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PHARMACEUTICAL FORMULATION FOR ORAL OR TOPICALL ADMINISTRATION FOR IMPROVING BIOAVAILABILITY OF HYDROPHOBIC ACTIVE INGREDIENTS

机译:口服或局部给药的药物配方,可提高疏水性活性成分的生物利用度

摘要

A method of increasing viscosity of a pharmaceutical formulation for oral or topical administration comprises the steps of combining: a) an effective amount of one or more hydrophobic active ingredients; b) 5 to 50% of one or more compounds selected from polyglycerol esters of fatty acids of formula (1) CH2OR-CHOR-CH2O-ÄCH2CHOR-CH2O-ÜNCH2-CHOR-CH2OR wherein n is an integer from 4 to 13 and R is H or CO.R' wherein R' is C8-22 saturated, unsaturated or hydroxylated alkyl and wherein at least one group R is not hydrogen; c) 5 to 50% of one or more compounds selected from polyglycerol esters of fatty acids and/or unsaturated fatty acids of formula (2). CH2OR-CHOR-CH2O-ÄCH2CHOR-CH2OÜNCH2-CHOR-CH2OR wherein n is an integer from 0 - 10 and R = H or CO.R" wherein R" is C8-22 saturated, unsaturated or hydroxylated alkyl, and wherein while at least one group R is not hydrogen; d) 5 to 50% of one or more compounds selected from triglyceride macrogol glycerol esters, partial glycerides or fatty acids or macrogol esters of fatty acids in which the average quantity of reacted ethylene oxide in the synthesis of these substances ranges between 50 to 150 mols and concurrently the ratio between components b) and d) is from 0.1 : 1 to 10 : 1; wherein the above percentages are selected to total 100%; and wherein upon dilution with water 1:1 by volume the viscosity of the formulation increases by at least 5 times in comparison to the undiluted composition.
机译:增加用于口服或局部给药的药物制剂的粘度的方法包括以下步骤:a)有效量的一种或多种疏水活性成分; b)5至50%的一种或多种选自式(1)的脂肪酸的聚甘油酯的化合物:CH2OR-CHOR-CH2O-ÄCH2CHOR-CH2O-ÜNCH2-CHOR-CH2OR其中n为4至13的整数,R为H或CO.R',其中R'是C8-22饱和,不饱和或羟基化的烷基,并且其中至少一个基团R不是氢; c)5至50%的一种或多种选自式(2)的脂肪酸和/或不饱和脂肪酸的聚甘油酯的化合物。 CH2OR-CHOR-CH2O-ÄCH2CHOR-CH2OÜNCH2-CHOR-CH2OR其中n为0-10的整数且R = H或CO.R“,其中R”为C8-22饱和,不饱和或羟基化的烷基,且其中一个基团R不是氢; d)5至50%的一种或多种选自甘油三酸酯聚乙二醇甘油酯,部分甘油酯或脂肪酸或脂肪酸的聚乙二醇酯的化合物,其中这些物质的合成中环氧乙烷的平均反应量为50至150摩尔同时组分b)和d)之间的比例为0.1∶1至10∶1。其中上述百分比选择为总计100%;并且其中在用水以1:1体积稀释时,与未稀释的组合物相比,制剂的粘度增加了至少5倍。

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