摘要
制备聚酸酐-吡柔比星长效缓释植入剂,用于治疗膀胱癌及预防膀胱癌术后复发。将吡柔比星(THP)与聚酸酐,按一定比例于玛瑙研钵内充分混合并溶于二氯甲烷中,浇注于膜具中置干燥器内4℃下成膜。每片植入剂含THP 5.0 mg。将聚酸酐-吡柔比星缓释植入剂植入大耳白兔膀胱黏膜内,分别于术后不同时间取血和尿,用高效液相色谱法测定尿与血液内THP药物质量浓度。尿液内THP质量浓度明显高于血药浓度,在术后250 d时尿液中药物浓度达(92.5±7.4)μg/L。聚酸酐-吡柔比星长效缓释植入剂具有一级释放动力学,可在体内长期维持稳定的药物释放量,本实验经膀胱黏膜缓释给药,为膀胱癌治疗及预防术后复发进行了有益的探索。
This paper aims to prepare polyanhydride-Pirarubicin dose long-acting sustained-release implants for the treatment of bladder cancer and for the prevention of postoperative recurrence of bladder cancer.Pirarubicin hydrochloride（THP） and polyanhydride,in accordance with a certain proportion,were fully mixed in the agate morta and dissolved in dichloromethane,and then were cast into a film within a mold put in the dryer set at 4℃.Each tablet implanted contained 5.0 mg of THP.Polyanhydride-pirarubicin sustained-release was implanted into the bladder mucosa of the rabbits,and blood and urine samples were taken at different times after the operation.The THP drug concentrations in urine and blood were determined with high-performance liquid chromatography.The THP concentration in urine was significantly higher than the THP concentration in plasma. The drug concentration in urine reached（92.5±7.4） μg/L at 250 d time after the operation.Polyanhydride-pirarubicin implants possess long-acting sustained-release level dynamics in the body.It can maintain a stable long-term drug release and can be expected to last a year and can effectively prevent recurrence of bladder cancer.The present experiments proved that the implants with sustained-release drug treatment are expected to be useful in the clinical application in prevention of bladder cancer recurrence.
出处
《生物医学工程学杂志》
EI
CAS
CSCD
北大核心
2011年第2期322-325,共4页
Journal of Biomedical Engineering
关键词
膀胱癌治疗
聚酸酐
吡柔比星缓释植入剂
生物降解
Bladder cancer treatment
Polyanhydride
Pirarubicin implanted sustained-release agent
Biodegradable
