Wu Hui-Fei, Wang Xiang-Yu, Deng Ji-Feng, Quan Shi-Jian, Wang Qi, Li Wei-Rong
Institute of Clinical Pharmacology, Guangzhou University of Chinese Medicine, No. 12 Jichang Road, Guangzhou, 510405, Guangdong, China.
School of Chinese Meteria Medica, Guangzhou University of Chinese Medicine, Guangzhou, 510405, China.
Eur J Drug Metab Pharmacokinet. 2018 Dec;43(6):645-653. doi: 10.1007/s13318-018-0476-8.
Danggui-Shaoyao-San (DSS), a famous Chinese formula, has been widely used to treat gynecological disorders since ancient times and has recently showed efficacy in treating Alzheimer's disease. Butylidenephthalide (BDPH) and alisol B (ALI) are recognized as the primary active ingredients of DSS. The objectives of the present study were to evaluate the pharmacokinetic comparative study of BDPH and ALI in herbal extracts and their purified forms.
A sensitive and specific high-performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS) methodology was developed to determine the concentration level of BDPH and ALI in rat plasma. This approach enables a real-time pharmacokinetics profiling of BDPH and ALI in DSS extracts as well as their purified forms in rats after oral administration.
The validated method showed an evident linearity over a wide range of dosages (r > 0.99) with sensitivity down to 1.0 ng/mL for each analyte. The extraction recovery of the analyte ranged from 80.8 to 99.1%. The pharmacokinetic parameters were significantly different in herbal extracts and their purified forms. The results showed that the absorption of both BDPH and ALI from DSS extracts was significantly greater compared with their purified forms.
A highly specific, sensitive and rapid HPLC-MS/MS method was developed and applied for the determination of BDPH and ALI in rat plasma. It was found that BDPH and ALI had higher bioavailability in the DSS extract compared with their purified forms.
当归芍药散（DSS）是一种著名的中药方剂，自古以来就被广泛用于治疗妇科疾病，最近还显示出对阿尔茨海默病的治疗效果。丁烯基苯酞（BDPH）和泽泻醇B（ALI）被认为是DSS的主要活性成分。本研究的目的是评估BDPH和ALI在草药提取物及其纯化形式中的药代动力学比较研究。
建立了一种灵敏且特异的高效液相色谱串联质谱（HPLC-MS/MS）方法，用于测定大鼠血浆中BDPH和ALI的浓度水平。该方法能够对口服给药后大鼠体内DSS提取物及其纯化形式中的BDPH和ALI进行实时药代动力学分析。
验证后的方法在很宽的剂量范围内显示出明显的线性关系（r＞0.99），每种分析物的灵敏度低至1.0 ng/mL。分析物的提取回收率在80.8%至99.1%之间。草药提取物及其纯化形式的药代动力学参数有显著差异。结果表明，与纯化形式相比，DSS提取物中BDPH和ALI的吸收均显著更高。
建立了一种高特异性、灵敏且快速的HPLC-MS/MS方法并应用于大鼠血浆中BDPH和ALI的测定。发现与纯化形式相比，BDPH和ALI在DSS提取物中的生物利用度更高。
