Department of Pharmaceutics, Poona College of Pharmacy, Bharti Vidyapeeth University, Erandwane, Pune, 411038 Maharashtra, India.
AAPS PharmSciTech. 2010 Mar;11(1):267-77. doi: 10.1208/s12249-010-9384-1. Epub 2010 Feb 24.
The purpose of the present work was the development and evaluation of stomach-specific controlled release mucoadhesive drug delivery system prepared by ionotropic gelation of gellan beads, containing acid-soluble drug amoxicillin trihydrate, using 3(2) factorial design with concentration of gellan gum and quantity of drug as variables. The study showed that beads prepared in alkaline cross-linking medium have higher entrapment efficiency than the acidic cross-linking medium. The entrapment efficiency was in the range of 32% to 46% w/w in acidic medium, which increased up to 60% to 90% w/w in alkaline medium. Batches with lowest, medium, and highest drug entrapment were subjected to chitosan coating to form a polyelectrolyte complex film. As polymer concentration increases, entrapment efficiency and particle size increases. Scanning electron microscopy revealed spherical but rough surface due to leaching of drug in acidic cross-linking solution, dense spherical structure in alkaline cross-linking solution, and rough surface of chitosan-coated beads with minor wrinkles. The in vitro drug release up to 7 h in a controlled manner following the Peppas model (r = 0.9998). In vitro and in vivo mucoadhesivity study showed that beads have good mucoadhesivity and more than 85% beads remained adhered to stomach mucosa of albino rat even after 7 h. In vitro growth inhibition study showed complete eradication of Helicobacter pylori. These results indicate that stomach-specific controlled release mucoadhesive system of amoxicillin gellan beads may be useful in H. pylori treatment.
本工作的目的是开发和评价胃溶型、离子凝胶化的、具有粘弹性的、载阿莫西林三水合物的控制释放给药系统，采用 3(2) 析因设计，以凝胶多糖浓度和药物量为变量。研究表明，在碱性交联介质中制备的胶珠包封率高于酸性交联介质。在酸性介质中，包封率在 32%至 46%w/w 范围内，在碱性介质中增加至 60%至 90%w/w。包封率最低、中等和最高的三个批次进行壳聚糖包衣，形成聚电解质复合膜。随着聚合物浓度的增加，包封率和粒径增加。扫描电子显微镜显示，由于药物在酸性交联溶液中的溶出，球形但粗糙的表面；碱性交联溶液中，致密的球形结构；壳聚糖包衣珠的表面有轻微的皱纹，呈粗糙状。按照 Peppas 模型（r = 0.9998），在 7 小时内实现了受控的体外药物释放。体外和体内粘膜粘附性研究表明，珠具有良好的粘膜粘附性，即使在 7 小时后，仍有超过 85%的珠粘附在白化大鼠的胃粘膜上。体外生长抑制研究表明，阿莫西林胶珠可完全根除幽门螺杆菌。这些结果表明，阿莫西林胶珠的胃溶型、控制释放、粘弹性给药系统可能对幽门螺杆菌的治疗有用。
