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 designatiou, in vitro or in vivo t...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 designatiou, 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 17.0-19.1μg/d, the safe dosage was 70.2mg/kg, C1hr. was 2.91 ± 1.25 ng/ml, Tmax was 8.86± 4.32 h, C 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 ahnost 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 tong effective contraceptive and may be promising.展开更多
目的:研制复方孕二烯酮阴道环,并考察其体外释放度。方法:首先将2种药物分别制备成以PVPK30为载体的固体分散体,然后以硅橡胶为载体,采用热压硫化法,以两段结合式制备阴道环药芯,并包覆一定厚度的无活性硅橡胶膜,制得复方孕二烯酮阴道...目的:研制复方孕二烯酮阴道环,并考察其体外释放度。方法:首先将2种药物分别制备成以PVPK30为载体的固体分散体,然后以硅橡胶为载体,采用热压硫化法,以两段结合式制备阴道环药芯,并包覆一定厚度的无活性硅橡胶膜,制得复方孕二烯酮阴道环。采用单因素考察方法对阴道环制备工艺及处方进行优化。以200 ml pH4.0磷酸盐缓冲液为释放介质,采用高效液相色谱法考察阴道环的体外释放度,并对其进行释放拟合。结果:通过优化确定最佳复方孕二烯酮阴道环制备工艺及处方,阴道环中药物可以维持21 d缓慢释放,释药速率符合Higuchi方程。结论:复方孕二烯酮阴道环具有良好的释药特性,制备工艺稳定;采用高效液相色谱法考察阴道环的体外释放度方便、快速和准确。展开更多
文摘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 designatiou, 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 17.0-19.1μg/d, the safe dosage was 70.2mg/kg, C1hr. was 2.91 ± 1.25 ng/ml, Tmax was 8.86± 4.32 h, C 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 ahnost 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 tong effective contraceptive and may be promising.
文摘目的:研制复方孕二烯酮阴道环,并考察其体外释放度。方法:首先将2种药物分别制备成以PVPK30为载体的固体分散体,然后以硅橡胶为载体,采用热压硫化法,以两段结合式制备阴道环药芯,并包覆一定厚度的无活性硅橡胶膜,制得复方孕二烯酮阴道环。采用单因素考察方法对阴道环制备工艺及处方进行优化。以200 ml pH4.0磷酸盐缓冲液为释放介质,采用高效液相色谱法考察阴道环的体外释放度,并对其进行释放拟合。结果:通过优化确定最佳复方孕二烯酮阴道环制备工艺及处方,阴道环中药物可以维持21 d缓慢释放,释药速率符合Higuchi方程。结论:复方孕二烯酮阴道环具有良好的释药特性,制备工艺稳定;采用高效液相色谱法考察阴道环的体外释放度方便、快速和准确。
