Compositions and methods for combination antiviral therapy

摘要

The present invention relates to therapeutic combinations of [2-(6-amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Viread®) and (2R,5S,cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtriva™, (−)-cis FTC) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors. The present invention is also concerned with pharmaceutical compositions and formulations of said combinations of tenofovir disoproxil fumarate and emtricitabine, and their physiologically functional derivatives, as well as therapeutic methods of use of those compositions and formulations.

主权项

1. A fixed dose combination pharmaceutical dosage form comprising 300 mg tenofovir disoproxil fumarate and 200 mg emtricitabine; a binder selected from the group consisting of povidone, gelatin, hydroxypropyl methylcellulose, cellulose, microcrystalline cellulose, starch, and acacia; a disintegrant selected from sodium starch glycolate, crosslinked-povidone, cross-linked sodium carboxymethylcellulose, and alginic acid; and a lubricant selected from the group consisting of magnesium stearate, stearic acid, and talc; wherein said pharmaceutical dosage form exhibits equal to or less than 5% degradation of the tenofovir disoproxil fumarate or emtricitabine after 6 months when packaged and stored with silica gel dessicant at 40° C./75% relative humidity; and wherein said pharmaceutical dosage form is a tablet.