Question

Discuss the method of preparation of suppositories and pessaries including their displacement value and evaluation

Answer 1

Answer:

Explanation:

Suppositories and pessaries

1. SUPPOSITORIES AND PESSARIES Presented by Nabina 1

2. DEFINITION A suppository is a medicated solid dosage form generally intended for use in the rectum, vagina and to a lesser extent, the urethra. After insertion they melt or soften at body temperature, whereas vaginal suppositories sometimes called as pessaries, are also made as compressed tablets that disintegrate in body fluids. 2

3. BP DEFINITION : SUPPOSITORY  “Suppositories are solid, single-dose preparations. The shape, volume and consistency of suppositories are suitable for rectal administration.” 3

4. BP DEFINITION: PESSARIES “ Pessaries are single dose preparations. They have various shape usually ovoid with a volume and consistency suitable or insertion into vagina. They contain one or more active substances dispersed or dissolved in suitable basses that may be soluble or dispersible or melt at body temperature. Excipients such as diluents, adsorbents, surface active agents, lubricants, antimicrobial preservatives and colorizing material authorized by the competent authority may be added if necessary.” 4

5. PESSAARIES Common ingredients for inclusion in pessaries for local action include:  antiseptics  contraceptive agents  local anaesthetics  various therapeutic agents to treat trichomonal, bacterial and monilial infections. 5

6. Advantages Oral route not useful. Patient – GIT problems, Nauseous or post operative. Very young , very old, or the mentally disturbed. Drug have GI side effects.Drug - not stable at GI pH or susceptible to enzymatic attack in the GI tract Drug - first pass metabolism. Drugs with an unacceptable taste can be administered. Drug that may be abused as in suicide. 6

7. Disadvantages Mucosal irritation Traditional Issues- feeling of aversion Leakage Sometimes incomplete absorption. Inter and intra subject variation. Proctitis. Large scale production difficult and costly Shelf life (stringent storage conditions) . GI state affects absorption 7

8. DOSAGE FORM CHARACTERISTICS: a. Rectal suppositories for adults weigh 2 g and are torpedo shape . Children's suppositories weigh about 1 gm. b. Vaginal suppositories or Pessaries weigh about 3-5gm and are molded in globular or oviform shape or compressed on a tablet press into conical shape. c. Urethral suppositories called Bougies are pencil shape. Those intended for males weigh 4 g each and are 100-150 mm long. Those for females are 2 g each and 60-75 mm in length. 8

9. d. Nasal suppositories: Called nasal bougies or buginaria meant for introduction in to nasal cavity. •They are prepared with glycerogelatin base. •They weigh about 1 g and length 9-10 cm. e. Ear cones: • Aurinaria and meant for introduction into ear. • Rarely used. • Theobroma oil is used as base. • Prepared in urethral bougies mould and cut according to size. 9

10. SHAPE OF SUPPOSITORIES 10

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12. THERAPEUTIC USES  Suppository can be used for local or systemic effect.  The action depends on nature of drug , concentration and rate of absorption  Rectal suppository are intended for treatment of constipation and hemorrhoids.  Suppositories are also administered for systemic action (analgesics, antispasmodics, sedatives & tranquilizers). 12

13. LOCATION OF SUPPOSITORY 13

14. FACTOR AFFECTING DRUG ABSORPTION FORM RECTAL SUPPOSITORY: 1) Physiologic Factor: The human rectum is approximately 15-20 cm in the length, when empty of fecal material; it contains 2-3 ml of inert mucous fluid. In resting state, the rectum is non motile. There is no villa or microvillus on rectal mucosa. Physiological factors include: 14

15. A) Colonic Content: When systemic effect are desired from suppository greater absorption may be expected from a rectum that is void than that with fecal matter. An evacuation enema maybe administered before insertion of a suppository. Diarrhea, colonic obstruction and tissue dehydration influence the rate & degree of drug absorption from rectum. 15

16. B) Circulation: Drugs absorbed rectally partially by pass portal circulation, thereby enabling drug destroyed in liver to exert systemic effect. Depending on the height at which absorption occurs at rectum, the drug passes into inferior, middle or superior hemorrhoid veins. The inferior is nearest to the anus, the upper hemorrhoid vein —> portal circulation .thus it is advisable to keep suppositories in the lower part of rectum. 50% -70% of drug administered rectally, reported to go directly into general circulation. 16