycol would classify the Levigating Agent as?

<p>Water-Soluble (C)</p> Signup and view all the answers

When making an ointment, which do you do first?

<p>Weigh Ingredients (B)</p> Signup and view all the answers

To prepare hard troches, which of the following is the MOST typical method?

<p>Fusion (C)</p> Signup and view all the answers

What would you commonly combine a Troche with to flavor it?

<p>Sugar (A)</p> Signup and view all the answers

What is the correct temperature to prepare a hard troche?

<p>154 - 160 Degrees (C)</p> Signup and view all the answers

You are preparing an oleaginous ointment. Which of the following actions is MOST important?

<p>Using geometric dilution (C)</p> Signup and view all the answers

What crucial factor determines the technique used in gel preparation?

<p>The color of the gelling agent (B)</p> Signup and view all the answers

What is the main purpose of incorporating stiffening agents into semisolid formulations?

<p>To decrease viscosity (B)</p> Signup and view all the answers

When preparing ointments using the fusion method, in what order should the materials be added?

<p>Highest melting points first (B)</p> Signup and view all the answers

What is the typical base used in hand-molded suppositories?

<p>Cocoa butter (B)</p> Signup and view all the answers

What is the purpose of using a humectant in semisolid dosage forms?

<p>To increase viscosity (B)</p> Signup and view all the answers

What is the primary function of a semisolid dosage form?

<p>To bypass the digestive system for drugs that are easily degraded. (C)</p> Signup and view all the answers

How does increasing the duration of contact between a medicated semisolid and the skin generally affect drug absorption?

<p>It decreases drug absorption due to the skin's natural barrier function. (B)</p> Signup and view all the answers

What is a key limitation of oleaginous bases that affects patient compliance?

<p>They are prone to microbial contamination. (C)</p> Signup and view all the answers

What is the role of an emulsifier in anhydrous absorption bases?

<p>To facilitate the formation of a water-in-oil emulsion when water is added. (C)</p> Signup and view all the answers

What is a significant disadvantage associated with water-removable bases regarding chemical stability?

<p>They tend to cause skin irritation due to their high water content. (C)</p> Signup and view all the answers

Why is solubility and stability a key focus during the pre-formulation stage of compounding?

<p>To optimize the drug's effectiveness and shelf life in the compounded formulation. (C)</p> Signup and view all the answers

Which of the following statements BEST describes the function of excipients in pharmaceutical dosage forms?

<p>Excipients provide the therapeutic effect of the dosage form. (C)</p> Signup and view all the answers

What is the purpose of incorporating stiffening agents into semisolid formulations like ointments and creams?

<p>To enhance the solubility of the active pharmaceutical ingredient (API). (C)</p> Signup and view all the answers

Why is the presence of water in a semisolid formulation a key consideration when determining the need for a preservative?

<p>Water acts as a natural preservative, preventing microbial growth. (C)</p> Signup and view all the answers

Why is it important for an ointment to spread easily and not be gritty?

<p>To enhance absorption of the active ingredient. (C)</p> Signup and view all the answers

In the preparation of ointments using the incorporation method, what is the purpose of levigating a solid material?

<p>To dissolve the solid material completely. (C)</p> Signup and view all the answers

During the fusion method of ointment preparation, what is the rationale behind adding materials with the lowest melting points last?

<p>To reduce the overall cooling time of the ointment. (B)</p> Signup and view all the answers

What is a critical consideration when using creams for burn treatment, particularly in terms of application?

<p>Creams should be warmed before application to improve absorption. (C)</p> Signup and view all the answers

What role do gelling agents play in the formation of gels?

<p>They provide a jelly-like consistency to an aqueous liquid vehicle. (C)</p> Signup and view all the answers

What is the primary reason for using suppositories as a drug delivery system when compared to oral medications?

<p>To provide a more cost-effective method of drug administration. (C)</p> Signup and view all the answers

What is a crucial factor in the selection of a suppository base related to its physical properties?

<p>It should remain solid at room temperature but soften, melt, or dissolve readily at body temperature. (C)</p> Signup and view all the answers

What potential issue is of MOST concern when cocoa butter is overheated during the preparation of suppositories?

<p>It may become more viscous and difficult to mold. (C)</p> Signup and view all the answers

What is the primary reason commercial suppository products may be preferred over those compounded with cocoa butter?

<p>Commercial products are less expensive to manufacture. (C)</p> Signup and view all the answers

Why must glycerinated gelatin suppositories be protected from atmospheric moisture?

<p>To prevent the growth of microorganisms within the suppository. (D)</p> Signup and view all the answers

When preparing suppositories by hand molding, what characteristic of cocoa butter makes it a suitable base?

<p>Its high melting point allows for rapid solidification. (B)</p> Signup and view all the answers

Before pouring a melted suppository base into a mold, why is lubrication of the mold generally recommended?

<p>To improve the drug's distribution throughout the suppository. (B)</p> Signup and view all the answers

What is the preferred method of preparing the active drug during suppository compounding to ensure maximal efficacy?

<p>Adding the drug directly to the base without any pre-treatment. (B)</p> Signup and view all the answers

In the preparation of suppositories, after mixing and pouring, what is the final step before packaging and labeling?

<p>Allowing the suppositories to set and then removing any excess material. (B)</p> Signup and view all the answers

For which type of suppository bases is the cold compression molding method MOST appropriate?

<p>Bases containing volatile active ingredients. (B)</p> Signup and view all the answers

What is the MOST significant advantage of troches over traditional tablets or capsules for local oral conditions?

<p>Troches are less expensive to manufacture. (B)</p> Signup and view all the answers

What is a primary safety concern associated with troches, especially in households with children?

<p>They can be easily mistaken for candy, leading to accidental ingestion. (B)</p> Signup and view all the answers

What is a distinguishing characteristic of hard troches (lozenges) compared to other types of troches?

<p>They are designed to be chewed for rapid drug release. (C)</p> Signup and view all the answers

What type of base is typically used in the formulation of chewable troches, enhancing their palatability?

<p>A gelatin base. (C)</p> Signup and view all the answers

According to the information provided, what is the BUD (Beyond-Use Date) for water containing preparations?

<p>90 days (B)</p> Signup and view all the answers

If the API is heat sensitive when using the fusion method to create a cream, when should it be added to the water and oil mixture?

<p>When the mixture is close to congealing (A)</p> Signup and view all the answers

What substance should be used when levigating the solid material of an ointment with the base in which water is the external phase?

<p>Propylene Glycol (D)</p> Signup and view all the answers

What is a key determinant of the technique used when preparing Gels?

<p>The characteristics of the selected Gelling Agent (B)</p> Signup and view all the answers

What is a key factor for ensuring the desired properties of suppositories made with cocoa butter?

<p>Using high shear mixing to ensure proper drug distribution. (B)</p> Signup and view all the answers

What is the reason for making a slight excess of material when creating a Glycerinated Gelatin suppository?

<p>To ensure that there is extra raw material in case there are spillers. (B)</p> Signup and view all the answers

A pharmacist needs to compound a topical ointment for a drug that is prone to hydrolysis. Considering the stability of the drug, which base type would be MOST appropriate for this formulation?

<p>Absorption base (Anhydrous absorption base) (C)</p> Signup and view all the answers

In preparing an ointment using the fusion method, a pharmacist is formulating an ointment with beeswax (melting point: 62-64°C), white petrolatum (melting point: 38-56°C), and a heat-labile active ingredient. In which order should these components be combined and heated?

<p>Heat beeswax to 70°C until melted, add white petrolatum, cool to just above congealing point, and then incorporate the active ingredient. (C)</p> Signup and view all the answers

A patient requires a topical medication for a weeping skin lesion. Considering the properties of different semisolid dosage forms, which of the following would be the MOST suitable choice for application to this type of lesion?

<p>Oleaginous ointment due to its occlusive and emollient properties. (B)</p> Signup and view all the answers

When formulating suppositories using cocoa butter as the base, what is the MOST critical consideration regarding its polymorphic nature?

<p>Avoiding overheating to prevent the formation of unstable polymorphs with lower melting points. (B)</p> Signup and view all the answers

A pharmacist is compounding troches for oral administration. For a medication intended to provide a localized effect in the mouth and mask an unpleasant taste, which type of troche would be MOST appropriate?

<p>Glycerinated gelatin troches, offering a water-soluble base for quick release. (C)</p> Signup and view all the answers

A patient is prescribed a topical medication. They are instructed to apply a 2-inch strip of ointment. Given that 1 gram of this ointment is approximately equivalent to a 1-inch strip, what quantity of ointment, in grams, should the patient apply per dose?

<p>1 gram (C)</p> Signup and view all the answers

When selecting a base for a topical semisolid formulation, which factor is MOST critical to consider to ensure optimal drug delivery and therapeutic effect?

<p>The cost-effectiveness of the base for economic manufacturing (C)</p> Signup and view all the answers

An oleaginous base is chosen for a topical ointment formulation. What inherent characteristic of oleaginous bases presents the GREATEST challenge to patient compliance?

<p>Their potential to cause skin irritation due to occlusive properties (B)</p> Signup and view all the answers

For a drug that is susceptible to hydrolysis, which type of semisolid base would be LEAST suitable due to its composition and potential to exacerbate degradation?

<p>Oleaginous base (C)</p> Signup and view all the answers

When compounding a topical ointment using an anhydrous absorption base like Aquaphor to incorporate a small volume of an aqueous solution, what is the rationale behind using this type of base?

<p>To enhance the cooling effect of the ointment on the skin. (C)</p> Signup and view all the answers

A pharmacist is formulating a hydrophilic ointment, categorized as a water-removable base. What is the primary characteristic of this base that distinguishes it from oleaginous bases in terms of patient experience?

<p>Greasy and emollient nature, providing prolonged skin hydration (C)</p> Signup and view all the answers

Water-soluble bases, such as PEG ointments, offer the advantage of being easily washable and leaving no residue. However, what is a key limitation associated with their use, particularly concerning skin compatibility?

<p>They cannot incorporate solid substances effectively, limiting drug delivery. (B)</p> Signup and view all the answers

During the pre-formulation stage of compounding a semisolid dosage form, the pharmacist's primary focus is on solubility and stability. Why are these two factors considered paramount at this stage?

<p>To determine the most cost-effective manufacturing process. (C)</p> Signup and view all the answers

Excipients are integral components of semisolid dosage forms. Which of the following BEST describes their primary role in these formulations?

<p>To act as the primary therapeutic agent in treating the disease. (C)</p> Signup and view all the answers

Stiffening agents, such as waxes, are often incorporated into oleaginous bases in semisolid formulations. What is the MAIN purpose of these agents?

<p>To increase the viscosity and consistency of the ointment, making it more solid. (C)</p> Signup and view all the answers

When is the inclusion of a preservative MOST critical in a semisolid formulation, particularly concerning product safety and efficacy?

<p>Only in anhydrous formulations to prevent oxidation of oils and fats. (C)</p> Signup and view all the answers

Ointments are generally preferred for application to dry, scaly lesions. What property of ointments makes them particularly suitable for this skin condition?

<p>Their ability to be easily washed off, preventing buildup on scaly skin. (C)</p> Signup and view all the answers

In the incorporation method of ointment preparation, levigation is a crucial step, especially when dealing with solid materials. What is the primary purpose of levigating a solid material before incorporating it into an ointment base?

<p>To increase the drug's penetration through the skin by enhancing its solubility. (B)</p> Signup and view all the answers

During the fusion method of ointment preparation, materials are added in a specific order based on their melting points. Why are materials with the lowest melting points typically added last, during the cooling phase?

<p>To prevent degradation of heat-sensitive materials by minimizing their exposure to high temperatures. (B)</p> Signup and view all the answers

Creams are often preferred over ointments for application to moist, weeping lesions. What characteristic of creams makes them more suitable for this type of skin condition?

<p>Their enhanced ability to deliver drugs systemically through the skin. (C)</p> Signup and view all the answers

Gels are characterized as semisolid systems where the movement of the dispersing medium is restricted by a network of cross-linked particles or dissolved macromolecules. What is the primary component responsible for this gel structure?

<p>Humectants that reduce water evaporation. (B)</p> Signup and view all the answers

The preparation technique for gels is primarily determined by the characteristics of which component?

<p>The packaging material to ensure product stability. (C)</p> Signup and view all the answers

Suppositories, upon insertion into body orifices, are designed to act in various ways to release medication. What is the MOST common mechanism by which suppositories facilitate drug release?

<p>The pressure exerted by the body forces the drug out of the suppository. (B)</p> Signup and view all the answers

Suppositories can provide both local and systemic effects. Which of the following is an example of a LOCAL effect that a suppository is typically designed to achieve?

<p>Relieving nausea and vomiting. (C)</p> Signup and view all the answers

What is a key advantage of using suppositories as a drug delivery system compared to oral medications, particularly for patients experiencing certain conditions?

<p>Suppositories can be used in patients experiencing nausea, vomiting, or difficulty swallowing. (C)</p> Signup and view all the answers

A desirable property of a suppository base is to remain solid at room temperature but soften, melt, or dissolve at body temperature. Why is this property crucial for effective drug delivery and patient comfort?

<p>To ensure the suppository is easy to handle and insert, and releases the drug at the intended site. (A)</p> Signup and view all the answers

Cocoa butter is a commonly used oleaginous suppository base. Which of the following BEST describes cocoa butter's behavior when used as a suppository base concerning its melting properties?

<p>It melts at a very high temperature, ensuring slow drug release. (C)</p> Signup and view all the answers

Commercial suppository products are sometimes favored over those compounded with cocoa butter, particularly for large-scale manufacturing. What is the primary reason for this preference?

<p>Cocoa butter is prone to oxidation and requires special handling. (C)</p> Signup and view all the answers

Glycerinated gelatin suppositories are water-soluble bases that dissolve rather than melt. What is a critical consideration regarding the storage and handling of glycerinated gelatin suppositories due to their hygroscopic nature?

<p>They should be packaged in airtight containers to allow for proper hydration before use. (B)</p> Signup and view all the answers

When preparing suppositories by hand molding, cocoa butter is generally the base of choice. What property of cocoa butter makes it particularly suitable for hand molding?

<p>Its water solubility ensures easy cleanup and removal from molds. (B)</p> Signup and view all the answers

When preparing a mold for suppository fusion molding, lubrication is often necessary. What is the MOST important principle to follow when selecting a lubricant for suppository molds?

<p>Select a lubricant with solubility characteristics opposite to that of the suppository base. (C)</p> Signup and view all the answers

What is the preferred method of preparing the active drug before incorporating it into a suppository base to ensure optimal drug dispersion and efficacy?

<p>Agglomerating the drug particles to improve flow properties during molding. (B)</p> Signup and view all the answers

In the final steps of suppository preparation using fusion molding, after mixing and pouring the molten base and drug into molds, what is the immediate next step before packaging and labeling?

<p>Applying a protective coating to the suppositories before demolding. (B)</p> Signup and view all the answers

Cold compression molding is a method used for suppository preparation. For which type of suppository bases is this method MOST suitable, considering the physical properties required for this technique?

<p>Bases that melt readily at room temperature. (C)</p> Signup and view all the answers

Troches, or lozenges, are designed for slow dissolution in the oral cavity. What is the MOST significant advantage of this dosage form over traditional tablets or capsules for treating local oral conditions?

<p>Troches provide immediate systemic drug absorption for rapid relief. (B)</p> Signup and view all the answers

While troches are advantageous for local oral therapy, what is a primary safety concern associated with them, especially in households with young children?

<p>The risk of rapid systemic absorption leading to overdose. (B)</p> Signup and view all the answers

Hard troches, also known as lozenges, are distinct from other types of troches in their formulation and characteristics. What is a key distinguishing characteristic of hard troches compared to soft or chewable troches?

<p>They have a smooth, hard texture and are intended to dissolve slowly. (C)</p> Signup and view all the answers

Chewable troches are formulated to enhance palatability and ease of administration, particularly for pediatric patients. What type of base is typically used in chewable troches to achieve this desired texture and taste?

<p>A base of hard sugar and corn syrup, similar to hard candies. (C)</p> Signup and view all the answers

According to general pharmaceutical compounding guidelines, what is the typical BUD (Beyond-Use Date) assigned to water-containing preparations, such as certain creams and lotions, compounded for topical use?

<p>No more than 1 year (B)</p> Signup and view all the answers

When using the fusion method to create a cream, and the API is known to be heat sensitive, at what point in the process should the API be incorporated into the water and oil mixture to minimize degradation?

<p>API should be added to the water phase before heating, to protect it from direct heat. (C)</p> Signup and view all the answers

When levigating a solid material for incorporation into an ointment, the choice of levigating agent is crucial. If you are preparing an ointment with a base in which water is the external phase (e.g., a water-removable cream base), which substance would be MOST appropriate as a levigating agent?

<p>Glycerin (B)</p> Signup and view all the answers

The technique used in gel preparation is heavily reliant on the characteristics of the gelling agent. Which property of the gelling agent is the MOST significant determinant of the preparation technique?

<p>The hydration and swelling properties of the gelling agent in the chosen solvent. (C)</p> Signup and view all the answers

Ensuring the desired properties of suppositories made with cocoa butter requires careful control of temperature during preparation. What is the key factor related to temperature control that is MOST critical for maintaining the quality and efficacy of cocoa butter suppositories?

<p>Rapidly cooling the molten cocoa butter to induce immediate solidification. (B)</p> Signup and view all the answers

When preparing Glycerinated Gelatin suppositories, it is advised to make a slight excess of material. What is the primary reason for this practice?

<p>To account for potential volume contraction upon cooling and solidification. (A)</p> Signup and view all the answers

When formulating suppositories using cocoa butter as the base, what is the MOST critical consideration regarding its polymorphic nature to ensure product stability and efficacy?

<p>Ensuring the cocoa butter is heated to the highest possible temperature to destroy all polymorphs. (B)</p> Signup and view all the answers

A pharmacist is developing a topical formulation with an API that exhibits poor penetration through the stratum corneum. Which approach would be MOST effective to enhance drug permeation?

<p>Using an oleaginous base to create a thick, occlusive layer on the skin. (B)</p> Signup and view all the answers

A pharmacist is compounding a cream containing an API prone to oxidation. To mitigate degradation, which strategy is MOST appropriate?

<p>Incorporating an antioxidant excipient in the formulation. (B)</p> Signup and view all the answers

During the preparation of hard troches, a pharmacist notices the sugar solution is darkening rapidly and emitting a burnt odor. What is the MOST likely cause, and what corrective action should be taken?

<p>The temperature is too high; reduce heat and closely monitor the solution. (C)</p> Signup and view all the answers

A pharmacist is preparing suppositories using glycerinated gelatin as the base. Which technique is MOST crucial to ensure the quality and stability of the final product?

<p>Heating the base to a high temperature to ensure complete sterilization. (C)</p> Signup and view all the answers

A community pharmacist is asked to compound a topical ointment containing a potent corticosteroid for a patient with eczema. The pharmacist must select an appropriate base to ensure optimal drug delivery and minimize potential side effects. Considering the need for both skin hydration and enhanced drug penetration, which base would be the MOST appropriate?

<p>An oleaginous base such as white petrolatum. (C)</p> Signup and view all the answers

Flashcards

Semisolid Dosage Form

A material that conforms to its container at room temperature and easily distorted when force is applied.

Topical Dosage Forms

Dosage that delivers the drug into the skin to treat skin disorders.

Transdermal

Dosage that delivers drugs through the skin to reach the general circulation for systemic effects.

Drug Penetration Factors

Amount of drug penetrating the skin from a semisolid depends on pressure, vigor, area, and skin condition.

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Base Selection Criteria

Choosing the base depends on systemic/topical needs, drug stability, release rate, application site characteristics, and occlusion needs.

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Oleaginous Base

Inert vehicle for ointment

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Oleaginous Base Features

Advantage: Inexpensive, non-irritating, occlusive and protective. Disadvantage: greasy, not easily washable, and limited water absorption

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Water-removable base (oil-in-water)

Inert vehicle for cream

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Anhydrous Absorption Bases

Hydrocarbon bases that contain an emulsifier to form water-in-oil emulsions when water/aqueos solution is added.

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Water-Removable Features

Advantage: Non-greasy, washable, absorbs water/alcohol. Disadvantage: less protective, microbial growth

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Water-Soluble Base Traits

Advantages: Leaves no oil residue, easily removed by washing. Disadvantages: Irritating, PEG compatibility issues.

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Levigating Agent

Substance used to reduce the particle size of solids.

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Stiffening agents role

Increase viscosity

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If the product contains water...

Preservatives are normally required

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Ointment

Medicated or unmedicated semisolid for external application that softens/melts at body temperature and is used on dry, scaly legions.

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Incoporating solids into ointments method

Reduce particle size, levigate, then spatulate in geometric proportions

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Incorporating Liquids in Ointments

Dissolve the solid in a compatible solvent and then incorporate into base, considering the base's capacity.

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Ointment Fusion Method

Combine components by melting together and cooling with constant stirring

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Cream

Semisolid with medicinal agents dispersed in W/O or O/W emulsion

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Cream Incorporation Steps

Triturate drug in a mortar into a fine powder; levigate drug into base with spatula

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Cream Fusion Method

Melt oil and water soluble components separately, mix phases, then add API when cooled

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Gel

Semisolid of dispersed molecules in an aqueous liquid rendered jellylike by a gelling agent

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Gel Gelling Agents

Synthetic macromolecules like carbomers or cellulose derivatives

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Suppository

Solid dosage for insertion into body orifices that melt, soften, or dissolve to exert local or systemic effects.

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Suppository Advantages

Alternative admin route, avoid first-pass, target local or systemic

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Ideal Suppository Base

Solid at room temp, stable, compatible, non-irritating, and absorbs water

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Oleaginous Suppository Bases

Cocoa butter and hydrogenated vegetable oils

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Cocoa Butter Traits

Advantage: Non-irritating, emollient, readily available. Disadvantage: Low melting point, polymorphic forms

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Water-Soluble Suppository Bases

Glycerinated gelatin and polyethylene glycol (PEG)

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Hand Molding

Manually shaping cocoa butter with active ingredient

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Suppository Fusion Molding

Melt base, add drug, pour into molds, cool, trim, and weigh.

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Cold Compression Molding

Grate base, mix with drug, and compress into molds

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Preparing Suppository Mold

Clean, dry, and lubricated with opposite solubility to the base

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Preparing Active Drug

Triturate drug to uniform size, mix into base or levigate with agent matched to base type.

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Troche/Lozenge

Solid dosage dissolved slowly in the oral cavity local/systemic effect

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Troche Advantages

Easy admin, prolonged contact. Disadvantage: Mistaken for candy

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Troche Types

Hard troches - lozenges, drops. Soft troches - pastilles. Chewable troches - gummies

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Hard Troche Preparation

Sugar, corn syrup, water, plus drug, boiled carefully to avoid burning.

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Soft Troche Preparation

Mix drug, sugar, wax, PEG; heat in a water bath, stir, and pour into lubricated molds.

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Chewable Troche

Drug, gelatin, glycerin, and water with commercial Jello.

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Adsorbents

Keep powders dry

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Antioxidant Role

Prevents oxidation with ascorbic or sodium ascorbate

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Binder agents function

Adhesive, includes acacia and sucrose

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Coatings Role

Prevents degradation, masks taste, and may use Shellac or gelatin.

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Diluents (filler)

Used to add bulk, starch, calcium salts, lactose and others

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Topical dosage

Delivers drug into the skin, treating skin disorders.

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Skin Penetration Factors

Volume of drug penetrating the skin from a semisolid, affected by many factors.

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Semisolid Base Selection considerations

A base may be selected based on several considerations.

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Water-removable base

Inert vehicle for a cream.

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What is the role of stiffening agents?

Increase product thickness/viscosity.

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Role of Preservatives

Needed to prevent microbial growth since water promotes bacterial growth.

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Ointments Incorporation Method

Reduce particle size, levigate, then spatulate in geometric proportions.

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Ointment Preparation

Combine components by melting together and cooling with constant stirring

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Cream Preparation

Triturate drug, levigate drug into base with spatula

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Fusion Method

Melt oil and water soluble components separately, mix phases, then add API when cooled

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Gel Base Ingredients

Synthetic macromolecules like carbomers, cellulose derivatives

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Suppositories Advantages

Alternative admin route and avoid first-pass effect

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Ideal Suppository

Solid at room temp, non-irritating and compatible

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Cocoa Butter

Non-irritating and emollient

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Hand Molding Prep

Manually shaping cocoa butter with active ingredient

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Fusion Molding

Melt base, cool, trim and weigh

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Cold Compression

grate the base then compress into mold

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Prepping a Suppository Mold

clean and dry. Lubricate to allow the product to come out easily

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Prepare suppository for action

Triturate active ingredient.

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Troches

Solid dosage dissolved slowly in oral for local/systemic effects

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Hard Roche

Sugar must be boiled

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Soft Troche

Mix drug heat and pour into a lubricate mold

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Antioxidants

Prevents oxidation. Ascorbic or sodium ascorbate

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Binders

Adhesives that include sucrose a gum or gelatin

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Coatings Purpose

Prevents degradation

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Filler

Lactose

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Topical Dosage Forms Objectives

Delivers the drug into the skin to treat skin disorders by protecting, hydrating and providing a specific effect.

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Semisolid Drug Penetration

Determined by pressure applied, vigor of rubbing, surface area covered, and skin condition.

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Prescriber's Role in Base Selection

May specify the base, but if not, selection must consider the drug's intended effect.

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Occlusive Properties

A base that promotes moisture retention, and enhances drug penetration.

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Yellow Petrolatum

Yellow petrolatum with impurities, offering emollient and protective properties.

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Aquaphor Absorption Capacity

Aquaphor absorbs this amount of water relative to its volume.

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Lotion Formation

If diluted enough, this dosage form can be formed from water-removable bases.

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Water-Soluble Base Use

Help incorporate solid substances into water-soluble bases.

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Drug Particle Size for Semisolids

Drugs contained should be triturated to a fine powder.

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Ointments: Key Properties

Emollient, rehydrates dry skin

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Solvent's Capacity Consideration

Considered when incorporating liquids into ointments to prevent instability or separation.

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Lowest Melt Points

Materials with these characteristics are added last during fusion preparation.

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Burn Cream Application

Creams for burns do not require this when applied.

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Heat Sensitivity

If the API is heat sensitive or volatile, add the active ingredient at this time.

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Gels: Ideal Drug

Dosage form used especially for poor oral bioavailability and administered for local or systemic effects.

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Suppository Definition

A semi-solid, jelly-like emulsion typically used for rectal, vaginal, or urethral application.

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Polymorphic Forms

Cocoa butter solidifies, resulting in this crystalline structure.

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Water-soluble Base Storage

Requires protection from atmospheric moisture.

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Hand-Molding Active Mix

Mix active ingredients in this ingredient thoroughly for uniform distribution.

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Wetting Agent Choices

Use products with this property as wetting agents.

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Troches Description

Dosage form intended to be dissolved slowly in the oral cavity

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Troches Formula

Formulation may contain drug, sugar, syrup, water.

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Adsorbents Role

They keep powders dry

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Diluents

Adding bulk such as starch while compounding.

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The amount of pressure applied

Vigor with which the semisolid is rubbed +The surface area covered

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Oleaginous bases (Hydrocarbon bases) Advantages

Inexpensive, non-irritating + Good emollient and protective and occlusive properties+Not water-washable

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Oleaginous bases Disadvantages

Poor patient acceptance b/c of greasy nature+Not easily removed with washing +Cannot absorb water and can absorb only limited amounts of alcoholic solutions

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Anhydrous absorption bases Advantages

Moderately good protective, occlusive, and emollient properties+ Do not wash off easily + Can absorb liquid

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Anhydrous absorption bases Disadvantages

Poor pt acceptance b/c of greasy nature+Some lanolin types have a somewhat sticky nature and unpleasant smell+Not easily removed with washing+Bases containing wool wax may be sensitizing

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Water-removable bases Advantages

Can be used to absorb water or alcohol+Can be removed from skin by washing+Non-greasy

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Water-soluble bases Advantages

Mostly used for the incorporation of solid substances+Can absorb some water and alcohol+Soluble in water, easily removed by washing+Leaves no oil residue

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Water-soluble bases Disadvantages

Irritating+ Compatibility problems with PEG type bases+Subject to microbial growth+Little to no emollient properties

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Semisolids, volume of drug that penetrates the skin is determined by

The amount of pressure applied and the vigor with which the semisolid is rubbed

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Design formulation fundamentals

Stability + Compliance+ Bioavailability+ Marketing

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Excipients role

Excipients may support the absorption or stability of the active drug, may accomplish dosage form objectives, or may be needed for manufacturing

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Stiffening agents

Waxes that have high melting points+Blend into oleaginous bases to enhance viscosity

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Ointment Qualities

May be medicated or not+Soften or melt at body temperature+Semisolid preparation intended for external application to the skin or mucous membranes

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Incorporation of liquids

Solids soluble in a common solvent that will not affect the stability of the drug or efficacy of the product may first be dissolved in that solvent and the solution added to the ointment base

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Qualities for creams

Creams are relatively soft and easy to spread and remove+Semisolid preparations containing one or more medicinal agents dissolved or dispersed in either a W/O emulsion or an O/W emulsion

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Gelling Agents

Synthetic macromolecules like carbomers, Cellulose derivatives like methylcellulose, natural gums like tragacanth

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Semisolid Volume Penetration

Volume of drug that penetrates the skin is determined by the amount of pressure applied and the vigor with which the semisolid is rubbed.

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Application Area Size

The larger the area of application, the larger the quantity of drug absorbed.

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Skin Hydration Effect

Hydration generally favors percutaneous absorption.

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Dosage Form Application

Absorption increases when the dosage form is applied to a site with a thin layer.

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Heat and Absorption.

Vasodilation leads to more absorption.

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Base Selection

Consider topical or systemic needs, drug stability, desired release rate, application surface, and occlusion needs.

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White Petrolatum

White petrolatum with impurities removed.

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White Ointment

White petrolatum with beeswax added.

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Aquaphor Absorption

It absorbs an equal volume of water (1:1 ratio).

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Water-Removable Dilution

If this is diluted enough, it can become a lotion.

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Cream Base Example

Hydrophilic ointment is an example.

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Water-Soluble Base

Used for the incorporation of solid substances.

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Humectants

Helps maintain product consistency and prevent water loss.

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Absorption Enhancers Role

Facilitates drug transport through skin.

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Ointment Application

External application to skin.

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Emollient Properties

Emollient properties aid in rehydration of the skin.

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Levigating Oil

Mineral oil for bases in which oils are the external phase.

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Levigating Glycerin

Glycerin for bases in which water is the external phase

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Geometric Proportions

Ensures everything is evenly distributed.

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Lowest Melting Points

Materials with this melting points or that are liquids are added last

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Burn Cream Gentle Touch

Do NOT scrub off creams, no additional trauma to the skin

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Gel Opportunity

Drugs with poor oral bioavailability.

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Local Action

Base melts, softens, or dissolves, distributing its medications to the tissues of the region.

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Suppository Benefits

Alternative route of administration plus no GI issues.

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Suppository base

Cocoa butter solidified quickly. Hand molding

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Wetting Property

A wetting agent should have the same property as base to maximize effects

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Coloring Agents

Give color to the compounded product.

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Study Notes

Semisolid Dosage Forms

  • Material that conforms to its container at room temperature.
  • It easily distorts when force is applied, assuming a new shape after the force is removed.
  • Topical dosage forms deliver drugs into the skin for treating skin disorders.
    • They protect injured areas from the environment and permit the skin to heal.
    • They provide the skin with hydration or produce an emollient effect.
    • They convey a medication to the skin for a specific effect.
  • Transdermal forms deliver drugs through the skin into the general circulation for systemic effects.
  • Types of Semisolid Dosage Forms include:
    • Ointments
    • Creams
    • Gels
    • Lotions
    • Pastes
    • Plasters
    • Sticks
    • Glycerogelatins

Factors Affecting Drug Penetration

  • Volume of drug that penetrates the skin via semisolids is determined by:
    • The amount of pressure applied and the vigor with which the semisolid is rubbed.
    • The surface area covered, where a larger area of application leads to a greater quantity of drug absorbed.
    • Skin condition, where hydration generally favors percutaneous absorption, and greater absorption occurs with thin layers.
    • The base that is used
    • Occlusive dressings
  • Generally, longer contact between the medicated application and the skin increases total drug absorption.
  • Heat-induced vasodilation enhances the absorption of drugs.

Nitro-Bid Ointment

  • 1 gram is equivalent to approximately 1 inch when squeezed from the tube.
  • It is essential to be cautious with the dose due to the product’s potency.

Selection of a Base

  • Things to consider:
    • Topical or systemic application preference
    • Drug stability
    • Desired release rate
    • Surface characteristics where it will be applied
    • Need for occlusion or ease of removal
  • Prescribers may specify the base.

Oleaginous Bases (Hydrocarbon Bases)

  • Also known as ointment bases
  • Advantages:
    • Inexpensive and non-irritating.
    • Good emollient and protective with occlusive properties to smooth and soften the skin.
    • Not water-washable
  • Disadvantages:
    • Poor patient acceptance because of its greasy nature
    • Not easily removed with washing, possibly requiring a detergent.
    • Cannot absorb water and absorbs only limited quantities of alcoholic solutions.
  • Types:
    • Yellow petrolatum contains impurities (e.g., Vaseline).
    • White petrolatum has had the impurities removed.
    • White ointment contains white petrolatum with beeswax added.

Absorption Bases

  • Anhydrous Absorption Bases: hydrocarbon bases containing an emulsifier that forms water-in-oil emulsions when water or aqueous solution is added.
    • Aquaphor absorbs an equal volume of water i.e. a 1:1 ratio
  • Water-in-Oil Emulsions: absorption bases containing water, with the amount depending on the base.
  • Advantages:
    • Moderately good protective occlusive, and emollient properties.
    • Aqueous solutions can incorporate into an oleaginous base.
    • Does not wash off easily because the external phase is oleaginous.
    • Capable of absorbing liquids.
  • Disadvantages:
    • Greasy nature causing poor patient acceptance.
    • Sticky nature and unpleasant smell in some lanolin types.
    • Not easily removed with washing.
    • Bases containing wool wax may be sensitizing.
    • Potential chemical stability problems with ingredients sensitive to hydrolysis, and subject to microbial growth.
  • Water in preparation has a BUD of 14 days

Water-Removable Bases

  • Also known as Oil-in-water emulsions.
  • Advantages:
    • Non-greasy and washable from skin.
    • Capable of absorbing some water or alcohol, and enables dissipation of fluids from injured skin.
  • Disadvantages:
    • Less protective and occlusive
    • Less emollient
    • Chemical stability problems with hydrolysis-sensitive ingredients.
    • Subject to Microbial growth
    • Possible evaporation of water which may cause a "dry out" effect.
  • Hydrophilic ointment is a cream base.
  • Vanishing cream is an example.

Water-Soluble Bases

  • Advantages:
    • Leaves no oil residue, is soluble in water making them easily removed by washing.
    • Can absorb some water and alcohol and is used in the incorporation of solid substances.
  • Disadvantages:
    • Irritating, and they have little to no emollient properties.
    • Compatibility and chemical stability problems with PEG type bases.
    • Subject to microbial growth

Properties Comparison of Semisolid Bases

  • Oleaginous Base (Hydrocarbons):
    • Hydrophobic compounds
    • Anhydrous
    • Low affinity for water
    • Difficult to spread
    • Not washable
    • Greasy, solids, or oils
    • Mineral oil levigating agent
    • Occlusive
    • Examples include white petrolatum, white ointment, and yellow petrolatum
  • Absorption Base (Hydrocarbon base + wlo surfactant):
    • Hydrophobic compounds
    • W/O surfactants
    • Anhydrous
    • Low affinity for water
    • Difficult to spread
    • Not washable
    • Greasy, solids, oils, small amounts of aqueous solutions
    • Mineral oil
    • Low HLB surfactant
    • Occlusive
    • Examples include Aquabase, Aquaphor, and hydrophilic petrolatum
  • W/O Base (Hydrocarbon base + <45% w/w water+ who surfactant with HLB < 8):
    • Hydrophobic compounds
    • W/O surfactants and water
    • Moderate affinity for water
    • Moderate to spread
    • Moderate greasiness
    • Moderate occlusiveness
    • Examples include eucerin, hydrocream, and Nivea
  • Oil/water Base (Water-removable base):
    • Hydrophobic compounds + water + o/w surfactant
    • Hydrous water content.
    • High affinity for water
    • Easy spreadability
    • Washable
    • Not greasy
    • Solids and aqueous solutions
    • Glycerin with a high HLB surfactant
    • Non-occlusive
    • E.g., Hydrophilic ointment, Vanishing cream, Dermabase
  • Water-Soluble Base:
    • Polyethylene Glycols (PEG)
    • Hydrous
    • High affinity for water
    • Easy spreadability - Washable
    • Non-greasy
    • Solids and aqueous solutions Drug Incorporation
    • Glycerin
    • Propylene glycol Levigating Agent
    • Non-occlusive - PEG ointment, Polybase Examples
  • Hydrophilic Base (Gels):
    • Methylcellulose or carbomer dispersion
    • Water content > 95%
    • High affinity for water
    • Easy spreadability
    • Washable
    • Not greasy.
    • Solids and aqueous solutions
    • Glycerin with a high HLB surfactant
    • Non-occlusive
    • Examples include Methylcellulose and Carbomer gels.

Compounding Approach

  • Focuses on pre-formulation, which examines drug properties.
  • Solubility and stability are key when regarding drug properties.
  • Check reference books for formulations with stability
  • Commercial products can be used as reference.
  • Design formulation fundamentals with bioavailability, stability, compliance, and marketing.

Dosage Form Fundamentals

  • Active Pharmaceutical Ingredient (API) is the active drug and the reason to take the dosage form.
  • Excipients support absorption, stability, or other dosage form objectives and can be needed for manufacturing.
  • Packaging protects the integrity of the dosage form from stability issues or adverse effects.
  • Administration devices are the materials and equipment needed for drug administration.

Semisolid Compounding Considerations

  • Commonly compounded include:
    • Ointments
    • Creams
    • Lotions
    • Gels
  • Selection of base, excipients, calculations, and chosen technique.

Semisolid Excipients

  • Stiffening agents include waxes with high melting points that blend into oleaginous bases to enhance viscosity.
    • Incorporation into dosage forms usually involves heat use.
    • Chapstick and medicated sticks are stiffening agents.
  • Emulsifying agents
  • Humectants will decrease the evaporation rate of water from the preparation.
  • Preservatives are normally needed is the product contains water.
  • Absorption (penetration) enhancers can facilitate drug absorption through the skin.
  • Not required to be sterile except for ophthalmic preps

Ointments

  • Semisolid preparations are intended for external application to the skin or mucous membranes.
  • May be medicated or not.
  • Should soften or melt at body temperature and spread easily, avoiding a gritty texture.
  • Generally used on dry, scaly lesions where emollient properties aid in rehydration of the skin.
  • Prepared through incorporation and fusion methods.

Ointment Preparation: Incorporation of Solids

  • Reduce the particle size of a crystalline material.
  • Levigate the solid material using mineral oil for bases that have oils as the external base, or glycerin if water is present within.
  • After levigation, incorporate the dispersion to the ointment base by spatulation in geometric proportions.

Ointment Preparation: Incorporation of Liquids

  • Solids soluble in a common solvent
  • Do not affect the drug's stability or efficacy, and the solvent solution should be added to the ointment base
  • Consider the ointment base's capacity to accept the volume required
  • Only incorporate small amount in oleaginous ointment.
  • Hydrophilic bases need to readily accept aqueous solutions.
  • All bases have their limits to retain liquids.
  • Adding an aqueous preparation to a hydrophobic base.
    • First incorporate solution into a minimal amount of hydrophilic base, then mix with the hydrophobic base

Ointment Preparation: Fusion Method

  • Melts some or all components of the ointment together and cools with constant stirring until congealed.
  • Can be done in a glass beaker or porcelain evaporating dish.
  • Materials with the highest melting points are heated to the required temperature of the melt.
  • Materials with lower melting points are added during the cooling of the melt.
  • Materials with the lowest melting point or liquid are added last.

Creams

  • Semisolid preparations containing one or more medicinal agents dissolved or dispersed in either W/O emulsion or an OlW emulsion.
  • Relatively soft and easy to spread and remove.
  • Opaque, soft solids, or thick liquids for external application, and generally applied to moist, weeping lesions. Creams for burns do not have to be scrubbed off, so no additional trauma to the skin.

Cream Preparation

  • Incorporate into an existing cream or base
  • Triturate drug in a mortar and pestle into a fine powder.
  • Remove the drug from the mortar and pestle with a rubber spatula.
  • On an ointment slab: levigate the drug into the base in geometric proportions using a metal spatula.
  • Fusion Method Separation:
    • Separate the formula components into two portions - oil soluble and water soluble.
  • Heat both phases to a temperature that is above the highest melting component
  • Mix phases by adding the aqueous phase to the oil phase.
  • An API that is not heat-sensitive or volatile and is soluble can be added either at the beginning or last, when the mixture is almost congealed, or by levigating on an ointment slab.

Gels

  • Semisolid systems of small or large molecules dispersed in an water liquid vehicle by adding a gelling agent.
    • Androgel has poor oral bioavailability, but can be a gel.
  • Gelling agents: synthetic macromolecules (carbomers), cellulose derivatives (methylcellulose), natural gums (tragacanth)
  • Types:
    • Single phase gels: Uniform distribution of liquid and gelling agent.
    • Two phase gels: Floccules of small distinct particles.
      • Example: milk of magnesia.
  • Preparation characteristics:
    • Gelling agent determines preparation
    • Dispersing API in continuous phase.

Suppositories

  • Solid dosage form where APIs are dispersed in a suitable base and molded or otherwise formed into a shape which is inserted into body orifices such as rectal, vaginal, or urethral where it melts, softens, or dissolves.
  • Local Action:
    • The base melts, softens, or dissolves to distribute medications to the tissues of the targeted region.
    • Intended for retention within the cavity for local effects such as constipation relief, pain/irritation/inflammation relief, contraception, anti-infectives, and local anesthetic.
  • Systemic Action
    • Mucous membranes permit drug absorption which helps nausea and vomiting, and analgesics.

Suppositories: Advantages

  • Alternative route of administration when the oral route is inadvisable.
  • Useful for drugs that may irritate oral, GI mucosa, or have unpleasant taste/smell.
  • Patient unconscious.
  • Avoids nausea and vomiting.
  • Avoids the first-pass effect and breakdown of certain drugs susceptible to gastric degradation.
  • Delivers higher doses than using the oral administration.
  • Less expensive than parenteral.

Suppository Bases: Desirable Properties

  • Remains solid at room temperature and softens, melts, or dissolves readily at body temperature.
  • Chemically and physically stable under normal conditions of use and storage.
  • Non-reactive and compatible with a wide variety of drugs and auxiliary agents.
  • Non-irritating
  • Mixes with or absorbs some water

Suppository Bases: Categories:

  • Oleaginous
  • Water-soluble
  • Oleaginous (Fatty) Base - Most frequently used:
    • cocoa butter is a yellowish solid with a mild order
    • Non-irritating
    • Excellent emollient
    • Used for hand-molding
    • Readily available.
  • Low melting point - so store at controlled room temperature or refrigerate.
    • Exists in many polymorphic forms.
    • Easily/quickly overheats, then solidifies at a lower melting point of polymorph.
  • Hydrogenated vegetable oils (palm, palm kernel, coconut oils)
    • easier to work with than cocoa butter because they do not exist in polymorphic forms -Fattibase -Witepsol -Fattyblend
  • Water-soluble: -Glycerinated Gelatin: soft, rubbery consistency and dissolves.
  • slower to soften and mix with physiologic fluids. -tendency to absorb moisture so it needs to be protected from atmospheric moisture.
  • Polyethylene Glycol (PEG):
    • composed of blends of various molecular weight PEG polymers
    • PEG 300, 400, 600, 1000, 1500, 1540, 3350, 4000, 6000, 8000
    • does not melt at body temperature but rather dissolves in the body's fluids which allows for slower release of medication from the base Convenient storage Convenient use Incompatible with many drugs (prone to oxidation) Can be irritating to body cavity tissues

Suppository Preparation

  • Hand molding generally uses cocoa butter
    • Grate cocoa butter and add the active ingredient.
    • Mix the ingredients thoroughly.
    • Press the mixture together until it re-solidifies and shape the mixture into a long cylinder.
    • Cut into the desired lengths, round the tips and then package, and label.
  • Fusion molding requires you to calibrate the mold.
    • Obtain and melt sufficient suppository base to fill 6 to 12 molds.
    • Pour the base into the molds, cool, and trim.
    • Remove the suppositories and weigh and divide the total weight by the number of suppositories prepared to obtain the average weight of each suppository for this particular base.
  • Preparing the mold:
    • Ensure the mold is clean and dry.
    • Lubricate in terms of solubility: water soluble bases require mineral oil and oil-soluble bases need glycerin or propylene glycol lubricant.
    • Add minimal lubricant so it doesn't pool and produce misshapen suppositories.
  • Preparing the base:
    • At lowest possible heat, melt the base in a porcelain dish over water bath.

Suppository Preparation: Preparing the Active Drug:

Triturate drug to a uniform, small particle size.

  • Either mixed directly into the base or wetted before incorporation as preference
    • Levigate with a wetting agent for both Oil and water-soluble bases.
  • Mixing, Pouring, Finishing Ensure ingredients are mixed uniformly when added and use a stirring rod to mix the drug to the base.
  • Pour into the mold and ensure glycerinated gelatin will set quickly or else it will pour quickly. Slight excess of material build-up may be allowed. Allow the suppositories to set; any material can be removed Remove suppositories from the mold, package, and label.
  • Cold Compression Molding
    • For bases that can be formed in the suppositories
    • Weight and the density factor of each mold is needed.
    • Amount is need to fill
    • Base is grated, drug, cold mold prepared.

Troches

  • Various-shaped solid dosage forms usually containing a medicinal agent & flavoring substance.
  • Intended to be dissolved slowly in the oral cavity for localized or systemic effect.
  • Advantages:
    • Easy to administer
    • Extends the time a drug remains in the oral cavity
  • Disadvantage:
    • Can be mistaken for candy
  • Hard troches:
    • lozenges and drops in mixture of sugar
    • Smooth surface texture or pleasant flavor
    • High temperature required for preparation
  • Soft troches:
    • pastilles in mixture various PEGs, acacia or other
      • Either be slow or be chewed
  • Chewable troches:
    • formulation gelatin
    • High flavored

Troches Preperation

  • Hard troches:
    • formulation may contain drug, sugar, corn syrup, and water
    • drug is dissolved
    • Amorphous mass transfered and a mold filled
  • Soft troches:
    • formulation may contain drug, sugar, wax, and PEGs
    • binders / gummies and flavoring/ coloring agents
  • Chewable Troches
    • formulation may contain drug, sugar, corn syrup, and water
    • Other ingredients may inlcude gums, binders, flavoring and coloring

Dosage Form Fundamentals, Excipients

  • Adsorbents: keep powders dry
    • Examples: Magnesium oxide/carbonate
  • Antioxidants: Prevents oxidation
    • Examples: Ascorbic acid, sodium ascorbate
  • Binders: Adhesive properties which is intended to hold
    • Example: Acacia and syrup
  • Color agents: Color the compounded product
    • Examples: FD&C Red and Yellow
  • Diluents: Add size to very small dosage
    • Starch, Calcium, Lactose
  • Lubricants: prevents or assists in sticking to the equipment
    • PEG and minerals.
  • Preservative: prevent growth and other pathogens
    • sodium benzoate, benzoc acid, benzalkonium chloride, cetypyridium.
  • Disintegrant: Causes tablet to swell and burst.
    • Alginic acid, polacrilin potassium
    • cellulose products
    • starches
  • Enteric coating: Protective layer and prevention of dissolution in the stomach.
    • Shellac
  • Flavoring agent, sweetener: -Masks bitter flavors, gives sweetness to a preparation.
    • Syrups and lactos
  • Humectant: -Prevents preparations from becoming brittle -Glycerin, Sorbitol

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Description

Semisolid dosage forms are topical treatments that can deliver drugs to the skin, protecting injured areas and helping them heal. Drugs can be delivered into the skin to treat skin disorders or through the skin for systemic effects. Types of Semisolid Dosage Forms include ointments, creams, gels, lotions, and pastes.

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