Lecture 17

Question 1

Suppositories

Answer 1

• Solid dosage forms for insertion into the rectum, vagina or urethra.
• Formulation: usually made with either a fatty or water miscible base (can also be hand molded or made by compression.
• Usually made in a plastic or metal mold.

Question 2

Advantages of Suppositories

Answer 2

• Local and systemic delivery both possible.
• Avoid first pass metabolism
• Delivers medication systemically when the patient can not take the medicine orally or by injection.

Question 3

Suppository Base

Answer 3

• Selection based on:
– Drug substance characteristics. – Desired release pattern.

• Solid at room temp
– Melt or soften at body temperature
– Dissolve in body fluids.

Question 4

Vaginal Drug Delivery

Answer 4

• Ideal target for local delivery and excellent route for systemic drug delivery
• Large surface area
• Similar to buccal mucosa
• Only a limited number of drugs are available for delivery by this route
• Thickness of epithelium varies with age and hormonal activity

Question 5

Normal Biochemistry of Vagina May Affect Drug Disposition

Answer 5

• Dependson:
– Cellular Uptake
– Metabolism
– Enzyme Activities
• Life Cycle of the Woman 
• Menstrual Cycle
• Sexual Activity
• Infection

Question 6

Vaginal Formulation Factors

Answer 6

• External factors can cause a disbalance in the vaginal environment.
• Can be subdivided into four categories:
– mechanical
– hygienic
– chemical factors
– sexual intercourse

Question 7

Urethral Suppositories

Answer 7

• Typically more rigid and with a higher melting point
• Formulation considerations are the same as for rectal suppositories.
• Almost all urethral suppositories are made by molding.
• A suppository applicator is often used to insert the urethral suppository.