Kowalski, James,Lakshman, Jay Parthiban,Patel, Arun P.
申请号：
ES15199440
公开号：
ES2684325T3
申请日:
2005.01.17
申请国别(地区):
ES
年份:
2018
代理人:
摘要：
A pharmaceutical tablet by direct compression, wherein the tablet comprises: a) from 22% to 28% by weight on a dry weight basis of a DPP-IV inhibitor which is (S) -1 - [(3- hydroxy-1- adamantyl) amino] acetyl-2-cyanopyrrolidine in free form or in the form of acid addition salt； b) from 45% to 50% by weight on a dry weight basis of a pharmaceutically acceptable microcrystalline cellulose； c) from 20% to 25% by weight on a dry weight basis of a pharmaceutically acceptable lactose； d) from 1.5% to 2.5% by weight on a dry weight basis of a pharmaceutically acceptable sodium starch glycolate； and e) from 0.1% to 2% by weight on a dry weight basis of magnesium stearate； wherein the dispersion contains particles comprising said DPP-IV inhibitor which is (S) -1 - [(3-hydroxy-1- adamantyl) amino] acetyl-2-cyanopyrrolidine in free form or as an addition salt of acid, and wherein at least 80% of the particle size distribution of the particles comprising (S) -1 - [(3-hydroxy-1- adamantyl) amino] acetyl-2-cyanopyrrolidine in free form or in Acid addition salt form in the tablet is between 10 μ250 μm as determined by laser diffraction.Un comprimido farmacéutico por compresión directa, en en el que el comprimido comprende: a) de 22% a 28% en peso sobre una base de peso seco de un inhibidor de DPP-IV que es (S)-1-[(3-hidroxi-1- adamantil)amino]acetil-2-cianopirrolidina en forma libre o en forma de sal de adición de ácido； b) de 45% a 50% en peso sobre una base de peso seco de una celulosa microcristalina farmacéuticamente aceptable； c) de 20% a 25% en peso sobre una base de peso seco de una lactosa farmacéuticamente aceptable； d) de 1,5% a 2,5% en peso sobre una base de peso seco de un glicolato de almidón de sodio farmacéuticamente aceptable； y e) de 0,1% a 2% en peso sobre una base de peso seco de estearato de magnesio； en donde la dispersión contiene partículas que comprenden dicho inhibidor de DPP-IV que es (S)-1-[(3-hidroxi-1- adamantil)amino]acetil-2-cianopirrolidina en forma
