体外溶出法测定柚皮素SNEDDS的释放度

Gendis Purno Yudanti, Ilham Kuncahyo, Endang Diyah Ikasari
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摘要

柚皮素是葡萄柚中主要的黄酮,具有抗炎、抗癌、保肝、抗脂质过氧化等作用。它在水中的溶解度低,口服时导致溶解和低生物利用度。本研究旨在利用SNEDDS技术提高柚皮素的溶解度和生物利用度。采用d -最优混合设计方法对SNEDDS进行初步表征,确定最佳配方,即以三乙酸乙酯为油相,吐温80为表面活性剂,transcutol P为助表面活性剂为独立因素,以乳化时间、载药量、粒径球和透光率为响应因素对SNEDDS的组成进行优化。优化结果表明,在三乙酸乙酯含量为10%、吐温含量为70%、吐温含量为80%、吐温含量为20%的条件下,柚皮素的最佳溶出度为87,50%±1,73,溶出度为28,93,表明柚皮素与柚皮素胶囊的溶出度不完全相同。
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In vitro Naringenin SNEDDS Release Test by Dissolution
Naringenin is the main flavanone in grapefruit which has anti-inflammatory, anti-cancer, hepatoprotective and antilipid peroxidation effects. Its low solubility in water causes dissolution and low bioavailability when taken orally. This study aims to increase the solubility and bioavailability of naringenin by using the SNEDDS technique. Initial characterization to determine the optimum formula was carried out using the D-optimal mixture design method, namely by optimizing the composition of SNEDDS which consisted of triacetin as the oil phase, tween 80 as surfactant and transcutol P as cosurfactant as an independent factor and SNEDDS characterization included emulsification time, drug loading, size globules and percent transmittance in response. The optimization results showed that the optimum formula was obtained at the composition of 10% triacetin, 70% tween 80 and 20% transcutol P. The dissolution test showed that the SNEDDS of naringenin was capable of dissolution (Q30) of 87,50% ±1,73 at the 30th minute and the f2 value of 28,93 so it can be concluded that the dissolution profile between the SNEDDS of naringenin and the naringenin capsules is not identical.  
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