A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/341 (2006.01) A61K 9/10 (2006.01) A61K 9/14 (2006.01) A61K 9/18 (2006.01) A61K 38/55 (2006.01) A61K 47/48 (2006.01) A61P 31/18 (2006.01) C12N 9/99 (2006.01) C07K 14/81 (2006.01)
Patent
CA 2295588
The present invention describes formulations of nanoparticulate HIV protease inhibitors comprising a cellulosic surface stabilizer. The nanoparticulate formulations have an increased rate of dissolution in vitro, an increased rate of absorption in vivo, a decreased fed/fasted ratio variability, and a decreased variability in absorption. The present invention is also directed to methods of making the novel formulations. In particular, nanoparticulate formulations of HIV type 1(HIV-1) and type 2 (HIV-2) protease inhibitors are described.
La présente invention concerne des formulations en nanoparticules d'inhibiteurs de la protéase du VIH, comprenant un stabilisant superficiel cellulosique. Ces formulations en nanoparticules se caractérisent par une vitesse de dissolution in vitro accrue, une vitesse d'absorption in vivo accrue, une variabilité réduite du rapport rassasié/à jeun, et une variabilité de l'absorption réduite. La présente invention concerne également des procédés de préparation de ces nouvelles formulations. Elle porte, en particulier, sur des formulations en nanoparticules d'inhibiteurs de la protéase du VIH de type I (VIH-1) et de type II (VIH-2).
Engers David A.
Liversidge Gary G.
Roberts Mary E.
Ruddy Stephen B.
Wong Sui-Ming
Elan Pharma International Limited
Fetherstonhaugh & Co.
Nanosystems L.l.c.
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