Professional Documents
Culture Documents
C 12 Suppositories PDF
C 12 Suppositories PDF
Suppositories
Are solid dosage forms intended for insertion into body orifices
where they melt, soften, or dissolved and exert localized or
systemic effects.
Suppositories
Shape
Dimensions
1.Rectal
Suppository
Infant: 1 gram
Adult: 2 grams
2.Vaginal
Suppository
Pessaries
About 3 to 5
grams
3. Urethral
Suppositories
Bougies
Slender, pencil-shaped
suppositories.
For males: 4 g,
100-150 mm long.
Females: 2 g, 60
to 70 mm.
Types of Suppositories
1. Rectally
2. Occasionally Urethrally
3. Nasal Insertion
4. Vaginally
5. Rarely aurally
Local Actions:
Once inserted, the suppository base melts, softens or dissolves, distributing
the medicaments it carries to the tissues of the region.
Rectal Suppositories: relieves constipation or pain irritation, itching and
inflammation associated with hemorrhoids or other anorectal conditions
(pinworms, dermatitis)
Vaginal suppositories: as antiseptic in feminine hygiene and as specific agents
to combat an invading pathogen. (vaginitis - by Trichomonas vaginalis and
Candida albicans)
Urethral Suppositories: as antibacterial and as a local anesthetic preparatory
to urethral examination
Systemic Actions:
For system effects, the mucous membranes of the rectum and vagina
permits absorption of many soluble drugs.
Rectal suppositories:
Aminophylline & Theophylline - relief of asthma
Prochlorperazine & Chlorpromazine - nausea & vomiting, & as
tranquilizer
Chloral hydrate -sedative and hypnotic
Oxymorphine HCl - narcotic analgesic
Belladonna & Opium - analgesia and antispasmodic effect
Ergotamine tartrate - migraine syndrome
Aspirin - analgesic and antipyretic
Factors Affecting Drug Absorption of Suppositories
Physiological Factors:
1. Colonic content - When systemic effects are desired from the
administration of a medicated suppository, greater absorption
may be expected from a rectum that is empty than one that is
distended w/ fecal matter because of more absorbing surface.
So when deemed desirable, an evacuate enema will be used first.
Other conditions: diarrhea, colonic obstruction due to tumors,
tissue dehydration can influence the rate and degree of
absorption
2. Circulation Route - drugs absorbed rectally, unlike those absorbed
orally, by pass the portal circulation during their first pass into the
general circulation, thereby enabling drugs otherwise destroyed
in the liver to exert systemic effect.
The lower hemorrhoidal veins surrounding the colon receive the
absorbed drug and initiate its circulation throughout the body, by
passing the liver.
3. pH and Lack of Buffering Capacity of the Rectal Glands
The rectal fluids are essentially neutral in pH and have no
effective buffer capacity so no chemical change will occur in this
area.
The suppository base has a marked influence in the release of
active constituents incorporated into it.
Cocoa butter melts rapidly at body temperature but immiscible
with body fluids and therefore fails to readily release fat-soluble
drugs.
For systemic drug action, it is preferable to incorporate the
ionized rather than the unionized form of a drug to maximize
bioavailability
4. Physiochemical Factors:
a.
Drug
i.
Relative solubility of the drug in lipid & in water
ii.
Particle size of a dispersed drug
1) Lipid-water solubility - a lipophilic drug that
is distributed in a fatty suppository base in
A. Uy | Page 1 of 5
5)
3.
Preparations Of Suppositories
1. Molding from a melt/Fusion (Pour Molding)
2. Cold Compression (No heat Application)
3. Hand molding/rolling and shaping (No Heat Application)
4. Compression in a tablet press
*** The method most commonly employed in both small scale and industrial
scale is molding.
Preparation By Molding
1. Melting of the base preferably in water or steam bath to avoid
local overheating.
2. Incorporating the required medicament - either emulsified or
suspend in it.
3. Pouring the melt into cooled metal molds, which are usually
chrome or nickel plate.
4. Allowing the melt to cool and congeal thoroughly using
refrigerator in a small scale or refrigerated air on a larger scale.
5. Removing the formed suppositories from the mold.
Note: Suppositories of cocoa butter, glycerinated gelatin, polyethylene
glycol and most other suppository bases are suitable for preparation by
molding.
A. Uy | Page 2 of 5
Suppository Molds
Molds in common use are made from stainless steel, aluminum,
plastic. The molds which separate into sections generally
longitudinally, are opened for cleaning before and after preparing
a batch of suppository, closed when the melt is poured and
opened again to removed the cold, molded suppository.
Scratches in the molds should be avoided especially the plastic.
Lubrication Of The Molds
Depending upon the formulation, suppository molds may require
lubrication before the melt is poured to facilitate the clean and
easy removal of the molded suppository.
Lubricant is a thin coating of mineral oil or expressed almond oil
applied with the finger to the molding surface is sufficient.
2.
The two halves of the mold are held together with either
nuts or some molds have 1 centered screw.
2. Plastic suppository shells
3.
4.
5.
6.
7.
Second Method
o
Requires the following steps:
a.
Weigh the active ingredient for the preparation
of a single suppository
b. Dissolve or mix it with a portion of melted base
insufficient to fill one cavity of the mold.
c.
Place the mixture to the mold
d. Add additional melted base to the cavity to
completely fill the mold.
e. Remove the suppository from mold and weigh
f.
Then subtract the weight of the ingredient from
the total weight of the suppository to get the
amount of the base needed.
g.
Then multiplied by the number of suppository
made to get the total base needed.
Preparation of ingredient:
Glycerin
Stearic acid
Sodium carbonate
Water
Preparing the mold
Base preparation
Mxing and pouring
Opening a suppository mold
Suppository packaging
Strip ware
A. Uy | Page 3 of 5
Roll ware
various opening methods like tear open slot, tear open strap, peel
off strap "long", peel off strap "short"
Preparing and Pouring of the Melt
Using the least possible heat, the weighed suppository base material is
melted, generally over a water bath.
The medicinal substance are usually incorporated into portion of the melted
base by mixing on glass or porcelain tile with spatula, stir and allowed to cool
almost to its congealing point.
It is generally best to chill the mold in the refrigerator before pouring the
melt. Then, the melt is placed carefully and continuously in the filling of
each cavity in the mold.
The pouring must be continuous to prevent layering which may lead to a
product easily broken on handling.
When solidified the excess material is scraped off the top of the mold with
spatula. The mold is placed in the freezer to hasten hardening of the
suppository.
When suppositories are hard, the mold is removed from the freezer and
dislodged the suppositories from the mold.
Generally, little pressure is required to let fall the suppository of their mold.
2. Preparation By Compression
Suppositories may be prepared by forcing the mixed mass of the suppository
base and the medicament into special molds using suppository making
machines.
On a small scale, a mortar is heated in warm water before use and then
dried, the softening of the base and the mixing process are greatly facilitated
forming a paste-like consistency.
The compression process is especially suited for making suppositories which
contain substances that are heat labile and for suppositories containing a
great deal of substances insoluble in base.
The suppository mass is placed in the cylinder which is then closed, pressure
is applied from one end, by turning wheel and the mass is forced out of the
other end into the suppository mold or die. When the die is filled with the
mass, a movable end plate at the back of the die is removed and when
additional pressure is applied to the mass in the cylinder, the formed
suppositories are ejected.
Advantages of Compression:
1. The method is simple
2. The resulting suppository is more elegant than that of hand
molding
3. Avoid the possibilities of sedimentation of the insoluble solids in
the suppository base
Disadvantages:
1. Too slow for large scale operation
2. Air entrapment in molding fat type base suppositories. This
results in uncontrolled weight variation and favors the possible
oxidation of the base and active ingredients.
Preparation by hand rolling and shaping (no longer used today)
1. A plastic mass is formed from the base of grated Cocoa butter &
other ingredients.
2. Triturate in a mortar, then formed into a ball in the palms of the
hands, previously cooled in the ice water.
3.
4.
Product
Dulcolax
Thorazine
Effect
local
systemic
Ergomine tartrate
Cafergot
systemic
Hydrocortisone
Anusol-HC
local
Indomethacin
Indocin
systemic
Prochlorperazine
Promethazine HCl
Compazine
Phenergan
systemic
systemic
Category
Cathartic
Anti-emetic,
tranquilizer
Adrenergic
blocking agents
Pruritis, Inflamed
Hemmarhoids
Antiinflammatory,
analgesic
Anti-emetic
Anti-histaminic,
antiemetic,
sedative
A. Uy | Page 4 of 5
Vaginal Suppositories
g.
Product
AVC suppositories
Active Constituents
Sulfanilamide, 1.05gm
Betadine medicated
Povidone-iodine, 10%
Gyne-Lotrimin
Clotrimazole, 100 mg
Monistat 7
Semicid vaginal
contraceptive insert
nonoxynol-9,100 mg
Sulfathiazole, sulfacetamide
sulfabenzamide, 500 mg
Terconazole, 80 mg
Terazol 3
Category
Candida albicans
infections
relief of vaginitis due
to Candida albicans,
Trichomonas, and
Gardnerella vaginalis
Vulvovaginal yeast
(candida) infections
Antifungal for
vulvovaginal
candidiasis
(moniliasis)
Non-systemic
reversible method of
birth control
Haemophilus
vaginalis vaginitis
Antifungal for
vulvovaginal
candidiasis
(moniliasis)
h.
i.
2.
e.
f.
Other examples:
Miconazole 7
Clotrin-V
g.
h.
JELLIES
-
Examples of supp.:
Vaginal
a.
b.
c.
d.
Anucort HC 25mg
Hemril-HC 25mg
Cotecxin supp.
Hemmorhoidal-HC 25mg
Administration
1. Rectal
a.
b.
c.
d.
e.
f.
A. Uy | Page 5 of 5