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目的：建立左旋多巴血药浓度的测定方法并对左旋多巴控释片进行人体药代动力学研究。方法：高效液相色谱法，色谱柱：Ｌｉｃｈｒｏｓｐｈｅｒ １００Ｃ１８柱（５ｕｍ，２５０ｍｍ×４ｍｍ）；流动相：水（含ＥＤＴＡ０．０８ｍｍｏl／L，ＫＨ２ＰＯ４７０ｍｍ７０ｍｍｏｌ／Ｌ，庚烷磺酸钠２．０８ｍｍｏｌ／Ｌ）：甲醇（９０：１０）；流速：１.０ｍｌ／ｍｉｎ；荧光检测：激发波长为２７８ｎｍ，发射波长为３２５ｎｍ；血浆样品用高氯酸沉淀蛋白后直接进样。结果：方法回收率为９５．５０％～１０２．５５％，最低检测限为０．２５ｎｇ，日内ＲＳＤ＜４．２９％（ｎ＝４），日间ＲＳＤ＜６．７３％（ｎ＝４），线性范围为０．１２５～４．０ｕｇ／ｍｌ。８名健康受试者单次口服左旋多巴控释片２５０ｍｇ后，药－时曲线符合二室模型，ＡＵＣ为（２９７．３６±５２.1８）ｕｇ／（ｍｌ·ｍｉｎ），Ｃｍａｘ为（１．０４±０．４２）ｕｇ／ｍｌ，Ｔｍａｘ为（１５２．６５±４６．７１）ｍｉｎ，Ｔ１／２ａ为（１２４．７６±４３．８７）ｍｉｎ，Ｔ１／２β为（１５７．８３±３０．８２）ｍｉｎ．与左旋多巴相比，Ｔｍａｘ和Ｔ１／２ａ具有显著性差异，相对生物利用度为（７０．１７±７．４１）％。
OBJECTIVE: To establish a method for the determination of levodopa in human plasma and study the pharmacokinetics of levodopa controlled release tablets in human. METHODS: High performance liquid chromatography (HPLC) was performed on a Lichrospher 100C18 column (5um, 250mm × 4mm). The mobile phase consisted of water (EDTA 0.08mmol / L, KH 2 PO 4 70mm 70mmol / L and sodium heptane sulfonate 2.08mmol / L) Methanol (90:10); flow rate: 1.0 ml / min; fluorescence detection: excitation wavelength of 278nm, emission wavelength of 325nm; plasma samples were precipitated with perchloric acid directly into the sample. Results: The recoveries were 95.50% -102.55%, the lowest detection limit was 0.25ng, the intraday RSD was 4.29% (n = 4), and the interday RSD was 6.73% (n = 4) , Linear range of 0.125 ~ 4.0ug / ml. After a single oral administration of levodopa 250 mg in 8 healthy volunteers, the drug-time curve conformed to the two-compartment model with AUC of (297.36 ± 52.18) ug / (ml · min) and Cmax of (1 Tmax was (152.65 ± 46.71) min, T1 / 2a was (124.76 ± 43.87) min, T1 / 2β was (157.83 ± 30) 82) min. Compared with levodopa, Tmax and T1 / 2a had significant difference, the relative bioavailability was (70.17 ± 7.41)%.