Suppositories, Inserts, and Sticks

promote defecation, introduce drugs into the body, treat anorectal diseases

general uses of suppositories

lack of technical difficulties, alternative for oral and parenteral route, low cost

advantages of suppositories

esthetics, potential for rectal irritation, stigma of violating person’s dignity, difficulty in titrating a correct dose

disadvantages of suppositories

32 mm/ 1.5 inch

size of rectal supp

cylindrical, bullet, torpedo, little finger

shapes of rectal supp

rectal supp

one or both ends tapered

2g for adults, 1g for infants/children

weight of rectal supp for adults and children

0\.1%-40%

API content of rectal supp

vaginal inserts

aka pessaries

globular, oviform, or cone-shaped

shapes of vaginal inserts

cocoa butter

base used in vaginal inserts

5g

weight of vaginal inserts

urethral inserts

aka bougies

slender, pencil-shaped

shapes of urethral inserts

3-6mm, 140 mm, 4g

diameter, length, weight of male urethral inserts

1-3 mm, 70 mm, 2g

diameter, length, weight of female urethral inserts

cylindrical

shape of medication sticks

5-25 g

weight of urethral inserts

circulation route, pH and lack of buffering capacity of rectal fluids, colonic content

physiological factors and drug effect

rectal fluid

has pH of 7.2-7.4, negligible buffering capacity, drug is unchanged in the rectal fluid

unchanged

in rectal fluid, drug is ---

4-4.5, with buffering capacity

vaginal fluid: pH, with or without buffering capacity

true

true/false: drug should maintain acidic environment

lipid-water solubility, particle size

physicochemical factors of the drug

fatty or oleaginous bases, water soluble bases and water-miscible bases

classification of suppository bases

fatty or oleaginous bases

most frequently employed base

palm kernel oil, cottonseed oil

2 hydrogenated fatty acids or vegetable oils

glyceryl monostearate, glyceryl monopalmitate

2 glycerin with high molecular weight fatty acids

fettibase, wecobee bases, witepsol bases

other fatty or oleaginous bases

oleopalmitostearin and oleodistearin

cocoa butter is a triglyceride of

30-36 deg

MP of cocoa butter

20% granular gelatin, 70% glycerin, 10% medication, water

composition of vaginal suppositories

60% granular gelatin, 20% gelatin, 20% medication, water

composition for urethral suppositories