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.

中文翻译：

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通过使用 D 最优混合物设计配制微乳剂来提高依巴斯汀的溶解度：优化和表征

依巴斯汀是一种组胺 H1 拮抗剂，具有非镇静作用，属于 BCS II 类，用于治疗过敏性鼻炎和慢性特发性荨麻疹。^{本研究旨在通过相滴定法分别使用油酸、Transcutol ®} HP 和 Tween ^® 80 作为油相、助表面活性剂和表面活性剂配制微乳液系统，从而提高依巴斯汀的水溶性和溶解速率。使用 Design Expert ^{®使用具有最优性 D 的自定义混合物设计来设计配方}软件（版本 11；Stat-Ease, Inc.，美国明尼苏达州明尼阿波利斯）。使用数值优化技术进行配方优化，其中优化基于合意性。对优化后的配方进行了透光率、粘度、小球大小、多分散指数、zeta 电位、药物含量、形态学研究和体外研究的评估。优化的处方显示累积药物释放百分比，溶出度研究后获得的百分比范围为 82.9% 至 90.6%，扩散研究后的累积药物释放百分比范围为 83.3% 至 100%。体外释放数据经过动力学处理。零阶和一阶图是线性的，并显示R ^{2的最高值}，表示混合顺序发布。Higuchi 图是线性的，表明扩散是释放机制。从 Peppas 图进一步证实，溶出研究的释放是异常的，扩散研究是零级的。因此，研究得出结论，微乳技术是提高 BCS II 类药物依巴斯汀的溶解度和溶出度的非常好的方法。