公开(公告)号：WO2012036529A2

公开(公告)日：2012-03-22

申请号：PCT/KR2011006892

申请日：2011-09-16

Applicant: SK CHEMICALS CO LTD ,  OH JUNG-HOON ,  RYU KEUN-HO ,  KIM JAE-SUN ,  KIM TAE KON ,  LEE SOO-MIN ,  LEE BONG-YONG ,  PARK MINSEOK ,  HONG SEOK HYUN ,  LEE JUNG A ,  KIM HYUK MIN

Inventor： OH JUNG-HOON ,  RYU KEUN-HO ,  KIM JAE-SUN ,  KIM TAE KON ,  LEE SOO-MIN ,  LEE BONG-YONG ,  PARK MINSEOK ,  HONG SEOK HYUN ,  LEE JUNG A ,  KIM HYUK MIN

IPC: C07F9/10 ,  A61K31/661 ,  A61P15/00

CPC classification number: A61K31/661 ,  C07F9/091

Abstract: Disclosed are novel dapoxetine derivatives and pharmaceutically acceptable salts thereof. The compounds are soluble in water, stable, and easy to process into preparations. In addition, the compounds exhibit improved dissolution rate and taste. Furthermore, the compounds exhibit a small difference in dissolution rate depending on pH. Further disclosed are pharmaceutical compositions including the compounds. The pharmaceutical compositions are useful for the treatment, management or prevention of premature ejaculation. Methods for preparing the dapoxetine derivatives are also disclosed.

Abstract translation: 公开了新的达泊西汀衍生物及其药学上可接受的盐。 该化合物可溶于水，稳定，易于加工成制剂。 此外，化合物表现出改善的溶解速率和味道。 此外，根据pH，化合物的溶出速率差异很小。 进一步公开的是包含该化合物的药物组合物。 药物组合物可用于治疗，管理或预防早泄。 还公开了制备达泊西汀衍生物的方法。

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

Applicant: 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

Inventor： 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: A61K9/14 ,  A61K9/22 ,  A61K31/57 ,  C08J3/12

CPC classification number: A61K9/1694 ,  A61K9/16 ,  A61K9/1647 ,  A61K31/4196 ,  A61K31/551 ,  C08J3/05 ,  C08J3/12 ,  C08J3/16 ,  C08J2367/04

Abstract: 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.

Abstract translation: 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。

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

Applicant: 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

Inventor： 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: A61K9/16 ,  A61K9/14 ,  A61K31/551 ,  A61P25/24

CPC classification number: A61K31/551 ,  A61K9/5021

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2012036529A3

公开(公告)日：2012-03-22

申请号：PCT/KR2011/006892

申请日：2011-09-16

Applicant: SK CHEMICALS CO., LTD. ,  OH, Jung-Hoon ,  RYU, Keun-Ho ,  KIM, Jae-Sun ,  KIM, Tae Kon ,  LEE, Soo-Min ,  LEE, Bong-yong ,  PARK, Minseok ,  HONG, Seok Hyun ,  LEE, Jung A ,  KIM, Hyuk Min

Inventor： OH, Jung-Hoon ,  RYU, Keun-Ho ,  KIM, Jae-Sun ,  KIM, Tae Kon ,  LEE, Soo-Min ,  LEE, Bong-yong ,  PARK, Minseok ,  HONG, Seok Hyun ,  LEE, Jung A ,  KIM, Hyuk Min

IPC: C07F9/10 ,  A61K31/661 ,  A61P15/00

Abstract: Disclosed are novel dapoxetine derivatives and pharmaceutically acceptable salts thereof. The compounds are soluble in water, stable, and easy to process into preparations. In addition, the compounds exhibit improved dissolution rate and taste. Furthermore, the compounds exhibit a small difference in dissolution rate depending on pH. Further disclosed are pharmaceutical compositions including the compounds. The pharmaceutical compositions are useful for the treatment, management or prevention of premature ejaculation. Methods for preparing the dapoxetine derivatives are also disclosed.

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

Applicant: 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

Inventor： 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: A61K9/14 ,  A61K9/22 ,  A61K31/57 ,  C08J3/12

Abstract: 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.

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

Applicant: 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

Inventor： 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: A61K9/14 ,  A61K9/22 ,  A61K31/57 ,  C08J3/12

Abstract: 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.

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

Applicant: 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

Inventor： 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: A61K9/16 ,  A61K31/4196 ,  A61K47/30 ,  A61P35/00

CPC classification number: A61K31/4196 ,  A61K9/0019 ,  A61K9/19 ,  A61K9/5026 ,  A61K9/5031

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2012011740A9

公开(公告)日：2012-01-26

申请号：PCT/KR2011/005347

申请日：2011-07-20

Applicant: 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

Inventor： 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: A61K9/14 ,  A61K9/22 ,  A61K31/57 ,  C08J3/12

Abstract: 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.