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PROLIPOSOMAL AND LIPOSOMAL COMPOSITIONS OF POORLY WATER-SOLUBLE COMPOUNDS

机译:水溶性化合物的脂溶性和脂溶性组成

摘要

Concentrates or proliposomal compositions of poorly water-soluble drugs and compounds, comprising of one or more membrane forming lipids, a membrane stabilizing agent, in a suitable vehicle, and optionally containing a Polyethylene Glycol (PEG)-coupled phospholipid or a mixture thereof and further, optionally containing pharmaceutically acceptable excipients such as antioxidants, buffering agents, acidifying agents etc. are provided, which have superior long term stability. The concentrates of proliposomal compositions instantly form liposomes of the said poorly water-soluble drugs and compounds on rapid injection to a diluting fluid, the liposomal composition so obtained, characterized by a physical stability more than 24 hours, = 95% drug encapsulation and having a particle size diameter of less than 100 nm. The liposomal compositions so obtained can further be directly administered to patients in need of treatment of the poorly water-soluble drugs and compounds.
机译:水溶性差的药物和化合物的浓缩物或脂质体组合物,在合适的溶媒中包含一种或多种成膜脂质,膜稳定剂,并可选地包含聚乙二醇(PEG)偶联的磷脂或其混合物,还包括本发明提供了具有优异的长期稳定性的,任选地包含药学上可接受的赋形剂,例如抗氧化剂,缓冲剂,酸化剂等。原脂质体组合物的浓缩物在快速注射到稀释液中后立即形成所述水溶性差的药物和化合物的脂质体,如此获得的脂质体组合物的特征在于24小时以上的物理稳定性,≥95%的药物包封并具有粒径小于100 nm。如此获得的脂质体组合物可以进一步直接施用于需要治疗水溶性差的药物和化合物的患者。

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