FORMULATION AND EVALUATION OF FINASTERIDE SUSTAINED-RELEASE MATRIX TABLETS USING DIFFERENT RATE CONTROLLING POLYMERS

Igwe J. Chibueze

doi:10.22270/ujpr.v1i2.r3

Abstract

Objective: Finasteride is chemically considered a synthetic 4-azasteroid drug used in the treatment of anti-hyperplasia. In matrix system of sustained release drug is dispersed homogenously throughout a polymeric matrix. The aim of the present investigation was to develop oral controlled release matrix tablet formulations of Finasteride with different polymer ratios. Methods: The granules were evaluated for angle of repose, bulk density and Compressibility index before being punched as tablets. Total 5 varieties o of tablets were compressed using polymers (HPMC, EC, Eudragit RS100) in different ratio. The tablets were subjected to weight variation test, drug content, hardness, friability, and in vitro release studies. Different models for kinetic study were applied like zero order, first order, Higuchi, Hixson Crowell and Korsmeyer to study the release pattern and mechanism. Results: All the formulations showed uniform thickness. In a weight variation test, the pharmacopoeial limit for percentage deviation for the tablets of more than 250 mg is ±5%. The formulation MT5 showed a comparatively high hardness value of 4.8±0.22 kg/cm2. Matrix tablets of batch MT1 shows maximum release 86.42% in 10 hrs. Conclusion: Observations of all formulations for physical characterization had shown that, all of them comply with the specifications of official pharmacopoeias and/or standard references. Study concludes that Finasteride can be delivered effectively in the form of matrix tablets. Peer Review History: Article received on- 16 November, Revised on- 25 December, Accepted on- 28 December, Available online 15 January 2017 UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file: Reviewer's Comments: Average Peer review marks at initial stage: 4.0/10 Average Peer review marks at publication stage: 7.0/10 Reviewer(s) detail: Dr. Barkat Ali Khan, Kampala International University , Uganda, barki.gold@gmail.com Dr. Dalia Kamal Zaffar Ali, Modern University for technology and information, Egypt, dr.moda88@gmail.com Similar Articles: FORMULATION AND EVALUATION OF COLON TARGETED MATRIX TABLETS CONTAINING EXTRACT OF SOLENOSTEMMA ARGEL (HARGEL) A COMPREHENSIVE REVIEW ON SUSTAINED RELEASE MATRIX TABLETS: A PROMISING DOSAGE FORM DEVELOPMENT AND CHARACTERIZATION OF DIRECT COMPRESSED MATRIX MINI TABLETS OF NAPROXEN SODIUM

Highlights

In matrix system of sustained release drug is dispersed homogenously throughout a polymeric matrix[3]. It includes coating and pelletization during manufacturing and rate of drug release from the dosage form is controlled mainly by the type and proportion of polymer used in the preparations
The granules prepared by wet granulation of drug, filler and hydrophilic polymers were compressed into flat faced tablets using by using KBr press
Hausner’s ratio Hausner ratio (Hr) is an indirect index of ease of powder flow[15]. It is calculated by the following formula: 5. Drug content An accurately weighed amount of powdered Finasteride granules (100 mg) was extracted with water and the solution was filtered through 0.45μ membrane

Summary

INTRODUCTION

Sustained release systems drug delivery system achieves slow release of drug over an extended period of time. In matrix system of sustained release drug is dispersed homogenously throughout a polymeric matrix[3] It includes coating and pelletization during manufacturing and rate of drug release from the dosage form is controlled mainly by the type and proportion of polymer used in the preparations. Finasteride is chemically considered a synthetic 4azasteroid drug[8] The mechanism of action of Finasteride is based on its preferential inhibition of Type II 5a-reductase by formation of a stable complex with the enzyme. This enzyme converts testosterone to dihydrotestosterone (DHT), which is a more potent androgenic hormone. The bulk density and tapped density were calculated by using the bulk volume and tapped volume[14]

MATERIALS AND METHODS

In vitro release studies

AND DISCUSSION

CONCLUSION