colon targeted metronidazole matrix tablet

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matrix tablet of metronidazole seminar for thesis

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FORMULATION & EVALUATION OF ENTERIC COATED MATRIX TABLET OF METRONIDAZOLE FOR COLON TARGETing: 

FORMULATION & EVALUATION OF ENTERIC COATED MATRIX TABLET OF METRONIDAZOLE FOR COLON TARGETing By : Mr.Jawalkoti Sunil P. M.Pharm (2 nd year) Guided by Mr.Prakash Jadhav (Dept.of pharmaceutics) ARVIND GAVALI COLLEGE OF PHARMACY,SATARA.

contents: 

contents INTRODUCTION LITERATURE SURVEY NEED OF WORK PLAN OF WORK SELECTION OF DRUG & POLYMER METHOD OF PREPARATION EVALUATION & EQUIPMENT COLON TARGETED DRUG DELIVERY SYSTEM 2

INTRODUCTION Anatomy & Physiology of Colon : 

INTRODUCTION Anatomy & Physiology of Colon COLON TARGETED DRUG DELIVERY SYSTEM 3 GIT: Stomach Small intestine Large intestine COLON: Colon Rectum Anal canal Colon consists: Ceacum Ascending colon Transverse colon Descending colon Sigmoid colon

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Lag Phase of 5 hrs. observed COLON TARGETED DRUG DELIVERY SYSTEM

Disorders of Colon: 

COLON TARGETED DRUG DELIVERY SYSTEM 5 Disorders of Colon AMOEBIASIS

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Ulcerative colitis Inflammatory bowels disease (IBD) Crohn’s disease Colonic polyps Colorectal cancer Diarrhoea etc. COLON TARGETED DRUG DELIVERY SYSTEM 6

LITERATURE SURVEY: 

LITERATURE SURVEY Ma Gauda M et al Design evaluation studies on colon specific ciprofloxacin matrix tablet for IBD treatment almond gum could be used for development of colon matrix tablets of ciprofloxacin hydrochloride. The matrix tablet containing almond gums was susceptible to bacterial degradation. Bala venkata pradeep Et al Development of enteric coated pectin matrix tablet of metronidazole for colon targeting. Formulation & in vitro evaluation of microbially triggered colon specific drug delivery using sesbania gum Formulation & in vitro evaluation of dextrin matrix tablet of Ibuprofen for colon targeted drug delivery COLON TARGETED DRUG DELIVERY SYSTEM 7

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Hiren patel Et Al.Development & in vitro evaluation of colon specific coated matrix tablet of metronidazole Y.S.R.krishnaiah Et Al.Development of colon targeted drug delivery system for mebendazole Clement jackson Et Al.Use of xanthan gum & ethyl cellulose in the formulation of metronidazole for colon drug delivery Jitendra R. Et Al Chitosan – chondroitin sulphate matrix tablet for colon specific delivery of Indomethacin COLON TARGETED DRUG DELIVERY SYSTEM 8

Need OF the work: : 

Need OF the work : Colon as a promising site for drug delivery. Colon was considered as BLACK-BOX as most of the drugs are absorbed from upper part of the GI tract. Local disorders Systemic absorption Drugs unstable in upper GIT Drugs poorly absorbed from GIT Drugs that necessitate targeting at site COLON TARGETED DRUG DELIVERY SYSTEM 9

PLAN OF WORK: 

PLAN OF WORK Compatability study (FTIR) The goal is utilization of carriers that are degraded exclusively by colonic bacteria/pH depended polymers. Preformulation studies on the drug Selection and Screening of appropriate biodegradable polysaccharides/pH depended polymers. Preparation of granules and study of precompression parameters. Preparation of the dosage form and study of post compression parameters. Coating of matrix tablet Evaluation of granules Tablet evaluation COLON TARGETED DRUG DELIVERY SYSTEM 10

SELECTION OF DRUG: 

SELECTION OF DRUG Metronidazole COLON TARGETED DRUG DELIVERY SYSTEM 11 Pharmacokinetic data B ioavailability 100% (oral) 59–94% (rectal) Metabolism Hepatic Half-life 6–7 hours Excretion Renal (60-80%), biliary (6–15%)

Routes….. Oral , I/V infusion, topical gel, cream . Absorption ----- almost complete from GIT, colon. Distribution------- Rapid & wide. Distributed to all tissues & high concentrations in body fluids– CSF, Vaginal secretions ,saliva, semen Adverse Effects GIT: Dry mouth, metallic taste --- most common. Nausea, anorexia, abdominal cramps , Diarrhea. Neurotoxicity: Headache, Insomnia, numbness or paraesthesias , dizziness Rarely glossitis,neutropenia,rash, seizures. Disulfiram like action with alcohol.

Therapeutic Uses: 

Therapeutic Uses Amoebiasis : - Acute intestinal Amoebiasis / Amoebic colitis with dysentery -Mild intestinal amoebiasis - Hepatic Amoebiasis Giardiasis Trichomoniasis Bacterial vaginosis Eradication of H. Pylori in Peptic ulcer Pseudomembranous enterocoliti s

selection of polymer approch of colon targeting with the aid of polysaccharide: 

selection of polymer approch of colon targeting with the aid of polysaccharide Polysaccharides offer an alternative substrate for the bacterial enzymes present in the colon. Most of them are hydrophilic in nature. Natural polysaccharides are either modified or mixed with water insoluble polymers. 14

Polysaccharides used for Colon Drug Delivery: 

Polysaccharides used for Colon Drug Delivery Chitosan Pectin Guar gum Chondroitin sulphate Dextran COLON TARGETED DRUG DELIVERY SYSTEM 15 Cyclodextrins Almond gum Locust bean gum Inulin Boswellia gum Karaya gum

Enzymes in Colon: 

Enzymes in Colon Reducing enzymes Nitroreductase Azoreductase N-oxide reductase Sulphoxide reductase COLON TARGETED DRUG DELIVERY SYSTEM 16 Hydrolytic enzymes Esterases Amidases Glycosidases Glucuronidase Sulfatase Azoreductases, which reduces azo-bonds selectively. Polysaccharidases, which degrades the polysaccharides

METHOD OF PREPARATION Pharmaceutical Approaches for Targeting Drugs to Colon : 

pH sensitive system Time release systems Microbially triggered systems Prodrugs Hydrogel Polysaccharide based system Osmotically controlled drug delivery systems Pressure dependent release systems METHOD OF PREPARATION Pharmaceutical Approaches for Targeting Drugs to Colon COLON TARGETED DRUG DELIVERY SYSTEM 17

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pH dependent system Mechanism of action pH sensitive polymer + drug core DRUG CORE Colonic pH Release of drug in Colon Formulated as solid dosage forms and coated with pH sensitive polymer as in enteric coating. polymers which are available are methacrylic resins ( Eudragits ), Hydroxy propyl methyl cellulose phthalate .

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Polymer Threshold pH Eudragit ® L 100 6.0 Eudragit ® S 100 7.0 Eudragit ® L –30D 5.6 Eudragit ® FS 30D 6.8 Eudragit ® L 100-55 5.5 Polyvinyl acetate phthalate 5.0 Hydroxy propyl methyl cellulose phthalate 4.5-4.8 Hydroxy propyl methyl cellulose phthalate 50 5.2 HPMC 55 5.4 Cellulose acetate trimelliate 4.8 Cellulose acetate phthalate 5.0 COLON TARGETED DRUG DELIVERY SYSTEM 19 Polymer of methacrylic acid are mostly used

Microbialy Triggered Systems: 

Microbialy Triggered Systems Bacterial count in the colon is much higher around 10 11 -10 12 CFU/ml. 400 species Fundamentally anaerobic in nature. Predominant species: Bacteroides, Bifidobacterium and Eubacterium . Major metabolic processes occurring in the colon are hydrolysis and reduction . COLON TARGETED DRUG DELIVERY SYSTEM 20

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21 # Matrix Type Tablet Also called as Monolith dissolution controlled system. Controlled dissolution by: 1.Altering porosity of tablet. 2.Decreasing its wettability. 3.Dissolving at slower rate. First order drug release. Drug release determined by dissolution rate of polymer. Examples: Soluble drug Slowly dissolving matrix

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COLON TARGETED DRUG DELIVERY SYSTEM 22 The technique involved in enteric coating is protection of the tablet core from disintegration in the acidic environment of the stomach by employing pH sensitive polymer, which swell or solubilize in response to an increase in pH to release the drug. Aims of Enteric protection: To mask taste or odour Protection of active ingredients, from the acidic environment of the stomach. Protection from local irritation of the stomach mucosa. Release of active ingredient in specific target area within colon. ENTERIC COATING

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23 Tablet Coating Dissolution rate of coat depends upon thickness of coating. Examples:pH dependant polymer Eudragit S-100 Soluble drug Slowly dissolving or pH dependanterodible coat PAN COATING

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Enteric coated matrix tablet Enteric coated matrix tablet in upper GI Solublization of enteric coat and swelling of inner matrix followed by degradation by colonic bacteria Degradation of swelled matrix tablet and drug release Behaviour of Enteric-coated Matrix Tablet Colonic bacteria COLON TARGETED DRUG DELIVERY SYSTEM 24

EVALUATION: 

EVALUATION COLON TARGETED DRUG DELIVERY SYSTEM 25 #Evaluation of Granules -Bulk density -Tap density -Carrs index -Angle of repose -Housners ratio

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COLON TARGETED DRUG DELIVERY SYSTEM 26 #Tablet evaluation -Weight variation test -Disintegration test -Hardness -Friability -Drug content -Dissolution profile -In vitro drug release study -Drug release kinetics

EQUIPMENTS: 

EQUIPMENTS COLON TARGETED DRUG DELIVERY SYSTEM 27 TABLET PUNCHING MACHINE U.V.SPECTOPHOTOMETER FTIR

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Dissolution test appratus Vernier Calliper Hardness Tester Friability appratus

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Thank You COLON TARGETED DRUG DELIVERY SYSTEM 29 RS