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Questions and Answers
What is a key advantage of the rectal administration of drugs?
What is a key advantage of the rectal administration of drugs?
What factors make rectal administration preferable over oral administration?
What factors make rectal administration preferable over oral administration?
What is a primary characteristic of suppositories?
What is a primary characteristic of suppositories?
What is the typical length of a rectal suppository?
What is the typical length of a rectal suppository?
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What historical materials were used to create suppositories?
What historical materials were used to create suppositories?
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What shapes are prevalent in vaginal suppositories?
What shapes are prevalent in vaginal suppositories?
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Which of the following is a disadvantage of using suppositories?
Which of the following is a disadvantage of using suppositories?
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What is the weight range typically for adult rectal suppositories?
What is the weight range typically for adult rectal suppositories?
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Why might suppositories be preferred over oral medication?
Why might suppositories be preferred over oral medication?
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What is the diameter of urethral suppositories?
What is the diameter of urethral suppositories?
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Which patient group is particularly suitable for suppository administration?
Which patient group is particularly suitable for suppository administration?
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Which of the following routes is generally preferred for drug administration?
Which of the following routes is generally preferred for drug administration?
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What are retention enemas primarily used for?
What are retention enemas primarily used for?
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In infants and children, how does the size of rectal suppositories compare to those for adults?
In infants and children, how does the size of rectal suppositories compare to those for adults?
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How do suppositories impact first-pass metabolism?
How do suppositories impact first-pass metabolism?
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What percentage of the large intestine is comprised by the rectum?
What percentage of the large intestine is comprised by the rectum?
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What is often a reason for poor patient acceptance of suppositories?
What is often a reason for poor patient acceptance of suppositories?
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How are urethral suppositories commonly referred to?
How are urethral suppositories commonly referred to?
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Which of the following dosage forms is NOT typically classified under rectal or vaginal preparations?
Which of the following dosage forms is NOT typically classified under rectal or vaginal preparations?
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What is a significant advantage of vaginal administration compared to oral administration?
What is a significant advantage of vaginal administration compared to oral administration?
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What disadvantage might occur with vaginal administration related to patient experience?
What disadvantage might occur with vaginal administration related to patient experience?
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Which dosage form is specifically intended to dissolve or melt within the vagina?
Which dosage form is specifically intended to dissolve or melt within the vagina?
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What characteristic is NOT true about vaginal tablets?
What characteristic is NOT true about vaginal tablets?
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Which attribute should be optimized for vaginal products to ensure effective drug delivery?
Which attribute should be optimized for vaginal products to ensure effective drug delivery?
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What is a main purpose of mucoadhesives in vaginal films?
What is a main purpose of mucoadhesives in vaginal films?
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What is a key feature of vaginal rings that differentiates them from other dosage forms?
What is a key feature of vaginal rings that differentiates them from other dosage forms?
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Which of the following statements about vaginal semisolids is correct?
Which of the following statements about vaginal semisolids is correct?
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What is a possible benefit of using vaginal films in medication delivery?
What is a possible benefit of using vaginal films in medication delivery?
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What common component is found in the formulation of vaginal tablets?
What common component is found in the formulation of vaginal tablets?
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What is the primary reason fatty bases are preferred for rectal suppositories?
What is the primary reason fatty bases are preferred for rectal suppositories?
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Which of the following statements about cocoa butter is accurate?
Which of the following statements about cocoa butter is accurate?
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What characteristic contributes to cocoa butter's unique properties when compared to semi-synthetic fatty bases?
What characteristic contributes to cocoa butter's unique properties when compared to semi-synthetic fatty bases?
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What is a limitation of using cocoa butter in suppository formulations?
What is a limitation of using cocoa butter in suppository formulations?
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Why is it important for drugs to partition out of the suppository base and dissolve in the body?
Why is it important for drugs to partition out of the suppository base and dissolve in the body?
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What factor significantly affects the release rate of oil-soluble drugs in suppositories using fatty bases?
What factor significantly affects the release rate of oil-soluble drugs in suppositories using fatty bases?
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Which veins drain the inferior and middle rectum directly into systemic circulation?
Which veins drain the inferior and middle rectum directly into systemic circulation?
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What is the primary mechanism of drug absorption from the rectum?
What is the primary mechanism of drug absorption from the rectum?
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If a drug is placed too high in the rectum, what metabolic process may it undergo?
If a drug is placed too high in the rectum, what metabolic process may it undergo?
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What factor can influence drug absorption from rectal fluids?
What factor can influence drug absorption from rectal fluids?
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How does osmotic effect impact the process of drug dissolution in the rectum?
How does osmotic effect impact the process of drug dissolution in the rectum?
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What is the rectal pH in adults roughly around?
What is the rectal pH in adults roughly around?
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What happens to drugs after a suppository dissolves in the rectum?
What happens to drugs after a suppository dissolves in the rectum?
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Which factor does NOT affect drug absorption variability in the rectum?
Which factor does NOT affect drug absorption variability in the rectum?
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What is a significant characteristic of the rectal epithelium compared to the upper gastrointestinal tract epithelium?
What is a significant characteristic of the rectal epithelium compared to the upper gastrointestinal tract epithelium?
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What might result from placing a suppository delivery system too high in the rectum?
What might result from placing a suppository delivery system too high in the rectum?
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The pre-blended suppository base, MBK is similar to what other base?
The pre-blended suppository base, MBK is similar to what other base?
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True or false. MBK exhibits polymorphism.
True or false. MBK exhibits polymorphism.
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What are the MWs of PEG (a water soluble base) as a liquid?
What are the MWs of PEG (a water soluble base) as a liquid?
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Glycinerated gelatin suppositories contain what components?
Glycinerated gelatin suppositories contain what components?
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Glycinerated gelatin suppositories are used to make what types of suppositories?
Glycinerated gelatin suppositories are used to make what types of suppositories?
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A low fat/oil solubility means what water solubility and choice of base?
A low fat/oil solubility means what water solubility and choice of base?
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A high fat/oil solubility means what water solubility and choice of base?
A high fat/oil solubility means what water solubility and choice of base?
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A low fat/oil solubility means was water solubility and choice of base?
A low fat/oil solubility means was water solubility and choice of base?
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What is the purpose of determining the density factor (DF) in the formulation process?
What is the purpose of determining the density factor (DF) in the formulation process?
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In the preparation of suppositories, why are certain bases preferred over others?
In the preparation of suppositories, why are certain bases preferred over others?
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What is the molar ratio of atropine to atropine sulfate used in the formulation?
What is the molar ratio of atropine to atropine sulfate used in the formulation?
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How is the active ingredient amount for morphine hydrochloride calculated in the given formulation?
How is the active ingredient amount for morphine hydrochloride calculated in the given formulation?
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What is the significance of using extra suppositories in the total calculation?
What is the significance of using extra suppositories in the total calculation?
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What is the blank suppository weight for fatty base in the atropine formulation?
What is the blank suppository weight for fatty base in the atropine formulation?
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What would be a key consideration when selecting the active ingredient for a formulation?
What would be a key consideration when selecting the active ingredient for a formulation?
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How does the molecular weight of an active ingredient affect its dosage calculation?
How does the molecular weight of an active ingredient affect its dosage calculation?
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In the formulation of a suppository, what role does the balance with a low weight quantity (LWQ) play?
In the formulation of a suppository, what role does the balance with a low weight quantity (LWQ) play?
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Which factor is least likely to affect the stability of the active ingredients in suppositories?
Which factor is least likely to affect the stability of the active ingredients in suppositories?
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What is a primary characteristic of the double-casting method for preparing suppositories?
What is a primary characteristic of the double-casting method for preparing suppositories?
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Which technique is crucial for ensuring accurate dosage when preparing suppositories?
Which technique is crucial for ensuring accurate dosage when preparing suppositories?
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What is a significant advantage of using density factors when formulating suppositories?
What is a significant advantage of using density factors when formulating suppositories?
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Which of the following statements about pharmaceutical stability in suppository formulation is true?
Which of the following statements about pharmaceutical stability in suppository formulation is true?
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When formulating a suppository with multiple active ingredients, which consideration is essential?
When formulating a suppository with multiple active ingredients, which consideration is essential?
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Which of the following might hinder the absorption of active ingredients in suppository bases?
Which of the following might hinder the absorption of active ingredients in suppository bases?
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Which factor can impact the active ingredient release rate in fatty suppositories?
Which factor can impact the active ingredient release rate in fatty suppositories?
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What role does the density factor play in the preparation of suppositories?
What role does the density factor play in the preparation of suppositories?
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Which statement about the importance of active ingredient selection in suppository formulation is accurate?
Which statement about the importance of active ingredient selection in suppository formulation is accurate?
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What is the density factor for acetaminophen in a PEG base if the blank suppository weight is 2.72 g and the final weight is 2.76 g?
What is the density factor for acetaminophen in a PEG base if the blank suppository weight is 2.72 g and the final weight is 2.76 g?
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Which statement is accurate regarding the preparation of suppositories using the double-casting method?
Which statement is accurate regarding the preparation of suppositories using the double-casting method?
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If a pharmacist determined the final individual suppository weight to be 1.95 g with a blank weight of 2 g, what is the calculated density factor for zinc oxide in the glycerin base?
If a pharmacist determined the final individual suppository weight to be 1.95 g with a blank weight of 2 g, what is the calculated density factor for zinc oxide in the glycerin base?
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What impact does overheating cocoa butter have on its stability when preparing suppositories?
What impact does overheating cocoa butter have on its stability when preparing suppositories?
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Which method can be employed to minimize the oxidation of fatty suppository bases?
Which method can be employed to minimize the oxidation of fatty suppository bases?
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Which statement about the use of salt forms versus non-salt forms of drugs in cocoa butter suppositories is correct?
Which statement about the use of salt forms versus non-salt forms of drugs in cocoa butter suppositories is correct?
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Which characteristic is false regarding suppositories?
Which characteristic is false regarding suppositories?
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When calculating the density factor, which element is essential to determine?
When calculating the density factor, which element is essential to determine?
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What is the primary concern when preparing suppositories if a drug's melting point is significantly lower than that of the base?
What is the primary concern when preparing suppositories if a drug's melting point is significantly lower than that of the base?
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Which statement regarding the double-casting method for preparing suppositories is correct?
Which statement regarding the double-casting method for preparing suppositories is correct?
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What is the primary purpose of density factor calculations in suppository formulation?
What is the primary purpose of density factor calculations in suppository formulation?
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What factor can negatively impact the physical stability of cocoa butter when preparing suppositories?
What factor can negatively impact the physical stability of cocoa butter when preparing suppositories?
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In the context of rectal administration, what is a significant advantage of avoiding first pass metabolism?
In the context of rectal administration, what is a significant advantage of avoiding first pass metabolism?
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When preparing suppositories using the molding/fusion method, which statement is true?
When preparing suppositories using the molding/fusion method, which statement is true?
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If the individual suppository weight was 2 g and the final weight was 1.95 g, what does this indicate about the density factor for the active ingredient?
If the individual suppository weight was 2 g and the final weight was 1.95 g, what does this indicate about the density factor for the active ingredient?
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Which ingredient is often included in base formulations to enhance disintegration of suppositories?
Which ingredient is often included in base formulations to enhance disintegration of suppositories?
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Which of the following describes a typical characteristic of pharmaceutically elegant suppositories?
Which of the following describes a typical characteristic of pharmaceutically elegant suppositories?
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What is the main concern when using non-salt forms of a drug in cocoa butter suppositories?
What is the main concern when using non-salt forms of a drug in cocoa butter suppositories?
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Study Notes
Suppositories
- Solid dosage form for rectal, vaginal, or urethral use
- Contains active ingredient and a base that melts, softens, or dissolves in the body
- Provides local or regional action by distributing medication to tissues
- Can offer systemic action through absorption via rectal or vaginal mucous membranes
History of Suppositories
- Historically, suppositories were made using cloth, plants, wood, or other materials
- These materials were used plain or soaked in medication solutions
Drawbacks of Suppositories
- Strong feelings of aversion towards their use in some countries, notably the US and UK
- Significant inter- and intra-subject variation in absorption
- Challenges with large-scale manufacturing, including creating products with a long shelf life
- Not typically the first choice for drug administration
Advantages of Suppositories
- Safe and effective alternative for oral routes
- Enables sustained systemic and local drug delivery
- Allows for interruption of therapy by removal
- Novel polymers enable controlled drug release
- Convenient, non-messy, and non-staining
Enemas
- Liquid preparations administered rectally
- Retention enemas: retain medication
- Evacuation enemas: remove feces, used for constipation, impaction, and preparation for lower GI exams
Other Related Dosage Forms
- Inserted into the rectum or vagina for local or systemic action
- Examples: ointments, creams, aerosol foams, vaginal films
Uses of Suppositories
- Administration of drugs to infants, small children, debilitated patients, nauseated or vomiting patients, those unable or unwilling to take oral medication, and those unsuitable for parenteral routes.
Suppository Advantages and Disadvantages
Advantages
- Effective for drugs that degrade in the gastrointestinal tract (GIT)
- Minimizes first-pass metabolism
- Allows administration of large drug doses
- Offers some control over the duration of action
Disadvantages
- Poor patient acceptance and compliance
- Potential for messiness and leakage
- Slower absorption compared to intravenous or oral administration
- Upward migration from the site of administration can increase first-pass metabolism
Various Sizes and Shapes
Rectal Suppositories
- Conical or cylindrical
- Tapered or pointed on one end (bullet or torpedo shaped)
- Length: 1 to 5 inches
- Weight: 1 to 4 g, typically 2 g
- Smaller sizes and weights are used for infants and children
Vaginal Suppositories
- Also known as pessaries
- Globular, ovi-form, or cone-shaped
- Often use the same molds as rectal suppositories
Urethral Suppositories
- Also known as bougies
- Less common
- Slender, pencil-shaped, typically 3-6 mm in diameter
- Vary in length by gender: females 25-70 mm, males 50-125 mm
- Compounded using thin, long molds or oral dosing syringes
Rectal Route
- Preferred route is oral, but rectal administration is used when oral administration is impractical or infeasible.
- This might occur when a patient has nausea or vomiting, altered consciousness, is uncooperative, has restricted oral intake, or oral administration is not feasible.
Rectal Route Physiology
- The rectum is 15-20 cm long
- Contains the anal canal (4-5 cm).
- Highly vascularized rectal epithelium resembles upper GIT epithelium but lacks villi.
- Lower Rectum: Inferior and middle hemorrhoidal veins drain directly into systemic circulation.
- Upper Rectum: Superior hemorrhoidal vein drains directly into portal circulation.
Drug Absorption from Rectum
- Drugs absorbed from the lower rectum avoid first-pass hepatic metabolism due to lower and middle rectal vein drainage into systemic circulation.
- Drugs absorbed from the upper rectum are carried directly to the liver, undergoing first-pass metabolism, if placed too high.
- Patients should be instructed not to place the delivery system too high in the rectum unless directed by their physician.
Main Mechanism of Drug Absorption
- Passive diffusion
- Absorption is influenced by:
- Molecular weight of the drug
- Lipid solubility
- Degree of ionization
- Rectal fluid pH influences drug absorption
Rectal Fluid pH
- Adult rectal pH is roughly 7.2, but varies based on rectal contents.
- Independent of sex and age after puberty.
- Limited buffer capacity.
- Significantly lower than in children (9.6±0.9).
Factors Affecting Drug Absorption
- Diarrhea
- Disease States
- Large inter- and intra-subject variability in absorption
Drug Release from a Suppository
- Suppository dissolves or melts onto the mucous layer.
- Drug diffuses outward towards the rectal membranes.
- Drug absorption occurs through passive diffusion.
How Drugs Dissolve
- Small volume of rectal fluid (~3 mL) results in incomplete dissolution and requires additional water.
- Osmotic effect draws water out of rectal tissues, which can be uncomfortable for patients.
- Suspended drugs may lead to undesirable systemic side effects.
Vaginal Administration
Advantages
- Local or systemic drug administration
- Absorption is not affected by gastrointestinal, or GI disturbances.
- Venous drainage bypasses the hepatic portal vein, avoiding the first-pass effect.
- Convenience of self-administration, potentially releasing drug for weeks.
- Ease of self-administration.
- Painless application.
- Discreet use.
- Can effectively deliver lower doses of hormones.
Disadvantages
- Erratic and unpredictable systemic drug absorption, due to variations in vaginal epithelium thickness and pH.
- Leakage or slipping out may occur, soiling undergarments or clothing.
- Some patients are hesitant to use vaginal delivery systems.
Dosage Forms for Vaginal Administration
- Solids: tablets, suppositories (also known as pessaries, ovules, and inserts), films, inserts (rings).
- Semisolids: foams, ointments, creams, gels.
- solutions.
Vaginal Tablets
- Stable and less messy than ointments or creams.
- Intended to disintegrate in the vagina, releasing their contents.
- Commonly contain:
- Lactose as a filler
- Disintegrating agent (e.g., starch)
- Dispersing agent (e.g., polyvinylpyrrolidone)
- Tablet lubricant (e.g., magnesium stearate).
- Easy to manufacture and insert.
Vaginal Suppositories
- Stable and less messy than ointments or creams.
- Intended to dissolve or melt in the vagina, releasing their contents.
- Not as easy to manufacture as tablets, but easy to compound and insert.
Vaginal Films
- Paper-thin translucent films that dissolve quickly.
- Primarily provide local action.
- Most contain spermicides or other drugs like antibacterial agents.
- Mucoadhesives may improve retention time.
Vaginal Rings
- Flexible, circular polymeric delivery systems.
- Approximately 5.5 cm in diameter.
- Made of non-irritating materials like ethylene acetate copolymers, silicone, or poly(dimethylsiloxane).
- Non-messy to use.
- Release pre-determined amounts of drug per day over extended periods.
- Polymer is non-biodegradable.
- Reservoir system: drug is located in the center core, released via diffusion through the polymeric membrane coat.
- Release rate can be modified by modifying the thickness of the membrane coat or the diameter of the core.
Vaginal Semisolids
- Used for local vaginal action.
- Deliver spermicides, antibacterial drugs, hormones, and drugs for cervical ripening.
- Usually delivered with a plastic applicator.
- Result in high local drug concentrations for short durations.
- More viscous products remain in place longer.
- Bioadhesive or mucoadhesive gel formulations can extend contact time with epithelial surfaces.
Vaginal Semisolids - Disadvantages
- Messy to use.
- Can be uncomfortable for patients.
- Prone to leakage rather than remaining in place.
Vaginal Foams
- Similar advantages and disadvantages to other semisolids.
- Contain propellants to aid drug delivery.
- Pressure exerted by the propellant ensures the formulation fills the applicator space.
Dosage Form Design Considerations for Vaginal Products
- Product pH: Some products are formulated to match vaginal pH, which is crucial for drug solubility and stability.
- Microbial presence: Products should be free from microorganisms, yeast, and molds.
-
Product attributes after administration:
- Retention: Products should be retained long enough for drug distribution.
- Liquefaction: Products should disintegrate, dissolve, or melt within a reasonable timeframe.
- Distribution: Products should spread well throughout the vaginal cavity (e.g., high-density particles).
- The base should not bind to or interfere with drug release and absorption.
Suppository Bases
-
Classes of base:
- Fatty bases
- Water-soluble bases
- Choosing a base: Requires practical experience and cannot be solely guided by scientific data.
-
General guidelines:
- Fatty bases are preferred for rectal suppositories, providing soothing and emollient action, and are less irritating to rectal tissues.
- Water-soluble bases are used for vaginal and urethral suppositories, as oily material is less desirable in these scenarios due to the lack of sphincter muscles to prevent leakage.
-
Desired release rate:
- Oil-soluble drugs: slow release with fatty bases, moderate release with water-soluble bases.
- Water-soluble drugs: rapid release with fatty bases, moderate release with water-soluble bases.
Fatty or Oleaginous Bases
- Soothing and emollient action.
- Most used bases today are semi- or fully synthetic.
- Preferred for rectal suppositories due to less rectal tissue irritation.
- Less commonly used for vaginal and urethral suppositories, as oily material is less desirable.
-
Release drugs after melting in the rectum.
- The drug must partition out of the base and dissolve in sufficient aqueous media at the site of action.
- Absorption occurs after the drug is in solution.
Cocoa Butter (Theobroma Oil)
- Mixture of liquid triglycerides entrapped in a network of crystalline, solid triglycerides.
- Soothing and emollient action.
- Melts quickly at body temperature.
- Softens at 30°C and melts at 34°C.
- Must be stored in a refrigerator to avoid melting.
- Exhibits polymorphism, with the β form being the most stable.
- Should not be heated above 34°C.
Cocoa Butter - Disadvantages
- Fat-soluble drugs are trapped in the base and do not mix with body fluids, leading to potential trapping.
- Water-soluble drugs are quickly released, often leading to rapid absorption.
- Leakage from the body orifice, as it is immiscible with body fluids.
- Some drugs lower the melting point (e.g., chloral hydrate, phenol).
- Potential for polymorphism.
- Poor contraction on cooling, making removal from molds challenging, particularly in industrial settings.
- Low softening point.
- Chemical instability.
- Poor water-absorption power.
- Higher cost.
Semi-Synthetic Fatty Bases
- Also known as adeps solidus.
- Hard fats consisting of a mixture of triglycerides, diglycerides, and monoglycerides.
- Obtained from natural fatty acid esterification with glycerol or by natural fats transesterification.
- Characteristics:
- Melting point
- Hydroxyl value
- Saponification value
- Contain no additives.
Semi-Synthetic Fatty Bases - Comparison to Cocoa Butter
- Semi-synthetic: Most acids are saturated.
- Cocoa Butter: Contains considerable unsaturated oleic acid (primarily responsible for unique properties).
Base | Melting Range | Acid Number (AN) | Hydroxyl Number (HN) | Iodine Number (IN) |
---|---|---|---|---|
Cocoa Butter | 31-34 °C | |||
Semi-Synthetic |
Suppository Preparation and Advantages
- Advantages of Suppositories: Provide potential advantages over oral dosage forms (e.g., capsules and tablets) due to bypassing the first-pass metabolism, circumventing the gastrointestinal tract, and avoiding potential inactivation by digestive enzymes.
- Rectal Administration Advantages: Rectal administration can offer increased bioavailability and consistent systemic drug absorption.
- Suppository Disintegration: Polysorbate 80, a surfactant, can facilitate the disintegration of suppositories after administration.
Molding and Fusion Method
- Molding/Fusion: Typically results in pharmaceutically elegant suppositories. Molding requires heat, which may not be suitable for heat-sensitive drugs.
- Double-Casting Method: This method enables the preparation of suppositories with a uniform drug distribution and eliminates the need for additional calculations.
- Density Factor: The density factor is essential for calculating the amount of active ingredient and base needed to prepare suppositories accurately.
- Double-Casting Steps: The first step involves blending the drug with a portion of the melted base and pouring it into the bottom portion of the molds. The second step involves pouring the remaining melted base into the molds after the initially poured mixture has solidified.
- Calculating Density Factor: The density factor is calculated by dividing the difference between the final weight and the blank suppository weight by the blank suppository weight. For example, if the blank suppository weight is 2.72 g and the individual suppository weight is 2.76 g, the density factor is 0.0148 (2.76 g - 2.72 g) / 2.72 g. This density factor is then applied to the final weight to determine the amount of drug required.
Suppository Base Considerations
- Cocoa Butter: Overheating cocoa butter can lead to a change in its polymorphic form, resulting in a less stable and less desirable product.
- Fatty Base Oxidation: The addition of antioxidants, such as ascorbyl palmitate, can help minimize the oxidation of fatty suppository bases.
Suppository Formulation and Dosage
- Suppository Flexibility: Suppositories provide a degree of dosing flexibility but are limited by the unit-dose and size limitations.
- Salt Form: The salt form of a drug is often preferred when preparing cocoa butter suppositories because it generally exhibits increased solubility and better physical stability compared to the non-salt form.
Example Prescription Calculations
- Atropine and Atropine Sulfate: For a prescription with a 1.75 mg/supp dosage, a total of 56 mg of atropine is needed.
- Morphine Hydrochloride and Theobroma Oil: For a prescription with a 125 mg/25 supp dosage, a total of 135 mg of morphine is needed.
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Description
Explore the world of suppositories, a unique dosage form for rectal, vaginal, or urethral use. This quiz delves into their history, advantages, drawbacks, and the challenges faced in manufacturing. Test your knowledge on how suppositories provide both local and systemic action.