PREPARATION OF ANTI-AIDS AGENT AND ANTI-AIDS PREPARATION

摘要

PURPOSE: To provide a process for the preparation of an anti-AIDS agent easily absorbable through the digestive tracts, having improved bioavailability and suitable for oral administration and provide an anti-AIDS agent prepared by the process. ;CONSTITUTION: This anti-AIDS agent is produced by finely pulverizing a compound of formula (Ar is 5-isoquinolinyl or 3-pyridyl; R is methylthiomethyl or isopropyl; X is S or CH₂) by a pulverizer such as a jet-mill to fine powder having particle diameter of from 0.1μm to several μm, mixing the powder with a solid acidic substance having particle diameter of 3-10μm and applying high impact, compression force or shearing force to the mixture to coat the surface of the acidic substance with the fine powder. A drug preparation having high bioavailability can be produced by using the compound of formula and the acidic substance at a weight ratio of 1:(2-5), especially 1:(2-3). The compound of formula is, e.g. N-t-butyl-3-[2-hydroxy-3-N-[2-N-(5-isoquinolyloxyacetyl)amino-3 methylthiopropanoyl]amino-4-phenylbutanoyl] pyrrolidine-4-carboxamide.;COPYRIGHT: (C)1995,JPO