Department of Pharmacy, Health and Well Being, Faculty of Applied Sciences, University of Sunderland, City Campus, Sunderland, UK.
Drug Dev Ind Pharm. 2013 Jul;39(7):1142-51. doi: 10.3109/03639045.2012.725734. Epub 2012 Sep 25.
The aim of this study was to produce cinnarizine loaded Eudragit(®) L100-55 microparticles by coacervation technique in order to achieve pH responsive drug release using hydroxypropyl methycellulose (HPMC) as stabilizer. The effect of enteric polymer: HPMC ratio on properties of microparticles was investigated with regard to particle size distribution, morphology, yield, encapsulation efficiency, in vitro drug release profiles and interaction between cinnarizine and Eudragit(®) L100-55. High drug encapsulation efficiency was seen in all microparticles. Particle diameter increased when the enteric polymer content was higher relative to HPMC. In vitro dissolution studies demonstrated that the drug release from the microparticles was dependent upon enteric polymer: HPMC ratio and particle size distribution. At the ratio of at least 3.75:1 of enteric polymer: HPMC, drug release was suppressed most significantly in low pH (hydrochloric acid as medium) while rapid drug release was observed in pH 7.4.
本研究旨在通过凝聚技术制备桂利嗪载 Eudragit(®) L100-55 微粒,并用羟丙甲纤维素(HPMC)作为稳定剂以实现 pH 响应型药物释放。考察了肠溶聚合物:HPMC 比例对微粒性质的影响,包括粒径分布、形态、产率、包封效率、体外药物释放曲线以及桂利嗪与 Eudragit(®) L100-55 之间的相互作用。所有微粒均显示出较高的药物包封效率。与 HPMC 相比,当肠溶聚合物含量较高时,粒径增大。体外溶出度研究表明,微粒中药物的释放取决于肠溶聚合物:HPMC 的比例和粒径分布。在肠溶聚合物:HPMC 的比例至少为 3.75:1 时,药物在低 pH(盐酸为介质)下的释放受到最显著的抑制,而在 pH7.4 时则观察到快速释放。