利巴韦林眼用在体凝胶剂的制备及流变学性质(英文)

Preparation and rheological evaluation of ribavirin ophthalmic in situ-gel

背景:利巴韦林易被泪液稀释,生物利用度低。在体凝胶剂可使药物在生理条件下由溶液向凝胶转化,延长药物在角膜前的滞留时间。目的:制备利巴韦林眼用在体凝胶剂,并评价其流变学性质。设计、时间及地点:体外对比观察实验,于2006-09/10在天津中医药大学现代中药发现与制剂技术教育部工程研究中心完成。材料:海藻酸钠、卡波姆、利巴韦林。方法:质量分数分别为0.01,0.02的海藻酸钠和质量分数为0.003,0.006,0.02的卡波姆进行不同的组合制备在体凝胶,凝胶中再加入利巴韦林。主要观察指标:用黏度计在不同角速度下测定不同质量浓度配比在体凝胶的黏度。结果:质量分数为0.01的海藻酸钠和质量分数为0.006的卡波姆制备的利巴韦林眼用在体凝胶剂黏度最大,其黏度变化不受加入利巴韦林的影响。海藻酸钠和卡波姆的混合溶液制备的在体凝胶剂接触泪液后发生相转变反应形成凝胶。结论:质量分数为0.01的海藻酸钠和质量分数为0.006的卡波姆制备的利巴韦林眼用在体凝胶剂流变学性质最佳,能显著延长药物在角膜前的滞留时间。

BACKGROUND： Ribavirin is easily diluted by lacrimal fluid and has low bioavailability. In situ ophthalmic gel changes from liquid drug to gel phase upon exposure to physiological conditions, resulting in an increase in the precomeal residence time of drugs. OBJECTIVE： To prepare ribavirin in situ ophthalmic gel and valuate its rheological feature. DESIGN, TIME AND SETTING： In vitro controlled observation, performed at the Engineering Research Center of Modem Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine between September and October 2006. MATERIALS： Sodium alginate, Carbopol, and dbavirin. METHODS： Sodium alginate 0% and 2%） and Carbopol （0.3%, 0.6%, and 2%） were combined at different proportions to prepare in situ ophthalmic gel, then in which ribavirin was added. MAIN OUTCOME MEASURES： Viscosity determinations of prepared different concentrations of formulations were determined using a cone and plate viscometer. RESULTS： Ribavirin in situ ophthalmic gel prepared with 1% sodium alginate and 0.6% Carbopol had the largest viscosity. The viscosity change was not influenced by the addition of ribavirin. The in situ ophthalmic gel prepared with sodium alginate and Carbopol changed to the gel phase upon exposure to lacrimal fluid. CONCLUSION： 1% sodium alginate and 0.6% Carbopol produced the best rheological feature and could prolonge the precomeal residence time of drug than that of conventional ophthalmic solution.