摘要
用放射免疫法测定18-甲基炔诺酮和雌二醇的血药浓度,比较不同粒度的复方18-甲基炔诺酮注射剂的生物利用度。制剂Ⅱ微晶平均粒度小于5μm,给药初期药物释放快,d3达峰值。制剂Ⅰ微晶平均粒度为15μm,药物释放较制剂Ⅱ慢而平稳,最初数天血药浓度较制剂Ⅱ为低。而给药中、后期的血药浓度高于制剂Ⅱ.两制剂曲线下总面积无显著差异。雌二醇的血药浓度、达峰时间及血药浓度下降速度相似。
The serum concentrations of levonorgestrel (LNG) and estradiol(E_2) following im injection in rabbits of composite injection of norgestrel withdifferent particle size were measured using RIA. Injections I and II containedmicrocrystals of LNG and E_2 with a mean particle size of 15μm, and 5 μm,respectively. Peak plasma LNG concentration with II (16. 10 ng/ml) was reachedat d3 and then decreased rapidly. High concentration of LNG (7.95 ng/ml) withI was observed at d1; the mean concentrations at d3 and d5 were 7.51 and7.98 ng/ml, respectively; then declined slowly.There was no significant differencein the area under curves between I and II. The serum levels of E_2 seemed tobe similar after administration of I or II.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
1989年第11期501-503,共3页
Chinese Journal of Pharmaceuticals
关键词
18-甲炔诺酮
注射液
生物利用度
composite injection of norgestrel, radioimmunoassay,bioavailability,particle size of microcrystals
