MORI HIROSHI,森 博志,KOBAYASHI KENSUKE,小林 健介,TANAKA KENJI,田中 健次
申请号：
JP2011267552
公开号：
JP2013119527A
申请日:
2011.12.07
申请国别(地区):
JP
年份:
2013
代理人:
摘要：
PROBLEM TO BE SOLVED: To provide slightly-soluble active pharmaceutical ingredient powder having improved solubility and stability especially, to provide high-purity form I crystal powder especially of candesartan cilexetil in which the average particle size is comparatively small and particles having a particle size of ≥100 μm are not contained substantially (high solubility), and increase of a desethyl body is small (high stability), concerning candesartan cilexetil and to provide a simple method for producing the same.SOLUTION: Small-particle powder of slightly-soluble active pharmaceutical ingredient powder is produced by a production method including a step in which powder containing aimed crystalline large particles is supplied, and a crushing step in which, assuming that D90 of the powder containing large particles is D1 (m) and D90 of small-particle powder obtained after crushing is D2 (m), the powder containing large particles is crushed with a workload whose value of {(1/D2)-(1/D1)} is 10-50 (1/m), to thereby obtain small-particle powder not containing substantially particles having the particle size of ≥100 μm which disturb improvement of solubility.COPYRIGHT: (C)2013,JPO&INPIT【課題】溶解性および安定性の向上した難溶性医薬品原体粉末を提供すること、特にカンデサルタンシレキセチルにおいて、平均粒子径が比較的小さく粒径100μm以上の粒子を実質的に含まない(高溶解性)、かつデスエチル体の増加が少ない(高安定性)、高純度の特にカンデサルタンシレキセチルのフォームI結晶粉末を提供すること、およびその簡便な製造方法を提供すること。【解決手段】本発明の難溶性医薬品原体粉末の小粒子粉末を、目的とする結晶型の大粒子を含む粉末を供給する工程、及び当該大粒子を含む粉末を、当該粉末のD90をD1(m)とし、粉砕後に得られる小粒子粉末のD90をD2(m)としたときに{(1/D2)-(1/D1)}の値が10~50(1/m)である仕事量で粉砕して、溶解性向上の妨げとなる粒径100μm以上の粒子を実質的に含まない前記小粒子粉末を得る粉砕工程、を含む製造方法により製造する。【選択図】なし
