Abstract
Blood stasis, that is, the decrease of blood flow velocity and the increase of blood viscosity indicates hemorheological abnormalities and pharmacokinetic difference of drugs. Therefore, it is very important to investigate the pharmacokinetics of drugs in patients with blood stasis syndrome, which may influence absorption, distribution, metabolism, and excretion of drugs in blood. The aim of this study was to compare the pharmacokinetics of 140 mg hydroxysafflor yellow A (HSYA) in healthy subjects and patients with blood stasis syndrome due to stable angina pectoris (SAP), and indentify the therapeutic regimen for patients and promote clinical rational drug use. This study was carried out in 12 healthy volunteers and 24 patients with blood-stasis syndrome due to SAP using a single-dose of HSYA (140 mg) under fasting conditions. Venous blood samples were drawn through indwelling cannula from each volunteer prior to drug administration and at 0.5, 1, 1.25, 1.5, 2.0, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, and 15 h after the drug administration. Plasma obtained after centrifuge was analyzed to determine HSYA by high-performance liquid chromatography (HPLC). HSYA pharmacokinetics have a significant difference between healthy subjects and patients with blood-stasis syndrome due to SAP: ratios of Cmax and AUC(0-∞) were 116.5% (105.0 to 134.2)and 132.2% (116.5 to 153.7), respectively; mean terminal half-life (t1/2) was 4.2 h as compared to 2.5 h in healthy subjects. The blood stasis syndrome has an impact on the pharmacokinetic parameters including Cmax, AUC0-∞, and t1/2, and dose adjustment should be required for patients with blood-stasis syndrome. Key words: Hydroxysafflower yellow A, safflower, pharmacokinetics differences, blood stasis.
Highlights
Safflower yellow injection is a new Chinese drug made of extraction from single herb, Flos Carthamus tinctorius and prepared by Shandong Lvye Natural Medicine Research and Development Center, China, having the effect of activating blood circulation and removing stasis
The Cmax and AUC(0-∞) values for hydroxysafflor yellow A (HSYA) were higher in patients with blood stasis syndrome due to stable angina pectoris (SAP) than in healthy subjects
It is suggested that blood stasis syndrome has statistically significant effect on the pharmacokinetic variables of HSYA in patients with blood stasis syndrome due to SAP
Summary
Safflower yellow injection is a new Chinese drug made of extraction from single herb, Flos Carthamus tinctorius and prepared by Shandong Lvye Natural Medicine Research and Development Center, China, having the effect of activating blood circulation and removing stasis. Pharmacokinetics is the study of what the body does to a drug and human’s physical state has a close relationship to drug transport in human body (Pfeifrs, 1999a). Diseases including hepatic impairment and kidney impairment have significant impact on the pharmacokinetic characteristic of drugs in human (Pfeifrs, 1999b, c). Our previous study indicated that the pharmacokinetic characteristic of HSYA has altered in rats with blood stasis syndrome, as compared to the healthy rats. There was no report about whether the blood stasis, this especial pathological condition has impact on the absorption, distribution, metabolism, and excretion of drugs in human body
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