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1. 发明申请

WO2012015168A3 PHARMACEUTICAL COMPOSITION COMPRISING ROSUVASTATIN OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF 审中-公开
标题翻译：包含罗司他汀或其药学上可接受的盐的药物组合物
公开(公告)号：WO2012015168A3
公开(公告)日：2012-04-19
申请号：PCT/KR2011004539
申请日：2011-06-22
申请人： CJ CHEIL JEDANG CORP , JEON LL-SOON , SHON SOO-KYUNG , JEON EUN-KYUNG , CHAE GANG-SOO , OH MI-HWA , CHOI YONG-HWAN , LEE YOON-JUNG , BAEK SEUNG-HEE , HONG JOO-YONG
发明人： JEON LL-SOON , SHON SOO-KYUNG , JEON EUN-KYUNG , CHAE GANG-SOO , OH MI-HWA , CHOI YONG-HWAN , LEE YOON-JUNG , BAEK SEUNG-HEE , HONG JOO-YONG
IPC分类号： C07D239/42 , A61K31/505 , A61P3/06
CPC分类号： A61K31/505 , A61K9/00
摘要： Provided is a pharmaceutical composition comprising rosuvastatin or a pharmaceutically acceptable salt thereof and an anhydrous dibasic calcium phosphate as a stabilizer. The composition of the present invention has outstanding storage stability.
摘要翻译：本发明提供包含瑞舒伐他汀或其药学上可接受的盐和无水磷酸氢钙作为稳定剂的药物组合物。本发明的组合物具有优异的储存稳定性。

2. 发明申请

WO2012011740A2 METHOD FOR PREPARING MICROSPHERES AND MICROSPHERES PRODUCED THEREBY 审中-公开
标题翻译：制备微生物和生产的微生物的方法
公开(公告)号：WO2012011740A2
公开(公告)日：2012-01-26
申请号：PCT/KR2011/005347
申请日：2011-07-20
申请人： SK CHEMICALS CO., LTD. , EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION , SAH, Hong Kee , LEE, Bong-Yong , UM, Key-An , OH, Joon-gyo , HWANG, Yong Youn , KIM, Hong-Kee , LEE, Kyu Ho , HONG, Seok Hyun , LEE, Yoon-Jung
发明人： SAH, Hong Kee , LEE, Bong-Yong , UM, Key-An , OH, Joon-gyo , HWANG, Yong Youn , KIM, Hong-Kee , LEE, Kyu Ho , HONG, Seok Hyun , LEE, Yoon-Jung
IPC分类号： A61K9/14 , A61K9/22 , A61K31/57 , C08J3/12
CPC分类号： A61K9/1694 , A61K9/16 , A61K9/1647 , A61K31/4196 , A61K31/551 , C08J3/05 , C08J3/12 , C08J3/16 , C08J2367/04
摘要： The present invention relates to a method for preparing microsphere1- and microspheres produced by thereby. More particularly, the present invention relates to a method for preparing a polymeric microsphere comprising the steps of: mixing a water-insoluble organic solvent with a dispersion solvent; mixing a polymer compound, a drug and a water-insoluble organic solvent so as to prepare a dispersed phase; mixing the dispersed phase with the dispersion solvent mixed with the water-insoluble organic solvent so as to prepare an emulsion; and adding a base or an acid to the prepared emulsion so as to remove the water-insoluble organic solvent from the emulsion and a polymeric microsphere thereby, and a composition for drug delivery comprising the microspheres. In the inventive preparation method, it is possible to conveniently prepare a drug-containing polymeric microsphere within a short time using a small amount of water, with the generation of a minimized amount of waste solution without a requirement of a conventional solvent-evaporation or solvent-extract ion process. Also, since a low concentration of remaining solvent within a prepared polymeric microsphere can be maintained, it is effective in preparation in sustained-release type medicines.
摘要翻译：本发明涉及由此制备的微球和微球的制备方法。更具体地，本发明涉及一种制备聚合物微球的方法，包括以下步骤：将水不溶性有机溶剂与分散溶剂混合; 混合高分子化合物，药物和水不溶性有机溶剂以制备分散相; 将分散相与与水不溶性有机溶剂混合的分散溶剂混合以制备乳液; 并向制备的乳液中加入碱或酸，从而从乳液和聚合物微球中除去水不溶性有机溶剂，以及用于药物递送的组合物，其包含微球。在本发明的制备方法中，可以使用少量的水在短时间内方便地制备含药聚合物微球体，同时产生最少量的废溶液，而不需要常规的溶剂蒸发或溶剂 - 提取离子过程。此外，由于可以保持制备的聚合物微球体内的低浓度剩余溶剂，因此在缓释型药物的制备中是有效的。

3. 发明申请

WO2011139107A2 PICOLINAMIDE AND PYRIMIDINE-4-CARBOXAMIDE COMPOUNDS, PROCESS FOR PREPARING AND PHAMACEUTICAL COMPOSITION COMPRISING THE SAME 审中-公开
标题翻译：吡啶酰胺和嘧啶-4-羧酰胺化合物，其制备方法和包含其的药物组合物
公开(公告)号：WO2011139107A2
公开(公告)日：2011-11-10
申请号：PCT/KR2011/003362
申请日：2011-05-04
申请人： SK Chemicals Co.,Ltd. , RYU, Je Ho , KIM, Shin Ae , RYU, Keun Ho , KIM, Jae Sun , KIM, Nam Ho , HAN, Hye Young , KIM, Yong Hyuk , YOUN, Won-No , LEE, Yoon-Jung , SON, Hyun Joo , LEE, Bong-yong , PARK, Sung Hoon , LEE, Ju Young , LEE, Hyun Jung , JUNG, Hoe Chul , SHIN, Young Ah , LEE, Jung A , LEE, Bo Ram , SA, Joon Ho
发明人： RYU, Je Ho , KIM, Shin Ae , RYU, Keun Ho , KIM, Jae Sun , KIM, Nam Ho , HAN, Hye Young , KIM, Yong Hyuk , YOUN, Won-No , LEE, Yoon-Jung , SON, Hyun Joo , LEE, Bong-yong , PARK, Sung Hoon , LEE, Ju Young , LEE, Hyun Jung , JUNG, Hoe Chul , SHIN, Young Ah , LEE, Jung A , LEE, Bo Ram , SA, Joon Ho
IPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , A61K31/444 , A61K31/496 , A61P3/10 , A61P3/06
CPC分类号： C07D401/04 , C07D213/81 , C07D239/557 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/12 , C07D405/14
摘要： Provided are picolinamide and pyrimidine-4-carboxamide compounds, a method for preparing the same, a pharmaceutical composition containing the same, and a medical use using the compound as an agent for preventing, regulating, and treating diseases related to regulation of glucocorticoids by using selective inhibitory activity of the compound for an 11β-HSD1 enzyme. The picolinamide and pyrimidine-4-carboxamide compounds of the present invention are selective inhibitors of human-derived 11β-HSD1 enzymes, and are useful in an agent for preventing, regulating, and treating diseases related to glucocorticoid regulation in which human- derived 11β-HSD1 enzymes are involved, for example, metabolic syndromes such as, type 1 and type 2 diabetes, diabetes later complications, latent autoimmune diabetes adult (LAD A), insulin tolerance syndromes, obesity, impaired glucose tolerane (IGT), impaired fasting glucose (IFG), damaged glucose tolerance, dyslipidemia, atherosclerosis, hypertension, etc.
摘要翻译：提供了吡啶酰胺和嘧啶-4-甲酰胺化合物，其制备方法，含有该组合物的药物组合物，以及使用该化合物作为预防，调节和治疗与糖皮质激素调节有关的疾病的药物的用途化合物对11β-HSD1酶的选择性抑制活性。本发明的吡啶酰胺和嘧啶-4-甲酰胺化合物是人源性11β-HSD1酶的选择性抑制剂，可用于预防，调节和治疗与糖皮质激素调节有关的疾病的药剂，其中人源性11β- 涉及HSD1酶，例如代谢综合征，例如1型和2型糖尿病，糖尿病后期并发症，潜伏性自身免疫性糖尿病成人（LAD A），胰岛素耐受综合征，肥胖症，葡萄糖耐量降低（IGT），空腹血糖受损 IFG），葡萄糖耐量受损，血脂异常，动脉粥样硬化，高血压等。

4. 发明申请

WO2012064088A3 PHARMACEUTICAL COMPOSITION INCLUDING POLYMER MICROSPHERE CONTAINING OLANZAPINE AS ACTIVE INGREDIENT 审中-公开
标题翻译：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
公开(公告)号：WO2012064088A3
公开(公告)日：2012-07-19
申请号：PCT/KR2011008470
申请日：2011-11-08
申请人： SK CHEMICALS CO LTD , UNIV EWHA IND COLLABORATION , SAH HONG KEE , LEE KYU HO , HONG SEOK HYUN , LEE YOON-JUNG , OH JOON-GYO , UM KEY-AN , LEE BONG-YONG , HWANG YONG YOUN , YUN SUN KYU , KIM HONG-KEE
发明人： SAH HONG KEE , LEE KYU HO , HONG SEOK HYUN , LEE YOON-JUNG , OH JOON-GYO , UM KEY-AN , LEE BONG-YONG , HWANG YONG YOUN , YUN SUN KYU , KIM HONG-KEE
IPC分类号： A61K9/16 , A61K9/14 , A61K31/551 , A61P25/24
CPC分类号： A61K31/551 , A61K9/5021
摘要： 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.
摘要翻译：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。

5. 发明申请

WO2011139107A3 PICOLINAMIDE AND PYRIMIDINE-4-CARBOXAMIDE COMPOUNDS, PROCESS FOR PREPARING AND PHAMACEUTICAL COMPOSITION COMPRISING THE SAME 审中-公开
标题翻译：吡啶酰胺和嘧啶-4-羧酰胺化合物，其制备方法和包含其的药物组合物
公开(公告)号：WO2011139107A3
公开(公告)日：2012-05-18
申请号：PCT/KR2011003362
申请日：2011-05-04
申请人： SK CHEMICALS CO LTD , RYU JE HO , KIM SHIN AE , RYU KEUN HO , KIM JAE SUN , KIM NAM HO , HAN HYE YOUNG , KIM YONG HYUK , YOUN WON-NO , LEE YOON-JUNG , SON HYUN JOO , LEE BONG-YONG , PARK SUNG HOON , LEE JU YOUNG , LEE HYUN JUNG , JUNG HOE CHUL , SHIN YOUNG AH , LEE JUNG A , LEE BO RAM , SA JOON HO
发明人： RYU JE HO , KIM SHIN AE , RYU KEUN HO , KIM JAE SUN , KIM NAM HO , HAN HYE YOUNG , KIM YONG HYUK , YOUN WON-NO , LEE YOON-JUNG , SON HYUN JOO , LEE BONG-YONG , PARK SUNG HOON , LEE JU YOUNG , LEE HYUN JUNG , JUNG HOE CHUL , SHIN YOUNG AH , LEE JUNG A , LEE BO RAM , SA JOON HO
IPC分类号： C07D401/04 , A61K31/444 , A61K31/496 , A61P3/06 , A61P3/10 , C07D401/14 , C07D413/14
CPC分类号： C07D401/04 , C07D213/81 , C07D239/557 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/12 , C07D405/14
摘要： Provided are picolinamide and pyrimidine-4-carboxamide compounds, a method for preparing the same, a pharmaceutical composition containing the same, and a medical use using the compound as an agent for preventing, regulating, and treating diseases related to regulation of glucocorticoids by using selective inhibitory activity of the compound for an 11ß-HSD1 enzyme. The picolinamide and pyrimidine-4-carboxamide compounds of the present invention are selective inhibitors of human-derived 11ß-HSD1 enzymes, and are useful in an agent for preventing, regulating, and treating diseases related to glucocorticoid regulation in which human- derived 11ß-HSD1 enzymes are involved, for example, metabolic syndromes such as, type 1 and type 2 diabetes, diabetes later complications, latent autoimmune diabetes adult (LAD A), insulin tolerance syndromes, obesity, impaired glucose tolerane (IGT), impaired fasting glucose (IFG), damaged glucose tolerance, dyslipidemia, atherosclerosis, hypertension, etc.
摘要翻译：提供了吡啶酰胺和嘧啶-4-甲酰胺化合物，其制备方法，含有该组合物的药物组合物，以及使用该化合物作为预防，调节和治疗与糖皮质激素调节有关的疾病的药物的用途化合物对11β-HSD1酶的选择性抑制活性。本发明的吡啶酰胺和嘧啶-4-甲酰胺化合物是人源性11β-HSD1酶的选择性抑制剂，可用于预防，调节和治疗与糖皮质激素调节有关的疾病的药剂，其中人源性11β- 涉及HSD1酶，例如代谢综合征，例如1型和2型糖尿病，糖尿病后期并发症，潜伏性自身免疫性糖尿病成人（LAD A），胰岛素耐受综合征，肥胖症，葡萄糖耐量降低（IGT），空腹血糖受损 IFG），葡萄糖耐量受损，血脂异常，动脉粥样硬化，高血压等。

6. 发明申请

WO2012011740A8 METHOD FOR PREPARING MICROSPHERES AND MICROSPHERES PRODUCED THEREBY 审中-公开
公开(公告)号：WO2012011740A8
公开(公告)日：2012-01-26
申请号：PCT/KR2011/005347
申请日：2011-07-20
申请人： SK CHEMICALS CO., LTD. , EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION , SAH, Hong Kee , LEE, Bong-Yong , UM, Key-An , OH, Joon-gyo , HWANG, Yong Youn , KIM, Hong-Kee , LEE, Kyu Ho , HONG, Seok Hyun , LEE, Yoon-Jung
发明人： SAH, Hong Kee , LEE, Bong-Yong , UM, Key-An , OH, Joon-gyo , HWANG, Yong Youn , KIM, Hong-Kee , LEE, Kyu Ho , HONG, Seok Hyun , LEE, Yoon-Jung
IPC分类号： A61K9/14 , A61K9/22 , A61K31/57 , C08J3/12
摘要： The present invention relates to a method for preparing microsphere and microspheres produced by thereby. More particularly, the present invention relates to a method for preparing a polymeric microsphere comprising the steps of: mixing a water-insoluble organic solvent with a dispersion solvent; mixing a polymer compound, a drug and a water-insoluble organic solvent so as to prepare a dispersed phase; mixing the dispersed phase with the dispersion solvent mixed with the water-insoluble organic solvent so as to prepare an emulsion; and adding a base or an acid to the prepared emulsion so as to remove the water-insoluble organic solvent from the emulsion and a polymeric microsphere thereby, and a composition for drug delivery comprising the microspheres. In the inventive preparation method, it is possible to conveniently prepare a drug-containing polymeric microsphere within a short time using a small amount of water, with the generation of a minimized amount of waste solution without a requirement of a conventional solvent-evaporation or solvent-extract ion process. Also, since a low concentration of remaining solvent within a prepared polymeric microsphere can be maintained, it is effective in preparation in sustained-release type medicines.

7. 发明申请

WO2012011740A3 METHOD FOR PREPARING MICROSPHERES AND MICROSPHERES PRODUCED THEREBY 审中-公开
公开(公告)号：WO2012011740A3
公开(公告)日：2012-01-26
申请号：PCT/KR2011/005347
申请日：2011-07-20
申请人： SK CHEMICALS CO., LTD. , EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION , SAH, Hong Kee , LEE, Bong-Yong , UM, Key-An , OH, Joon-gyo , HWANG, Yong Youn , KIM, Hong-Kee , LEE, Kyu Ho , HONG, Seok Hyun , LEE, Yoon-Jung
发明人： SAH, Hong Kee , LEE, Bong-Yong , UM, Key-An , OH, Joon-gyo , HWANG, Yong Youn , KIM, Hong-Kee , LEE, Kyu Ho , HONG, Seok Hyun , LEE, Yoon-Jung
IPC分类号： A61K9/14 , A61K9/22 , A61K31/57 , C08J3/12
摘要： The present invention relates to a method for preparing microsphere1- and microspheres produced by thereby. More particularly, the present invention relates to a method for preparing a polymeric microsphere comprising the steps of: mixing a water-insoluble organic solvent with a dispersion solvent; mixing a polymer compound, a drug and a water-insoluble organic solvent so as to prepare a dispersed phase; mixing the dispersed phase with the dispersion solvent mixed with the water-insoluble organic solvent so as to prepare an emulsion; and adding a base or an acid to the prepared emulsion so as to remove the water-insoluble organic solvent from the emulsion and a polymeric microsphere thereby, and a composition for drug delivery comprising the microspheres. In the inventive preparation method, it is possible to conveniently prepare a drug-containing polymeric microsphere within a short time using a small amount of water, with the generation of a minimized amount of waste solution without a requirement of a conventional solvent-evaporation or solvent-extract ion process. Also, since a low concentration of remaining solvent within a prepared polymeric microsphere can be maintained, it is effective in preparation in sustained-release type medicines.

8. 发明申请

WO2008072939A1 INCLUSION COMPLEX CONTAINING CLOPIDOGREL WITH IMPROVED STORAGE STABILITY 审中-公开
标题翻译：包含CLOPIDOGREL的复合物具有改进的储存稳定性
公开(公告)号：WO2008072939A1
公开(公告)日：2008-06-19
申请号：PCT/KR2007/006599
申请日：2007-12-17
申请人： SK CHEMICALS CO., LTD. , KIM, Jae-Sun , KIM, Nam Ho , LEE, Jin Young , LEE, Nam Kyu , OH, Joon Gyo , SHIN, Ji Young , KIM, Tae-Kon , YOON, Mi-Sun , SUNG, Jin-Heung , LEE, Yoon-Jung , PARK, Yeo-Jin , UM, Key An
发明人： KIM, Jae-Sun , KIM, Nam Ho , LEE, Jin Young , LEE, Nam Kyu , OH, Joon Gyo , SHIN, Ji Young , KIM, Tae-Kon , YOON, Mi-Sun , SUNG, Jin-Heung , LEE, Yoon-Jung , PARK, Yeo-Jin , UM, Key An
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The present invention relates to an inclusion complex containing clopidogrel with superior storage stability, more particularly to a pharmaceutically stable and suitable inclusion complex obtained by reacting S-(+)-clopidogrel [methyl (+)-(S)-α- (o-chlorophenyl)-6/7-dihydrothieno[3,2-c]pyridin-5(4H)-acetate] represented by the formula (1) below with β-cyclodextrin at a specific equivalence ratio, and an antiplatelet agent composition comprising the same as an active ingredient:
摘要翻译：本发明涉及具有优异储存稳定性的含有氯吡格雷的包合络合物，更具体地涉及通过使S-（+） - 氯吡格雷[甲基（+） - （S）-α-（o- 氯苯基）-6,7-二氢噻吩并[3,2-c]吡啶-5（4H） - 乙酸酯]和具有特定当量比的β-环糊精的抗血小板药剂组合物作为有效成分：

9. 发明申请

WO2008004796A1 SALTS OF PYRROLOPYRIMIDINONE DERIVATIVES AND PROCESS FOR PREPARING THE SAME 审中-公开
标题翻译：吡咯烷酮衍生物的制备方法及其制备方法
公开(公告)号：WO2008004796A1
公开(公告)日：2008-01-10
申请号：PCT/KR2007/003213
申请日：2007-07-03
申请人： SK CHEMICALS CO., LTD. , KIM, Jae-Sun , KIM, Nam Ho , LEE, Jin Young , LEE, Nam Kyu , LEE, Yoon-Jung , JANG, Woo Jae , YOUN, Won-No , OH, Joon Gyo , SUNG, Jin-Heung , UM, Key An
发明人： KIM, Jae-Sun , KIM, Nam Ho , LEE, Jin Young , LEE, Nam Kyu , LEE, Yoon-Jung , JANG, Woo Jae , YOUN, Won-No , OH, Joon Gyo , SUNG, Jin-Heung , UM, Key An
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to salts of a pyrrolopyrimidinone derivative having superior PDE-5 inhibition activity and a process for preparing the same. More particularly, the present invention relates to a crystalline acid addition salt prepared by reacting a pyrrolopyrimidinone derivative with an acid selected from gentisic acid, maleic acid, citric acid, fumaric acid and tartaric acid. With no hygroscopic property and superior long-term storage stability, photostability and thermal stability, the salts of the pyrrolopyrimidinone derivative are appropriate to be prepared into medications and, with superior PDE-5 inhibition activity, are useful for the treatment and prevention of erectile dysfunction, pulmonary arterial hypertension, chronic obstructive pulmonary disease, benign prostatic hypertrophy and lower urinary tract diseases.
摘要翻译：本发明涉及具有优异的PDE-5抑制活性的吡咯并嘧啶酮衍生物的盐及其制备方法。更具体地，本发明涉及通过使吡咯并嘧啶酮衍生物与选自龙胆酸，马来酸，柠檬酸，富马酸和酒石酸的酸反应制备的结晶酸加成盐。无吸湿性和优异的长期保存稳定性，光稳定性和热稳定性，吡咯并嘧啶酮衍生物的盐适于制备成药物，并且具有优异的PDE-5抑制活性，可用于治疗和预防勃起功能障碍肺动脉高压，慢性阻塞性肺疾病，良性前列腺肥大和下尿路疾病。

10. 发明申请

WO2012064087A3 PHARMACEUTICAL COMPOSITION INCLUDING POLYMER MICROSPHERE CONTAINING ANASTROZOLE AS ACTIVE INGREDIENT 审中-公开
标题翻译：药物组合物，包括含有作为活性成分的氮杂噻唑的聚合物微球
公开(公告)号：WO2012064087A3
公开(公告)日：2012-07-19
申请号：PCT/KR2011008469
申请日：2011-11-08
申请人： SK CHEMICALS CO LTD , UNIV EWHA IND COLLABORATION , SAH HONG KEE , KIM HONG-KEE , LEE KYU HO , HONG SEOK HYUN , LEE YOON-JUNG , OH JOON-GYO , UM KEY-AN , LEE BONG-YONG , HWANG YONG YOUN , YUN SUN KYU
发明人： SAH HONG KEE , KIM HONG-KEE , LEE KYU HO , HONG SEOK HYUN , LEE YOON-JUNG , OH JOON-GYO , UM KEY-AN , LEE BONG-YONG , HWANG YONG YOUN , YUN SUN KYU
IPC分类号： A61K9/16 , A61K31/4196 , A61K47/30 , A61P35/00
CPC分类号： A61K31/4196 , A61K9/0019 , A61K9/19 , A61K9/5026 , A61K9/5031
摘要： The present invention relates to a pharmaceutical composition including a polymer microsphere that contains anastrozole as an active ingredient, and more particularly, to a pharmaceutical composition for cancer treatment or prevention including a polymer microsphere that contains anastrozole, which is prepared by a method comprising the following steps: preparing a dispersion by mixing a polymer compound, anastrozole, and a water insoluble organic solvent; preparing an emulsion by mixing the dispersion with a dispersion solvent; eliminating the water insoluble organic solvent from the emulsion by adding a base or an acid; and obtaining the polymer microsphere from which the water insoluble organic solvent is removed and re-dispersing same in the heated dispersion solvent. The present invention also relates to a method for treating or preventing the cancer and usage thereof. The composition 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, and allows low density of solvent remnants inside the polymer microsphere. Also, the present invention is effective for manufacturing sustained-release medicine including anastrozole, as the speed of releasing anastrozole in the body can be adjusted.
摘要翻译：本发明涉及包含含有阿那曲唑作为活性成分的聚合物微球体的药物组合物，并且更具体地涉及包含含有阿那曲唑的聚合物微球体的用于癌症治疗或预防的药物组合物，其通过包括以下的方法制备步骤：通过混合聚合物化合物，阿那曲唑和水不溶性有机溶剂来制备分散体; 通过将分散体与分散溶剂混合来制备乳液; 通过加入碱或酸从乳液中除去不溶于水的有机溶剂; 并获得去除了水不溶性有机溶剂的聚合物微球并将其重新分散在加热后的分散溶剂中。本发明还涉及治疗或预防癌症的方法及其用途。本发明的组合物不涉及溶剂蒸发或溶剂提取的现有步骤，使用少量的水，从而使废水产生最小化，并且允许聚合物微球体内的溶剂残余物的低密度。而且，由于可以调节体内释放阿那曲唑的速度，所以本发明对于制造包含阿那曲唑的缓释药物是有效的。

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