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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。
Ten patients with domestic CLa subcutaneous implants (L-18-norgestrel, referred to herein as skin burying agent), which were used to remove the blasting effect (referred to as de-blasting in this paper), were given 5-year blood levels, drug release rates and Drug clearance pharmacokinetics observed, the results showed that: Buried blasting CLa skin embedding agent, 24h blood drug levels are steady-state level of about 4.5 times, 5-year average blood level of 0.96 ± 0.41nmol / L, The drug release rate was 36.21μg / d, which was enough to reach the contraceptive effective concentration. The average plasma blood level was basically the same after implantation of CLa skin implants. The average blood drug level was slightly lower at 5 years than that at early drug release rate Similar to the changes of plasma concentration. The average release rate of 1 ~ 5 years was 43.96μg / d. After 5 years of planting, the remaining LNG in the implants was 52.13% of the total content. After removing the implants, elimination half-life of 44.55h, clearance rate of 334.00L / d.