Alpinetin, a bioactive flavonoid, has attracted great attention due to its diverse therapeutic effects, namely anti-oxidant, anti-tumor and anti-inflammatory effects with low systemic toxicity. Various determination methods have been developed in quality control and plant chemistry areas. However, quantification and pharmacokinetics of alpinetin in biological matrix have not been studied. In the present research, a sensitive, efficient and reliable ultrahigh performance liquid chromatography-tandem mass spectrometry (UHPLC–MS/MS) method for the determination of alpinetin in rat plasma was developed and validated. Plasma samples were processed with protein precipitation (PP) followed by a 5-fold acetonitrile/water (50:50, v/v) dilution to significantly decrease matrix effect which exited in one step PP method. Determination of alpinetin was conducted using positive electrospray ionization tandem mass spectrometry in multiple reaction monitoring mode. Results demonstrated that the method was precise (3.3%–12.3%), accurate (−5.8% to 10.8%) and linear in the range of 1–1000 ng/mL. The new developed method was subsequently applied to a pharmacokinetic research of alpinetin following oral and intravenous dosing to healthy Sprague-Dawley rats. Alpinetin was demonstrated rapid absorption after oral administration with an absolute bioavailability of ∼15.1% and extensive distribution after dosing.

具有生物活性的类黄酮高山素由于具有多种治疗作用，即具有低全身毒性的抗氧化剂，抗肿瘤和抗炎作用而备受关注。在质量控制和植物化学领域已经开发出各种测定方法。但是，尚未研究高山生物素在生物基质中的定量和药代动力学。在本研究中，开发并验证了一种灵敏，高效且可靠的超高效液相色谱-串联质谱法（UHPLC–MS / MS）测定大鼠血浆中的阿尔卑斯碱。用蛋白质沉淀（PP）处理血浆样品，然后用5倍乙腈/水（50:50，v / v）稀释液处理，以显着降低基质效应，这是一步法进行的。使用正电喷雾电离串联质谱法在多个反应监测模式下进行高山素的测定。结果表明，该方法准确度（3.3％–12.3％），准确度（−5.8％至10.8％）且线性范围为1–1000 ng / mL。新开发的方法随后应用于对健康Sprague-Dawley大鼠进行口服和静脉内给药后，alpinetin的药代动力学研究。口服后，Alpinetin被证明吸收迅速，绝对生物利用度约为15.1％，给药后分布广泛。新开发的方法随后应用于对健康Sprague-Dawley大鼠进行口服和静脉内给药后，alpinetin的药代动力学研究。口服后，Alpinetin被证明吸收迅速，绝对生物利用度约为15.1％，给药后分布广泛。新开发的方法随后应用于对健康Sprague-Dawley大鼠进行口服和静脉内给药后，alpinetin的药代动力学研究。口服后，Alpinetin被证明吸收迅速，绝对生物利用度约为15.1％，给药后分布广泛。