PHARMACEUTICAL INSERTS

Prepared by: Guada Marie O. Ruiz, RPh

PHARMACEUTICAL INSERTS

1.Suppositories

2.Vaginal Inserts
1. Suppositories

 solid dosage forms intended to be inserted in body orifices where they would melt & dissolve to exert their
local or systemic effects
 From Latin word supponere means “to place under”
 Egyptians recorded is history as the first who utilized suppositories.

Types of Suppositories and Local action:

 Rectal Suppositories – relieve constipation or pain, irritation, itching, inflammation associated with
hemorrhoids.
 Vaginal Suppositories/ Pessaries- contraceptive, antiseptic in feminine hygiene.
 Urethral Suppositories/ Bougies – antibacterial or local anesthetic preparation for urethral examination.
1.5 inch is the average size of adult suppositories.
Reasons why suppositories are generally
employed in therapeutics

To promote defecation

Introduce drugs into the body
Treat anorectal disease
Suppositories are administered when:

 A local effect is desired

 A systemic effect is desired
 A drug cannot be tolerated orally

Suppositories when inserted into body cavities

 Melt
 Soften
 Dissolves
Suppository Bases:

1. Oleaginous Base (Fatty Base)

2. Water-Soluble or Water-miscible Base
3. Miscellaneous Bases
Suppository Bases:

1. Oleaginous Base (Fatty Base) b. Wecobee

-the most frequently employed suppository - source from coconut

a. Cocoa Butter, NF - roasted seeds of Theobroma Cocoa (fam. c. Witepsol

Sterculiaceae)
-saturated fatty acids
-also known as Theobroma Oil
- At room temperature – yellowish white solid
d. Other examples:
-melts at 30-36 degree C (86-97 F)
-ideal suppository base
-hydrogenated fatty acids of vegetable oils

Exhibits marked polymorphism because of its triglyceride content Palm Kernel Oil
Cottonseed Oil
Theobromine- 3,7-dimethylxanthine -containing compounds of glycerin
Caffeine- 1,3,7-trimethylxanthine (Pierre Robiquet) Palmitic Acid (Glyceryl monopalmitate)
Theophylline- 1,3-dimethylxanthine Stearic Acid (Glyceryl monostearate)
Suppository Bases:

2. Water-Soluble or Water-miscible Base

Precaution: Moisten the Tip of the Suppository to prevent mucosal irritation & to facilitate the smooth
passage of suppository in the body-orifices.
a. Glycerinated Gelatin
- most frequently used in preparation of vaginal suppositories
- slower to soften & mix w/ the physiologic fluids
b. Polyethylene Glycols
- polymers of ethylene oxide & water
- do not melt at body temperature but rather dissolve slowly in the body’s fluid
- for vaginal administration
Suppository Bases:

3. Miscellaneous Bases
- generally combination of lipophilic & hydrophilic substances
- mixtures of oleaginous & water-soluble or water- miscible materials

Example:
Polyoxyl 40 stearate
a surface-active agent that is employed in a number of commercial suppository base
General Specifications of an Ideal Suppository
Base:

1. Nontoxic & Non-irritating to mucous membranes

2. Compatible with a variety of drugs
3. Melts or dissolves in rectal fluids
4. Stable on storage: Should not bind or otherwise interfere with release & absorption of drug substances
5. Inert
6. Should melt within body temperature
Preparation of Suppositories:

Reading assignment: Please read Ansel book 9th edition pages 318-323.
Rectal Suppositories:
Rectal Suppositories

 Route of administration is useful if the patient is unwilling

or unable to take medication by mouth.
 not usually compressed as tablets unlike vaginal
suppositories
 relieves constipation
Vaginal Inserts/ Vaginal Tablets

 are uncoated, cone, bullet-shaped, or ovoid (egg-formed) inserter into the vagina for local
effects
 prepared by compression & shaped to fit smugly on “Plastic Inserter “devices that
accompany the product
Glycerinated gelatin
- most frequently used base in the preparation of vaginal suppositories where the
prolonged localized action of the medicinal agent.
- require lubrication before pouring the liquid based into the suppository mold
Polyethylene glycol
-suppository base for vaginal administration

Methods: Direct Compression

contains: Antimicrobial Agent
Alginic Acid a compound that promotes slow release of morphine suppositories.
Morphine is isolated by a German pharmacist Friedrich Sertuner
Glycerine suppositories are solidified by Sodium stearate
Thank You! 