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MICROEMULSION PRECONCENTRATES WHICH CONTAIN CYCLOSPORINES AND CORRESPONDING MICROEMULSIONS

机译:微胎浓缩液含有环孢菌素和相应的微胎液

摘要

The invention relates to compositions provided in the form of microemulsion preconcentrates containing: (a) a mixture consisting of a medium chain triglyceride and of an omega-9-fatty acid and/or of an omega-6-fatty acid, and; (b) a surface-active constituent containing a surfactant of the polyoxethylene type; however, containing essentially none of the following constituents which can be mixed with water or which are soluble in water: C1-C5 alkyl diether or tetrahydrofurfuryl diether or partial ether of low-molecular monooxy or polyoxy C2-C12 alkane diols; 1,2-propylene glycol; low alkanols; esterification products or polycarboxylic acids with 2-10, especially 3-5 carboxyl groups with C1-C10 alcohols, and; esterification products of polyols with 2-10, especially 3-5 carboxyl groups with C2-C11 carboxylic acids. These microemulsion preconcentrates form microemulsions when brought into contact with water or with an aqueous medium, whereby those of the O/W type have an average particle size of less than 150 nm, preferably of less than 100 nm. The inventive microemulsion preconcentrates and microemulsions are suited for use as a vehicle for substances, namely active substances, which are poorly soluble in water but, however, are soluble in constituents (a) and/or (b). In their water-phase, said microemulsions can contain water-soluble substances.
机译:本发明涉及以微乳液预浓缩物形式提供的组合物,其包含:(a)由中链甘油三酸酯和ω-9-脂肪酸和/或ω-6-脂肪酸组成的混合物,和(b)含有聚氧乙烯型表面活性剂的表面活性成分;但是,基本上不含有以下任何一种成分,这些成分不能与水混合或溶于水:低分子单氧或多氧C2-C12烷二醇的C1-C5烷基二醚或四氢糠基二醚或部分醚; 1,2-丙二醇;低烷醇;与C1-C10醇具有2-10个,特别是3-5个羧基的酯化产物或多元羧酸,和具有2-10个,尤其是3-5个羧基的多元醇与C2-C11羧酸的酯化产物。当与水或水性介质接触时,这些微乳液预浓缩物形成微乳液,由此,O / W型那些的平均粒径小于150nm,优选小于100nm。本发明的微乳液预浓缩物和微乳液适合用作物质的载体,即活性物质,其难溶于水但可溶于组分(a)和/或(b)。在它们的水相中,所述微乳液可以包含水溶性物质。

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