Abstract

FORMULATION AND DEVELOPMENT OF COLON TARGETED MATRIX TABLET OF TENOFOVIR DF

Shivam Sahu, Dr. Jitendra Banweer, *Praveen Tahilani and Gaurav Goyanar

ABSTRACT

Tenofovir disoproxil fumarate (a prodrug of tenofovir), marketed by Gilead Sciences under the trade name Viread®, belongs to a class of antiretroviral drugs known as nucleotide analogue reverse transcriptase inhibitors (nRTIs), which block reverse transcriptase, an enzyme crucial to viral production in HIV-infected people. In vivo tenofovir disoproxil fumarate is converted to tenofovir, an acyclic nucleoside phosphonate (nucleotide) analog of adenosine 5'-monophosphate. Tenofovir inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5'-triphosphate and, after incorporation into DNA, by DNA chain termination. The present investigation was concerned with the development of the colon targeted tablets, which after oral administration were designed to prevent the drug release in stomach and small intestine. It improves the bioavailability of the drug as well as its half life. Various formulations were developed by using release rate controlling polymers like Xanthan Gum, Guar Gum by direct compression method. Wet granulation method was followed to manufacture the matrix tablets of Tenofovir DF. The tenofovir df matrix tablets were further coated with Eudragit S-100 solution. All the tablets were evaluated for following different parameters which includes general appearance Thickness and diameter, Drug content, hardness, Friability, Uniformity of weight, Dissolution rate studies etc.

Keywords: Tenofovir disoproxil fumarate, Matrix tablet, wet granulation, Guar gum, Eudragit.