Unit 6: SUPPOSITORIES, INSERTS, STICKS AND DDS FOR VAGINAL ADMINISTRATION

Local action

distinct class of suppositories most frequently used to relieve constipation or pain, irritation, itching, and inflammation associated with hemorrhoids.

Systemic action

distinct class of suppositories Used for Anti-asthma, antirheumatic and analgesic drugs.

RECTAL SUPPOSITORIES

• These have 32 mm (1.5 inches) in length, cylindrical, one or both ends tapered and some are bullet shaped. Depending on the density of the base and the medicaments in the suppository, the weight may vary

• 2 g

• Bullet, Pencil like (torpedo)

• ½ of adult dose

• for both male and female

• Intended for both local and systemic actions.

cocoa butter

Adult rectal suppositories weigh about 2 grams when____ (theobroma oil) is used as a base.

bougies

URETHRAL SUPPOSITORIES is also called as

URETHRAL SUPPOSITORIES

slender, pencil-shaped suppositories intended for insertion into the male or female urethra

Male urethral suppositories

may be 3 to 6 mm in diameter and approximately 140 mm long, cocoa butter is employed as the base, and weigh about 4g

Female urethral suppositories

about half the length and weight of the male urethral suppository, being about 70 mm long and weighing about 2g when made of cocoa butter.

pessaries

VAGINAL SUPPOSITORIES is also called as

VAGINAL SUPPOSITORIES

The most common of all the vaginal preparations, usually globular, oviform, or cone-shaped and weigh about 5 g when cocoa butter is the base

MEDICATED STICKS

• A preparation considered used for both cosmetic and medical purposes.

• provide a unique, convenient, relatively stable, easy-to-prepare dosage form for the topical delivery of drugs.

• The medication in a soft stick is applied by raising the stick above the tube level and simply rubbing it onto the skin, where it softens and flows easily onto the affected area.

Cocoa butter or Theobroma cacao

it is a triglyceride (combination of glycerin and one or different fatty acids) primarily of oleopalmitostearin and oleodistearine.

Alpha form

OLEAGINOUS BASES / FATTY BASES melting point (20°C)

Beta form

OLEAGINOUS BASES / FATTY BASES more stable form (solid at 32°C, melting point 34.5°C)

Hydrogenated fatty acid of veg. oils

these are used as a substitute of Theobroma oil.

Glycero-gelatin base

It is a mixture of glycerin and water which is made stiff by the addition of gelatin, primarily used for vaginal insertion.

Soap-glycerin base

combination of stearic acid + sodium carbonate in glycerin solution stearin soap.

Examples: curd soap, sodium stearate - used as a suppository base.

Polyethylene glycol

do not melt at body temperature but rather dissolve slowly in the body's fluids. Therefore, the base need not be formulated to melt at body temperature.

MISCELLANEOUS BASES

A mixture or a combination of classification Oleaginous bases/ Fatty bases and Water-Soluble and Water Miscible bases/ Hydrophilic bases

HAND ROLLING

it is the oldest and simplest method of suppository preparation and may be used when only a few suppositories are to be prepared in a cocoa butter base.

FUSION METHOD

• Can be used with all types of suppositories and must be used with most of them.

• It comes with melting the suppository base then dispersing or dissolving the drug in the melted base.

COLD COMPRESSION METHOD

Method of preparing suppositories from a mixed mass of grated suppository base and medicaments which is forced into a special compression mold using suppository making machines.

vaginal douches and solutions

They are used for irrigation and cleansing of vagina.

unit dose douches

prepared through mixing with water and applied by applicator into a clean vagina.

Vaginal rings

circular ring type drug delivery devices designed to release drugs in a controlled release fashion after insertion in the vagina.

RESERVOIR TYPE

Drugs are dispersed in a central core, which is then encapsulated by a drug free layer.

COMBINED CONTRACEPTIVE RING

• To release a combination of hormones simultaneously.

• Consist of major reservoir, minor reservoir and glass closures

SANDWICH TYPE

The devices consist of a narrow drug containing layer located below the surface of the ring and positioned between a non medicated central core and a non-medicated outer band.

VAGINAL INSERTS

• these types of systems contain flat rectangular polymeric slab enclosed in a pouch of knitted polyester removal system.

• The buff colored semi-transparent hydrogel slab contains drugs.

• The retrieval system is in the shape of long knitted tape that is used to retrieve the slab

VAGINAL GEL

• A type of vaginal product with extended action

• It contains micronized progesterone and the polymer polycarbophil in an oil-in-water emulsion system.

Medicated vaginal tampons

it is approved as a medical device by FDA used to absorb menstrual fluid while gradually releasing lactic acid and citric acid.

Vaginal films

are polymeric drug delivery systems shaped as thin sheets, usually ranging from 220 to 240 micro meters in thickness. These are usually often square 5x5cm, colorless, and soft, presenting a homogenous surface.

Microbicides

Provide protection only against microbial infections, including Acquired Immune Deficiency Syndrome (AIDS) and other sexually transmitted diseases (STDs). Examples: Used in treatment of vulvovaginal infection, vaginitis, anti-infective such as clotrimazole, miconazole, clindamycin, sulfonamide, etc