本文選題：對(duì)乙酰氨基酚　切入點(diǎn)：重氮化反應(yīng)　出處：《藥學(xué)學(xué)報(bào)》2015年05期

【摘要】：建立血清對(duì)乙酰氨基酚濃度的測(cè)定方法,用于評(píng)價(jià)胃排空功能。對(duì)乙酰氨基酚水解后與亞硝酸發(fā)生重氮化反應(yīng),所得產(chǎn)物在312 nm處具有特征吸收峰,繪制標(biāo)準(zhǔn)曲線,計(jì)算血清對(duì)乙酰氨基酚濃度和回收率。ICR小鼠灌胃對(duì)乙酰氨基酚(500 mg·kg-1),動(dòng)態(tài)測(cè)定其血藥濃度;用該方法評(píng)價(jià)小鼠皮下注射長(zhǎng)效GLP-1類似物GW002對(duì)胃排空的影響。對(duì)乙酰氨基酚在0~160μg·m L-1內(nèi)發(fā)生重氮化反應(yīng)的線性關(guān)系良好(R2=0.999 7);以該方法測(cè)定血清對(duì)乙酰氨基酚濃度的線性也較好(R2=0.998 2),回收率為97.4%~116.7%。對(duì)乙酰氨基酚灌胃后血藥濃度于0.5 h達(dá)峰。GW002能夠明顯降低小鼠血清對(duì)乙酰氨基酚濃度,使藥時(shí)曲線下面積(AUC)降低28.4%。本研究建立了一種測(cè)定血清對(duì)乙酰氨基酚濃度的方法,準(zhǔn)確性高,可用于評(píng)價(jià)小鼠的胃排空功能。
[Abstract]:A method for the determination of serum paracetamol was established to evaluate gastric emptying function.After hydrolysis of paracetamol and diazotization of nitrite, the obtained product has a characteristic absorption peak at 312 nm, and draws the standard curve.The concentration and recovery of paracetamol in serum. ICR mice were gavaged with paracetamol 500 mg kg ~ (-1), and their blood concentration was determined dynamically, and the effect of subcutaneous injection of long-acting GLP-1 analogue GW002 on gastric emptying in mice was evaluated by this method.The linear relationship between paracetamol and paracetamol in the concentration of paracetamol in the concentration of paracetamol in the serum was good. The linear relationship between paracetamol and paracetamol was good in the range of 160 渭 g mL ~ (-1) for diazotization. The linearity of the method for the determination of paracetamol in serum was also good, and the recovery was 97.4% (116.7%).After oral administration of paracetamol, the concentration of paracetamol at the peak of 0.5 h, GW002 significantly decreased the concentration of paracetamol in serum of mice, and the area under the curve decreased by 28.4%.A method for the determination of paracetamol in serum was established. The method is accurate and can be used to evaluate gastric emptying function in mice.
【作者單位】： 中國(guó)醫(yī)學(xué)科學(xué)院北京協(xié)和醫(yī)學(xué)院藥物研究所天然藥物活性物質(zhì)與功能國(guó)家重點(diǎn)實(shí)驗(yàn)室;
【基金】：重大新藥創(chuàng)制資助項(xiàng)目(2012ZX09301002-004)
【分類號(hào)】：R96

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