长效抗生育埋植剂CaproF体内药物释放的研究  

In vivo drug release evaluation of long-term levonorgestrel-releasing implants(CaproF)

作　　者：唐丽娜[1] 孙洪范[1] 宋存先[1] 冷希岗[1] 崔秀敏[1] 史瑞文[1] 

机构地区：[1]中国医学科学院中国协和医科大学生物医学工程研究所天津市生物医学材料重点实验室,天津300192

出　　处：《生物医学工程与临床》2007年第1期17-19,共3页Biomedical Engineering and Clinical Medicine

基　　金：国家高科技研究发展计划(863计划)(2004AA2Z3060)

摘　　要：目的对可降解长效抗生育埋植剂CaproF的体内药物释放动力学进行评价。方法将CaproF植入Wister大鼠皮下。每隔一定时间处死动物,取出埋植剂,用紫外分光光度法测药物残留量,计算单位长度埋植剂平均每日药物释放量。放射免疫法测定左炔诺孕酮(LNG)血药浓度。结果CaproF埋植剂在60、120、180、360、720d药物平均释放速率分别为(11.0±3.0)、(11.7±3.7)、(8.0±1.2)、(7.3±0.4)、(9.3±0.9)μg/(d·cm),并可维持基本恒定的血药浓度。结论左炔诺孕酮CaproF埋植剂植入体内后,平均药物释放速率达到7.6μg/(d·cm),并可维持2年的基本稳定释放。Objective To evaluate the release pharmacokinetics of levonorgestrel （LNG） from degradable long acting contraceptive implant drug CaproF in vivo. Methods Each Wister rat was subcutaneous implanted with a piece of CaproF. Then,the implanted CaproF pieces were removed at different time interval,and the residual LNG in CaproF was measured by ultraviolet spectrophotometry to calculate the drug release rate. Serum LNG levels were also measured by radioimmune assay （RIA）. Results Drug release studies revealed that after administrations of 60 days, 120 days, 180 days, 360 days and 720 days ,the mean release rate of CaproF implant drug were （11.0 ± 3.0）, （11.7 ± 3.7）, （8.0 ± 1.2）, （7.3 ± 0.4）, （9.3 ± 0.9） μg/ （d·cm） respectively. A relative constant serum LNG level was maintained. Conclusion It is demonstrated that the in vivo release rate of 7 μg/（d·cm） implant CaproF capsule was established. It is hypothesized that the implantation of 2 pieces of 3 cm long CaproF capsule would provide effective contraceptive effect for 2 years in women.

关 键 词：埋植剂 左炔诺孕酮 药物释放 

分 类 号：R96[医药卫生—药理学]