OBJECTIVE: To investigate the release of Hydroxycamptothecin (HCPT) sustained-release tablets in cerebral tissue of rats. METHODS: HCPT sustained-release tablets were implanted into cerebral tissue of 40 SD rats. Those rats were sacrificed on 1, 3, 7, 10, 13, 17, 21, 28 d. Residual medicine was obtained and HPLC was used to determine the amount of residual medicine and cumulative release rate was calculated. Concentrations of medicine in cerebral tissue and plasma were determined. RESULTS: The cumulative release rates of HCPT sustained-release tablets were (12.13 ± 7.58)% on the first day and(72.31 ± 15.17)% on 28th day. It indicated that drug release of HCPT sustained-release tablets lasted for more than 28 days. The concentrations of HCPT in cerebral tissue and plasma were (135.41 ±17.48) μg·mL-1 and (133.75 ± 10.81) ng·mL-1. The concentration of HCPT in cerebral tissue was higher than in plasma. CONCLUSION: HPCT sustained-release tablets can achieve ideal release effect and reduce general toxicity.%目的:考察羟基喜树碱(HCPT)缓释片植入大鼠脑内的释放情况.方法:将HCPT缓释片植入40只SD大鼠脑内,分别于第1、3、7、10、13、17、21、28天时处死大鼠,取出残留缓释片采用高效液相色谱法考察其未释放的药量并计算累积释放百分率；另取大鼠血浆和脑组织检测其中药物浓度.结果:HCPT缓释片在大鼠脑内第1、28天的累积释放百分率分别为(12.13±7.58)％、(72.31±15.17)％,表明其释放时间达28 d以上；其在大鼠脑组织和血浆中第28天的药物浓度分别为(135.41±17.48) μg·mL-1、(133.75±10.81) ng·mL-1,表明在脑组织中的药物浓度明显高于在血浆中的浓度.结论:自制的HCPT缓释片在大鼠脑内有较好的缓释效果,且可降低全身性毒副作用.
展开▼
