Rectal And Vaginal Products

Question 1

What are the uses of the rectal route?

Answer 1

*local treatment- haemorrhoids, infections
*access to descending colon- laxatives, steroids for crohns, ulcerative colitis.
*systemic use- unconscious patients, patients liable to vomit, gastro-irritant drugs (NSAIDS), acid sensitive drugs

Question 2

What is the mode of action of a suppository?

Answer 2

*base either melts at or below body temp (witepsol H15) or dissolves in rectal fluid (PEG)
*drug released in rectum
*drug dissolves in available fluid
*drug diffuses to cell surface
*drug exerts therapeutic affect- systemic or local

Question 3

What are properties of an ideal base?

Answer 3

*melts at or just below body temp (but solid at ambient temp) or dissolves in rectal fluid
*non toxic and non irritating
*compatible with all drugs
*physically and chemically stable

Question 4

What are examples of ideal suppository bases?

Answer 4

*theobroma oil (cocoa butter)-beta form-most stable, melting point 34-35°- depressed by added liquids or soluble drugs so need to add WAX to raise MP. Glycerides
*witepsol family H15 (for insoluble) and E75 (for soluble/liquids)- synthetic triglycerides
*glycerin-gelatin mixtures (used for laxatives)
*PEG- low MW PEGs are liquid (200 to 600). Can mix MW’s to get desired properties.

Question 5

Disadvantages of metal moulds.

Answer 5

*require lubrication, must
*must ensure two halves secure
*need wrapped in grease-proof paper

Question 6

How are suppositories manufactured at production scale?

Answer 6

*into heated mixer-add base, melt it, add drug, mix
*liquid doses through nozzle into mould strips controlled by volume.
*moulds sealed and packaged into cardboard boxes
*25,000 per hour

Question 7

What does a DV of 2 mean?

Answer 7

2g of drug will displace 1g of base.

Question 8

What are problems with vaginal creams and gels?

Answer 8

*must be water based to avoid stinging
*may need up to 5h of cream (large vol)
*messy
*need applicator