Suppositories

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Suppositories
a Latin word “supponere” meaning “to place
under”, as derived from
sub=under and ponere=to place

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Definition
 “Solid or semi-solid dosage form of various weights and
shapes, usually medicated , intended for insertion into the
body orifices/ cavities like rectum, vagina or urethra ,where
they soften, melt, disperse or dissolve in the cavity fluid.”
 It is prepared from such a base which is solid at room
temperature and melts at body temperature.
 The shape is like pencil, cylindrical, conical or torpedo.
 Local or systemic effects.
They have various shapes and weights(usually 1-4 gram).
The drug content varies from 0.1% up to almost 40%
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Advantages of suppositories
 Available for Patients who can not swallow medications. e.g.:
Baby / Geriatric ….
 When oral administration of a drug is not suitable as in infants
or patients suffering from nausea, vomiting and gastrointestinal
disturbances; suppositories serve as an alternate for drug
administration.
 Drug with GI irritation problems.
 For some drug which act locally.
 Avoid of Hepatic first pass metabolism.
 Dugs inactivated /destroyed by GIT
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Disadvantages
 Un-comfort

 Variation of Absorption

 Irritation for mucous caused by some drugs

or bases

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On the basis of their uses these are classified as

1. Rectal suppositories
2. Vaginal suppositories/pessaries
3. Urethral suppositories/bougies
4. Nasal suppositories /nasal bougies
5. Ear cones/aurinaria
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1.Rectal suppositories unioffaisalabad

 meant for insertion into the rectum.

Shape: (1.5 in.) long, are cylindrical, and have one or both ends tapered.
Weight: Weight is 2g for adult and for children half of adult dose.
weight may vary Depending upon
 The density of base
 and medicament.

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Rectal
Uses:
suppositories:-
For systemic action
 sedative ,tranquillizers, and analgesic
Locally
 to treat constipation ,pain ,inflammations, in condition
of piles or hemorrhoids remedy

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2.Vaginal suppositories
meant for insertion into vagina.
Also called as Pessaries.

Shape:- Globular, oviform, or cone-shaped and

weigh about 5 g when cocoa butter is the base.
Uses:
 For local effect
as contraceptives, antiseptics in feminine
hygiene, vaginitis 9
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3.Urethral suppositories
meant to introduce into urethra .
Also called as Bougies.
Types:
Male urethral suppositories. 3 to 6 mm in
diameter and approximately 140 mm long with 4g weight.
Female urethral suppositories. 3 to 6 mm in
diameter and approximately 70 mm long with 2g weight.
•Uses:
 Antibacterial or local anesthetics 11
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Components of suppositories
Solid dosage forms
consist of

1. Active ingredient
2. Base
3. Additives

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Physicochemical factors
• Physicochemical factors of the drug and suppository base
affecting rectal absorption are
 Drug solubility in vehicle
 Particle Size
 Nature of the base
 Spreading Capacity
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Drug solubility in vehicle

• The rate at which a drug is released from a suppository and
absorbed by the rectal mucous membrane is directly related to
its solubility in the vehicle or, in other words, to the partition
coefficient of the drug between the vehicle and the rectal
liquids
• .When drugs are highly soluble in the vehicle the tendency to
leave the vehicle will be small and so the release rate into the
rectal fluid will be low
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Particle size

• For drugs present in a suppository in the undissolved

state, the size of the drug particle will influence its
rate of dissolution and its availability for absorption.
• The smaller the particle size the more readily the
dissolution of the particle the greater chance for rapid
absorption
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Nature of the base

• The base must be capable of melting, softening, or dissolving to
release its drug components for absorption.
• If the base interacts with the drug inhibiting its release drug
absorption will be impaired or even prevented. Also, if the base
is irritating to the mucous membranes of the rectum it may
initiate a colonic response and a bowel movement incomplete
drug release and absorption.
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Spreading Capacity
• The rapidity and intensity of the therapeutic effects of suppositories are related to the
surface area of the rectal mucous membrane covered by the melted base
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Classification Of Suppository Bases

• Fatty or Oleaginous bases
• Water soluble and water miscible Bases
• Miscellaneous Bases
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I)Fatty or Oleaginous bases

• Fatty bases in use now a days are almost exclusively semi synthetic or
fully synthetic.
• In a fatty base lipophilic or hydrophillic drug is dispersed.
• Among the fatty materials used in suppository bases are many
hydrogenated fatty acids of vegetable oil such as
 cotton seed oil
 Palm kernel oil
 Glyceryl mono palmitate
 Glyceryl mono sterate are found in fatty bases.
• These bases in many commercial products are used to achieve desired
hardness ,desired property of melting and softening of suppository .
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Cocoa butter
Fat obtained from roasted seed of theobroma
cocoa . Properties:
 Yellowish white solid at room temperature
 A triglyceride (combination of glycerin & one or
different fatty acids)
 Melts at 30 – 36 ⁰C ,
 Melts at body temp: easily,
 liquefies on heating easily
 solidifies at room temp:
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• Now ,Cocoa Butter is no longer used as a

suppository base because of its many
disadvantages.Such as
o Its well known polymorphic behavior
o low softening point
o poor water absorptive property
• other bases includes Fattibase ,Wecobee
base ,and witepsol base.
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ii)Water soluble and water miscible Bases

The main members of this group are
• Glycerinated gelatin
• Polyethylene glycols(PEG).
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Glycerinated gelatin
• Glycerinated gelatin may be prepared by dissolving 20%
granular gelatin in 70% glycerine and adding water,or
suspension of 10% medicaments.
• Urethral suppositories may be prepared by dissolving 60%
granular gelatin in 20% glycerine and adding water,or
suspension of 20% medicaments.
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Advantages
• It is most frequently used in preparation of vaginal suppositories with in
which prolonged action of medicinal agent is required.
• This base is slower to soften and mix with the surrounding aqueous fluid
and slower to release medicinal agent
• Provide prolonged effect
Disadvantages
 Glycerinated gelatin based suppositories are hygroscopic in nature ,so
their should be enough water in suppository base or it should be moistened
prior to insertion in an order to avoid
 Dehydration of mucous membrane
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Polyethylene glycols(PEG)
• These are polymers of ethylene oxide and water prepared to various chain
lengths,molecular weights and physical states.
• Their molecular weight ranges 300, 400, 600, 1000 ,1500, 1540, 3350, 4000,6000 &
8000 .
• These bases do not melt readily at body temprature but rather dissolve slowly in the
body fluids.
• In preparation of PEG base melting point can be higher than body
Advantages
• These bases are not moistened prior to insertion in the body in order to avoid
mucosal irritation,
• No leakage of drug from body orifices .
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iii)Miscellaneous Bases
• These are mixture of oleaginous and water soluble bases.These may be physical or
chemical mixture.
• These are mixture of many fatty acids with emulsifying agent capable of forming
water in oil emulsions.
• For Example Polyoxal sterate 40.
o These bases have an intermediate drug releasing tendency (for hydrophillic and
hydrophobic drug) into surrounding aqueous fluid