赖氨酸布洛芬缓释液体栓的制备及体内外评价

发布时间：2018-11-23 21:05

【摘要】：目的:制备赖氨酸布洛芬缓释液体栓剂,并进行体内外评价。方法:以泊洛沙姆溶液为主要基质、卡波姆为生物黏附剂、月桂氮酮为渗透剂,制备赖氨酸布洛芬缓释液体栓剂。以胶凝温度、凝胶强度、生物黏附力及体外释放度为指标筛选泊洛沙姆407(P407)-泊洛沙姆188(P188)比例和卡波姆的含量,比较所制液体栓剂与普通固体栓剂经直肠给药后在Beagle犬体内的药-时曲线和药动学参数。结果:处方中P407-P188比例为1∶1.2时缓释液体栓剂的胶凝温度为30.4~38.1℃,最接近直肠温度;卡波姆含量为0.8%时缓释液体栓剂的体外释放符合零级方程,相关性最好(R~2=0.996)。普通固体栓的tmax为3.206 h,随后血药浓度下降明显,缓释时间不超过12 h,AUC_(0-∞)为501.826 mg·h/L;缓释液体栓剂的t_(max)为8.814 h,随后血药浓度下降,缓释时间超过24 h,AUC_(0-∞)为715.489 mg·h/L。结论:成功制得赖氨酸布洛芬缓释液体栓剂,与普通固体栓剂比较其缓控释效果更佳、体内外相关性良好。
[Abstract]:Objective: to prepare lysine ibuprofen sustained-release liquid suppository and evaluate it in vivo and in vitro. Methods: Lysine ibuprofen sustained-release liquid suppository was prepared with Poloxamer solution as main matrix, carbomer as biological adhesive and lauroxone as osmotic agent. The ratio of Poloxamer 407 (P407) to Poloxamer 188 (P188) and the content of carbomer were screened by gel temperature, gel strength, bioadhesion and in vitro release. The pharmacokinetic parameters and pharmacokinetic parameters of liquid suppositories and general solid suppositories were compared in Beagle dogs after rectal administration. Results: the gelation temperature of sustained-release liquid suppository was 30.4 鈩，

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