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对本室设计制备的左炔诺孕酮(Levonorgestrel,LNG)阴道避孕环(以20μg/d速度恒速释药)的体内血药浓度和消除动力学进行测定。5名健康妇女于放入此环8d中及环取出后72h内的不同时间取血,用放射免疫法测定血药浓度。结果发现放环后药物的吸收和消除特性与国外报道的相似,体内血药浓度变化与其体外释药规律相符。环放入阴道后,药物吸收1h内即达稳态,8h左右出现一个血药浓度峰,以后血药浓度趋于平稳。环取出后的药物消除分二相。取环后24h内,半衰期为14.3h;24～72h内,平均半衰期为61.9h。
The in vivo plasma concentration and elimination kinetics of the vaginal contraceptive ring of levonorgestrel (LNG) designed and prepared in our laboratory (constant-rate delivery at 20 μg / d) were determined. Five healthy women received blood at different times within 8 days and within 72 hours after removing the ring, and the blood concentration was measured by radioimmunoassay. The results showed that the drug absorption and elimination characteristics after releasing the ring were similar to those reported in foreign countries. The change of the plasma concentration in vivo was consistent with the in vitro release pattern. Ring into the vagina, the drug absorption within 1h that is steady state, a plasma concentration peak around 8h, after the plasma concentration tends to be stable. Remove the drug after the ring was divided into two phases. Within 24 h, the half-life was 14.3 h; within 24-72 h, the average half-life was 61.9 h.