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本文建立固相萃取结合柱前衍生化测定人血浆中的卡托普利浓度的RP-HPLC法,并利用该方法研究两种国产卡托普利片在健康受试者中的药物动力学与相对生物利用度。以对溴苯乙酰基溴 (p-BPB) 为衍生化试剂,衍生化产物经固相萃取后由VP-ODS 柱分离测定,流动相为乙腈-水-冰醋酸 (100:150:1.25) (v/v),紫外检测波长为257 nm,线性范围为 5~1000 ngmL-1,(r=0.9987),平均回收率为 98.652.04%,日内和日间 RSD 分别小于3.4% 和 8.4%。以自身对照随机交叉方式,单计量分别给予18名健康男性志愿者两种国产卡托普利片50 mg,卡托普利在人体内符合一室开放模型。两种卡托普利片的AUC0-T,Cmax 和 Tmax 分别为424.5125.7 mghL-1 和439.4113.3 mghL-1,505.9244.6 mgL-1和 504.8172.2 mgL-1,0.6620.181 h和0.5280.176 h。两种制剂间的各参数无明显差异,双单侧t检验结果表明二者为生物等效制剂,其相对生物利用度为96.114.6%。
In this paper, RP-HPLC method for the determination of the concentration of captopril in human plasma by solid phase extraction combined with pre-column derivatization was established. The pharmacokinetics and pharmacokinetics of two domestic captopril tablets in healthy subjects were compared with Relative bioavailability. The p-BPB was used as a derivatization reagent. The derivatized product was separated by VP-ODS column after solid phase extraction. The mobile phase consisted of acetonitrile-water-glacial acetic acid (100: 150: 1.25) The average UV detection wavelength was 257 nm with a linear range of 5 ~ 1000 ng mL-1 (r = 0.9987). The average recovery was 98.652.04%. The intra- and inter-day RSD were less than 3.4% and 8.4%, respectively. In a randomized crossover way with their own control, 18 healthy male volunteers were given two domestic captopril tablets 50 mg, respectively. Captopril conformed to the one-compartment open model in the human body. The AUC0-T, Cmax, and Tmax for the two captopril tablets were 424.5125.7 mghL-1 and 439.4113.3 mghL-1, 505.9244.6 mgL-1, and 504.8172.2 mgL-1, 0.66620.181 h, and 0.5280, respectively. 176 h. There was no significant difference in the parameters between the two preparations. The results of the two-sided t-test showed that the two preparations were bioequivalent and their relative bioavailability was 96.114.6%.