SUPPOSITORIES Flashcards
Are solid dosage forms in which one
or more active pharmaceutical
ingredients (APIs) are dispersed in a
suitable base molded or otherwise
formed into a suitable shape for
insertion into the rectum to provide
local or systemic effect.
SUPPOSITORIES
Are solid dosage forms intended for
insertion into body orifices where they melt, soften, or dissolve and exert localized or systemic effects.
SUPPOSITORIES
Suppositories is derived from the Latin word ______ which means “to place
under”, as from sub (under) and
ponere (to place).
SUPPONERE
What is the meaning of supponere?
TO PLACE UNDER
Used rectally, vaginally, and occasionally
urethrally.
SUPPOSITORIES
pain, constipation, irritation,
itching, and inflammation associated with
hemorrhoids or other anorectal d
RECTAL
contraceptives, antiseptics in
feminine hygiene, antibacterial
VAGINAL
comes in various shapes
and weights. The shape and size must be
such that it can be easily inserted into the
intended orifice without causing undue
distension, and once inserted, it must be
retained for the appropriate period.
SUPPOSITORIES
Are intended for insertion into body
orifices where they melt, soften, or
dissolve and exert localized or systemic
effects.
SUPPOSITORIES
Types of Suppositories
RECTAL
VAGINAL
URETHRAL
BURGINARIUM
Are inserted into the rectum with the fingers.
RECTAL
• Are cylindrical and have one or both ends tapered.
• Some are shaped like a bullet, a torpedo, or the little finger.
• Length: Usually about 32 mm (1 ½inches)
• Weight: Adult: 2 grams - when made of
cocoa butter (pencil-like shape)
• Infants: 1 grams
RECTAL
Also called Pessary or Pessaries
VAGINAL
• Are usually globular, oviform, or cone-
shaped
• Weight: about 5 grams - when made
cocoa butter base.
VAGINAL
Urethral is also called as?
BOUGIES
Are slender, pencil-shaped intended for
insertion into the male or female urethra.
Male:
• Diameter - 3-6 mm
• Length: 140 mm (14 cm)
• Weight: about 4 grams - when made of
cocoa butter
Female: Length: 70 mm (7 cm)
• Weight: about 2 grams - when made of
cocoa butter
URETHRAL
same as urethral suppositories but shorter and thinner.
BURGINARIUM
same as urethral suppositories but shorter and thinner.
BURGINARIUM
Vaginal suppositories is also called as?
PESSARY OR PESSARIES
Are slender, pencil-shaped intended for
insertion into the male or female urethra.
Male:
• Diameter - 3-6 mm
• Length: 140 mm (14 cm)
• Weight: about 4 grams - when made of
cocoa butter
Female: Length: 70 mm (7 cm)
• Weight: about 2 grams - when made of
cocoa butter
URETHRAL
The most widely used suppository
base.
COCOA BUTTER (THEOBROMA OIL)
Good base for rectal suppositories,
but it is less ideal for vaginal and
urethral suppositories.
COCOA BUTTER
Good base for rectal suppositories,
but it is less ideal for vaginal and
urethral suppositories.
COCOA BUTTER
______ can replace to coca butter to replace part of it to obtain proper melting point?
WHITE WAX
3 fatty or oleaginous bases:
COCOA BUTTER (THEOBROMA OIL)
HYDROGENATED FATTY ACIDS OF VEGETABLE OIL
GLYCERIN WITH HIGHER MOLECULAR WEIGHT FATTY ACIDS
•Kernel oil and Cottonseed oil
HYDROGENATED FATTY ACIDS OF VEGETABLE OILS
2 HYDROGENATED FATTY ACIDS OF VEGETABLE OILS
KERNEL OIL
COTTONSEED OIL
These are fat-based compounds containing compounds of Glycerin with the higher molecular weight fatty acids such as Palmitic acid and Stearic acids.
GLYCERIN WITH HIGHER MOLECULAR WEIGHT FATTY ACIDS
• Glyceryl Monostearate and Glyceryl
Monopalmitate
GLYCERIN WITH HIGHER MOLECULAR WEIGHT FATTY ACIDS
Are polymers of ethylene oxide and water,
prepared to various chains lengths,
molecular weight, and physical states.
POLYETHYLENE GLYCOLS (PEG)
They are available in a number of
molecular weights ranges, the more
commonly used being polyethylene glycol
300, 400, 600, 1000, 1500, 1540, 3350,
4000, 6000, 8000.
POLYETHYLENE GLYCOL
They are available in a number of
molecular weights ranges, the more
commonly used being polyethylene glycol:
300
400
600
1000
1500
1540
3350
4000
6000
8000
These bases are water soluble; however, the dissolution process is very slow.
These do not melt at body temperature
but rather dissolve slowly in the body’s
fluids. Therefore, the base needs not to be
formulated to melt at body temperature.
In rectum and vagina, where the amount of fluid is very small, they dissolve very slow, but they soften and spread.
POLYETHYLENE GLYCOLS (PEG)
At room temperature:
PEG 300, 400, 600-
CLEAR, COLORLESS LIQUID
PEG 1000-
WHITE SEMI-SOLID
PEG 1500, 1540–
FAIRLY FIRM SEMI-SOLID
PEG 3350, 4000, 6000–
FIRM, WAX-LIKE SOLIDS
PEG - clear, colorless liquid
300
400
600
PEG- white semi-solid
1000
PEG- fairly firm semi-solid
1500
1540
PEG- firm, wax-like solids
3350
4000
6000
May be prepared by dissolving granular
gelatin (20%) in glycerin (70%) and
adding a solution or suspension of the
medication (10%).
GLYCERINATED GELATIN
May have a tendency to absorb moisture
due to the hygroscopic nature of glycerin,
they must be protected from atmospheric
moisture for them to maintain their
consistency.
GLYCERINATED GELATIN
Is most frequently used in the preparation of vaginal suppositories, where the prolonged localized action of the medicinal agent is usually desired.
GLYCERINATED GELATIN
Is slower to soften and mix the physiologic fluids than in cocoa butter and therefore provides a more prolonged release.
GLYCERINATED GELATIN
This is a type that is used to prepared with Cocoa/Cacao Butter or Theobroma Oil.
FIRST TYPE
will soften when used with:
Phenol, Camphor, Chloral hydrate, and other volatile oils. However this can be remedied by the addition of: Wax or Spermaceti to raise the melting point in the warmest weather.
CACAO BUTTER
Acts by melting at body temperature.
THEOBROMA OIL
Are those prepared with Glycerin and
Gelatin
SECOND TYPE
o Are water-soluble or water miscible
o Are employed to provide a continuous
medicating or germicidal action
o By mixing the aqueous solution of
suspension of the medicament with
glycerin and gelatin.
SECOND TYPE
Are the Glycerin or Soap suppositories
shaped from Castille soap
THIRD TYPE
o This performs their function in part
mechanically and in part by dissolving and
producing some irritation.
o Their chief value is as stimulation to
peristalsis, through their presence in the
rectum.
o They are mostly for small children to avoid the use of laxatives
THIRD TYPE
3 methods of preparation:
MOLDING (FUSION)
COMPRESSION
HAND ROLLING AND SHAPING
Is the principal way of making suppositories commercially.
Capable of producing 6-12 or more suppositories
Molds are made of Stainless steel,
Aluminum, Brass or Nickel-Copper alloys, or plastic.
Primary bases used are: Cocoa butter,
Polyethylene glycol, Glycerinated gelatin
Mineral oil is used as lubrication.
Suppository Molds:
SUPPOSITORY MOLDS
Preparation:
Melting of the base
Incorporation of any of the medicaments
Pouring the melt into molds
Allowing the melt to cool and congeal into suppositories
Removing the formed suppositories from the mold
MOLDING
lubrication is seldom necessary as these
materials contact sufficiently on cooling to
separate from the inner surfaces and
allow easy removal.
COCOA BUTTER OR POLYETHYLENE GLYCOL
lubrication is usually
necessary. A thin coating of mineral oil
applied within the finger to the molding
surfaces usually suffices.
GLYCERINATED GELATIN
Is generally employed when cocoa butter is used as a base.
Capable of producing a 2 g suppository.
COMPRESSION
Preparation:
Uniform mixture of drug and base (hand-rolling method)
Mixture is placed into a chamber mold.
Mold is then cooled.
COMPRESSION
Involves molding the suppository with
the fingers after the formation of
plastic mass.
HAND ROLLING AND SHAPING
must be-stored below 30°C and preferably in a refrigerator (2°C to 8°C)
COCOA BUTTER SUPPOSITORIES
This can be stored at controlled room temperature (20°C to 25°C).
GLYCERINATED SUPPOSITORIES
Official Bases
COCOA BUTTER or THEOBROMA OIL
HIGH MOLECULAR WEIGHT POLYETHYLENE GLYCOL (PEG)
GLYCERINATED GELATIN
Are solid dosage forms that is inserted
into a naturally occurring (nonsurgical)
body cavity other than the mouth or
rectum, including the vagina and urethra.
INSERTS
Are usually ovoid in shape and are
accompanied in their packaging with a
plastic inserter, a device for easy
placement of the tablet within the vagina.
VAGINAL INSERTS
It contains the same types of anti-infective
and hormonal substances as the vaginal
suppositories.
VAGINAL INSERTS
Are a convenient form for
administering topical medications.
MEDICATION STICKS
Their development is interesting
because it involves the history of
cosmetics, which parallels human
history.
Are cylindrical in shape and generally
range from 5-25 g.
MEDICATION STICKS
Used for both cosmetics and medical
purposes, includes styptic pencils and lip
balm sticks which became available in the
early 1940’s.
MEDICATION STICKS
Today,________ provide pharmacists, patients and primary care providers with a unique, convenient, relatively stable, easy-to-prepare dosage form for the topical delivery of drugs
medication sticks
are prepared
similar to suppositories except that
the melt is poured into the
administering device, or tube.
MEDICATION STICKS
They come in different sizes and
shapes, are readily transportable,
and can be applied directly to the
affected site of the body.
MEDICATION STICKS
The stick is pushed up from the
bottom or using a screw-type device
to raise the stick.
MEDICATION STICKS
They are generally packaged in an
applicator tube for topical
administration, and the applicator can
be adjusted to continually expose
new, fresh stick from inside the tube
MEDICATION STICKS
It facilitates the passage of therapeutic
quantities of drug substances through the
skin and into the general circulation for their systemic effect.
TRANSDERMAL DRUG DELIVERY SYSTEMS (TDDSs)
The blood concentration needed to
achieve therapeutic efficacy may be
determine by comparative analysis of
patient response to drug blood levels.
It is considered ideal if the drug
penetrates through the skin to the
underlying blood supply without drug buildup in the dermal layers.
TRANSDERMAL DRUG DELIVERY SYSTEMS (TDDSs)
Are designed to deliver a constant and
controlled dosage over extended periods of
time for systemic therapy.
PATCHES
consists of an adhesive material
containing 5% lidocaine, which is applied
to a nonwoven polyester felt backing and
covered with a PET film release liner. The
release liner is removed just prior to
application.
Lidoderm (Lidocaine; Endo) 5% patch
To treat post herpetic neuralgia.
Applied to intact skin to cover the
most painful area. Depending upon
the direction for use, the patient can
apply up to three patches, only once
for up to 12 hours within a 24-hour
period.
PATCHES
Is a dosage form that is suitable for
delivering drugs to the skin. It consists of
a drug that is impregnated into a flexible,
durable woven fabric or extruded synthetic
material that is coated with an adhesive
agent
TAPES
