本文選題：鹽酸格拉司瓊透皮貼劑 + beagle犬��； 參考：《中國(guó)比較醫(yī)學(xué)雜志》2017年02期

【摘要】：目的建立鹽酸格拉司瓊透皮貼劑在Beagle犬中的血藥濃度測(cè)定方法,通過(guò)Beagle犬多劑量給藥,揭示鹽酸格拉司瓊透皮貼劑在Beagle犬體內(nèi)的藥代動(dòng)力學(xué)變化規(guī)律,闡明其在Beagle犬體內(nèi)的藥代動(dòng)力學(xué)特征,提供重要的動(dòng)力學(xué)參數(shù)。方法 Beagle犬給予鹽酸格拉司瓊透皮貼劑6次,每次貼片持續(xù)72 h,每次撤藥和下次給藥間隔24 h。用建立的HPLC-MS/MS法測(cè)定血漿中的格拉司瓊的濃度,根據(jù)所得的血漿藥物濃度-時(shí)間曲線,計(jì)算藥動(dòng)學(xué)參數(shù)。結(jié)果第1次給藥和第6次給藥后的谷濃度Cmin分別0.0459 ng/m L和0.2593 ng/m L,峰濃度Cmax分別為0.4637 ng/m L和1.3428 ng/m L,AUC0~96分別為18.92 h·ng/m L和40.21 h·ng/m L,第1次給藥和第6次給藥后的Tmax分別為48.3 h和45.3 h,MRT0-96分別為48.9 h和45.84 h。結(jié)論多次給藥后格拉司瓊在體內(nèi)存在一定的蓄積效應(yīng),并在多次給藥后第16天到達(dá)穩(wěn)態(tài)。
[Abstract]:Objective to establish a method for the determination of blood concentration of granisetron hydrochloride transdermal patch in Beagle dogs, and to reveal the pharmacokinetic changes of granisetron hydrochloride transdermal patch in Beagle dogs. To elucidate the pharmacokinetic characteristics in Beagle dogs and provide important kinetic parameters. Methods Beagle dogs were treated with granisetron hydrochloride transdermal patch for 6 times for 72 hours each time and the interval between withdrawal and the next administration was 24 hours. The concentration of granisetron in plasma was determined by HPLC-MS / MS method. The pharmacokinetic parameters were calculated according to the plasma concentration-time curve. Results after the first and sixth administration, the valley concentration of Cmin was 0.0459 ng/m / L and 0.2593 ng/m / L, respectively. The peak concentration C _ (max) was 0.4637 ng/m / L and 1.3428 ng/m / L respectively, and the peak concentration C _ (max) was 18.92 h / ng/m / L and 40.21 h / ng/m / L, respectively. The Tmax of the first and sixth dose was 48.3 ng/m / L, respectively. H and 45.3 h MRT 0-96 were 48.9 h and 45.84 h, respectively. Conclusion granisetron has a certain accumulative effect in vivo after multiple administration and reaches steady state on the 16th day after repeated administration.
【作者單位】： 浙江省醫(yī)學(xué)科學(xué)院藥物研究所;
【基金】：浙江省科技廳培育創(chuàng)新載體項(xiàng)目(編號(hào):2015F10032) 浙江省中醫(yī)藥科學(xué)研究基金項(xiàng)目(編號(hào):2011ZA017)
【分類號(hào)】：R965

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本文編號(hào)：2079842