阿奇霉素在中国健康人体血浆中的药动学研究

目的:研究阿奇霉素在健康中国人体中的血浆药动学,为临床用药提供参考。方法:10名健康志愿者单剂量口服阿奇霉素500 mg后,HPLC法测定血浆药物浓度。采用F检验结合AIC法判别房室模型,DAS药动学程序计算药动学参数。结果:最佳房室模型为二室模型(W_i=1/C~2,AIC=-7.48),主要的药动学参数:α为(0.29±0.13)h~(-1),B为(0.02±0.003)h~(-1),Ka为(0.72±0.22)h~(-1),t_(1/2β)为(38.93±7.74)h,t_(max)为(2.60±0.49)h,C_(max)为(434.74±47.65)μg·L~(-1),AUC_(0-144)和AUC_(0-∞)分别为(12179.42±3001.11)μg·h·L~(-1)和(13338.35±3062.56)μg·h·L~(-1)。结论:阿奇霉素片在中国健康人体中的血浆药动学参数与国内外文献报道基本一致。     

Simultaneous determination of five anthraquinones in medicinal plants and pharmaceutical preparations by HPLC with fluorescence detection

A reversed-phase high-performance liquid chromatography (RP-HPLC) method with fluorescence detection for simultaneous determination of five anthraquinones in Rhubarb collected from nine different locations in China, Polygonum cuspidatum, Polygoni multiflori and three pharmaceutical preparations is proposed and validated. Chromatography was carried out at 25 °C on a Hypersil C18 column with the isocratic mobile phase of methanol–0.1% aqueous formic acid (85:15, v/v) at a flow rate of 1.0 ml/min. The excitation and emission wavelengths were set at 440 and 540 nm, respectively. A comprehensive validation of the method included tests of sensitivity, linearity, precision and accuracy. The linear regressions were acquired with r > 0.999. Satisfactory intra- and inter-day precisions were achieved with R.S.D.s less than 3.95% and the average recovery factors obtained were in the range of 93.2–103.8%.     

Quantitative and qualitative control of cytotoxic preparations by HPLC-UV in a centralized parenteral preparations unit

The constantly growing incidence of cancer and long-term treatment are leading to an increasing number of cytotoxic preparations in hospital pharmacies. Security and quality standards of cytotoxic preparations are essential to assure treatment efficiency and limit iatrogenic toxicity. In order to secure the process of cytotoxic preparations; we decided to install a quantitative and qualitative High Performance Liquid Chromatography (HPLC) control of cytotoxic preparations carried inside our pharmacotechnic unit. A 100 μl sample of each preparation was assayed by HPLC with ultraviolet/visible–diode array detection, which enabled the identification of all cytotoxic agents thanks to their characteristic UV spectra. We developed rapid and specific HPLC assays that determined qualitatively and quantitatively the presence of 21 different cytotoxic agents in less than 3.5 min. A fifteen per cent tolerance from the theoretical concentration was chosen in agreement with preparation and dosage bias, and a first period control of more than 4400 preparations revealed that around 7.7% preparations did not conform. The main objective of these controls was to avoid the administration of defective chemotherapies to patients and finally to use their results to identify error factors; as a result we will take corrective measures in order to reduce error frequency.     

三种西酞普兰制剂在中国健康男性体内的生物等效性

目的:研究西酞普兰在人体的药代动力学过程及其相对生物利用度。方法:西酞普兰血药浓度用HPLC-UV检测,色谱柱:Lichrospher ODS(5μm,250mm×4.6mm),流动相为乙腈:0.1mol/LKH2PO4:三乙胺(35:65:0.3,v/v/v),pH4.5,流速:1mL/min,检测波长:240nm,18名健康志愿者口服20mg西酞普兰制剂。结果:血浆标准曲线在2～128μg/L范围内线性良好(r=0.9992),血样最低定量限为1μg/L,平均绝对回收率为80%～88%,日内、日间变异系数(RSD)小于15%。三种西酞普兰制剂的主要药动学参数,达峰时间tmax:(4.6±1.0)、(4.4±1.4)、(4.0±1.4)h;峰浓度Cmax:(70±19)、(71±17)、(66±21)μg/L;消除半衰期t1/2:(37±9)、(37±6)、(36±6)h。试验制剂西酞普兰片和胶囊与喜普妙的相对生物利用度分别为100%±8%、99%±10%。结论:三种西酞普兰的主要药动学参数无明显差异,三种制剂生物等效。