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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。
Preparation of polyanhydride - pirarubicin sustained-release sustained-release implants for the treatment of bladder cancer and prevention of postoperative recurrence of bladder cancer. The pirarubicin (THP) and polyanhydride, according to a certain proportion of agate mortar thoroughly mixed and dissolved in methylene chloride, cast in a film with a dryer at 4 ℃ membrane. Each tablet contains THP 5.0 mg. The polyanhydride-pirarubicin sustained-release implants were implanted into the bladder mucosa of rabbits. Blood and urine were collected at different time points after surgery. The concentrations of THP in urine and blood were determined by HPLC. The concentration of THP in urine was significantly higher than that in plasma, and the drug concentration in urine was (92.5 ± 7.4) μg / L at 250 days after operation. Polyanhydride - pirarubicin sustained release sustained-release implants have a release kinetics, long-term in the body to maintain a stable drug release, the experiment by the bladder mucosa sustained release drug delivery for the treatment of bladder cancer and prevention of postoperative Recurrence of a useful exploration.