Ramteke Suman, Jain Narendra K
School of Pharmaceutical Sciences, Rajiv Gandhi Technical University, Airport Bypass, Gandhinagar, Bhopal, India.
J Drug Target. 2008 Jan;16(1):65-72. doi: 10.1080/10611860701733278.
The aim of the present work was to prepare and evaluate the oral mucoadhesive sustained release nanoparticles of clarithromycin and omeprazole in order to improve patient compliance by improving its therapeutic effect and reducing its dose-related side effects. The clarithromycin- and omeprazole-containing gliadin nanoparticles were prepared by the desolvation method using Pluronic F-68 as a stabilizing agent. The results showed that this method is reproducible, easy, and leads to the efficient entrapment of drug as well as formation of spherical particles ranging from 400 to 650 nm. The maximum percentage of drug entrapment for clarithromycin and omeprazole was 81.7 +/- 2.2 and 73.7 +/- 3.9%, respectively, whereas the percentage of yield of the system was 85.1 +/- 1.9%. The sustained release behavior of gliadin nanoparticles was evaluated in phosphate-buffered saline (pH 7.4) and simulated gastric fluid (pH 1.2), at 37 +/- 1 degrees C. Their mucoadhesive properties were determined by in vitro and in vivo methods. In vitro antibacterial activity of the formulations was performed on isolated culture of Helicobacter pylori, which showed greater eradication effect of dual therapy entrapped formulations when compared with single therapy containing formulations and plain drugs.
本研究的目的是制备并评估克拉霉素和奥美拉唑的口腔黏膜黏附性缓释纳米颗粒，以通过提高其治疗效果和减少剂量相关副作用来提高患者的依从性。采用去溶剂化法，以普朗尼克F-68为稳定剂，制备了含克拉霉素和奥美拉唑的麦醇溶蛋白纳米颗粒。结果表明，该方法具有可重复性、简便性，能有效包封药物，并形成粒径在400至650nm之间的球形颗粒。克拉霉素和奥美拉唑的最大药物包封率分别为81.7±2.2%和73.7±3.9%，而该体系的产率为85.1±1.9%。在37±1℃下，在磷酸盐缓冲液（pH 7.4）和模拟胃液（pH 1.2）中评估了麦醇溶蛋白纳米颗粒的缓释行为。通过体外和体内方法测定了它们的黏膜黏附特性。对幽门螺杆菌分离培养物进行了制剂的体外抗菌活性测试，结果表明，与含单一疗法的制剂和普通药物相比，双重疗法包封制剂的根除效果更佳。
