Yu Meili, Du Zhi, Xue Junchen, Wang Keming
Tianjin Third Central Hospital, Tianjin Key Laboratory of Artificial Cells, Tianjin 300170, China.
Sheng Wu Yi Xue Gong Cheng Xue Za Zhi. 2011 Apr;28(2):322-5.
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 degrees C. 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) microg/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.
本文旨在制备聚酸酐-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。将盐酸吡柔比星(THP)与聚酸酐按一定比例在玛瑙研钵中充分混合,溶于二氯甲烷,然后倒入置于4℃干燥箱内的模具中制成薄膜。每片植入剂含5.0mg THP。将聚酸酐-吡柔比星缓释剂植入兔膀胱黏膜,术后不同时间采集血样和尿样。采用高效液相色谱法测定尿和血中THP药物浓度。尿中THP浓度显著高于血浆中THP浓度。术后250d时尿中药物浓度达到(92.5±7.4)μg/L。聚酸酐-吡柔比星植入剂在体内具有长效缓释水平动力学。它能维持稳定的长期药物释放,预计可持续一年,并能有效预防膀胱癌复发。本实验证明,药物缓释植入剂有望在预防膀胱癌复发的临床应用中发挥作用。