Formulation and Evaluation of Floating Matrix Tablets of Esomeprazole

FORMULATION AND EVALUATION OF FLOATING MATRIX TABLET OF ESOMEPRAZOLE

M.PHARM DISSERTATION PROTOCOL

Submitted to

Rajiv Gandhi University of Health Sciences

Bangalore, Karnataka

By

PATEL ISHVAR C.

(M.PHARM)

Under the Guidance of

MR. HARIPRASANNA R.C.

M.PHARM (PH.D)

DEPARTMENT OF PHARMACEUTICS

R.M.E.S’s COLLEGE OF PHARMACY,

GULBARGA-585102

2009-2010

Rajiv Gandhi University of Health Sciences, Bangalore, Karnataka.

Curriculum Development Cell

Conformation for Registration of Subject for dissertation

Registration No.:

Name of the Candidate:Patel Ishvar Chotubhai

Address:R.M.E.S’s College of Pharmacy

Gulbarga, Karnataka.

Name of the Institution:R.M.E.S’s College of Pharmacy

Gulbarga, Karnataka.

Course of Study and Subject:M.Pharma in Pharmaceutics

Date of Admission to the Course:12th Oct. 2009

Title of the Topic:Formulation and Evaluation of Floating Matrix

Tablet of Esomeprazole.

Brief resume of the intended work:Enclosed

Signature of the student:

Guide Name: Prof. Hariprasanna R. C. M.Pharm (Ph.D)

Remarks of the Guide:Recommended for approval

Signature of the Guide:

Co-Guide Name:Mr. Mohan V. Kodli M.Pharm

Signature of the Co-Guide:

HOD Name:Prof. Hariprasanna R.C. M.Pharm(Ph.D)

Signature of the HOD:

Director/Principal Name: Prof. Kishoresingh K.Chatrapathi M.Pharm Ph.D

Mobile No:+919880200905

Director/Principal E-mail ID:

Remarks of Director/ principal: Recommended for approval

Director/Principal Signature:

RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCE, KARNATAKA

BANGALORE

ANNEXURE-II

PROFORMA FOR REGISTRATION OF SUBJECTS FOR DISSERTATION

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6.2 Review of Literature:

Literature survey was carried out on the proposed research work by referring various Scientific Research Journals, Helinet facilities and science direct.

1. Arora Shweta et. al., Floating drug delivery system- A Review to develop an efficient floating drug delivery (FDDS) was to compile the recent literature with special focus on the principle mechanism of floatation to achieve gastric retention.2

1. Singh Brahma N. et. al., Floating drug delivery system; an approach to oral controlled drug delivery via gastric retention have been made for rate- controlled drug delivery by overcoming physiological properties, such as gastric residence times (GRT) and unpredictable gastric emptying time (GET).7

1. Xiao Qiang Xu et. al., floating matrix dosage form for phenoporlamine HCL based on gas forming agent; In this work the in-vitro an in-vivo evaluation of formulation was done. Formulation showed increased bioavailability with good floating properties.8

1. Sunthongjeen Srisagul et. al., design and evaluation of floating multi-layer tablets based on gas formation were developed. In this work gas generating agent (sodium bicarbonate), protective layer (HPMC) and acrylic polymers (eudragit RL 30 D, NE 30 D) were used. Formulation showed good floating properties and sustained drug release was achieved.9

1. Baumgartner Sasa et. al., Optimization of floating matrix tablets and evaluation of their gastric residence time. In this work tablet containing hydroxyl propyl methyl cellulose (HPMC), drug and different additives were compressed, and incorporation of gas generating agent together with microcrystalline cellulose.Formulated tablet didn’t adhere tablet to the stomach mucus and that the mean gastric residence time was prolonged.10
2. Streuble A. et. al., Floating matrix tablets based on low density foam powder; effects of formulation and processing parameters on drug release. In this work different types of matrix polymers were studied; hydroxypropyl methylcellulose, polycrylates, sodium alginate, corn starch, carrageenan, guar gum and gum Arabic. Formulation of floating behaviour of low density drug delivery showed accurate control of the drug release patterns.11

1. Talwar Naresh et. al., Orally administered controlled drug delivery system providing temporal and spatial control. In this work various gas generating component, a swelling agent, viscolyzing agent, and optionally a gel forms polymer were used, causing the tablet or capsule to be retained in the stomach or upper part of the small intestine (spatial control).5

1. Jaimini M. et. al., Formulation and Evaluation of Famotidine floating tablets was reported. Different grades of Methocel K100 and Methocel K15M were used for gel forming properties, sodium bicarbonate was incorporated as gas generating agent. The drug release from the tablet was sufficiently sustained and non-Fickian transport of drug from tablets was confirmed.12

6.3 Objectives of the study:

1. Development of the floating tablet of esomeprazole using gas generating agent like sodium bicarbonate, citric acid, tartaric acid and hydroxypropyl methylcellulose(HPMC) is hydrophilic polymers.

1. Esomeprazole floating tablet is prepared by using direct compression method and wet granulation method.

1. Evaluation of prepared floating tablet such as floating time, drug content, drug polymer interaction and in-vitro evaluation study.

1. Provides increased gastric residence time and thereby a longer period of drug delivery system in GI tract.

1. Delivers the drug at controlled rate such that the drug is delivered over period of time.

1. It not only reduces the frequency of dosing but may also reduce the severity and frequency of side effects.

7. MATERIALS AND MTHODS:

7.1 Materials

Drugs: Esomeprazole

Swelling agent: Cross-linked polyvinyl pyrrolidone or cross-linked sodium carboxy methyl cellulose.

Gas generating component: calcium carbonate and carbonates sodium bicarbonates or sodium hydrogen carbonate or potassium hydrogen carbonate.

Other polymers: Hydroxypropyl methylcellulose, carbopol, Eudragit NE, Chitosan

Other excipients: Lactose, mannitol, dextrose, sorbitol and water soluble diluents such as starch, microcrystalline, powered cellulose or lubricants such as talc, citric acid, tartaric acid or ascorbic acid, magnesium state.

Equipments:

UV/Visible spectrophotometer 1700

Digital cover head stirrer electronic balance

Thermostatic Hot plate with magnetic stirrer

Electrolab dissolution apparatus

Punching machine.

Screw gauge, etc.

7.2 Method:

Preparation of Esomeprazole floating matrix tablet5:

The floating matrix tablet of the Esomeprazole will be prepared using above listed materials by direct compression and wet granulation.

Pre compression parameters:

• Angle of repose
• Bulk density
• Top density

Post compression parameters:

• Weight variation
• Hardness
• Friability
• Drug content estimation
• In-vitro drug release
• Drug-polymer interaction
• Floating lag time

The in vitro buoyancy was determined by floating lag time, per the method described by Rosa et al the tablets were placed in 100ml beaker containing 0.1N HCl. The time required for the tablet to rise to the surface and float was determined as floating lag time.13

7.3 Dose the study require any investigation or intervention to be conducted on patient or other humans or animals? If so, please describe briefly.

-- Not under the plan of the work—

7.4 Has ethical clearance be obtained from your institution in case of 7.3

-- Not Applicable—

8. LIST OF REFERENCES.

1. Chien YW. Controlled and Modulated Release Drug Delivery System in Swarbrik J, Boylan JC (Eds.). Encyclopaedia of Pharmaceutical Technology, Marcel Dekker, New York, 1990: 281-313.

1. Arora Shweta, Ali Javed, Ahuja Alka, Khar Roop K. and Baboota Sanjula. Floating Drug Delivery System: A review. AAPS PharmSciTech. 2005; 06(03): E372-E390.

1. Tripathi K D. Essential of Medical Pharmacy. 2003; (5):593.

1. Talwar Naresh, Sen Himardi,Staniforth John N. Orally Administered controlled drug delivery system providing temporal and spatial control. 1998.

1. Advance Drug Review, July 2008: Issue IX; 161.

1. Singh Brahma N, Kim Kwon H. Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. Journal of Controlled release. 2000; 63:235-259.

1. Xiao Qiang Xu, Minije Sun, Feng Zhi, Yiqiao Hu.Floating matrix dosage form for phenoporlamine HCL based on gas forming agent: In vitro and in vivo evaluation in healthy volunteers. Int J Pharm. 2006; 310:139-145.

1. Sunthongjeen Srisagul, Sriamornsak Pornsak, Puttipipatkhachorn Satit. Design and evaluation of floating multi-layer tablets based on gas formation. Eur. J Pharm and Biopharm 2008; 69:255-263.

1. Baumgartner Sasa, Kristl Julijana, Vrecer Franc, Vodopivec Polona, Zorko Bojan. Optimization of floating matrix tablets and evaluation of their gastric residence time.Int J Pharm. 2000; 195:125-135.

1. Streuble A, Siepmann J, Bodmeier R. Floating matrix tablets based on low density foam powder; effects of formulation and processing parameters on drug release.Euro. J Pharm Sci. 2003; 18:37-45.

1. Jaimini M, Rana A.C, Tanwar Y.S. Formulation and Evaluation of Famotidine floating tablets. Current Drug delivery, 2007; 4:51-55.

1. Dave BS, Amin AF, Patel MM. Gastro retentive Drug delivery system of Ranitidine hydrochloride: Formulation and in vitro evaluation. AAPS PharmSciTech.2004; 5(2): article 34.