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发明授权
CN1897975B 口服给药的水溶性药物纳米颗粒组合物及其制备方法 失效 - 权利终止 转让

口服给药的水溶性药物纳米颗粒组合物及其制备方法
摘要：
本发明涉及一种含有纳米颗粒的可口服给药组合物，此纳米颗粒的粒径为500nm或更小，该组合物包括：水溶性药物和抗衡离子物质的络合物，占0.1-30％(重量)，在此络合物中带电水溶性药物与抗衡离子物质结合；脂质，占0.5-80％(重量)；聚合物，占0.5-80％(重量)；以及乳化剂，占1-80％(重量)，其中脂质与聚合物的重量比为1∶0.05-3，本发明还涉及此组合物的制备方法。本发明的组合物在口服给药后具有高胃肠吸收率，在纳米颗粒中具有高药物包载率，而且还对脂肪酶稳定。
摘要（英）：

The present invention relates to an orally administrable composition containing nanoparticles with the particle size of 500 nm or less, comprising 0.1-30 weight% of a complex of a water-soluble drug and a counter-ion substance in which -the charged water-soluble drug is bonded with the counter-ion substance, 0.5-80 weight% of a lipid, 0.5-80 weight% of a polymer, and 1-80 weight% of an emulsifier, wherein the weight ratio of said lipid and said polymer is in the range of 1:0.05-3, and a preparation method thereof. The composition of the present invention has high gastrointestinal absorption rate upon oral administration, and has high drug entrapping rate in the nanoparticle, and is also stable against lipases.

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