埃巴斯汀,组胺H1拮抗剂,不镇静,属于BCSII类用于治疗过敏性鼻炎和慢性特发性荨麻疹。本研究旨在提高依巴斯汀的水溶性和溶解速率,通过使用油酸配制微乳液体系,Transcutol®HP,和Tween®80作为油相,助表面活性剂,和表面活性剂,分别,通过相滴定法。通过使用DesignExpert®软件(版本11;统计-Ease,Inc.,明尼阿波利斯,MN,美国)。使用数值优化技术进行配方优化,其中优化是基于可取性的。对优化后的配方进行了透光率评估,粘度,球的大小,多分散指数,zeta电位,药物含量,形态学研究,和体外研究。优化的配方显示了累积药物释放百分比,溶出研究后获得的药物释放百分比为82.9%至90.6%,扩散研究后的累积药物释放百分比为83.3%至100%。对体外释放数据进行动力学处理。零阶图和一阶图是线性的,并显示出R2的最高值,这表明混合顺序释放。Higuchi图是线性的,表明扩散是释放的机制。从Peppas的情节来看,进一步证实,溶出研究的释放是异常的,而扩散研究的释放是零级的。因此,研究得出结论,微乳技术是提高BCSII类药物依巴斯汀的溶解度和溶出速率的非常好的方法。
Ebastine, a histamine H1 antagonist, nonsedating, belonging to BCS class II is used in the treatment of allergic rhinitis and chronic idiopathic urticaria. The current study was intended in augmenting the aqueous solubility and dissolution rate of
ebastine, by formulating a microemulsion system using oleic acid, Transcutol® HP, and Tween®80 as oily phase, cosurfactant, and surfactant, respectively, by the phase titration method. A custom mixture design with optimality D was used to design the formulation by using the Design Expert® Software (Version 11; Stat-Ease, Inc., Minneapolis, MN, USA). Optimization of formulation was performed using the numerical optimization technique, where optimization is based upon the desirability. The optimized formulation was evaluated for transmittance, viscosity, globule size, polydispersity index, zeta potential, drug content, morphological studies, and in vitro studies. The optimized formulation displayed percent cumulative drug release, ranging from 82.9% to 90.6% obtained after dissolution studies and the percent cumulative drug release after diffusion studies ranged from 83.3% to 100%. The in vitro release data were subjected to kinetic treatment. The zero-order and first-order plots were linear and showed the highest values for R2, which indicated mixed-order release. The Higuchi plot was linear, indicating diffusion as the mechanism of release. From Peppas plot, it was further confirmed that the release for dissolution studies was anomalous and for diffusion studies it was zero order. Thus, the studies concluded that the microemulsion technique is a very good approach for enhancing the solubility and dissolution rate of the BCS class II drug
ebastine.