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A
PRESENTATION
ON

PHARMACEUTICAL APPROACHES TO COLON
TARGETED DRUG DELIVERY SYSTEM

Presented by: RAJ KISHOR
Tech Observe...
-:CONTENTS:
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Introduction
Anatomy and Physiology of colon
Factors governing Colonic drug delivery
Str...
INTRODUCTION
 Oral route is considered to be most convenient for administration of
drug to patient.
 Colon is used as si...
ADVENTAGES
 The site specific delivery of drug to lower part of GIT,
for localized treatment of several colonic diseases....
 Disadvantages
 Substantial variation in gastric retention time may
affect drug delivery.
 Diseased condition may affec...
ANATOMY AND PHYSIOLOGY OF COLON
 Location-in abdominal cavity
 Made up of Serosa – areolar tissue.
 Muscularis externa...
7
Contd…

 Ascending colon
 Transverse colon
 Descending colon
 Sigmoid colon

8
THE PH RANGES OF GIT

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Length and internal diameter colon & small intestine

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FUNCTION OF COLON

 Provides suitable environment for the growth of colonic
microorganisms,


Absorption of water and Na...
DISORDERS OF COLON
 Ulcerative colitis.
 Inflammatory bowel disease (IBD).
 Chron’s disease.
 Colo-Rectal cancer.
 Ot...
Continue…

13
FACTORS GOVERNING COLONIC DRUG DELIVERY
 Physiological Factors:Small intestinal transit
Colonic transit
Gastric emptyi...
Strategies for targeting Drug to colon
 An oral colonic delivery system should retard drug release
in the stomach and sma...
Continue…
 The most commonly used targeting mechanisms
are: pH – dependent delivery
 Time - dependent delivery
 Pressu...
TARGETING APPROACHES TO COLON
 The various targeting Approaches of orally administered
drugs to the colon include:(1)Cova...
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1.Covalent linkage of the drug with a carrier
 It involves the formation of a covalent linkage between
drug and carrier i...
1Azo bond conjugates-Drug is conjugated via azo bo

21
Similarly
 1.2. Glycoside conjugates:- Drug is
conjugated with Glycoside.
 1.3. Glucuronide conjugates:-Drug is
conjugat...
2 Approaches to deliver the intact molecule to colon

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2.1.Coating with polymers .
2.1.1. Coating wi...
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Biodegradable poly saccharides

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 Osmotically controlled colon targeted drug delivery
 Target the drug locally to
the colon
 Single or 5-6 push-pull
uni...
EVALUATION OF COLON TARGETED
DRUG DELIVERY

30
MARKETED PREPERATION

MARKETED PRODUCT

31
32
CONCLUSION

33
34
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''Pharmaceutical Approaches to colon Targeted Drug Delivery system'', Presented By: Raj Kishor [CRC] , Tech Observer iNDIA Pvt. Ltd ...The Global CRO

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''Pharmaceutical Approaches to colon Targeted Drug Delivery system'', Presented By: Raj Kishor [CRC] , Tech Observer iNDIA Pvt. Ltd ...The Global CRO

Published in: Business, Technology

''Pharmaceutical Approaches to colon Targeted Drug Delivery system'', Presented By: Raj Kishor [CRC] , Tech Observer iNDIA Pvt. Ltd ...The Global CRO

  1. 1. A PRESENTATION ON PHARMACEUTICAL APPROACHES TO COLON TARGETED DRUG DELIVERY SYSTEM Presented by: RAJ KISHOR Tech Observer India Pvt. Ltd The Global CRO Email ID-raryan859@gmail.com 1
  2. 2. -:CONTENTS:           Introduction Anatomy and Physiology of colon Factors governing Colonic drug delivery Strategies for Targeting drug to colon Targeting Approaches to colon Evaluation of C.T.D.D.S Marketed Preparation Applications Future Prospects Conclusion References 2
  3. 3. INTRODUCTION  Oral route is considered to be most convenient for administration of drug to patient.  Colon is used as site of Targeted drug delivery.  Colon was considered as a BLACK-BOX , as most of the drug are absorbed from the upper part of the GI tract.  Prime objective-Beneficial in the treatment of colon diseases. Increase the pharmacological activity. Reduce dosing & side effects. Prevent drug from degradation. 3
  4. 4. ADVENTAGES  The site specific delivery of drug to lower part of GIT, for localized treatment of several colonic diseases. (ulcerative colitis, Chron's disease, carcinomas and infections)  Prevent drug from degradation     Ensure direct treatment at disease site. Suitable absorption site for Protein & Peptide drug. Used to prolong the drug therapy. Improved drug utilization. 4
  5. 5.  Disadvantages  Substantial variation in gastric retention time may affect drug delivery.  Diseased condition may affect the colonic transit time and drug release profile.  pH level of colon may vary between individuals due to disease, state and temperature of food consumed. 5
  6. 6. ANATOMY AND PHYSIOLOGY OF COLON  Location-in abdominal cavity  Made up of Serosa – areolar tissue.  Muscularis externa – muscular coat.  Submucosa – connective tissue.  Mucosa – epithelium. 6
  7. 7. 7
  8. 8. Contd…  Ascending colon  Transverse colon  Descending colon  Sigmoid colon 8
  9. 9. THE PH RANGES OF GIT 9
  10. 10. Length and internal diameter colon & small intestine 10
  11. 11. FUNCTION OF COLON  Provides suitable environment for the growth of colonic microorganisms,  Absorption of water and Na+ from the lumen, concentrating the fecal content, Secretion of K+ ions,  Storage reservoir of faecal contents,  Expulsion of the contents of the colon at an appropriate time. 11
  12. 12. DISORDERS OF COLON  Ulcerative colitis.  Inflammatory bowel disease (IBD).  Chron’s disease.  Colo-Rectal cancer.  Others as amebiasis & Diarrhoea. 12
  13. 13. Continue… 13
  14. 14. FACTORS GOVERNING COLONIC DRUG DELIVERY  Physiological Factors:Small intestinal transit Colonic transit Gastric emptying Stomach and intestinal pH Colonic micro flora and enzymes  Pharmaceutical factors….(a)Drug candidates (b)Drug carrier 14
  15. 15. Strategies for targeting Drug to colon  An oral colonic delivery system should retard drug release in the stomach and small intestine but allow complete release in the colon.  A variety of strategies has been used and systems have been developed for the purpose of achieving colonic targeting .  These strategies are either drug specific ( prodrug ) or formulation –specific (coated or matrix preparation). 15
  16. 16. Continue…  The most commonly used targeting mechanisms are: pH – dependent delivery  Time - dependent delivery  Pressure- dependent delivery and  Bacteria—dependent delivery 16
  17. 17. TARGETING APPROACHES TO COLON  The various targeting Approaches of orally administered drugs to the colon include:(1)Covalent linkage of a drug with a carrier. (2)Coating with pH-sensitive polymers. (3)Formulation of timed released systems. (4) Exploitation of carriers that are degraded specifically by colonic bacteria. (5) bioadhesive systems and osmotic controlled drug delivery systems 17
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  20. 20. 1.Covalent linkage of the drug with a carrier  It involves the formation of a covalent linkage between drug and carrier in such a manner that upon oral administration the moiety remains intact in the stomach and small intestine.  This approach chiefly involves the formation of prodrug, which is a pharmacologically inactive derivative of a parent drug molecule that requires spontaneous or enzymatic transformation in the biological environment to release the active drug. 20
  21. 21. 1Azo bond conjugates-Drug is conjugated via azo bo 21
  22. 22. Similarly  1.2. Glycoside conjugates:- Drug is conjugated with Glycoside.  1.3. Glucuronide conjugates:-Drug is conjugated with Glucuronide.  1.4.Cyclodextrinconjugates:-Drug is conjugated with cyclodextrin.  1.5. Dextran conjugates:-Drug is conjugated with dextrin.  1.6. Amino-acid conjugates:-Drug is conjugated with amino acid. 22
  23. 23. 2 Approaches to deliver the intact molecule to colon            2.1.Coating with polymers . 2.1.1. Coating with pH-sensitive polymers 2.1.2. Coating with biodegradable polymers 2.2 Embedding in matrices 2.2.1. Embedding in biodegradable matrices and hydro gels 2.2.2. Embedding in pH-sensitive matrices 2.3. Timed release systems 2.4Redox-sensitive polymers 2.5. Bioadhesive systems 2.6. Coating with micro particles 2.7. Osmotic controlled drug delivery 23
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  28. 28. Biodegradable poly saccharides 28
  29. 29.  Osmotically controlled colon targeted drug delivery  Target the drug locally to the colon  Single or 5-6 push-pull units  Contains an osmotic push layer and a drug layer  Surrounded by a semi permeable membrane  Orifice is drilled through the membrane next to the drug layer 29
  30. 30. EVALUATION OF COLON TARGETED DRUG DELIVERY 30
  31. 31. MARKETED PREPERATION MARKETED PRODUCT 31
  32. 32. 32
  33. 33. CONCLUSION 33
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