Suppository, Inserts & Medication Sticks

Suppository

Solid dosage form in which one or more APIs are dispersed in a suitable base and molded or otherwise formed into a suitable shape for insertion into the rectum to provide local or systemic effects.

supponere

• “to place under”

• derived from sub (under) and ponere (to place)

Insert

Solid dosage form that is inserted into a naturally occurring (nonsurgical) body cavity other than the mouth or rectum, including the vagina (pessaries) and urethra (bougies)

Pessaries

Vagina

Bougies

Urethra

Medication stick

• Convenient for for administering topical drugs

• Involves the history of cosmetics

• styptic pencils, lip balm sticks, local anesthetics, oncology drugs

Inferior and middle hemorrhoidal veins

directly transport to the iliac veins and vena cava.

Superior hemorrhoidal vein

indirectly transport to the poral vein and the liver.

uterine arteries

supply blood to the upper vagina

inferior vesical arteries

middle portion of the vagina

hemorrhoidal and internal pudendal arteries

Lower Vagina

internal pudendal and vaginal arteries.

female urethra is supplied by blood vessels

inferior vesical and middle rectal arteries

male urethra is supplied by this blood vessels

7.2 to 7.4

pH of the recal fluid

4 to 4.5

pH of the vagina is in the range

1.5 g

Normal vaginal discharge consists of about this of vaginal fluid daily.

less tendency to escape to the surrounding aqueous fluids

A lipophilic drug that is distributed in a fatty suppository base in low concentrated has THIS than dose a hydrophilic substance in a fatty base.

Fatty or oleaginous bases

• Most frequently employed suppository bases

• Have good release results with water-soluble drugs

Fattibase

triglycerides from palm, palm kernel, and coconut oils with self-emulsifying glyceryl monostearate and polyoxyl stearate

Wecobee bases

triglycerides derived from coconut oil

Witepsol bases

triglycerides of saturated fatty acids C12 to C18

Cocoa Butter NF

• Fat obtained from the roasted seed of Theobroma cacao

• Yellowish-white solid having a faint, agreeable chocolate-like odor at room temperature

• Triglyceride primarily of oleoplamitostearin and oleodistearin

• Superior base in treating irritation or inflammation due to its emollient or soothing, spreading action

Water-soluble bases

• Main members are glycerinated gelatin and PEGs

• Readily releases fat-soluble drugs

Glycerinated gelatin

• Consists of granular gelatin in gelatin with the water or the medication

• Vaginal Suppository; for local action

Polyethylene glycol (PEG)

• Polymers of ethylene oxide and water prepared to various chain lengths, molecular weights, and physical states

• Do not melt at body temperature but rather dissolve slowly in body’s fluids

Poloxamers

• Water-soluble, block copolymers with a wide range of uses

• Have practically no odor or taste

• Have surfactant properties and may solubilize some drugs in the rectal fluid

Molding

• Most frequently employed both on a small scale and on an industrial scale

• Cocoa butter, glycerinated gelatin, PEG, and most other bases are suitabl

Lubrication

• facilitate clean and easy removal of the molded suppositories.

• Mineral Oil; applied with the finger to the molding substances usually suffices.

porcelain casserole

best utensil, because it later permits convenient pouring of the melt into the cavities of the mold.

Hand rolling and shaping

• Historic part of the art of the pharmacist

• Using simply the hands to roll and shape hardened suppository bases, like clay

Cocoa butter

below 30ºC, preferably in refrigerator

Glycerinated gelatin

Controlled room temperature (20ºC to 25ºC)

PEG

Usual room temperatures

Glycerin suppositories

• Popular laxative that promotes laxation by local irritation of the mucous membranes

• Caused by the dehydrating effect of glycern on the membranes

Trichomonacides

Drugs used to combat vaginitis caused by Trichomonas vaginalis

oil-soluble drug (oily base)

Slow release; poor escaping tendency

water-soluble drug (Oily Base)

Rapid Release

oil-soluble drug (water-miscible base)

Moderate release

water-miscible drug (water-miscible base)

Moderate release; based on diffusion, all water soluble

Ingredients incompatible with PEG Bases

• benzocaine

• iodochlorhydroxyquin

• sulfonamides

• ichthammol

• aspirin

• silver salts

• tannic acid

Materials that may crystallize out of PEG

• sodium barbital

• salicylic acid

• camphor

Local Action

RETENTION

Systemic Action

ABSORPTION