摘要
将抗滴虫药物甲硝唑进行疏水性修饰，制成甲硝唑月桂酸酯，将此前体药物载于脂质体中，包封率提高近１０倍。体外抗滴虫试验采用微量量热技术，测定用药后滴虫代谢产生热量改变，确定药物的抗滴虫作用。结果显示脂质体中前体药物最低于游离药物量１／６０，抗滴虫作用却强于后者，证实了前体药物脂质体的优越性，并说明微量量热法在药效学研究中有广泛应用前景。
etronidazole. an anti-trichomonas vaginalis
drug( MNA)carried in liposomes appeared rather low encapsulation
percentage (EP%)and poor stability because of small molecule and
water soluble。 In this paper MNA was modified by means of
esterification. Its lauric ester(L-MNA)was synthesi- zed and the
L-MNA lioposomes were prepared.The EP%of L-MNA in ilposomes was near
ten times ,as high as that of MNA in liposomes.The thermograms of
trichomonas vaginalis were used for bidogical activities comparision
beween the L-MNA liposomes and MNA-Iiposomes by technology of
microcalorimetry.The results were shown that the anti-trichomonas
activities of L-MNA liposomes was better than that of MNA-liposomes
in which drug concentration was 60 times as high as that of L- MNA
liposomes.The advantages of pre-drug liposomes were full
demonstrated.
出处
《北京医科大学学报》
CSCD
1994年第6期481-483,共3页
Journal of Peking University(Health Sciences)
基金
国家自然科学基金
