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目的：建立血浆中瑞巴匹特浓度的高效液相色谱分析方法，并用此方法研究瑞巴匹特在人体内的药代动力学。方法：血样经酸化，用乙酸乙酯单步萃取后，以甲醇ｐＨ３的磷酸盐缓冲液（５２∶４８）为流动相，在紫外２３０ｎｍ处检测。所得数据用３ｐ８７药代动力学程序处理，求出相应的参数。结果：瑞巴匹特血浓度在２０～１２００μｇ·Ｌ－１范围内与色谱峰高呈良好线性关系，血浆中药物最低检测浓度为１０μｇ·Ｌ－１，日内及日间ＲＳＤ（ｎ＝５）分别在１．１１％～３．７２％和３．８７％～７．６０％，方法回收率为９９．８４％～１００．２０％。药代动力学研究表明，口服国产和进口瑞巴匹特片剂的血药浓度时间曲线均符合一级吸收一级消除的一房室模型，体内药物达峰时间分别为（１．９５±０．７３）ｈ和（１．５７±０．５５）ｈ；ｃｍａｘ分别为（５１０．８±１５２．０）μｇ·Ｌ－１和（５６４．８±１８７．７）μｇ·Ｌ－１；ｔ１／２分别为（１．７５±０．６３）ｈ和（１．６６±０．３）ｈ；国产瑞巴匹特片的相对生物利用度为（９９．３６±７．８７）％。结论：此方法简便、可靠，测定灵敏度高，能较好地满足瑞巴匹特临床血药浓度监测及人体内药代动力学的研究。
OBJECTIVE: To establish a HPLC method for the determination of rebamipide in plasma and to study the pharmacokinetics of rebamipide in human by this method. Methods: The blood samples were acidified and extracted with ethyl acetate. The mobile phase consisted of methanol-phosphate buffer (52:48) and detected at 230 nm. The data obtained were processed using the 3p87 pharmacokinetic program to find the corresponding parameters. Results: The blood concentration of rebamipide in the range of 20 ~ 1200μg · L-1 showed a good linear relationship with the chromatographic peak height. The lowest concentration of the drug in plasma was 10μg · L-1, intra-day and inter-day RSD (n = 5) Respectively, 1.11% ~ 3.72% and 3.87% ~ 7.60%, the recovery rate was 99.84% ~ 100.20%. Pharmacokinetic studies have shown that the plasma concentration-time curves of oral and imported rebamipide tablets are in line with a one-compartment model of first-order absorption elimination, the peak drug in vivo were (1.95 ± 0.73) h and (1.57 ± 0.55) h, respectively. The values of cmax were (510.8 ± 152.0) μg · L-1 and (564.8 ± 187.7) μg · L- t1 / 2 were (1.75 ± 0.63) h and (1.66 ± 0.3) h, respectively. The relative bioavailability of domestic rebamipide tablets was (99.36 ± 7.87)%. Conclusion: This method is simple, reliable and sensitive to determination. It can better meet the requirements of the clinical monitoring of rebamipide and the pharmacokinetics in human body.