MORI HIROSHI,森 博志,KOBAYASHI KENSUKE,小林 健介,TANAKA KENJI,田中 健次
申请号：
JP2016043605
公开号：
JP2016106139A
申请日:
2016.03.07
申请国别(地区):
JP
年份:
2016
代理人:
摘要：
PROBLEM TO BE SOLVED: To provide a sparingly soluble active pharmaceutical intermediate with improved solubility and stability, especially in candesartan cilexetil, Form I crystalline powder of candesartan cilexetil, whose particle size is relatively small and contains essentially no particles having a particle size of 100 μm or more (high solubility), and which shows little increase in the amount of desethyl compound (high stability) and has high purity, and to provide a simple method for producing the same.SOLUTION: The fine particle powder of sparingly soluble active pharmaceutical intermediate of the present invention is produced by a production method comprising: a step of feeding powder containing large particles having a desired crystal form and a pulverization step of obtaining the small particle powder containing essentially no particles having a particle size of 100 μm or more, which inhibit improvement of solubility, by pulverizing the powder containing large particles with a work volume such that, when D90 of the powder containing large particles is denoted by D1 (m) and D90 of the small particle powder by D2 (m), a value of {(1/D2)-(1/D1)} is 10 to 50 (1/m).SELECTED DRAWING: NoneCOPYRIGHT: (C)2016,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
