CAJ | 학술논문

以丙烯酸酯压敏胶为黏合基质,采用透皮控释技术制备周效依托孕烯和炔雌醇的复方避孕贴剂.采用LC-MS/MS法测定家兔血浆中炔雌醇和依托孕烯的浓度,并考察其对家兔抗排卵的效果.结果表明,复方依托孕烯贴剂贴于家兔腹部透皮给药7d,能维持较恒定的血药浓度,移除贴剂后,血药浓度迅速降低.家兔抗排卵试验结果显示,给药1 d后,复方依托孕烯贴剂对家兔交配诱发排卵有明显的抑制作用,平均排卵点为0.60±1.3,与空白对照组平均排卵点6.0±1.9相比,其排卵抑制率为90.0%;给药7 d后,对家兔交配诱发排卵也有明显的抑制作用,平均排卵点为1.25±1.5,与相应的空白对照组平均排卵点4.5±1.0相比,排卵抑制率为72.2%.表明复方依托孕烯贴剂具有显著的抗排卵作用.
이병희산지압민효위점합기질,채용투피공석기술제비주효의탁잉희화결자순적복방피잉첩제.채용LC-MS/MS법측정가토혈장중결자순화의탁잉희적농도,병고찰기대가토항배란적효과.결과표명,복방의탁잉희첩제첩우가토복부투피급약7d,능유지교항정적혈약농도,이제첩제후,혈약농도신속강저.가토항배란시험결과현시,급약1 d후,복방의탁잉희첩제대가토교배유발배란유명현적억제작용,평균배란점위0.60±1.3,여공백대조조평균배란점6.0±1.9상비,기배란억제솔위90.0%;급약7 d후,대가토교배유발배란야유명현적억제작용,평균배란점위1.25±1.5,여상응적공백대조조평균배란점4.5±1.0상비,배란억제솔위72.2%.표명복방의탁잉희첩제구유현저적항배란작용.
The once-weekly compound etonogestrel (ET) and ethinly estradiol (EE) transdermal contraceptive patch was prepared with acrylic adhesive. The plasma concentration of EE and ET were determined by LC-MS/MS and the effects of ovulation inhibition of the patch in rabbits were evaluated. The steady plasma concentration in rabbits maintained for 7 days, but decreased rapidly after the patch was removed. The results of ovulation inhibition tests showed that the ovulation could be restrained after one day's deliverey of the patch, and the ovulation inhibition rate was 90.0% compared with the control group. And after seven days' delivery, the ovulation inhibition rate was 72.2%. The results showed that the compound enotogestrel and ethinly estradiol transdermal system could maintain the drug release through rabbit skin for at least 7days and achieve the intention of once-weekly contraception.