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盐酸环丙沙星缓释片的体外释放与体内吸收的相关性
IN VIVO AND VITRO CORRELATION OF EXTENDED-RELEASE TABLET OF CIPROFLOXACIN HYDROCHLORIDE
【Author】 LI Junfeng,lRUAN Yingli, GUO Ruichenl and ITANG Zhenxiang (Weihai Municipal Hospital, Weihai, 264200; Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan,250013)
【机构】 山东省威海市立医院; 山东大学齐鲁医院临床药理研究所;
【摘要】 目的对盐酸环丙沙星缓释片的体外释放与体内吸收相关性进行研究。方法体外释放采用中国药典2000年版二部的转篮法,体内血药浓度以RP-HPLC法测定和DAS软件计算药动学参数。结果在12h平均累积释放99%;20名男性健康志愿者口服单剂量500mg盐酸环丙沙星缓释片的体内过程符合开放-室模型,AUC0-t为10.889±1.385 μg·h·ml-1;Cmax 为1.026±0.247 μg·ml-1;Tmax为5.4±1.1h.结论将体外释放百分率即释放度(F)对体内吸收分数(f)同归得同归议程为:f=-0.51853±1.14322E对相关系数进行检验,两者之间存在显著相关性(p<0.05)。
【Abstract】 Objective: To study in vivo and vitro correlation of extended-release tablet of ciprofloxacin. Methods: The dissolution of ciprofloxacin was determined in vitro and the serum concentrations of ciprofloxacin in vivo was determined by RP-HPLC. Results: The dissolution of ciprofloxacin was 99% within 12h. The AUC0-t,Cmax and Tmax were 10.889±1.385 μ g, 1.026±0.247μ g · ml-1and 5.4±1.1h, respectively. Conclusions: There was significant correlation between in vitro dissolution and in vivo absorption of the tablet.
【Key words】 extended-release tablet; ciprofloxacin hydrochloride; dissolution; bioavailability; correlation in vivo and vitro;
- 【会议录名称】 山东省药学会第一届学术年会论文集(上)
- 【会议名称】山东省药学会第一届学术年会
- 【会议时间】2005-11
- 【会议地点】中国山东济南
- 【分类号】R96
- 【主办单位】山东省药学会