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首页> 外文期刊>Journal of Pharmaceutics >Preparation and Characterization of Self-Microemulsifying Drug Delivery System of Olmesartan Medoxomil for Bioavailability Improvement
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Preparation and Characterization of Self-Microemulsifying Drug Delivery System of Olmesartan Medoxomil for Bioavailability Improvement

机译：奥美沙坦美多西米自微乳化递药系统的制备和表征，以提高生物利用度

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Olmesartan medoxomil (OLM) is an angiotensin II receptor blocker (ARB) antihypertensive agent administered orally that has absolute bioavailability of only 26% due to the poor aqueous solubility (7.75 μg/ml). The aim of the present investigation was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral absorption of OLM. The solubility of OLM in various oils, surfactants, and cosurfactants was determined. Pseudoternary phase diagrams were constructed using Acrysol EL 135, Tween 80, Transcutol P, and distilled water to identify the efficient self-microemulsification region. Prepared SMEDDS was further evaluated for its emulsification time, drug content, optical clarity, droplet size, zeta potential,in vitrodissolution, andin vitroandex vivodrug diffusion study. The optimized formulation S2 contained OLM (20 mg), Tween 80 (33%v/v), Transcutol P (33%v/v), and Acrysol EL 135 (34%v/v) had shown the smallest particle size, maximum solubility, less emulsification time, good optical clarity, andin vitrorelease. Thein vitroandex vivodiffusion rate of the drug from the SMEDDS was significantly higher than that of the plain drug suspension. It was concluded that SMEDDS would be a promising drug delivery system for poorly water-soluble drugs by the oral route.
机译：口服奥美沙坦medoxomil（OLM）是一种血管紧张素II受体阻滞剂（ARB）降压药，由于水溶性差（7.75μg/ ml），因此绝对生物利用度仅为26％。本研究的目的是开发一种自微乳化药物递送系统（SMEDDS），以增强OLM的口服吸收。确定了OLM在各种油，表面活性剂和辅助表面活性剂中的溶解度。使用Acrysol EL 135，Tween 80，Transcutol P和蒸馏水构建伪三元相图，以鉴定有效的自微乳化区域。进一步评估了制备的SMEDDS的乳化时间，药物含量，光学透明度，液滴大小，ζ电位，体外溶出度以及体外和体内药物扩散研究。优化的配方S2包含OLM（20 mg），吐温80（33％v / v），Transcutol P（33％v / v）和Acrysol EL 135（34％v / v）的粒径最小，最大溶解度，较少的乳化时间，良好的光学透明度和体外释放。 SMEDDS中药物的体外和体外扩散速率显着高于纯药物悬液。结论是，通过口服途径，SMEDDS将是水溶性差的药物的有希望的药物递送系统。

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