摘要
对10例埋植国产去除爆破效应(本文简称除爆)的CLa皮下埋植剂(左旋18-甲基炔诺酮,本文简称皮埋剂)的妇女进行5年血药水平、释药速率及药物清除等药代动力学观察,结果显示:埋植除爆CLa皮埋剂后,24h血药水平是稳态水平的4.5倍左右,5年时平均血药水平为0.96±0.41nmol/L,释药速率36.21μg/d,足以达到避孕有效浓度,埋植除爆CLa皮埋剂后,各个时期平均血药水平基本恒定,用药5年时平均血药水平比用药早期略低,释药速率与血药浓度变化趋势相似。1～5年平均释药速率为43.96μg/d。经过5年埋植,埋植剂内剩余LNG为总含量的52.13％。取出埋植剂后,消除半衰期为44.55h,廓清率为334.00L/d。
The pharmacokinetics of Sino - CLa implants which were removed' burst release' were studied in the Chinese voluntary women for five years. The plasma level of levonorgestral (LNG) in each implant user has been measured by RIA. The result indicated that a steady - state LNG plasma level has been maintained throughout the course of 5 years application. The peak concentration of LNG was reached after 24 hours of the insertion of Sino - CLa implant which was fourflod higher than that of the 5th years. The plasma level of LNG was 0.96 ± 0.41nmol/L (mean ± se) at the end of 5th and this concentration has been proven highly effective for contraception. The result of the drug release rate in vivo was unified with the plasma concene-tration fluctuation the amount of LNG released from implant was 43. 96μg/d during 1 -5 years. Longterm implant through five years. The LNG of remaining in implants are 52.13% of total imply weigh.The elimination T1/2 was 44.55hr and the plasma clearance was 334.0L/d after implants removed.
出处
《中国计划生育学杂志》
1998年第4期151-153,共3页
Chinese Journal of Family Planning
