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出 处:《药学与临床研究》2012年第4期293-296,共4页Pharmaceutical and Clinical Research
基 金:国家"重大新药创制"科技重大专项(2009ZX09310-004)
摘 要:目的:研究加替沙星温敏型凝胶及离子敏感型凝胶的体外释药特性、机制及在家兔房水中的药动学特征。方法:采用无膜溶出法考察凝胶的体外溶蚀及药物释放;局部滴入加替沙星凝胶剂或滴眼液,以HPLC法测定兔眼房水中的药物浓度,计算药动学参数。结果:凝胶溶蚀与药物释放速率均随着振荡频率和释放面积的增加而增大,两者具有明显的相关性;给药后8 h内,温敏、离子敏感凝胶组与滴眼液组房水中药物峰浓度分别为(1.38±0.11)μg·mL-1、(1.19±0.20)μg·mL-1及(0.50±0.06)μg·mL-1,达峰时间分别为2.0 h、1.0 h和1.0 h,AUC0-8h分别为(5.61±0.25)μg·h·mL-1、(4.50±0.19)μg·h·mL-1和(1.29±0.22)μg·h·mL-1。结论:凝胶溶蚀与药物释放行为符合零级动力学方程,药物的释放主要由凝胶溶蚀决定。加替沙星凝胶剂较滴眼液可显著提高房水中的药物浓度及生物利用度并延长了作用时间。Objective: To study the in vitro release property and mechanism of gatifloxacin thermosensitive and ion-sensitive in situ gels and their pharmacokinetics in rabbit ocular aqueous humors. Methods: The membraneless model was used to investigate the release behavior of the gels; gatifloxacin gels or eye drops were dropped into rabbit's eyes, the drug levels in aqueous humors were assayed by HPLC, the pharmacokinetic parameters were accounted then. Results: The velocities of gel erosion and drug release were both increased with the increase of shaking frequency and release area, the correlation was apparent; during the 8 hours after instillation, the peak levels in aqueous humors were (1.38±0.11)μg·h·mL-1, (1.19±0.20)μg·h·mL-1and (0.50±0.06)μg·h·mL-1, the peak time were 2.0h, 1.0h and 1.0h, the AUC0h were (5.61±0.25) μg·h·mL-1, (4.50±0.19) μg·h·mL-1 and (1.29±0.22) μg·h·mL-1for thermo-sensitive, ion- sensitive gel and eye drop group, respectively. Conclusion: Gel erosion and drug release were in line with zero-order equation of dynamics, the release was controlled by erosion. Compared with the eye drops, the drug levels, bioavailabilities and action times of the in situ gels were all significantly increased.
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