SUPPOSITORIES, INSERT, AND STICKS

General Uses of Suppositories

• Promote defecation

• Introduce drugs into the body

• Treats anorectal disease

Suppositories

• From Latin word “supponere”

• A solid dosage form intended for insertion; rectal, vaginal, urethral

• It exert local or systematic effect

Reactal Suppositories

• cylindrical

• some are shape like a bullet, torpedo, or the little finger

• Cocoa butter as the base

• Contain at least 0.1-40% API

Vaginal Suppositories

• formerly called pessaries

• usually shaped like globular, oviform, or cone shaped and weight about 5g

• Cocoa butter is the base

Urethral Suppositories

• Also called bougies

• Has slender, pencil shaped

• Weight about 2g, cocoa butter is the base

Medication Sticks

• A convenient form for administering topical drugs

• Developments involves the history of cosmetics

• Examples are sunstick, and deodorant

local effect

type of effect where it targets a specific area

systematic effect

type of effect where it has no specif target area; all over the body

biscodyl

• rectal suppositories

• laxative

• example is dulcolax

• local effect

hydrocortisone

• rectal suppositories

• Anti-inflamation

• example is anusol-HS

• local effect

hydromorphone

• rectal suppositories

• analgesic

• example is Dilaudid

• systematic effect

indomethacin

• rectal suppositories

• anti-inflamatory

• example is indocin

• systematic effect

Clindamycin Phosphate

• vaginal inserts and tablets

• Antibiotic

• example is cleocin insert

• local effect

Miconazole Nitrate

• vaginal insert

• Anti-fungal

• example monistat 7 insert

• local effect

Nonoxynol-9

• vaginal insert

• Contraceptives

• semicid vaginal contraceptive insert

• local effect

acetaminophen

• suppositories and insert in the USP

• for fever

aminophylline

• suppositories and insert in the USP

• for asthma

bisacodyl

• suppositories and insert in the USP

• laxative

chlorpromazine

• suppositories and insert in the USP

• for cycosis

morphine sulfate

• suppositories and insert in the USP

• for pain management

Nystatin vaginal

• suppositories and insert in the USP

• for candidiasis

trichomonacide

• local effects for vaginal suppositories

• for trichomonas vaginalis (infection)

antifungals

• fro candida (Monilia) albicans - cheese like secretion

prochlorperazine and chlorpromazine, and ondasetron

• rectal suppositories

• for nausea and vomiting

morphine and oxymorphone

• rectal suppositories

• for opiod analgesic

ergotamine tartrate

• rectal suppositories

• for migraine syndrome

indomethacin

• rectal suppositories

• for NSAID

anatomic nd physiologic factors

• factors affect rectal absorption:

• constitution of the patient

• ability to transverse the physiologic barriers

physicochemical factors

• factors that affect rectal absorption:

• nature of the drugs

• nature of the suppository vehicle

• capacity of the vehicle to release drug

sodium salicyate, chloral hydrate, methylene blue, atropine morphine

• ingridients that absorbed better rectally than orally

iodideds, tracycline hydrochloride, sodium penicillin G

• absorbed better orally than rectally

sulfanilamide in a glycerinated gelatine base, prednisone

• comparable absorption rectally and orally

fatty or oleaginous bases

• most frequently employed suppository bases, cocoa butter is member of this group

fatty or oleaginous bases

• most frequently employed suppository bases, cocoa butter is member of this group

palm kernel oil, cottonseed oil

• part of oleaginous base

• hydrogenated fatty acids or vegetable oils

glyceryl monostearate, and glyceryl monopalmitate

• part of fatty bases

• glycerin with high molecular weight fatty acids

fattibase

• from palm, palm kernel, and cocunot oil with self emulsifying glyceryl monostearate and polyoxyl stearate

• melts at 35.5-37C

wecobee bases

• derived form coconut oil

• melts at 31.7-32.8C

witepsol bases

• from saturated fatty acids

• melts at 33-35C

glycerinated gelatin

• most frequently used in preparation of vaginal suppositories

• composed of 20% granular gelatin, 70% glycerin, 10% medication, and water

• hygroscopic

polyethylene glycol (PEGs)

• for extemporaneous compounding of progesterone vaginal supp.

• form in fusion of polymers f sthylene oxide and water

• do not melt at body tempt.

• dissolves slowly in body fluids

nature of the base

• ability to melt, soften, or dissolve at body temperature.

• ability to release the drug substances

• hydrophiic-hydrophobic character

• long-acting supp. example:

  • morphine sulfate

  • alginic acid

poloxamers

• pluronics

• water soluble block copolymers

• example: aspirin suppositories (blood thinner)

solid

• physical state of API:

• soluble

• not very water soluble

  • increase surface area by decreasing particle size

liquid

• physical state of API:

• forming an emulsion

paste

• physical state of API:

• mix with the solid

• mix with the base

viscosity

• high viscosity = slow release of the drug

• low viscosity = melt constantly

brittleness

• results when percentage of non0base materials exceed 30%

• brittle bases:

  • synthetic fat bases - more brittle

• skock cooling - can cause crack

oil-solubledrug: oily base

• drug release date:

• slow release; poor escaping tendency

water-soluble drug; oil base

• drug release date:

• rapid release

oil-soluble drug: water miscible base

• drug release date:

• moderate release

water-misceble drug: water-miscible base

• drug release date:

• moderate release; based on diffusion; all water soluble

vegetable extracts

• special problems in preparation of suppositories

• solution: moisten with levigation

hard crystalline materials

• special problems in preparation of suppositories

• solution: pulverize into a fine powder or dissolve in a small quantity of solvent

water-soluble materials and oily base

• special problems in preparation of suppositories

• solution: addition of wool fat to make a solution, and incorporate solution in the base

liquid materials

• special problems in preparation of suppositories

• solution: addition of inert powder

molding procedure

• type of suppositories preparation:

  • melt the base

  • incorporate any required medicaments

  • pour the melt into molds

  • allow the melt to cool and congeal into suppositories

  • removed the formed suppositories from the mold

• suitable bases

  • cocoa butter

  • glycerinated gelatin

  • PEG

aluminum foil

• temporary suppository molds

  • pressing to its desired shape

glass stirring rod

• temporary suppository molds

  • urethral suppositories

round pencils or pens

• temporary suppository molds

  • rectal suppositories

cone-shaped object

• temporary suppository molds

  • vaginal suppositories