离子和非离子表面活性剂胶束溶液提高舒林酸的水溶性

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引用次数: 1

摘要

在药理学中,溶解度对药物的有效性和生物利用度起着至关重要的作用。利用溶解度特性来提高各种弱溶性物质的生物利用度和药理作用,是药学专家和研究人员面临的一项艰巨任务。粒径、表面积、理化性质、药物的物理形态、溶剂和表面活性剂的使用是影响溶解度的参数。本研究的目的是提高非甾体抗炎药(NSAID)的溶解度:舒林酸。采用不同表面活性剂的胶束溶液法提高了效率。研究了非离子型表面活性剂(Tween 20、40、60和80,Brij为30、35和56)和离子型表面活性剂(SDS、SDBS、CTAB、TTAB和DTAB)对药物在水溶液中溶解度的影响。测定了表面活性剂溶液的聚集数、胶束-水分配系数(KM)、摩尔增溶比(MSR)、吉布斯增溶能(∆Gºs)、胶束大小和药物胶束结合常数等参数。结果表明,使用上述表面活性剂是提高舒林酸溶解度的一种很好的方法。此外,本工作提供了对水溶解度与表面活性剂的聚集数和结构的关系的理解。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Enhancement in aqueous solubility of sulindac medicine by using the micellar solution of ionic and non-ionic surfactants
In the science of pharmacology, solubility plays a crucial role in the efficacy and bioavailability of the drug. Utilizing solubility features to improve the bioavailability and pharmacological effect of diverse weakly soluble substances, is an arduous task for pharmaceutical experts and researchers. Particle size, surface area, physicochemical qualities, physical forms of drugs, solvents and surfactant usage are parameters that influence solubility. The objective of the current study was to enhance the solubility of the non-steroidal anti-inflammatory drug (NSAID): Sulindac. The micellar solutions method was employed with different surfactants to increase the efficiency. Both nonionic (Tween 20, 40, 60 and 80 with Brij 30, 35 and 56) and ionic (SDS, SDBS, CTAB, TTAB and DTAB) surfactants were investigated for their effect on drug solubility in aqueous solution. Various parameters of surfactant solutions such as aggregation number, micelle-water partition coefficient (KM), molar solubilization ratio (MSR), Gibbs energy of solubilization (∆Gº s), size of micelle and binding constant of the drug micelles were measured. Finding reveals that the use of mentioned surfactant is an excellent approach to enhancing the solubility of sulindac. Furthermore, the present work provides an understanding of the relation of aqueous solubility with aggregation number and structure of surfactants used.
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