Faculty of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin, China.
Planta Med. 2011 Sep;77(14):1600-4. doi: 10.1055/s-0030-1270998. Epub 2011 Apr 11.
Both borneol and menthol are bioactive substances derived from Chinese herbal medicines. In order to understand the pharmacokinetics of borneol and menthol in Qingyan drop pills, a rapid, sensitive, and simple gas chromatographic (GC) method with flame ionization detection (FID) was developed for the simultaneous determination of borneol and menthol in rat plasma. Sample preparations were carried out by liquid-liquid extraction (LLE) with an internal standard solution of naphthalene. The analytes and internal standard (IS, naphthalene) were separated well on an HP-1 capillary column. The pharmacokinetic parameters were estimated by a compartmental method using the Phoenix WinNonlin software program (Version 6.0). The standard curves were linear over a wide concentration range of 2.5-50.0 ng/µL ( R = 0.9963), 8.7-62.2 ng/µL ( R = 0.9994) for both borneol and menthol in plasma, respectively. The limits of quantification (LOQ) of borneol and menthol in plasma were 2.4 ng/µL and 5.0 ng/µL, respectively. The intra-day precisions for borneol and menthol were < or = 10.0 % R. S. D. at the LOQ and < or = 6.0 % at higher concentrations. The average value of CMAX was 18.97 ± 2.71 ng/µL with a TMAX at 20.00 ± 0.00 min for borneol after oral administration of the drop pills; for menthol, the average value of CMAX was 79.02 ± 11.40 ng/µL with a TMAX at 25.00 ± 4.40 min. This validated assay method was successfully applied to a pharmacokinetic study of borneol and menthol after oral administration of Qingyan drop pills in rat. The results showed that the kinetics of borneol and menthol can be described by an open one-compartment model. The pharmacokinetic parameters provide some information for clinical administration of Qingyan drop pills.
龙脑和薄荷醇均为来源于中草药的生物活性物质。为了了解清咽滴丸中龙脑和薄荷醇的药代动力学，我们建立了一种快速、灵敏、简单的气相色谱（GC）-火焰离子化检测（FID）法，用于同时测定大鼠血浆中的龙脑和薄荷醇。样品制备采用内标萘的液-液萃取（LLE）法。分析物和内标（萘）在 HP-1 毛细管柱上得到很好的分离。采用 Phoenix WinNonlin 软件程序（版本 6.0）的房室模型法估算药代动力学参数。龙脑和薄荷醇在血浆中的标准曲线在较宽的浓度范围内均呈线性，范围分别为 2.5-50.0 ng/μL（R=0.9963）和 8.7-62.2 ng/μL（R=0.9994）。龙脑和薄荷醇在血浆中的定量下限（LOQ）分别为 2.4 ng/μL 和 5.0 ng/μL。龙脑和薄荷醇在 LOQ 时的日内精密度<10.0%R.S.D.，在较高浓度时<6.0%。口服清咽滴丸后，龙脑的 CMAX 平均值为 18.97±2.71 ng/μL，TMAX 为 20.00±0.00 min；薄荷醇的 CMAX 平均值为 79.02±11.40 ng/μL，TMAX 为 25.00±4.40 min。该验证后的分析方法成功应用于大鼠口服清咽滴丸后龙脑和薄荷醇的药代动力学研究。结果表明，龙脑和薄荷醇的动力学可采用开放一室模型描述。药代动力学参数为清咽滴丸的临床给药提供了一些信息。
