Solanki Shailendra Singh, Sarkar Brajesh, Dhanwani Rakesh Kumar
Department of Pharmaceutics, College of Pharmacy, IPS Academy, Rajendra Nagar, Indore 452012, India.
ISRN Pharm. 2012;2012:108164. doi: 10.5402/2012/108164. Epub 2012 Jul 8.
Ampelopsin, one of the most common flavonoids, reported to possess numerous pharmacological activities and shows poor aqueous solubility. The purpose of this study was to enhance the dissolution rate and bioavailability of this drug by developing a novel delivery system that is microemulsion (ME) and to study the effect of microemulsion (ME) on the oral bioavailability of ampelopsin. Capmul MCM-based ME formulation with Cremophor EL as surfactant and Transcutol as cosurfactant was developed for oral delivery of ampelopsin. Optimised ME was evaluated for its transparency, viscosity, percentage assay and so forth. Solubilisation capacity of the ME system was also determined. The prepared ME was compared with the pure drug solution and commercially available tablet for in vitro drug release. The optimised ME formulation containing ampelopsin, Capmul MCM (5.5%), Cremophor EL (25%), Transcutol P (8.5%), and distilled water showed higher in vitro drug release, as compared to plain drug suspension and the suspension of commercially available tablet. These results demonstrate the potential use of ME for improving the bioavailability of poor water soluble compounds, such as ampelopsin.
白藜芦醇是最常见的黄酮类化合物之一，据报道具有多种药理活性，但水溶性较差。本研究的目的是通过开发一种新型给药系统——微乳（ME）来提高该药物的溶出速率和生物利用度，并研究微乳（ME）对白藜芦醇口服生物利用度的影响。开发了以Capmul MCM为基础、聚氧乙烯蓖麻油（Cremophor EL）为表面活性剂、二甲基亚砜（Transcutol）为助表面活性剂的微乳制剂用于白藜芦醇的口服给药。对优化后的微乳进行了透明度、粘度、含量测定等方面的评估。还测定了微乳体系的增溶能力。将制备的微乳与纯药物溶液和市售片剂进行体外药物释放比较。与普通药物混悬液和市售片剂的混悬液相比，含有白藜芦醇、Capmul MCM（5.5%）、聚氧乙烯蓖麻油（Cremophor EL，25%）、二甲基亚砜（Transcutol P，8.5%）和蒸馏水的优化微乳制剂显示出更高的体外药物释放。这些结果证明了微乳在提高难溶性化合物（如白藜芦醇）生物利用度方面的潜在应用。
