【摘要】 目的 評(píng)價(jià)麻敏維C緩釋膠囊(每粒含鹽酸偽麻黃堿90 mg和馬來(lái)酸氯苯那敏4 mg)在人體的生物等效性?!》椒ā∮?006年6月采用隨機(jī)交叉自身前后對(duì)照試驗(yàn)設(shè)計(jì),26例受試者分別單次和多次空腹口服麻敏維C緩釋膠囊(試驗(yàn)制劑)和復(fù)方鹽酸偽麻黃堿緩釋膠囊(參比制劑),與不同時(shí)間點(diǎn)取血樣,采用液-質(zhì)聯(lián)用(HPLC/MS)法測(cè)定人血漿中鹽酸偽麻黃堿和馬來(lái)酸氯苯那敏的濃度,以DAS軟件計(jì)算藥物代謝動(dòng)力學(xué)參數(shù),并進(jìn)行生物等效性評(píng)價(jià)?!〗Y(jié)果 單次給藥后,兩組分的主要藥物代謝動(dòng)力學(xué)參數(shù)無(wú)統(tǒng)計(jì)學(xué)意義(Pgt;0.05)。試驗(yàn)制劑中馬來(lái)酸氯苯那敏和鹽酸偽麻黃堿生物利用度分別為104.31%和109.19%。多次給藥后,兩組分的主要藥物代謝動(dòng)力學(xué)參數(shù)無(wú)統(tǒng)計(jì)學(xué)意義(Pgt;0.05)。試驗(yàn)制劑的馬來(lái)酸氯苯那敏和鹽酸偽麻黃堿的生物利用度分別為103.58%和99.37%?!〗Y(jié)論 麻敏維C緩釋膠囊和復(fù)方鹽酸偽麻黃堿緩釋膠囊具有生物等效性。【Abstract】 Objective To investigate the bioequivalence of delayed-release capsule of ephedrine-chlorphenamine-vitamin C. Methods In June 2006, 26 healthy volunteers were administrated with delayed-release capsule of ephedrine-chlorphenamine-vitamin C or delayed-release capsule of ephedrine-chlorphenamine in a randomized and two-way crossover design with single or multiple dosage. The plasma concentrations were determined by HPLC/MS method. The pharmacokinetic parameters and bioequivalence were calculated by DAS software. Results After single dose administration, no significant differences were found in tmax, Cmax, t1/2, and AUC0-t between the two preparations. The relative bioavailability of the test preparation was 104.31% in chlorphenamine and 109.19% in ephedrine, respectively. After multiple dose administration, no significant differences were found in tmax, Cmax, t1/2, and AUC0-t between the two preparations. The relative bioavailability of the test preparation was 103.58% in chlorphenamine and 99.37% in ephedrine, respectively. Conclusion Delayed-release capsule of ephedrine-chlophenamine-vitamin C is equivalent to the reference preparation.
目的 采用高效液相色譜法測(cè)定受試者口服埃索美拉唑腸溶膠囊與埃索美拉唑鎂腸溶片后血藥濃度,評(píng)價(jià)埃索美拉唑腸溶膠囊的生物等效性。 方法 2009年9月-10月,36例健康男性受試者單次交叉口服埃索美拉唑腸溶膠囊(試驗(yàn)制劑)和埃索美拉唑鎂腸溶片(參比制劑),測(cè)定給藥后不同時(shí)間點(diǎn)血漿中埃索美拉唑經(jīng)時(shí)血藥濃度,采用DAS 2.0軟件進(jìn)行藥物代謝動(dòng)力學(xué)參數(shù)計(jì)算和生物等效性評(píng)價(jià)。 結(jié)果 受試者單次口服試驗(yàn)制劑與參比制劑后,達(dá)峰時(shí)間分別為(2.19 ± 0.96)、(2.43 ± 0.92) h,峰濃度分別為(1 748.86 ± 615.81)、(1 442.92 ± 476.41) μg/L,藥時(shí)曲線下面積(AUC)0-t分別為(3 927.14 ± 1 839.10)、(3 878.79 ± 1 734.84) μg/L·h,AUC0-∞分別為(3 998.36 ± 1 866.22)、(3 918.31 ± 1 773.44) μg/L·h。試驗(yàn)制劑與參比制劑的生物等效性為94.0%,其90%CI為(82.3%,107.2%)。 結(jié)論 埃索美拉唑腸溶膠囊與埃索美拉唑鎂腸溶片生物等效。