Gattani Surendra Ganeshlal, Savaliya Pankaj Jayantilal, Belgamwar Veena Shailendra
R. C. Patel Institute of Pharmaceutical Education & Research, Maharashtra, India.
Chem Pharm Bull (Tokyo). 2010 Jun;58(6):782-7. doi: 10.1248/cpb.58.782.
An objective of the present study was to develop alginate/hydroxypropyl methylcellulose (HPMC) based floating-mucoadhesive beads of clarithromycin to provide prolonged contact time of antibiotic to treat stomach ulcer. Floating-mucoadhesive beads were prepared and characterized for in vitro performance followed by investigation of ex vivo study in albino-wistar rats. Beads were prepared by ionic gelation technique where calcium chloride used as gelating agent and incorporated liquid paraffin for floating of the beads. Prepared beads were evaluated extensively for particle size, drug entrapment; swelling and surface morphology by using scanning electron microscopy. X-ray radioimaging study in rabbits, in vitro mucoadhesion using rat stomach mucosal membrane and in vitro drug release studies were carried out. Ex vivo performance of alginate-HPMC beads were studied using albino rats in comparison to simple alginate-calcium beads. Alginate-HPMC beads may be suitable floating-muco-adhesive drug delivery system for delivering clarithromycin to treat stomach ulcers.
本研究的一个目标是开发基于藻酸盐/羟丙基甲基纤维素（HPMC）的克拉霉素胃漂浮型粘膜粘附微球，以延长抗生素的接触时间来治疗胃溃疡。制备了胃漂浮型粘膜粘附微球并对其体外性能进行了表征，随后在白化Wistar大鼠中进行了体内研究。微球通过离子凝胶技术制备，其中使用氯化钙作为凝胶剂，并加入液体石蜡以使微球漂浮。通过扫描电子显微镜对制备的微球进行了粒度、药物包封率、溶胀和表面形态的广泛评估。对兔子进行了X射线放射成像研究，使用大鼠胃粘膜进行了体外粘膜粘附研究以及体外药物释放研究。与单纯的藻酸盐-钙微球相比，使用白化大鼠研究了藻酸盐-HPMC微球的体内性能。藻酸盐-HPMC微球可能是一种适合用于递送克拉霉素治疗胃溃疡的胃漂浮型粘膜粘附给药系统。
