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Questions and Answers
In which region is the use of suppositories more common?
In which region is the use of suppositories more common?
What percentage of drugs are formulated as suppositories in the United States?
What percentage of drugs are formulated as suppositories in the United States?
What is the purpose of the chapter?
What is the purpose of the chapter?
What is one of the objectives of the chapter?
What is one of the objectives of the chapter?
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In which ancient civilization was the use of rectal suppositories first documented?
In which ancient civilization was the use of rectal suppositories first documented?
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What is the percentage of drugs formulated as suppositories in Germany?
What is the percentage of drugs formulated as suppositories in Germany?
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What is one of the topics covered in the chapter?
What is one of the topics covered in the chapter?
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What is one of the reasons for using suppositories?
What is one of the reasons for using suppositories?
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What is the active constituent in Dulcolax?
What is the active constituent in Dulcolax?
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What is one of the key counseling points a pharmacist should share with the patient?
What is one of the key counseling points a pharmacist should share with the patient?
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What is the base in Anusol-HC suppositories?
What is the base in Anusol-HC suppositories?
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What is the therapeutic effect of Bisacodyl?
What is the therapeutic effect of Bisacodyl?
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What is the commercial product name of the suppository containing Hydromorphone?
What is the commercial product name of the suppository containing Hydromorphone?
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What is the primary effect of Hydrocortisone in Anusol-HC suppositories?
What is the primary effect of Hydrocortisone in Anusol-HC suppositories?
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What is the dose of Bisacodyl in Dulcolax suppositories?
What is the dose of Bisacodyl in Dulcolax suppositories?
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What is the therapeutic indication of Anusol-HC suppositories?
What is the therapeutic indication of Anusol-HC suppositories?
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What is the purpose of adding a drying powder or a suitable thickening agent to the liquid when preparing semisolid or paste-type drugs?
What is the purpose of adding a drying powder or a suitable thickening agent to the liquid when preparing semisolid or paste-type drugs?
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Why may the release rate of the drug be slowed if the viscosity of the base is very high?
Why may the release rate of the drug be slowed if the viscosity of the base is very high?
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What is the effect of particle size on the dissolution rate of a highly water-soluble drug?
What is the effect of particle size on the dissolution rate of a highly water-soluble drug?
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What is a characteristic of brittle suppositories?
What is a characteristic of brittle suppositories?
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What is the result of adding a solid to a drug prior to mixing with the suppository base?
What is the result of adding a solid to a drug prior to mixing with the suppository base?
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What happens when the percentage of nonbase materials exceeds about 30%?
What happens when the percentage of nonbase materials exceeds about 30%?
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Why is it necessary to stir the melt constantly and keep it at the lowest possible temperature?
Why is it necessary to stir the melt constantly and keep it at the lowest possible temperature?
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What happens to poorly water-soluble drugs in the presence of a high-viscosity base?
What happens to poorly water-soluble drugs in the presence of a high-viscosity base?
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What is the purpose of adding acid to a suppository base?
What is the purpose of adding acid to a suppository base?
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What is the classification of suppository bases based on?
What is the classification of suppository bases based on?
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What is an important characteristic to consider when selecting a suppository base?
What is an important characteristic to consider when selecting a suppository base?
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What type of suppository base is cocoa butter an example of?
What type of suppository base is cocoa butter an example of?
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What is a characteristic of a good suppository base?
What is a characteristic of a good suppository base?
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What type of suppository base is used in tropical climates?
What type of suppository base is used in tropical climates?
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What is the purpose of using a fatty or oleaginous base?
What is the purpose of using a fatty or oleaginous base?
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What is a characteristic of a suppository base?
What is a characteristic of a suppository base?
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What is the significance of particle size of a solid active drug?
What is the significance of particle size of a solid active drug?
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What is the purpose of adding a suspending agent to the base?
What is the purpose of adding a suspending agent to the base?
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What is the significance of the active drug's physical state in suppositories?
What is the significance of the active drug's physical state in suppositories?
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What type of dosage form is formed when the active ingredient is insoluble in the base?
What type of dosage form is formed when the active ingredient is insoluble in the base?
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Why is it necessary to maintain homogeneity of the total mixture in suppositories?
Why is it necessary to maintain homogeneity of the total mixture in suppositories?
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What is the purpose of selecting a temperature just above the melting point of the suppository mixture?
What is the purpose of selecting a temperature just above the melting point of the suppository mixture?
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What is the significance of bulk density in suppositories?
What is the significance of bulk density in suppositories?
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What is the significance of viscosity in the preparation of suppositories?
What is the significance of viscosity in the preparation of suppositories?
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Study Notes
Suppositories, Inserts, and Sticks
- Suppositories are used more routinely in southern European countries and Latin American countries, but less than 1% of drugs are formulated as suppositories in the United States.
- Suppositories have not gained the same level of acceptability, respect, and usage as other dosage forms due to extensive first-pass metabolism upon oral administration and drug stability issues.
Advantages of Suppositories
- Avoiding the breakdown of certain drugs that are susceptible to gastric degradation
- Physiologic factors that influence drug absorption from rectal suppository and vaginal/urethral insert administration
- Physicochemical factors of the drug and suppository/insert base that influence absorption
Classification of Suppository Bases
- Fatty or oleaginous bases (e.g., cocoa butter)
- Water-soluble or water-miscible bases
- Miscellaneous bases (combinations of lipophilic and hydrophilic substances)
Characteristics of Suppository Bases
- Physically and chemically stable
- Nonirritating, nontoxic, and nonsensitizing
- Chemically and physiologically inert
- Compatible with a variety of drugs
- Stable during storage
- Esthetically acceptable (free from objectionable odor and pleasing appearance)
Active Drugs in Suppositories
- Physical state (solid, liquid, or semi-solid)
- Particle size (important for poorly water-soluble drugs)
- Solubility
- Dielectric constant
- Bulk density
Preparation of Suppositories
- Importance of viscosity in preparing suppositories
- Need for constant agitation during processing and filling
- Maintaining homogeneity of the mixture
- Temperature control during preparation
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Description
Compare and contrast suppository, insert, and stick dosage forms. Discuss advantages and disadvantages of these drug delivery methods versus oral drug delivery.