中国药物应用与监测
中國藥物應用與鑑測
중국약물응용여감측
CHINESE JOURNAL OF DRUG APPLICATION AND MONITORING
2015年
4期
205-208
,共4页
王梅%常占瑛%侯艳霞%高晓黎
王梅%常佔瑛%侯豔霞%高曉黎
왕매%상점영%후염하%고효려
黄体酮%凝胶剂%制备%药效
黃體酮%凝膠劑%製備%藥效
황체동%응효제%제비%약효
Progesterone%Gel%Preparation%Pharmacodynamics
目的:制备黄体酮凝胶剂,并初步考察黄体酮凝胶剂的药效.方法:进行黄体酮凝胶剂的处方优化,选用卡波姆-940为凝胶剂的基质,通过正交试验,以黏度、屈服值和触变性为指标,筛选天然黄体酮凝胶剂的最佳处方.在此基础上,采用兔子宫内膜转化实验考察兔子宫分级指数、子宫增重指数和子宫腺体数,以考察黄体酮凝胶剂的药效.结果:通过处方优化制备的黄体酮凝胶剂外观乳白色,粒径分布均匀,黏度适中.药效学结果表明,经过23 d给药,空白基质组,低、中、高剂量组兔体质量均有明显增加,子宫指数逐渐升高,子宫分级结果空白基质组,阳性对照组,低、中、高剂量组分别为(0.30±0.46)、(3.20±0.27)、(1.00±0.61)、(1.80±0.50)、(2.30±0.50),低、中、高剂量组较空白基质组子宫腺体数目增加,但增加不及阳性对照组显著.结论:黄体酮凝胶剂的制备方法可行,给药后黄体酮凝胶剂具有一定的孕激素活性,能促进兔子宫内膜发育,表明该剂型具有一定的可行性.
目的:製備黃體酮凝膠劑,併初步攷察黃體酮凝膠劑的藥效.方法:進行黃體酮凝膠劑的處方優化,選用卡波姆-940為凝膠劑的基質,通過正交試驗,以黏度、屈服值和觸變性為指標,篩選天然黃體酮凝膠劑的最佳處方.在此基礎上,採用兔子宮內膜轉化實驗攷察兔子宮分級指數、子宮增重指數和子宮腺體數,以攷察黃體酮凝膠劑的藥效.結果:通過處方優化製備的黃體酮凝膠劑外觀乳白色,粒徑分佈均勻,黏度適中.藥效學結果錶明,經過23 d給藥,空白基質組,低、中、高劑量組兔體質量均有明顯增加,子宮指數逐漸升高,子宮分級結果空白基質組,暘性對照組,低、中、高劑量組分彆為(0.30±0.46)、(3.20±0.27)、(1.00±0.61)、(1.80±0.50)、(2.30±0.50),低、中、高劑量組較空白基質組子宮腺體數目增加,但增加不及暘性對照組顯著.結論:黃體酮凝膠劑的製備方法可行,給藥後黃體酮凝膠劑具有一定的孕激素活性,能促進兔子宮內膜髮育,錶明該劑型具有一定的可行性.
목적:제비황체동응효제,병초보고찰황체동응효제적약효.방법:진행황체동응효제적처방우화,선용잡파모-940위응효제적기질,통과정교시험,이점도、굴복치화촉변성위지표,사선천연황체동응효제적최가처방.재차기출상,채용토자궁내막전화실험고찰토자궁분급지수、자궁증중지수화자궁선체수,이고찰황체동응효제적약효.결과:통과처방우화제비적황체동응효제외관유백색,립경분포균균,점도괄중.약효학결과표명,경과23 d급약,공백기질조,저、중、고제량조토체질량균유명현증가,자궁지수축점승고,자궁분급결과공백기질조,양성대조조,저、중、고제량조분별위(0.30±0.46)、(3.20±0.27)、(1.00±0.61)、(1.80±0.50)、(2.30±0.50),저、중、고제량조교공백기질조자궁선체수목증가,단증가불급양성대조조현저.결론:황체동응효제적제비방법가행,급약후황체동응효제구유일정적잉격소활성,능촉진토자궁내막발육,표명해제형구유일정적가행성.
Objective: To prepare progesterone gel and study its pharmacodynamics.Methods: Carbomer-940 was chosen as gel matrix, and the best preparation method was optimized through single factor and orthogonal test with viscosity, yield value and thixotropy as indicators. And the initial pharmacodynamics of progesterone gel was studied. The uterus grading number, uterus weight index and gland amounts were all measured by endometrial transformation experiment in rabbits.Results: The best preparation method of progesterone gel was decided, and a good progesterone gel with milky appearance, uniform particle size distribution, and moderate viscosity was made. In the initial pharmacodynamical study, the weight of the rabbits in control matrix group, low, middle and high dose group increased, the uterus grading number in control matrix group, positive control group, low, middle and high dose group was (0.30 ± 0.46), (3.20 ± 0.27), (1.00 ± 0.61), (1.80 ± 0.50), (2.30 ± 0.50) respectively. The uterus index and grading number improved. The uterine gland amounts in low, middle and high dose group were more than that in control matrix group, but the increase was not signiifcant compared with positive control group.Conclusion: The preparation method about progesterone gel is feasible with well product quality and high effect on uterus of rabbits, which indicates progesterone can be made into gel through our method.