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    • 1. 发明申请
    • METHOD FOR MANUFACTURING UNIFORM SIZE POLYMERIC NANOPARTICLES CONTAINING POORLY SOLUBLE DRUGS
    • 制造含有不溶性药物的均匀聚合物纳米颗粒的方法
    • WO2009134091A3
    • 2010-02-11
    • PCT/KR2009002289
    • 2009-04-30
    • KOREA RES INST OF BIOSCIENCECHUNG BONG HYUNLIM YONG TAIKHAN JUNG HYUN
    • CHUNG BONG HYUNLIM YONG TAIKHAN JUNG HYUN
    • B82B3/00
    • A61K9/1652A61K9/5153A61K31/235A61K31/343A61K31/513A61K31/519A61K31/5415A61K31/573A61K31/585A61K31/704A61K31/7048B01D65/00C08J3/03Y10S516/929
    • The present invention relates to a method for manufacturing uniform size polymeric nanoparticles containing poorly soluble drugs, and more particularly, to a method for manufacturing uniform size polymeric nanoparticles containing poorly soluble drugs, including a first step of dissolving a biodegradable polymer in a non-volatile polar organic solvent, a second step of adding poorly soluble drugs to water and the biodegradable polymer solution to produce a dispersion, and a third step of adding the dispersion to emulsifier solutions in a batch under the condition of low mechanical energy level stirring. The polymeric nanoparticles of the present invention is capable of manufacturing nano-sized small and uniform polymeric nanoparticles through a simple method of employing a non-volatile polar solvent, especially a solvent having a polarity similar to that of water, as a solvent for a mixture solution of biodegradable polymer and poorly soluble materials, and using a low mechanical energy condition and batch-adding of dispersion in an emulsifying process. The polymeric nanoparticles of the present invention are advantageous in that the dissolution rate of the poorly soluble drugs contained in polymeric particles is dramatically improved, and the poorly soluble drugs are gradually and steadily released and maintained at a constant density over a long period of time.
    • 本发明涉及一种制备均匀尺寸的含有难溶性药物的聚合物纳米颗粒的方法,更具体地说,涉及一种制备均匀尺寸的含有难溶性药物的聚合物纳米颗粒的方法,包括将生物可降解聚合物溶解在非挥发性物质中的第一步骤 极性有机溶剂,向水中添加难溶性药物和生物降解性聚合物溶液以产生分散体的第二步骤,以及在低机械能级搅拌的条件下将分散体分批加入到乳化剂溶液中的第三步骤。 本发明的聚合物纳米颗粒能够通过使用非挥发性极性溶剂,特别是极性类似于水的溶剂的简单方法作为混合物的溶剂来制造纳米尺寸的小且均匀的聚合物纳米颗粒 可生物降解聚合物和难溶物质的溶液,并使用低机械能条件和在乳化过程中分批添加分散体。 本发明的聚合物纳米颗粒的优点在于,包含在聚合物颗粒中的难溶性药物的溶解速度显着提高,并且难溶性药物在长时间内逐渐稳定地释放并保持在恒定的密度。
    • 2. 发明申请
    • POORLY SOLUBLE DRUG-CONTAINING RELEASE-CONTROLLED POLYMERIC NANOPARTICLE FORMULATION
    • 不溶解药物释放控制的聚合物纳米颗粒配方
    • WO2009134092A3
    • 2010-01-21
    • PCT/KR2009002291
    • 2009-04-30
    • KOREA RES INST OF BIOSCIENCECHUNG BONG HYUNLIM YONG TAIKHAN JUNG HYUN
    • CHUNG BONG HYUNLIM YONG TAIKHAN JUNG HYUN
    • A61K9/51A61K9/00A61K9/127A61K47/00
    • A61K9/5153
    • The present invention relates to a release-controlled polymeric nanoparticle formulation containing biphenyl-dimethyl-dicarboxylate, a poorly soluble drug, and more particularly, to a nano-sized polymer formulation having a particle size distribution of narrow range, in which the biphenyl-dimethyl-dicarboxylate, a poorly soluble drug, is impregnated in biodegradable polymer and the surface of the formulation is coated with an emulsifier. The polymeric nanoparticle formulation according to the present invention can be effectively used in the treatment of hepatic disease since the formulation enhances the dissolution rate of biphenyl-dimethyl-dicarboxylate which is a poorly soluble drug to increase bioavailability, and releases drugs gradually to keep the drugs at a constant density in blood over a long period of time. The polymeric nanoparticle formulation of the present invention may prevent an excessive use of biphenyl-dimethyl-dicarboxylate caused due to the low dissolution rate in a body and low bioavailability of conventional formulations containing biphenyl-dimethyl-dicarboxylate.
    • 本发明涉及含有联苯二甲酸二甲酯(一种难溶性药物)的释放控制聚合物纳米颗粒制剂,更具体地说,涉及一种具有窄范围的粒径分布的纳米尺寸聚合物制剂,其中联苯基 - 二甲基 二羧酸盐,一种难溶性药物,被浸渍在可生物降解的聚合物中,制剂的表面用乳化剂包衣。 本发明的聚合物纳米颗粒制剂可以有效地用于肝脏疾病的治疗,因为该配方增加联苯基 - 二甲酸二甲酯的溶出速率,其是难溶性药物以提高生物利用度,并逐渐释放药物以保持药物 在长时间的血液中以恒定的密度。 本发明的聚合物纳米颗粒制剂可以防止由于体内低溶解速率和含有联苯二甲酸二甲酯的常规制剂的低生物利用度引起的联苯二甲酸二甲酯的过量使用。