Podcast
Questions and Answers
Which of the following is NOT a physiological factor affecting drug absorption from rectal suppositories?
Which of the following is NOT a physiological factor affecting drug absorption from rectal suppositories?
What is the primary mechanism by which glycerin suppositories promote laxation?
What is the primary mechanism by which glycerin suppositories promote laxation?
Why are rectal suppositories sometimes preferred over oral administration for systemic effects?
Why are rectal suppositories sometimes preferred over oral administration for systemic effects?
Which of the following is NOT a common component found in anti-hemorrhoidal suppositories?
Which of the following is NOT a common component found in anti-hemorrhoidal suppositories?
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What is the primary advantage of using a suppository base that melts rapidly at body temperature?
What is the primary advantage of using a suppository base that melts rapidly at body temperature?
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Which of the following statements correctly describes the role of lymphatic circulation in rectal drug absorption?
Which of the following statements correctly describes the role of lymphatic circulation in rectal drug absorption?
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Why is it important to consider the physicochemical properties of the drug when formulating a rectal suppository?
Why is it important to consider the physicochemical properties of the drug when formulating a rectal suppository?
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Which of the following factors would MOST likely hinder the absorption of a rectally administered drug?
Which of the following factors would MOST likely hinder the absorption of a rectally administered drug?
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Which of the following drugs is commonly administered rectally for systemic effects?
Which of the following drugs is commonly administered rectally for systemic effects?
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What is the significance of the fact that rectal fluids have no effective buffer capacity?
What is the significance of the fact that rectal fluids have no effective buffer capacity?
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Why might the dose of a drug administered rectally differ from the oral dose of the same drug?
Why might the dose of a drug administered rectally differ from the oral dose of the same drug?
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Which of the following is NOT a physicochemical factor that can affect drug absorption from rectal suppositories?
Which of the following is NOT a physicochemical factor that can affect drug absorption from rectal suppositories?
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What is the primary reason why the vaginal route is not frequently used for systemic drug administration?
What is the primary reason why the vaginal route is not frequently used for systemic drug administration?
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Which of the following best describes the role of cocoa butter as a suppository base?
Which of the following best describes the role of cocoa butter as a suppository base?
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Which of the following statements accurately describes the advantages of rectal drug administration over oral administration for systemic effects?
Which of the following statements accurately describes the advantages of rectal drug administration over oral administration for systemic effects?
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Why is a lower lipid-water partition coefficient advantageous for a drug when using a fatty suppository base?
Why is a lower lipid-water partition coefficient advantageous for a drug when using a fatty suppository base?
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Which type of suppository base would be most suitable for a drug with low solubility in both water and fat?
Which type of suppository base would be most suitable for a drug with low solubility in both water and fat?
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Which of the following is NOT a desirable property of an ideal suppository base?
Which of the following is NOT a desirable property of an ideal suppository base?
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What is the primary reason for the rapid release of fat-soluble drugs from water-soluble suppository bases?
What is the primary reason for the rapid release of fat-soluble drugs from water-soluble suppository bases?
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What is the significance of the particle size of an undissolved drug in a suppository?
What is the significance of the particle size of an undissolved drug in a suppository?
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What is the primary function of a suppository base?
What is the primary function of a suppository base?
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Which of the following is a potential disadvantage of using a fatty suppository base like cocoa butter?
Which of the following is a potential disadvantage of using a fatty suppository base like cocoa butter?
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Why is it crucial to consider the potential interaction between the drug and the suppository base during formulation?
Why is it crucial to consider the potential interaction between the drug and the suppository base during formulation?
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Which of the following best describes the ideal melting point of a suppository base?
Which of the following best describes the ideal melting point of a suppository base?
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What is the main reason why cocoa butter is considered a superior base for treating anorectal disorders?
What is the main reason why cocoa butter is considered a superior base for treating anorectal disorders?
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What is the significance of a suppository base contracting on cooling?
What is the significance of a suppository base contracting on cooling?
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Which of the following represents the best practice for melting cocoa butter for suppository formulation?
Which of the following represents the best practice for melting cocoa butter for suppository formulation?
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Which of the following factors does NOT directly affect the rate of drug absorption from a suppository?
Which of the following factors does NOT directly affect the rate of drug absorption from a suppository?
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What is the primary advantage of using glycerinated gelatin or polyethylene glycol as suppository bases?
What is the primary advantage of using glycerinated gelatin or polyethylene glycol as suppository bases?
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Based on the text, what would likely happen if a suppository base irritates the mucous membranes of the rectum?
Based on the text, what would likely happen if a suppository base irritates the mucous membranes of the rectum?
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Which type of crystalline form of cocoa butter is more stable and has a higher melting point?
Which type of crystalline form of cocoa butter is more stable and has a higher melting point?
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What is the primary reason for adding a lubricant agent to a Theobroma oil based suppository?
What is the primary reason for adding a lubricant agent to a Theobroma oil based suppository?
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Which of the following bases is characterized by a slowly dissolving property in bodily fluids?
Which of the following bases is characterized by a slowly dissolving property in bodily fluids?
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Which of the following suppository bases is most commonly used in the preparation of vaginal suppositories?
Which of the following suppository bases is most commonly used in the preparation of vaginal suppositories?
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Which of the following is NOT a disadvantage of glycerinated gelatin-based suppositories?
Which of the following is NOT a disadvantage of glycerinated gelatin-based suppositories?
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What is the primary function of a surface-active agent in suppository bases?
What is the primary function of a surface-active agent in suppository bases?
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Which of the following statements accurately describes the melting properties of Polyethylene Glycol (PEG) suppositories?
Which of the following statements accurately describes the melting properties of Polyethylene Glycol (PEG) suppositories?
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What specific issue with cocoa butter makes it unsuitable for warm climates?
What specific issue with cocoa butter makes it unsuitable for warm climates?
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Which of the following ingredients is commonly included in commercial suppository bases to enhance water absorption?
Which of the following ingredients is commonly included in commercial suppository bases to enhance water absorption?
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Which of the following suppository bases is most likely to be preferred in a situation where the medication needs to be released quickly?
Which of the following suppository bases is most likely to be preferred in a situation where the medication needs to be released quickly?
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What is the primary reason why PEG suppositories should be dipped in water before insertion?
What is the primary reason why PEG suppositories should be dipped in water before insertion?
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Which of the following statements about the melting point of Theobroma oil is ACCURATE?
Which of the following statements about the melting point of Theobroma oil is ACCURATE?
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Which of these suppository bases is NOT a triglyceride?
Which of these suppository bases is NOT a triglyceride?
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Which of the following methods of suppository preparation is most commonly used in both small-scale and industrial settings?
Which of the following methods of suppository preparation is most commonly used in both small-scale and industrial settings?
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What is the average polymer length of Polyoxyl 40 Stearate, a surface-active agent used in suppository bases?
What is the average polymer length of Polyoxyl 40 Stearate, a surface-active agent used in suppository bases?
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Which of the following suppository bases is specifically designed to accommodate aqueous solutions?
Which of the following suppository bases is specifically designed to accommodate aqueous solutions?
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Which of these suppository bases can be used to prepare suppositories with a higher melting point than body temperature?
Which of these suppository bases can be used to prepare suppositories with a higher melting point than body temperature?
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Calculate the quantity of glycerin gelatin base required to prepare six glycero gelatin supps (4 g mold) each containing 100 mg aminophylline: (Displacement Value = 1.3).
Calculate the quantity of glycerin gelatin base required to prepare six glycero gelatin supps (4 g mold) each containing 100 mg aminophylline: (Displacement Value = 1.3).
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What is the primary reason for buffering vaginal suppositories to an acidic pH of approximately 4.5?
What is the primary reason for buffering vaginal suppositories to an acidic pH of approximately 4.5?
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Which of the following is not a common component of vaginal tablets (inserts)?
Which of the following is not a common component of vaginal tablets (inserts)?
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What is the primary reason for using a plastic inserter with vaginal tablets?
What is the primary reason for using a plastic inserter with vaginal tablets?
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Why are suppositories containing light-sensitive drugs wrapped in an opaque material?
Why are suppositories containing light-sensitive drugs wrapped in an opaque material?
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What is the primary reason for storing cocoa butter suppositories below 30°C?
What is the primary reason for storing cocoa butter suppositories below 30°C?
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What is the primary difference between vaginal suppositories and vaginal tablets (inserts) in terms of their composition?
What is the primary difference between vaginal suppositories and vaginal tablets (inserts) in terms of their composition?
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Which type of suppository base requires storage at controlled room temperature (20°C to 25°C)?
Which type of suppository base requires storage at controlled room temperature (20°C to 25°C)?
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How is the displacement value of a drug determined?
How is the displacement value of a drug determined?
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What adverse effect can occur if suppositories are stored in high humidity?
What adverse effect can occur if suppositories are stored in high humidity?
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Which of the following statements about suppository shapes and sizes is NOT accurate?
Which of the following statements about suppository shapes and sizes is NOT accurate?
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Which of the following suppository types is typically used for local anesthetic purposes?
Which of the following suppository types is typically used for local anesthetic purposes?
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Which of the following is NOT a common shape for vaginal suppositories?
Which of the following is NOT a common shape for vaginal suppositories?
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If a suppository base is primarily composed of cocoa butter, what is the approximate weight of a typical adult rectal suppository?
If a suppository base is primarily composed of cocoa butter, what is the approximate weight of a typical adult rectal suppository?
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What is the primary purpose of the suppository base in terms of its interaction with the body?
What is the primary purpose of the suppository base in terms of its interaction with the body?
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Which of the following statements accurately describes the fate of a suppository once inserted?
Which of the following statements accurately describes the fate of a suppository once inserted?
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What is the intended purpose of urethral suppositories for men, aside from their antibacterial properties?
What is the intended purpose of urethral suppositories for men, aside from their antibacterial properties?
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Which of the following statements accurately reflects the purpose of suppositories?
Which of the following statements accurately reflects the purpose of suppositories?
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What is the primary reason for preparing one or two extra suppositories when calculating the amount of base?
What is the primary reason for preparing one or two extra suppositories when calculating the amount of base?
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What is the main consideration when determining the amount of base required for a medicated suppository?
What is the main consideration when determining the amount of base required for a medicated suppository?
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Which of the following is NOT a suitable base for suppository preparation by molding?
Which of the following is NOT a suitable base for suppository preparation by molding?
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What is the primary reason for using a warm mortar when preparing suppositories by compression?
What is the primary reason for using a warm mortar when preparing suppositories by compression?
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Which of the following methods of suppository preparation is considered the oldest and simplest?
Which of the following methods of suppository preparation is considered the oldest and simplest?
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What is the volume of cocoa butter required if a 12 mL suppository mold is used and the medicaments have a collective volume of 2.8 mL?
What is the volume of cocoa butter required if a 12 mL suppository mold is used and the medicaments have a collective volume of 2.8 mL?
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What is the significance of the density factor in suppository preparation?
What is the significance of the density factor in suppository preparation?
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What is the displacement value of a drug that displaces an equivalent volume of the base?
What is the displacement value of a drug that displaces an equivalent volume of the base?
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If the density of a drug is greater than the density of the base, how will the displacement value affect the amount of base required?
If the density of a drug is greater than the density of the base, how will the displacement value affect the amount of base required?
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Which of the following is NOT a factor influencing the displacement value of a drug?
Which of the following is NOT a factor influencing the displacement value of a drug?
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What is the displacement value of hydrocortisone?
What is the displacement value of hydrocortisone?
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What is the total weight of codeine phosphate required to prepare 10 suppositories, each containing 60 mg of codeine phosphate?
What is the total weight of codeine phosphate required to prepare 10 suppositories, each containing 60 mg of codeine phosphate?
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If a suppository mold has a size of 1 g, how much base is displaced by 0.6 g of codeine phosphate with a displacement value of 1.1?
If a suppository mold has a size of 1 g, how much base is displaced by 0.6 g of codeine phosphate with a displacement value of 1.1?
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What is the total weight of base required to prepare 10 unmedicated suppositories using a 2 g mold?
What is the total weight of base required to prepare 10 unmedicated suppositories using a 2 g mold?
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What is the total quantity of zinc oxide required to prepare 10 suppositories, each containing 400 mg of zinc oxide?
What is the total quantity of zinc oxide required to prepare 10 suppositories, each containing 400 mg of zinc oxide?
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Why is it important to consider the volume of medicaments when preparing suppositories?
Why is it important to consider the volume of medicaments when preparing suppositories?
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Flashcards
Suppositories
Suppositories
Solid dosage forms for insertion into body orifices that melt, soften, or dissolve to deliver medications.
Rectal Suppositories
Rectal Suppositories
Cylindrical suppositories usually 32 mm long, used rectally, typically weighing about 2 g.
Vaginal Suppositories
Vaginal Suppositories
Globular or cone-shaped suppositories used vaginally, often weighing about 5 g when cocoa butter is used.
Urethral Suppositories
Urethral Suppositories
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Suppository Base
Suppository Base
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Adult vs. Pediatric Suppositories
Adult vs. Pediatric Suppositories
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Delivery Method
Delivery Method
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Fate of the Suppository
Fate of the Suppository
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Retention Medicaments
Retention Medicaments
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Slow-Release Suppositories
Slow-Release Suppositories
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Morphine Sulfate
Morphine Sulfate
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Glycerin Suppositories
Glycerin Suppositories
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Anti-Hemorrhoidal Suppositories
Anti-Hemorrhoidal Suppositories
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Local Vaginal Suppositories
Local Vaginal Suppositories
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Systemic Effects of Suppositories
Systemic Effects of Suppositories
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Advantages of Rectal Route
Advantages of Rectal Route
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Factors Affecting Absorption
Factors Affecting Absorption
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Physiological Factors
Physiological Factors
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Colonic Content
Colonic Content
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Bypassing Portal Circulation
Bypassing Portal Circulation
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pH of Rectal Fluids
pH of Rectal Fluids
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Physicochemical Drug Factors
Physicochemical Drug Factors
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Suppository Base Properties
Suppository Base Properties
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Cocoa Butter Melting
Cocoa Butter Melting
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Theobroma Oil Polymorphism
Theobroma Oil Polymorphism
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Stable β-Polymorph
Stable β-Polymorph
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Unstable γ-Form
Unstable γ-Form
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Cocoa Butter Adherence
Cocoa Butter Adherence
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Low Melting Point Issue
Low Melting Point Issue
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Water Absorption Problem
Water Absorption Problem
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Glycerinated Gelatin
Glycerinated Gelatin
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PEG Properties
PEG Properties
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PEG Chain Lengths
PEG Chain Lengths
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Preparation Methods for Suppositories
Preparation Methods for Suppositories
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Moisture Protection for Suppositories
Moisture Protection for Suppositories
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Irritation from Glycerinated Gelatin
Irritation from Glycerinated Gelatin
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Miscellaneous Suppository Bases
Miscellaneous Suppository Bases
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Molding Steps
Molding Steps
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Materials for Molding
Materials for Molding
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Suppository Molds
Suppository Molds
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Cleaning Molds
Cleaning Molds
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Preparation by Compression
Preparation by Compression
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Hand Rolling Method
Hand Rolling Method
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Calculating Base Amount
Calculating Base Amount
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Volume Consideration
Volume Consideration
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Density Calculations
Density Calculations
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Dosage Replacement Factor
Dosage Replacement Factor
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Displacement Value (D.V)
Displacement Value (D.V)
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Codeine Phosphate Example
Codeine Phosphate Example
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Zinc Oxide Calculation
Zinc Oxide Calculation
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Volume Methods
Volume Methods
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Lipid-Water Partition Coefficient
Lipid-Water Partition Coefficient
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Lipophilic Drug
Lipophilic Drug
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Hydrophilic Drug
Hydrophilic Drug
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Choice of Base
Choice of Base
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Amount of Drug
Amount of Drug
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Particle Size
Particle Size
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Ideal Suppository Base Properties
Ideal Suppository Base Properties
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Fatty Bases
Fatty Bases
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Water-Soluble Bases
Water-Soluble Bases
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Cocoa Butter
Cocoa Butter
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Polymorphism of Cocoa Butter
Polymorphism of Cocoa Butter
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Metastable Crystalline Form
Metastable Crystalline Form
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Rate of Absorption
Rate of Absorption
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Suppository Interaction
Suppository Interaction
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Wetting Properties
Wetting Properties
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Weight of Base Required
Weight of Base Required
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Displacement Value
Displacement Value
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Glycero-Gelatin Base
Glycero-Gelatin Base
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Vaginal Suppository Composition
Vaginal Suppository Composition
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Vaginal Tablets vs. Suppositories
Vaginal Tablets vs. Suppositories
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Storage Conditions for Suppositories
Storage Conditions for Suppositories
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Packaging for Suppositories
Packaging for Suppositories
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Acidic pH in Vaginal Suppositories
Acidic pH in Vaginal Suppositories
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Common Ingredients in Vaginal Tablets
Common Ingredients in Vaginal Tablets
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Effects of Humidity on Suppositories
Effects of Humidity on Suppositories
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Study Notes
Suppositories: Dosage Forms
- Suppositories are solid dosage forms for insertion into body orifices.
- They melt, soften, or dissolve to release local or systemic medication.
- Common insertion sites are rectum, vagina, and urethra.
Suppository Shapes and Sizes
- Suppository shapes and sizes vary based on intended use and content.
- Shapes must allow for easy insertion and retention.
- Rectal suppositories are typically cylindrical or bullet-shaped, often tapered.
- Vaginal suppositories are usually globular, oviform, or cone-shaped.
- Urethral suppositories are slender and pencil-shaped.
- Size and weight vary by site (adult vs. infant/child).
Rectal Suppositories
- Adult rectal suppositories are typically 32 mm long and 2g.
- Infant/child rectal suppositories are smaller and half the weight.
Vaginal Suppositories
- Vaginal suppositories (also called pessaries) are usually globular, oviform, or cone-shaped.
- Typical weight is 5g when cocoa butter is the base.
- Weights can vary based on base material and manufacture.
Urethral Suppositories
- Urethral suppositories (bougies) are slender and pencil-shaped for male or female use.
- Male suppositories are 3-6 mm in diameter and 140 mm in length.
- Female suppositories are shorter and half the weight.
- Used for antibacterial or local anesthetic purposes.
Fate of Suppository Base
- The base softens, melts, or dissolves, releasing medication into surrounding tissues.
- Medication can be retained locally or absorbed systemically.
- Slow-release suppositories are also available, and morphine sulfate is a common example.
Local Rectal Suppositories
- Commonly used to relieve constipation.
- Glycerin suppositories cause laxation through mucosal irritation.
- Other conditions include hemorrhoids and anoectal problems.
- Anti-hemorrhoidal suppositories often contain anesthetics, vasoconstrictors, astringents, analgesics, and emollients.
Local Vaginal Suppositories
- Commonly used for contraception, feminine hygiene, or treating infections.
- Nonoxynol-9 is common in contraceptives.
- Vaginal suppositories control infections like Trichomonas vaginalis and Candida albicans.
Systemic Effects of Rectal Suppositories
- Rectal and vaginal mucous membranes can absorb many soluble drugs for systemic effects.
- Rectal route offers advantages over oral administration:
- Preserves drugs sensitive to stomach pH or enzymes.
- Avoids stomach irritation.
- Bypasses the liver (partial).
- Convenient for patients unable or unwilling to swallow.
- Effective for vomiting patients.
- Prochlorperazine, indomethacin, and ondansetron are examples.
Factors Affecting Rectal Drug Absorption
- Physiological factors like rectum volume (empty is best), colonic contents (diarrhea, obstruction), and vascularization impact absorption.
- Physiochemical factors of the drug and base.
Rectal Absorption: Physiological Factors
- The human rectum is ~15-20 cm long, containing 2-3 mL of mucous fluid when empty.
- The rectum is not motile.
- Ample vascularization helps absorption.
- Rectal fluid pH is neutral (7), with no significant buffering.
Rectal Absorption: Physicochemical Factors
- Drug solubility (lipid/water partition coefficient) influences base selection.
- Lipophilic drugs absorb better from fatty bases.
- Water-soluble drugs use water-soluble bases.
- Particle size (fine particles dissolve faster), amount of drug, and pKa also matter.
Suppository Bases
- Ideal suppository bases are non-toxic, compatible with drug, manufactureable, melt/dissolve at body temp., solidify easily, non-irritating, and stable.
Main Types of Suppository Bases
- Fatty bases (oleaginous): cocoa butter, hydrogenated vegetable oils, and other fat-based compounds.
- Water-soluble/miscible bases: glycerinated gelatin, polyethylene glycols (PEGs).
- Miscellaneous bases: mixtures of lipophilic and hydrophilic substances.
Cocoa Butter (Theobroma Oil): Properties
- A yellowish-white solid, derived from cocoa beans.
- Melts at a temperature just below body temperature (30-36°C).
- Shows polymorphism (existence in several crystalline forms) that affects melting/solidification process.
Cocoa Butter Polymorphism: Disadvantages
- Polymorphism instability (beta crystal formation)
- Adherence to molds
- Low melting point
- Poor water absorbance
- Instability during storage
- Warm climates can affect it
Other Fatty Bases
- Various commercial fat-based bases are used, using combinations of materials for stability.
Glycerinated Gelatin Bases
- A slow-softening base that is typically used in vaginal suppositories.
- Hygroscopic; must be shielded from moisture.
Polyethylene Glycols (PEGs)
- Various types of PEGs (300, 400, 600, etc.) may be mixed as suppository bases.
- Do not melt at body temperature but dissolve slowly
- Stable in warm weather and convenient to use
- Should be dipped in water if not at least 20% water content.
Miscellaneous Bases
- Surfactant mixtures(Polyoxyl 40 stearate), Mixtures of fatty bases + emulsifying agents to improve water-holding capacity.
Preparation Methods
- Molding: The most common method (melt, mix, pour, cool).
- Compression: Using machines that press the base and active pharmaceutical ingredients into the mold.
- Hand rolling/shaping: Less common with modern tools' development.
Suppository Amount Calculation
- The pharmacist calculates required amounts of base and active, accounting for drug volume, losses, and mold dimensions.
Medicated Suppositories: Considerations
- Drug quantities less than 100 mg/2g are generally insignificant but larger quantities of active pharmaceutical ingredients require calculation.
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Description
Test your knowledge on the physiological and physicochemical factors affecting drug absorption from rectal suppositories. This quiz covers the mechanisms of laxation, components of anti-hemorrhoidal suppositories, and the advantages of different suppository bases. Perfect for students in pharmacology and related fields.