Miyazaki S, Kawasaki N, Kubo W, Endo K, Attwood D
Faculty of Pharmaceutical Sciences, Health Science University of Hokkaido, Ishikari-Tohbetsu, 061-0293, Hokkaido, Japan.
Int J Pharm. 2001 Jun 4;220(1-2):161-8. doi: 10.1016/s0378-5173(01)00669-x.
Three liquid formulations with in situ gelling properties have been assessed for their potential for the oral delivery of cimetidine. The formulations were dilute solutions of: (a) enzyme-degraded xyloglucan, which form thermally reversible gels on warming to body temperature; (b) gellan gum and; (c) sodium alginate both containing complexed calcium ions that form gels when these ions are released in the acidic environment of the stomach. The in vitro release of cimetidine from gels of each of the compounds followed root-time kinetics over a period of 6 h. Plasma levels of cimetidine after oral administration to rabbits of each of the formulations were compared with those resulting from administration of a commercial cimetidine/alginate suspension with an identical drug loading. In vivo release characteristics of each of the in situ gelling formulations were similar to those of the commercial preparation.
已对三种具有原位凝胶化特性的液体制剂用于西咪替丁口服给药的潜力进行了评估。这些制剂是以下物质的稀溶液:(a)酶降解的木葡聚糖,在升温至体温时形成热可逆凝胶;(b)结冷胶;以及(c)海藻酸钠,二者均含有络合钙离子,当这些离子在胃的酸性环境中释放时会形成凝胶。在6小时的时间段内,西咪替丁从每种化合物的凝胶中的体外释放遵循根时间动力学。将每种制剂经口给予兔子后西咪替丁的血浆水平与给予具有相同药物载量的市售西咪替丁/海藻酸盐混悬液后的血浆水平进行了比较。每种原位凝胶化制剂的体内释放特性与市售制剂相似。