Research on the New One Rod Contraceptive Implant Containing Gestodene

摘要

Objective To develop a new contraceptive implant containing gestodene featuring with only one rod for 5 years long effectiveness and safety. Methods Gestodene synthesis, polymer tube designation, in vitro or in vivo test, the pilot test was used for the establishing of minimum clinic dosage. Results It had a burst effect at beginning and become constantly releasing since 12th day. It had zero-order releasing, in vitro, the average releasing rate was 17.0-19.1 μg/d, the safe dosage was 70.2mg/kg, C1hr was 2.91 ± 1.25 ng/ml, Tmax was 8.86 ± 4.32 h, Cmax was 7.31 ± 1.09 ng/ml, Tss was 14 d,Css was 4.16 ± 0.48 ng/ml. Twenty-four hours later after removal of the implant, gestodene was almost cleaned out in the blood circulation and only trace amount of drug was detected after the removal. Conclusion One rod gestodene implant is a new long effective contraceptive and may be promising.