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目的建立血清中硝苯地平浓度的ＨＰＬＣ测定法，研究其在自发性高血压大鼠（ＳＨＲ）体内的药动学。方法ＳＨＲ灌胃给与硝苯地平１０ｍｇ／ｋｇ，用ＨＰＬＣ法测定硝苯地平血清浓度。用乙酸乙酯提取出血清中的硝苯地平，在５０℃水浴中用氮气吹干，残渣用流动相溶解后进样。选用ｓｈｉｍＰａｃｋＣＬＣ－ＯＤＳ柱，甲醇－水（６∶４）作流动相，检测波长２３５ｎｍ。结果：硝苯地平最低检出浓度为０．０２μｇ／ｍｌ，标准曲线线性范围为０．０２～５．０μｇ／ｍｌ（ｒ＝０．９９９７），血样平均回收率为９８．０９％。硝苯地平在大鼠体内的药动学符合一定开放模型，其参数为Ｔ１／２ｋａ＝０．８２８±０．５５ｈ，Ｔ１／２ｋｅ＝３．１７±２．３２ｈ，Ｔｍａｘ＝２．１２±１．４７ｈ，Ｃｍａｘ＝２．７８±１．５０μｇ／ｍｌ和ＡＵＣ＝２４．５±２９．２ｈ·μｇ／ｍｌ。结论本法能满足血清中硝苯地平浓度测定及药动学研究的需要。
OBJECTIVE: To establish an HPLC method for the determination of nifedipine in serum and to study its pharmacokinetics in spontaneously hypertensive rats (SHR). Methods SHR was administered to nifedipine 10 mg / kg and the nifedipine serum concentration was determined by HPLC. The nifedipine in serum was extracted with ethyl acetate and dried in a water bath at 50 ° C with nitrogen. The residue was injected into the mobile phase and dissolved. Use shimPackCLC-ODS column, methanol - water (6: 4) as the mobile phase, detection wavelength 235nm. Results: The minimum detectable concentration of nifedipine was 0.02μg / ml. The linear range of standard curve was 0.02-5.0μg / ml (r = 0.9997). The average recovery rate of nifedipine was 98.09%. The pharmacokinetics of nifedipine in rats was in accordance with a certain open model with parameters T1 / 2ka = 0.828 ± 0.55h, T1 / 2ke = 3.17 ± 2.32h and Tmax = 2.12 ± 1 .47 h, Cmax = 2.78 ± 1.50 μg / ml and AUC = 24.5 ± 29.2 h · μg / ml. Conclusion This method can meet the needs of determination of nifedipine in serum and pharmacokinetics.