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Laith J. Abdulredha
1
Suppositories
Contents
Introduction
Classification of suppositories
Advantages & disadvantages
Ideal properties of suppositories
Types of suppository bases
Evaluation of suppositores
2
Introduction
 Suppositories are medicated solid dosage forms
meant to be inserted into the body cavities like
vagina , urethra ,nose, ear and rectum ,where they
melt or soften to release the drugs and exert local or
systemic effects.
 They melt at body temperature , or dissolved in
small amount of fluids in the vaginal , rectal
mucosa
3
Classification Of Suppositories
 Rectal suppositories
 Vaginal suppositories ( PESSARIES )
 Urethral suppositories ( BOUGIES )
 Nasal suppositories
 Ear suppositories
4
VAGINAL SUPPOSITORY
 They are also called as PESSARIES.
 SHAPE : globular, oviform or cone-shaped.
 They are meant for insertion into the vagina
for local effects like contraceptives, anti-
infective etc..
 weight (3 – 5 gm)
5
•URETHRAL SUPPOSITORY
 Also called as BOUGIES .
 SHAPE – slender, pencil-shaped.
 They are meant for insertion into the urethra
for anti-bacterial or as a local anesthetic preparative
for urethral examination.
- male 4 gm
100 – 150 mm
- Female 60 – 75 mm
5 mm diameter
6
 They are meant for insertion into the
rectum for local action to relieve
constipation, irritation, and inflammatory
– 4 gm adult
– 1 gm child
RECTAL SUPPOSITORY
7
Nasal suppositories
 They are meant for the insertion into the
nasal cavity
 They are thin cylindrical in shape
 They are always prepared using the
glycero-gelatin base.
 1 gm
9-10CM long
Ear cone suppositories
 These are meant for introduction into the
ear
 They are long, thin, and cylindrical in
shape
 They weigh about 1gm
Hollow type suppository
 Its drug-containing matrix , hollow part of
the filled liquid or solid substances by
adjusting the opening part to achieve
controlled release
Classification Of Suppositories Via
Position Of Action
LOCAL EFFECT :
 In case of pain, itching and hemorrhoid.
 Locally active drugs include astringents,
antiseptics, local anesthetics, vasoconstrictors,
anti-inflammatory, soothing and protective
agents and some laxatives.
SYSTEMIC EFFECT :
 anti rheumatics, anti-pyretic and analgesics
11
ADVANTAGES
 Self administration
 Easily adminstersd to children, old persons, to
unconscious or sometimes to mentally unstable
persons who cannot swallow the drug.
 Drug that cause irritation to GIT or vomiting
 Avoid first pass effect and GI enzymatic
deactivation or degradation
 Rapid onset of action as compared to oral
administration
 show site specific action and reducing systemic
toxicity
12
DISADVANTAGES
 Patient compliance.
 The manufacturing process is difficult.
 some drugs cause irritation to the
mucous membrane.
 Most of the suppositories should be
stored at low temperature10-20°c in a
refrigerator
 GI state affects absorption (Diarrhea)
13
IDEAL PROPERTIES OF SUPPOSITORY
BASES
 Melts, dissolves, or disperses at 37oC
 It should release any medicament easily.
 keep its shape when being handled.
 non-toxic and non-irritant to the mucous
membrane.
 Chemically inert & Compatible with drugs
 Chemically and physically stable on storage
and also stable if heated above its M.P.
14
Suppository Bases
 Suppository bases may be classified
according to their composition and physical
properties:
1- Oleaginous (fatty) bases
2- Water soluble or miscible bases
IDEAL PROPERTIES OF
SUPPOSITORY BASES
 It should be easily molded and should not
adhere to the mold.
 It should possess good wetting and
emulsifying properties.
 It should be able to incorporate a high
percentage of water.
 It should be chemically and physically stable
16
Formulation of suppositories
1. Bases
2. Anti- oxidants
3. Emulsifying agents
4. Hardening agents
5. Preservatives
6. Thickening agents
7. Plasticizers
17
Suppository Bases
Theobroma oil:-
-Source: crushed roasted seeds of Theobroma
cacao
- Melting point: 30 – 35⁰C
-Suitable for: Rectal suppositories
Disadv.
•Fatty acids can become rancid
•Melt in warm weather
•Liquefy when certain drugs are incorporated
• Polymorphism
Fatty bases
Emulsifying bases
 These are synthetic fatty bases
Witepsol:
 It consist of triglycerides of saturated
vegetable fatty acids and partial esters
Massa estarinum:
 is a mixture of mono, di and triglycerides of
unsaturated fatty acids.
Massupol:
 It consist of glyceryl esters of lauric acid with
small amount of glyceryl stearate to improve
water absorbing capacity
Advantages of Witepsol:
a- Their solidifying points are unaffected by overheating.
b- They have good resistance to oxidation
c- They are marketed in a series of grades with different
melting point ranges.
d-They contain a proportion of w/o emulsifying agents,
and therefore, their water-absorbing capacities are
good.
e- No mould lubricant is necessary because they
contract significantly on cooling.
f- They are less liable to get rancid.
Water soluble bases
Glycero-gelatin base:
 Mixture of glycerin and water made stiff by
addition of gelatin
 Used to prepare all type of Suppositories but
practically most suitable for pessaries
 Prepared suppositories are translucent.
 They dissolve slowly and release medicament
DISADVANTAGES:
1 - Osmosis occurs during dissolving in the mucous
secretions of the rectum, producing a laxative effect.
2 - Can cause rectal irritation due to small amount of
liquid present.
3 - Hygroscopic: So, they should be packaged in tight
containers
4 - Microbial contamination likely.
5 - Long preparation time.
6 - Lubrication of the mould is essential.
7 - Glycerinated gelatin suppositories lose moisture in
dry climates and absorbs moisture in high humidity
Water soluble bases
Polyethylene glycols are synthetic polymers of ethylene
oxide and water
 The chain length may be varied to achieve polymers
having desired viscosity and physical (liquid, semisolid,
or solid) form.
 The general formula for this base calls for the
combining of polyethylene glycol 3350(a solid) and
polyethylene glycol 400 (a liquid) to prepare base
 Polyethylene glycol suppositories do not melt at body
temperature but rather dissolve slowly in the body's
fluids
 Test of appearance
 Test of physical strength (breaking )
 Test of dissolution rate
 Test of melting range
 Test of softening time
 Test of uniformity of drug content
 Test of drug uptake
Thank you

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Suppository

  • 2. Contents Introduction Classification of suppositories Advantages & disadvantages Ideal properties of suppositories Types of suppository bases Evaluation of suppositores 2
  • 3. Introduction  Suppositories are medicated solid dosage forms meant to be inserted into the body cavities like vagina , urethra ,nose, ear and rectum ,where they melt or soften to release the drugs and exert local or systemic effects.  They melt at body temperature , or dissolved in small amount of fluids in the vaginal , rectal mucosa 3
  • 4. Classification Of Suppositories  Rectal suppositories  Vaginal suppositories ( PESSARIES )  Urethral suppositories ( BOUGIES )  Nasal suppositories  Ear suppositories 4
  • 5. VAGINAL SUPPOSITORY  They are also called as PESSARIES.  SHAPE : globular, oviform or cone-shaped.  They are meant for insertion into the vagina for local effects like contraceptives, anti- infective etc..  weight (3 – 5 gm) 5
  • 6. •URETHRAL SUPPOSITORY  Also called as BOUGIES .  SHAPE – slender, pencil-shaped.  They are meant for insertion into the urethra for anti-bacterial or as a local anesthetic preparative for urethral examination. - male 4 gm 100 – 150 mm - Female 60 – 75 mm 5 mm diameter 6
  • 7.  They are meant for insertion into the rectum for local action to relieve constipation, irritation, and inflammatory – 4 gm adult – 1 gm child RECTAL SUPPOSITORY 7
  • 8. Nasal suppositories  They are meant for the insertion into the nasal cavity  They are thin cylindrical in shape  They are always prepared using the glycero-gelatin base.  1 gm 9-10CM long
  • 9. Ear cone suppositories  These are meant for introduction into the ear  They are long, thin, and cylindrical in shape  They weigh about 1gm
  • 10. Hollow type suppository  Its drug-containing matrix , hollow part of the filled liquid or solid substances by adjusting the opening part to achieve controlled release
  • 11. Classification Of Suppositories Via Position Of Action LOCAL EFFECT :  In case of pain, itching and hemorrhoid.  Locally active drugs include astringents, antiseptics, local anesthetics, vasoconstrictors, anti-inflammatory, soothing and protective agents and some laxatives. SYSTEMIC EFFECT :  anti rheumatics, anti-pyretic and analgesics 11
  • 12. ADVANTAGES  Self administration  Easily adminstersd to children, old persons, to unconscious or sometimes to mentally unstable persons who cannot swallow the drug.  Drug that cause irritation to GIT or vomiting  Avoid first pass effect and GI enzymatic deactivation or degradation  Rapid onset of action as compared to oral administration  show site specific action and reducing systemic toxicity 12
  • 13. DISADVANTAGES  Patient compliance.  The manufacturing process is difficult.  some drugs cause irritation to the mucous membrane.  Most of the suppositories should be stored at low temperature10-20°c in a refrigerator  GI state affects absorption (Diarrhea) 13
  • 14. IDEAL PROPERTIES OF SUPPOSITORY BASES  Melts, dissolves, or disperses at 37oC  It should release any medicament easily.  keep its shape when being handled.  non-toxic and non-irritant to the mucous membrane.  Chemically inert & Compatible with drugs  Chemically and physically stable on storage and also stable if heated above its M.P. 14
  • 15. Suppository Bases  Suppository bases may be classified according to their composition and physical properties: 1- Oleaginous (fatty) bases 2- Water soluble or miscible bases
  • 16. IDEAL PROPERTIES OF SUPPOSITORY BASES  It should be easily molded and should not adhere to the mold.  It should possess good wetting and emulsifying properties.  It should be able to incorporate a high percentage of water.  It should be chemically and physically stable 16
  • 17. Formulation of suppositories 1. Bases 2. Anti- oxidants 3. Emulsifying agents 4. Hardening agents 5. Preservatives 6. Thickening agents 7. Plasticizers 17
  • 19. Theobroma oil:- -Source: crushed roasted seeds of Theobroma cacao - Melting point: 30 – 35⁰C -Suitable for: Rectal suppositories Disadv. •Fatty acids can become rancid •Melt in warm weather •Liquefy when certain drugs are incorporated • Polymorphism Fatty bases
  • 20. Emulsifying bases  These are synthetic fatty bases Witepsol:  It consist of triglycerides of saturated vegetable fatty acids and partial esters Massa estarinum:  is a mixture of mono, di and triglycerides of unsaturated fatty acids. Massupol:  It consist of glyceryl esters of lauric acid with small amount of glyceryl stearate to improve water absorbing capacity
  • 21. Advantages of Witepsol: a- Their solidifying points are unaffected by overheating. b- They have good resistance to oxidation c- They are marketed in a series of grades with different melting point ranges. d-They contain a proportion of w/o emulsifying agents, and therefore, their water-absorbing capacities are good. e- No mould lubricant is necessary because they contract significantly on cooling. f- They are less liable to get rancid.
  • 22. Water soluble bases Glycero-gelatin base:  Mixture of glycerin and water made stiff by addition of gelatin  Used to prepare all type of Suppositories but practically most suitable for pessaries  Prepared suppositories are translucent.  They dissolve slowly and release medicament
  • 23. DISADVANTAGES: 1 - Osmosis occurs during dissolving in the mucous secretions of the rectum, producing a laxative effect. 2 - Can cause rectal irritation due to small amount of liquid present. 3 - Hygroscopic: So, they should be packaged in tight containers 4 - Microbial contamination likely. 5 - Long preparation time. 6 - Lubrication of the mould is essential. 7 - Glycerinated gelatin suppositories lose moisture in dry climates and absorbs moisture in high humidity
  • 24. Water soluble bases Polyethylene glycols are synthetic polymers of ethylene oxide and water  The chain length may be varied to achieve polymers having desired viscosity and physical (liquid, semisolid, or solid) form.  The general formula for this base calls for the combining of polyethylene glycol 3350(a solid) and polyethylene glycol 400 (a liquid) to prepare base  Polyethylene glycol suppositories do not melt at body temperature but rather dissolve slowly in the body's fluids
  • 25.  Test of appearance  Test of physical strength (breaking )  Test of dissolution rate  Test of melting range  Test of softening time  Test of uniformity of drug content  Test of drug uptake