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1. 发明公开

EP1951211A1 TRANSDERMAL PREPARATIONS CONTAINING HYDROPHOBIC NON-STEROIDAL ANTI-INFLAMMATORY DRUGS 有权转让
标题翻译：具有疏水不NSAIDs的透皮制剂
公开(公告)号：EP1951211A1
公开(公告)日：2008-08-06
申请号：EP06799399.8
申请日：2006-10-23
申请人： Amorepacific Corporation , Pacific Pharmaceutical Co., Ltd.
发明人： CHOI, Yang Gyu , AH, Young Chang , CHOI, Woo Jeong , KIM, Jung Ju
IPC分类号： A61K9/70
摘要： Disclosed is a transdermal preparation containing a hydrophobic drug. As a method of continuing the high drug permeation, it is used an unique hydrophilic polymer system in which the drug can be contained in a high concentration under no water environment, a solubility of the hydrophobic drug is decreased as the water is introduced to the patch from the skin, so that the drug is maintained at the saturation concentration even though the drug content is decreased as the drug is permeated to the skin. During the application of the transdermal preparation to the skin, it is possible to continuously permeate the high amount of drug, to maintain the sufficient adhesion during the use and to minimize the skin side effect, because the hydrophilic polymer absorbs the water from the skin. The hydrophilic polymer system can serve the function thereof through the hydrophobic adhesive layer capable of preventing the water quickly absorbed from the skin from being evaporated to the outside of the patch.

2. 发明申请

WO2005105058A1 SUSTAINED-RELEASING INJECTABLE FORMULATION FOR THE TREATMENT OR PREVENTION OF BONE-RELATED DISEASES COMPRISING BISPHORENATE-CONTAINING POLYMERIC MICROPARTICLES 审中-公开
标题翻译：持续发布包含含双硫含量聚合物微生物治疗或预防骨相关疾病的指导性配方
公开(公告)号：WO2005105058A1
公开(公告)日：2005-11-10
申请号：PCT/KR2005/001306
申请日：2005-05-04
申请人： AMOREPACIFIC CORPORATION , CHOI, Woo Jeong , LEE, Hyeok , YANG, Jeong Hwa , KIM, Jung Ju
发明人： CHOI, Woo Jeong , LEE, Hyeok , YANG, Jeong Hwa , KIM, Jung Ju
IPC分类号： A61K9/58
CPC分类号： A61K9/0019 , A61K9/1641 , A61K47/26
摘要： Disclosed is a sustained-release injectable formulation for treating or preventing bone-related diseases, comprising bisphosphonate-containing polymeric microparticles prepared by dissolving and dispersing a bisphosphonate in an aqueous solution containing a water-soluble polymer and a hydrophilic surfactant to provide a polymer solution; adding the polymer solution to another polymer solution, prepared by adding a secondary organic solvent to a primary organic solvent containing a biodegradable polymer and a hydrophobic surfactant, to provide a primary emulsion (water-in oil (W/O) type); and dispersing the primary emulsion in an external continuous phase. The injectable formulation has an effect of sustaining drug release in vivo for a period of 4 weeks or more using only a single administration, thereby reducing administration frequency and total dosage compared to conventional oral formulations administered every day, as well as remarkably reducing local irritation compared to a directly injected non-encapsulated bisphosphonate. Therefore, this sustained-release injectable formulation is more useful in the treatment or prevention of diseases against which bisphosphonate drugs have therapeutic or preventive effects than conventional oral formulations and direct injections of bisphosphonates.
摘要翻译：公开了一种用于治疗或预防骨相关疾病的缓释可注射制剂，其包含通过将二膦酸盐溶解并分散在含有水溶性聚合物和亲水性表面活性剂的水溶液中制备的含二膦酸盐的聚合物微粒，以提供聚合物溶液; 将聚合物溶液加入到通过将二级有机溶剂加入到含有可生物降解的聚合物和疏水性表面活性剂的初级有机溶剂中以提供初级乳液（油包水（W / O）型）制备的另一种聚合物溶液中; 并将初级乳液分散在外部连续相中。可注射制剂具有仅使用单一给药在体内维持药物释放持续4周或更长时间的效果，从而与每天施用的常规口服制剂相比降低施用频率和总剂量，并且显着降低局部刺激直接注射未包封的双膦酸盐。因此，这种持续释放的可注射制剂在治疗或预防双膦酸盐药物具有比常规口服制剂和直接注射双膦酸盐治疗或预防效果的疾病更有用。

3. 发明申请

WO2007049892A1 TRANSDERMAL PREPARATIONS CONTAINING HYDROPHOBIC NON-STEROIDAL ANTI-INFLAMMATORY DRUGS 审中-公开
标题翻译：含有疏水性非甾体抗炎药物的透皮制剂
公开(公告)号：WO2007049892A1
公开(公告)日：2007-05-03
申请号：PCT/KR2006/004330
申请日：2006-10-23
申请人： AMOREPACIFIC CORPORATION , PACIFIC PHAMACEUTICAL CO., LTD. , CHOI, Yang Gyu , AH, Young Chang , CHOI, Woo Jeong , KIM, Jung Ju
发明人： CHOI, Yang Gyu , AH, Young Chang , CHOI, Woo Jeong , KIM, Jung Ju
IPC分类号： A61K9/70
CPC分类号： A61K9/7061 , A61K31/00 , A61K31/19 , A61K31/192 , A61K31/196
摘要： Disclosed is a transdermal preparation containing a hydrophobic drug. As a method of continuing the high drug permeation, it is used an unique hydrophilic polymer system in which the drug can be contained in a high concentration under no water environment, a solubility of the hydrophobic drug is decreased as the water is introduced to the patch from the skin, so that the drug is maintained at the saturation concentration even though the drug content is decreased as the drug is permeated to the skin. During the application of the transdermal preparation to the skin, it is possible to continuously permeate the high amount of drug, to maintain the sufficient adhesion during the use and to minimize the skin side effect, because the hydrophilic polymer absorbs the water from the skin. The hydrophilic polymer system can serve the function thereof through the hydrophobic adhesive layer capable of preventing the water quickly absorbed from the skin from being evaporated to the outside of the patch.
摘要翻译：公开了含有疏水性药物的透皮制剂。作为持续高药物渗透的方法，使用独特的亲水性聚合物体系，其中药物可以在无水环境下以高浓度包含，疏水性药物的溶解度随着水被引入贴剂而降低即使在药物渗入皮肤时药物含量降低，药物也保持在饱和浓度。在将透皮制剂施用于皮肤时，由于亲水性聚合物从皮肤吸收水分，因此可以连续渗透大量的药物，以在使用过程中保持足够的粘附力和最小化皮肤的副作用。亲水性聚合物体系可以通过能够防止皮肤快速吸收的水蒸发到贴片外部的疏水粘合剂层来发挥功能。

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