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Questions and Answers
Based on the content, select the factor that MOST directly impacts the effectiveness of a topical drug formulation.
Based on the content, select the factor that MOST directly impacts the effectiveness of a topical drug formulation.
What is a key factor that needs to be considered when formulating a topical drug for treating skin disease?
What is a key factor that needs to be considered when formulating a topical drug for treating skin disease?
Which of the following is NOT a factor that contributes to physical deterioration of a topical formulation?
Which of the following is NOT a factor that contributes to physical deterioration of a topical formulation?
According to the content, what is the primary reason why greasy bases can interfere with normal skin functions?
According to the content, what is the primary reason why greasy bases can interfere with normal skin functions?
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What is the primary difference between a topical formulation that is 'free of pathogens' and one that is 'sterile'?
What is the primary difference between a topical formulation that is 'free of pathogens' and one that is 'sterile'?
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Which of the following is NOT a characteristic of a semi-solid?
Which of the following is NOT a characteristic of a semi-solid?
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What is the main function of a dermatological formulation?
What is the main function of a dermatological formulation?
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What is the term for the process where a semi-solid loses water and shrinks?
What is the term for the process where a semi-solid loses water and shrinks?
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What components are commonly included in semi-solid formulations to ensure their effectiveness and stability?
What components are commonly included in semi-solid formulations to ensure their effectiveness and stability?
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What factors affect the bioavailability of a dermatological formulation?
What factors affect the bioavailability of a dermatological formulation?
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Which of the following is NOT a type of semi-solid formulation?
Which of the following is NOT a type of semi-solid formulation?
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What is the key to understanding the concept of bioavailability in semi-solids?
What is the key to understanding the concept of bioavailability in semi-solids?
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What type of dermatological formulation is considered prophylactic?
What type of dermatological formulation is considered prophylactic?
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What is an example of plastic flow in Non-Newtonian fluids?
What is an example of plastic flow in Non-Newtonian fluids?
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What happens to thixotropic fluids when they are agitated?
What happens to thixotropic fluids when they are agitated?
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Which of the following is NOT a type of ointment base?
Which of the following is NOT a type of ointment base?
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What is negative thixotropy also known as?
What is negative thixotropy also known as?
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How does viscosity change in non-Newtonian fluids under increasing shear rate?
How does viscosity change in non-Newtonian fluids under increasing shear rate?
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Which type of emulsion has water as the bulk phase?
Which type of emulsion has water as the bulk phase?
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What is the defining characteristic of pseudoplastic flow?
What is the defining characteristic of pseudoplastic flow?
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What property of pastes makes them more effective than ointments at absorbing serous discharge?
What property of pastes makes them more effective than ointments at absorbing serous discharge?
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Which type of flow is characterized by an increase in viscosity with shear stress?
Which type of flow is characterized by an increase in viscosity with shear stress?
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In the context of emulsions, what does 'thermodynamically unstable' mean?
In the context of emulsions, what does 'thermodynamically unstable' mean?
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Creams are defined by which of the following characteristics?
Creams are defined by which of the following characteristics?
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Which type of emulsion is represented by butter?
Which type of emulsion is represented by butter?
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What is the primary property of Newtonian fluids?
What is the primary property of Newtonian fluids?
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Which of the following conditions can be treated using water-soluble bases?
Which of the following conditions can be treated using water-soluble bases?
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What is an advantage of using water-soluble bases for drug treatment?
What is an advantage of using water-soluble bases for drug treatment?
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Which of the following is a disadvantage of water-soluble bases?
Which of the following is a disadvantage of water-soluble bases?
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What characteristic of water-soluble bases is ideal for application to skin or mucous membranes?
What characteristic of water-soluble bases is ideal for application to skin or mucous membranes?
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Which statement best describes the stability of water-soluble bases compared to solid dosage forms?
Which statement best describes the stability of water-soluble bases compared to solid dosage forms?
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What is a possible risk when applying water-soluble bases with fingers?
What is a possible risk when applying water-soluble bases with fingers?
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Why might some patients not prefer ointments over water-soluble bases?
Why might some patients not prefer ointments over water-soluble bases?
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What does the term 'non-dehydrating' imply regarding water-soluble bases?
What does the term 'non-dehydrating' imply regarding water-soluble bases?
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What is a primary characteristic of oleaginous bases?
What is a primary characteristic of oleaginous bases?
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Which property distinguishes absorption bases from oleaginous bases?
Which property distinguishes absorption bases from oleaginous bases?
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What is a potential drawback of using oleaginous bases in topical treatments?
What is a potential drawback of using oleaginous bases in topical treatments?
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What is a common use for oleaginous bases in dermatology?
What is a common use for oleaginous bases in dermatology?
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How do oleaginous bases typically affect drug release?
How do oleaginous bases typically affect drug release?
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What type of base is Aquaphor classified as?
What type of base is Aquaphor classified as?
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What defines a property of absorption bases compared to other base types?
What defines a property of absorption bases compared to other base types?
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What is a significant limitation of oleaginous bases when applied to the skin?
What is a significant limitation of oleaginous bases when applied to the skin?
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Study Notes
Semisolid Dosage Forms
- Semisolid dosage forms include ointments, creams, gels, and pastes. They differ from other dosage forms in their physical characteristics.
- Ointment bases come in 5 types, each with unique characteristics. The correct base is chosen based on patient needs.
- Emulsions are a type of dosage form where one liquid is dispersed in another. The internal phase is dispersed throughout the other phase.
- Rheology (flow) is important to understand in dosage forms; various types of flow exist (plastic, pseudoplastic, and dilatant).
- Viscosity affects sedimentation rate; higher viscosity leads to slower sedimentation.
- Various suppository bases exist, some melt at body temperature while others dissolve.
- Penetration, permeation, and absorption are terms related to how drugs pass through the skin.
- Syneresis, swelling, and inhibition are important terms to learn.
Objectives
- Distinguish the characteristics of ointments, creams, gels, and pastes.
- Select the correct dosage form for a patient.
- Describe the characteristics of each ointment base, and the selection criteria
- Describe how to compound ointments by two methods.
- Explain geometric dilution.
- List suppository bases, and know which base should be stored in the fridge.
- Describe how to raise the melting point of a suppository.
- Define BUD in the context of pharmaceutical products.
Schedule of Topics
- Week 7: Semi-solids
- Week 8: Transdermal
- Week 9: Pulmonary
- Week 10: Radioactivity
- Week 11: Parenterals
Special Attributes of Semisolid Dosage Forms
- Bioavailability depends on application area, residue thickness, and formulation.
- Products must be free of pathogens but not necessarily sterile.
- Products need to be chemically stable.
- Products may cause local or systemic effects.
Signs of Physical Instability
- Changes in consistency
- Discoloration
- Emulsion breakdown
- Crystal growth
- Shrinking due to evaporation
- Microbial growth
- Changes in odor.
Factors to Consider for Skin Penetration
- Understanding skin penetration phases (penetration, permeation, and absorption).
- Understanding the need for aqueous and lipid solubility in treating skin diseases.
- Be aware of how animal fats (like lard and wool) affect skin penetration when combined with water.
- Understand how greasy bases can interfere with skin functions (like sweating).
Pharmaceutical Factors for Semisolid Products
- Drug penetration depends on physicochemical drug properties, vehicle, and skin condition.
- Drug release rate should be considered, as should the stability of the base.
- Solvent properties, and emulsifying properties should be accounted for.
- Product consistency must be able to withstand changes in temperature.
Emulsions
- Emulsions are thermodynamically unstable systems with at least two immiscible liquid phases.
- The two typical types are oil-in-water (o/w) and water-in-oil (w/o).
- Multiple and microemulsion systems exist as well.
Rheology and Flow Types
- Rheology is the study of deformation and flow of matter.
- Viscosity measures resistance to flow.
- Newtonian fluids have constant viscosity, regardless of applied stress.
- Non-Newtonian fluids have viscosity that changes with applied stress (plastic, pseudoplastic, and dilatant).
- Thixotropy is a time-dependent shear-thinning property.
Ointments
- Ointments are semisolid preparations for topical application to the skin or mucous membranes.
- Ointments are viscous, oleaginous, or polymeric.
- Ointments can contain drugs, and can be used to treat minor skin infections, itching, burns, diaper rash, insect bites, and other conditions.
Types of Ointment Bases
- Ointments are categorized by their composition (oleaginous, absorption, w/o, o/w, water soluble).
Ideal Properties of Ointments
- Smooth texture, elegant appearance, non-dehydrating, non-gritty, greasy and does not stain, and non-hygroscopic.
- It should be non-irritating and not alter skin function.
- Easy application, and effective drug release.
- High aqueous washability.
Absorption Bases
- Absorption bases have properties between oleaginous and w/o bases.
- They are often greasy and occlusive.
Emulsion Bases
- Water-in-oil (W/O) or Oil-in-water (O/W) permits the incorporation of varying quantities of water.
Water-Soluble Bases
- Water-soluble bases usually contain water and are water washable.
Selection of the Appropriate Base
- Release rate, desired effect (topical or systemic), stability, compatibility, and ease of removal are important factors.
Methods of Preparation
- Hand-rolling
- Compression molding
- Fusion molding
Quality Control
- Appearance, uniformity, weight/volume, viscosity, clarity, and pH are assessed.
- Packaging/ storage and labeling are important factors.
Additional Topical Formulations
- Pastes are thick, stiff ointments resistant to flow.
- Lotions are aqueous formulations, generally used for lubrication.
Suppositories
- Solid dosage forms for insertion into body orifices, to melt and exert local or systemic effects.
- Rectal, vaginal, and urethral are common types.
- Historical uses include cloth, plants, wood, and cocoa butter.
Disadvantage of Rectal Suppositories
- Not preferred by patients.
- Absorption is unpredictable.
- Some leak or expel after insertion.
Vaginal Suppositories (Pessaries)
- Water-soluble bases are most convenient.
- Progesterone compounded suppositories are used in hormone replacement therapy.
Situations where suppositories are useful
- Vomiting
- Destroyed or inactivated by stomach pH.
- Drugs irritating the stomach.
- Administering drugs to patients who can not or will not swallow medications.
Physicochemical Factors Affecting Suppository Drug Absorption
- Particle size
- Nature of the base (melting/dissolving for drug release)
- Drug solubility.
- Spreading capacity.
Some Factors of Drug Absorption from Rectal Suppositories
- Colonic content (empty better than full).
- Circulation route (bypasses first pass).
Ideal properties of a suppository base
- Melting at body temperature or dispersible in body fluids.
- Non-toxic and non-irritating.
- Easy drug release and stable.
- Capable of holding its shape.
- Compatible with drug properties.
- Stable on storage.
Additional Notes on Cocoa Butter, Other Problems, etc.
- Cocoa butter has multiple polymorphic forms.
- Different forms melt at different temperatures.
- Some ingredients/medications can reduce the melting point of cocoa butter.
- Cocoa butter has poor water-absorbing ability (can be improved with emulsifiers)
- Can be subject to oxidation.
- Synthetic Triglycerides are a better alternative if overheating or oxidation is a concern.
Water-Soluble Bases
- Glycerinated gelatin is one example, with the added disadvantage of a laxative effect.
- These are often better for water soluble drugs.
- Polyethylene glycols (PEGs) have better stability and fewer irritation concerns.
Methods of Preparation
- Hand rolling
- Compression molding
- Fusion molding is the most common.
Fusion Method Considerations
- Preparing molds
- Preparing the base
- Preparing the drug
- Mixing and pouring
- Cooling and finishing.
- Issues with chemical deterioration (oxidative or yellowing).
Important Counseling Points
- Discuss when to refrigerate, and how to safely handle product and use proper hygiene.
- Provide information on beyond-use dates, which should be stated in counseling instructions.
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Description
Test your knowledge on the key factors affecting the effectiveness of topical drug formulations. This quiz covers aspects such as formulation characteristics, bioavailability, and the differences between sterile and non-sterile products. Perfect for students and professionals in the pharmaceutical and dermatological fields.