MODULATION OF DRUG RELEASE AND BIOAVAILABILITY OF COMPOSITIONS CONTAINING DOLUTEGRAVIR SODIUM AND OTHER ANTI HIV DRUGS

摘要

The present invention relates to a compressed tablet core comprising dolutegravir sodium of formula (I), wherein the tablet core comprises granules and a tablet base, and to a coated tablet comprising said compressed tablet core. The granules of the tablet core comprise dolutegravir sodium of formula (I), and low to medium viscosity polyvinylpyrrolidone (PVR) binders. Additionally, the granules comprise one or more specific fillers selected from the group consisting of mannitol, sorbitol, lactose, dibasic calcium phosphate, and microcrystalline cellulose (MCC), and one or more disintegrants selected from the group consisting of crospovidone (cross-linked polyvinylpyrrolidone), croscarmelose sodium, and sodium starch glycolate. The tablet base comprises specific binders selected from the group consisting of hypromellose, hydroxyethylcellulose (HEC), sodium carboxymethylcellulose (NaCMC), and high viscosity PVP binders. The tablet base additionally comprises one or more disintegrants selected from the group indicated above for the granules. The present invention also relates to a process for preparing said tablet core, and to the compressed tablet core or the coated tablet for use in the treatment of human immunodeficiency virus (HIV-1) infection.