發(fā)布時(shí)間：2018-05-15 17:20

  本文選題：維特克拉 + 溶出曲線��； 參考：《中國(guó)藥學(xué)雜志》2017年17期

【摘要】：目的考察維特克拉(venetoclax)制劑的體外釋藥行為和在比格犬體內(nèi)的藥動(dòng)學(xué)過(guò)程,進(jìn)行體內(nèi)體外相關(guān)性(IVIVC)的研究。方法研究測(cè)定了維特克拉制劑在不同溶出介質(zhì)中的溶出曲線;建立維特克拉在比格犬血漿樣品中的HPLC測(cè)定方法,并對(duì)市售的維特克拉片進(jìn)行飽腹和空腹下比格犬體內(nèi)的藥動(dòng)學(xué)研究;將藥物在體外累積溶出度數(shù)據(jù)與在體內(nèi)的累積吸收百分?jǐn)?shù)數(shù)據(jù)進(jìn)行線性回歸,進(jìn)行IVIVC研究。結(jié)果維特克拉制劑在4種不同溶出介質(zhì)中體外的釋藥行為存在明顯差異;建立了維特克拉比格犬血樣測(cè)定方法,該方法簡(jiǎn)單、準(zhǔn)確;維特克拉制劑飽腹和空腹的AUC_(0→∞)分別為(32.38±5.87)和(27.70±6.32)mg·h·L~(-1),達(dá)峰濃度分別為(4.04±0.78)和(3.72±0.69)μg·m L~(-1),達(dá)峰時(shí)間分別(6.01±1.04)和(4.27±0.92)h,其中AUC_(0→∞)和達(dá)峰時(shí)間的差異具有顯著性(P0.05);體內(nèi)吸收百分?jǐn)?shù)與在0.2%SDS pH 6.8介質(zhì)中的體外溶出度有良好的IVIVC。結(jié)論食物可提高維特克拉制劑的生物利用度;本實(shí)驗(yàn)篩選出的0.2%SDS pH 6.8介質(zhì)(槳法,75r·min~(-1))可以作為與該制劑體內(nèi)釋藥相關(guān)的體外溶出條件。
[Abstract]:Objective to investigate the in vitro drug release behavior and pharmacokinetic process in Beagle dogs, and to investigate the in vivo and in vitro correlation of Vitamin B venetoclax (IVIVC). Methods the dissolution curve of Vitela preparation in different dissolution media was determined, and the HPLC method was established for the determination of Vitela in Beagle's plasma samples. The pharmacokinetics of Viterka tablets on the market was studied in full and empty stomach, and the cumulative dissolution data in vitro and the cumulative absorption percentage data in vivo were linear regressed, and the IVIVC study was carried out. Results there were significant differences in drug release behavior in vitro among the four different dissolution mediums, and a simple and accurate method was established for the determination of blood samples in Vitro Clapiga canines. The AUC_(0 鈭，

本文編號(hào)：1893224