国产长效皮下埋植剂和Norplant的药物体外释放比较

Comparison of Drug Release Rate between Chinese Subcutaneous Implants and Norplant in Vitro

本文研究了国产18-甲基炔诺酮硅橡胶长效皮下埋植剂的药物体外释放,并与进口Norplant进行了比较。释放试验采用水平振荡法,实验条件符合“漏槽”状态的要求。用紫外分光光度法在240 nm波长处测定18-甲基炔诺酮每天的体外释放量。二年多体外释放试验的实验结果表明:国产埋植剂的药物体外释放无爆破效应,释药速度稳定,为零级速度。平均每天释放量为85μg。体外释放的重现性好。进口Norplant则有明显的爆破效应,经10天释放,才趋于稳定,平均每天释药量为68μg。

Drug release from Chinese subcutaneous implants containing levonorgestrel was studied. It was compared with that of Norplant. A horizontal vibration method was applied in our experiment, all the conditions being in keeping with the requirements of 'sink condition'. The daily release of levonorgestrel in vitro was assayed by measuring the UV absorption of the solution at 240 nm, The results from two year's release experiments in vitro showed that the release rate of levonorgestrel of Chinese implant was constant with good reproducibility, and no bursting effect could be seen. The Chinese implants release levonorgestrel with zero order, The average daily release of levonorgestrel was 85 μg. Norplant has 10 day's bursting effect, before the release rate became constant' the daily release of levonorgestrel being 68μg.