Abstract

FORMULATION DEVELOPMENT AND EVALUATION OF TAPENTADOL HYDROCHLORIDE EXTENDED RELEASE MATRIX TABLETS

Murali Krishna B.*, Praveen Kumar Uppala, Prof. Dr. K. Atchuta Kumar, Sailaja Kumari R.

Abstract

Tapentadol hydrochloride is a central analgesic used to treat moderate to severe pain, which has a biological half-life of 4 hours. The present study involves the formulation and evaluation of extended release matrix tablets of Tapentadol hydrochloride by direct compression method. Matrix systems are drug delivery systems that utilize the principle of drug release through a matrix formed by the polymer system when exposed to the body fluids /release media. These systems are versatile, easy to manufacture and cost effective since they do not involve expensive coating processes. Tapentadol hydrochloride by direct compression method using HPMC K4M, HPMC E5, HPMC K100LV, Xanthangum, Chitosan, Surelease, Metalose as matrix material with lactose, starch, magnesium stearate and aerosil. Matrix tablets were evaluated by different parameters such as thickness, hardness, weight uniformity, content uniformity, in vitro drug release, in vitro drug permeation and FTIR studies. Optimized formulations for model drug were developed and evaluated for pharmacopoeial and non-pharmacopoeial tests. The test results were within the limits. The in vitro release studies for the developed formulations were carried out in 0.1 N HCL for 2 hours and then in pH 7 phosphate buffer for the next preceding hours using type-I apparatus (basket) at 100 rpm. Drug release from the HPMC matrices showed that viscosity of the HPMC plays important role and in the remaining polymer matrices, the type of polymer and concentration of the polymer plays important role. The order of retardation of drug release was Xanthangum > Surelease > Chitosan > Metalose. In view of the above findings, it can be suggested that formulation containing combinations of HPMC K4M and Xanthangum (F6) can be employed successfully for the development of extended release matrix tablets of Tapentadol hydrochloride.

Keywords: Matrix tablets, Tapentadol, HPMC, Xanthan gum, Invitro Drug Release.