COLON DRUG DELIVERY SYSTEM

BY, KEERTHIVARDHAN.D M-PHARM 2nd SEMESTER

CONTENTS: INTRODUCTION.

POTENTIAL APPLICATIONS OF CDDS.

ANATOMY & PHYSIOLOGY OF COLON. FACTORS GOVERNING THE CDDS. PHARMACEUTICAL APPROACHES FOR

TARGETING DRUG TO COLON. RATIONALE FOR COLONIC DRUG DELIVERY SYSTEM. ADVANTAGES. DISADVANTAGES. CONCLUSION.

INTRODUCTION
Definition:-Colon drug delivery system refers to

targeted delivery of drug in to the lower parts of GI tract , mainly large intestine.

POTENTIAL APPLICATIONS OF CDDS

Chronotherapy. Prophylaxis of colon cancer. Treatment of nicotine addiction. Potential site for the systemic delivery of therapeutic

proteins & peptides.

Potential side affects can be reduced. Drug instability problems also reduced.

ANATOMY & PHYSIOLOGY OF CDDS

Longest & Most mobile par Diameter 6cm.

LAYERS OF COLON

Contd

Major part

External coat of large intestine MAJOR FUNCTIONS OF COLON Create suitable environment for colonic microorganisms. Storage reservoir of faecal matter . Expulsion of the contents of the colon. Absorption of potassium & Water from the lumen

FACTORS GOVERNING THE COLON DRUG DELIVERY SYSTEM

Gastro intestinal transit time. PH along GIT . Colonic Micro Flora. Drug absorption in the colon. GIT disease state.

Gastro intestinal transit time.

The arrival of oral dosage form at the colon is determined by the

rate of gastric emptying & small intestinal transit time.

Gastric emptying of dosage form is highly variable depends

on. Subject Fed / fasted. Properties of dosage form.(Size & Density). Food increases gastric residence, some cases with regular feeding dosage forms residence in creases 12hrs.

PH along GIT .
Large PH variation along GIT.

STOMACH-1-2PH(During fasting) 6PH(After

eating , in feed) RIGHT COLON-6-4. MID COLON- 6.6. LEFT COLON -7

Colonic Micro Flora.

GIT Aerobic & Anaerobic bacteria. Upper region small number of bacteria (Gm+ve bacteria). Proximal areas high concentration of energy sources. COLONIC MICRO FLORA Eubacterium. Peptococcus. Peptostreptococcus. Clostridium. E.coli Lactobasillus etc., STOMACH-0-103CFU/ml JEJUNUM-0-105CFU/ml ILEUM-103-107CFU/ml COLON-1011-1012CFU/ml

 Pro drug
Azo reductase

Active Drug

Lacto bacillus. Bacteroids. Bifido bcteria

Glycosidase. Glucouronidase.

NORMAL CONDITIONS

DISEASE STATE

Composition , function, population Varies its composition , function, populat are constant

Drug absorption in the colon.

Hydrophilic drugs

Lipophilic drugs

Colon contentsMore viscous with progressive absorption of water & delays the diffusion of dr from the lumen to mucosa. Colonic epithelial permeability modified by enhancers. DISRUPTION. Ex:-Ca+2 EDTA, Saponins,Bile salts, Fatty acids. MODIFICATION. MODIFICATION & DISRUPTION

GIT disease state.

IBD.

Crohns disease.
Constipation. Diarrhea. Gastro Enteritis.

Affect the release & absorption properties of CSDDS

APPROACHES FOR TARGETING DRUG TO COLON

Pro drug based approach.

Polymer based approach.

PLAT FORM TECHNOLOGIES FOR CTDDS PULSINCAP SYSTEM. OROS CT SYSTEM. CODES SYSTEM. CHRONOTROPIC SYSTEM.

Pro drug based approach.

AzoBond Prodrug.

EX:- sulphasalazine.( Anti-inflamatory &

Rheumatoid arthritis).
Sulphasalazine =Sulphapyridine & 5-ASA

Polymer based approach.

PH SENSITIVE POLYMER SYSTEM
PH SENSITI VE LAYER

DRUG CORE

COLON PH

PULSINCAP SYSTEM.

PLUG MADE UP OF Polymethacrylates, HPMC, PVA.

OROS CT SYSTEM.

DRUG + EXCIPIENT

Phthalates, Keratin, Formalin treated protein oil, anionic polymers

CODES SYSTEM.

PORT SYSTEM

The Chronotropic System

RATIONALE FOR COLONIC DRUG DELIVERY SYSTEM

Local treatment of inflammatory

diseases(Ulcerative colitis).
Local treatment of colonic diseases.(Ameobiasis). Oral delivery of peptide & protein drug. Colon targeting can also be done for drugs which

are not suitable in the acidic environment of the stomach.(Aspirin, Iron supplements.)

ADVANTAGES
Drug directly available at the target site. Decreased dose of administration. Decreased side effect. Long time residence.

DISADVANTAGES
TIME DEPENDENT SYSTEMS:

Substantial variation in the gastric retention times.

Transit through colon is more rapid in the normal

than in patients with colon disease. PH DEPENDENT SYSTEMS: PH level in the small intestine & colon vary b/w & with in the individuals. MICROFLORA ACTIVATED SYSTEM: Diet & disease can affect colonic microflora.

REFERENCES
1.Philip AK, Dabas S, Pathak K. Optimized prodrug approach: A means

for achieving enhanced anti-inflammatory potential in experimentally induced colitis. J Drug Target 2009; 17:235-241. 2.Oluwatoyin AO, John TF. In vitro evaluation of khaya and albizia gums as compression coating for drug targeting to the colon. J Pharm Pharmacol 2005; 57: 63-168. 3.Chourasia MK, Jain S K. Pharmaceutical approaches to colon targeted drug delivery systems. J Pharm Sci 2003; 6:33-66. 4.Watts P, Illum L. Colonic drug delivery. Drug Dev Ind Pharm 1997; 23:893- 913.

Technology or design alone do not make a successful product. Technology needs to be implemented in an appropriate design for a successful product.