發(fā)布時(shí)間：2018-06-04 22:10

  本文選題：阿霉素 + 甘草次酸��； 參考：《沈陽藥科大學(xué)學(xué)報(bào)》2015年08期

【摘要】：目的制備甘草次酸(glycyrrhetinic acid,GA)介導(dǎo)的pH敏感主動靶向長循環(huán)阿霉素(doxorubicin,DOX)脂質(zhì)體(liposomes,LP)(GA-PEG2000-N=CH-DOXLP)并測定其在大鼠體內(nèi)藥物動力學(xué)參數(shù)。方法采用薄膜分散法制備甘草次酸介導(dǎo)pH敏感主動靶向長循環(huán)阿霉素脂質(zhì);采用陽離子交換樹脂-微柱離心法測定脂質(zhì)體的包封率和載藥量;動態(tài)激光散射法測定脂質(zhì)體的粒徑、粒徑分布和Zeta電位;透射電鏡觀察脂質(zhì)體形態(tài);透析法測定脂質(zhì)體在不同pH條件下的體外釋放;熒光分光光度法測定阿霉素血漿藥物濃度,得到藥-時(shí)曲線并計(jì)算藥物動力學(xué)參數(shù)。結(jié)果甘草次酸介導(dǎo)的脂質(zhì)體(GA-PEG2000-N=CH-DOXLP)和普通脂質(zhì)體(DOXLP)的粒徑分別為(135.5±2.6)nm和(105.6±4.0)nm;包封率分別為(53.8±5.8)%和(52.9±3.5)%,載藥量質(zhì)量分?jǐn)?shù)分別為(2.35±0.16)%和(2.39±0.26)%;Zeta電位分別為-(5.19±0.73)mV和-(1.53±0.57)mV;GAPEG2000-N=CH-DOXLP的AUC(0-72)分別是DOXLP的2.33倍和DOX溶液的5.62倍。結(jié)論所制備的甘草次酸修飾的pH敏感主動靶向長循環(huán)脂質(zhì)體制劑學(xué)性質(zhì)穩(wěn)定并能顯著延長其在大鼠體內(nèi)的循環(huán)時(shí)間。
[Abstract]:Objective to prepare liposome of glycyrrhetinic acid (GAA) -mediated active targeting of long-circulating doxorubicindox (doxorubicindox) liposome (GA-PEG2000-NCH-DOXLP) and determine its pharmacokinetic parameters in rats. Methods Glycyrrhetinic acid-mediated active targeting of long-circulation adriamycin lipids was prepared by thin-film dispersion method, and the entrapment efficiency and drug loading of liposomes were determined by cationic exchange resin-microcolumn centrifugation. The particle size, particle size distribution and Zeta potential of liposomes were measured by dynamic laser scattering method, the morphology of liposomes was observed by transmission electron microscope, the release of liposomes in vitro at different pH conditions was determined by dialysis, and the concentration of adriamycin in plasma was determined by fluorescence spectrophotometry. The drug-time curve was obtained and the pharmacokinetic parameters were calculated. 緇撴灉鐢樿崏嬈￠吀浠嬪鐨勮剛璐ㄤ綋(GA-PEG2000-N=CH-DOXLP)鍜屾櫘閫氳剛璐ㄤ綋(DOXLP)鐨勭矑寰勫垎鍒負(fù)(135.5鹵2.6)nm鍜，

本文編號：1979015