加替沙星温度敏感型原位凝胶质量和体内药动学研究论文.docVIP

加替沙星温度敏感型原位凝胶的质量和体内药动学研究 目录 摘要………………………………………………………………………1 前言………………………………………………………………………3 研究的背景及意义……………………………………………4 1.1 温敏型原位凝胶……………………………………………………4 1.2 泊洛沙姆水凝胶的胶凝机理………………………………………4 第二章 加替沙星温敏型眼用原位凝胶的处方前研究…………………6 2.1 主要试剂及仪器……………………………………………………6 2.2 处方前研究…………………………………………………………7 第三章 加替沙星温敏型眼用原位凝胶的质量考察…………………11 3.1 加替沙星温敏型原位凝胶的体外溶蚀与释放……………………11 3.2 胶凝温度的测定……………………………………………………13 第四章 加替沙星温敏型眼用原位凝胶的体内药动学研究…………16 4.1 眼内药动学研究…………………………………………………16 4.2 家兔的体内药动学实验……………………………………………19 参考文献…………………………………………………………………20 致谢………………………………………………………………………8 附录X…………………………………………………………………… 9 加替沙星温度敏感型原位凝胶的质量和体内药动学研究 黄莉 0841918 摘要：加替沙星是第4代氟喹诺酮类药物，为国家西药一类新药[2]。其应用特点为抗菌谱广、抗菌活性高、生物利用度好、半衰期长、给药方便、不良反应较少。临床上[3]主要为滴眼剂和普通凝胶剂，但是滴眼剂作用时间短、生物利用率低，需频繁滴眼，患者依从性差；凝胶剂黏度大，分剂量不准确，给药不方便。本课题以加替沙星为模型药物，制备温度敏感型原位凝胶，通过眼部给药后形成凝胶，达到维持药物缓慢释放，眼部滞留时间延长，提高生物利用度目的。 关键词：温敏型原位凝胶； 泊洛沙姆； 体外溶蚀； 胶凝温度；体内药动学 Research on the gatifloxacin temperature-sensitive in situ gel and in-vivo Pharmacokinetic Abstract： Gatifloxacin is a 4th generation fluoroquinolones drug, a class of [2] Western medicine for the country. Its application characteristics involves broad antibacterial, spectrum antibacterial activity, good bioavailability , long half-life, convenient dosing and few adverse reactions. Its clinical agents are mainly eye drops and gels. But eye drops has a lot of disadvantages including short active time, low bioavailability and frequent delivery in patients with poor compliance. Besides the viscosity of the gel is very high and its divided doses is not accurate. So the drug is not convenient. This topic is to add Gatifloxacin as a model drug and prepare temperature-sensitive in situ gel through the formation of the gel after ocular administration to maintain the drug slowly released, extend residence time in eye and enhance the bioavailability . Keywords：Temperature-sensitive in situ gel; poloxamer; in vitro dissolution; gelling temperature; pharmacokinetic 前言 智能材料是一种能从自身表层或内部获取环境条件及其变化规律，进行判断、处理和做出反应，以改变自身结构和功能使其