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    • 4. 发明申请
    • PHARMACEUTICAL COMPOSITION INCLUDING POLYMER MICROSPHERE CONTAINING OLANZAPINE AS ACTIVE INGREDIENT
    • 包含含有作为活性成分的氯氮平的聚合物微球的药物组合物
    • WO2012064088A3
    • 2012-07-19
    • PCT/KR2011008470
    • 2011-11-08
    • SK CHEMICALS CO LTDUNIV EWHA IND COLLABORATIONSAH HONG KEELEE KYU HOHONG SEOK HYUNLEE YOON-JUNGOH JOON-GYOUM KEY-ANLEE BONG-YONGHWANG YONG YOUNYUN SUN KYUKIM HONG-KEE
    • SAH HONG KEELEE KYU HOHONG SEOK HYUNLEE YOON-JUNGOH JOON-GYOUM KEY-ANLEE BONG-YONGHWANG YONG YOUNYUN SUN KYUKIM HONG-KEE
    • A61K9/16A61K9/14A61K31/551A61P25/24
    • A61K31/551A61K9/5021
    • The present invention relates to a pharmaceutical composition including a polymer microsphere that contains olanzapine as an active ingredient, and more particularly, to a pharmaceutical composition including a polymer microsphere containing olanzapine as an active ingredient, for treating or preventing a disease or a symptom thereof, the disease selected from a group comprised of schizophrenia and related mental illnesses, bipolar mania, bipolar disorder, seizure, obsessive/compulsive disorder, generalized anxiety disorder, post traumatic distress syndrome, extreme shyness, diabetic nerve pain, and depression, and to a method for preventing or treating, and usage thereof, and the pharmaceutical composition prepared by a method comprising the following steps: mixing a water insoluble organic solvent and a dispersion solvent; preparing a dispersion by mixing a polymer compound, olanzapine, and the water insoluble organic solvent; manufacturing an emulsion by mixing the dispersion with the dispersion solvent in which the water insoluble organic solvent while maintaining the temperature of the emulsion between 0°C to 10°C; and eliminating the water insoluble organic solvent from the emulsion by adding a base or an acid while maintaining the emulsion between 0°C to 10°C. The method for preparing of the present invention does not involve the existing steps of solvent evaporation or solvent extraction, uses little amount of water thereby minimizing waste water generation, while allowing for preparing the polymer microsphere including olanzapine in a swift and simple manner, maintains a low density of solvent remnants inside the polymer microsphere, and is effective for manufacturing sustained-release medicine including anastrozole, as the speed of releasing anastrozole in the body can be adjusted.
    • 本发明涉及包含含有奥氮平作为活性成分的聚合物微球的药物组合物,并且更具体地涉及包含含有奥氮平作为活性成分的聚合物微球的药物组合物,用于治疗或预防疾病或其症状, 选自精神分裂症和相关精神疾病,双相躁狂症,双相性精神障碍,癫痫发作,强迫症,广泛性焦虑症,创伤后窘迫综合征,极度羞怯,糖尿病性神经痛和抑郁症的组的疾病以及方法 用于预防或治疗,以及其用途,以及通过包括以下步骤的方法制备的药物组合物:混合水不溶性有机溶剂和分散溶剂; 通过混合聚合物化合物奥氮平和水不溶性有机溶剂来制备分散体; 通过将分散体与其中水不溶性有机溶剂在其中的分散溶剂混合,同时将乳液的温度保持在0℃至10℃之间来制备乳液; 并通过添加碱或酸从乳液中除去不溶于水的有机溶剂,同时保持乳液在0℃至10℃之间。 本发明的制备方法不涉及溶剂蒸发或溶剂萃取的现有步骤,使用少量的水,从而使废水产生最小化,同时允许以快速和简单的方式制备包括奥氮平的聚合物微球, 聚合物微球内部的溶剂残余物的密度低,并且因为可以调节体内释放阿那曲唑的速度,所以对于制造包括阿那曲唑的缓释药物是有效的。