论文部分内容阅读
目的:研究丹参主要活性成分丹酚酸B(lithospermate B,mlB)在冠心病血瘀证患者体内的药代特征,为临床合理用药提供依据;通过与健康人药代数据的比较,揭示中医证型对药物动态的影响。方法:采用高效液相-电化学方法检测静脉滴注200mg丹参多酚酸盐注射液后,不同时间点血浆中mlB的血药浓度。采用Winnolin软件计算药代参数。SPSS软件比较冠心病血瘀证患者和健康受试者体内的药代参数。结果:所建立的分析方法具有特异性,准确度、精密度以及回收率都满足临床药代试验要求。冠心病血瘀证患者的曲线下面积(AUC(0-t))、平均滞留时间(MRT(0-t))、末端消除半衰期(t1/2z)、清除率(CLz)和分布容积(Vz)分别为10.7±5.58 mg/h.L、22.14±8.78 h、1.71±0.78 h、0.31±0.12 L/kg.h和0.78±0.51 L/kg,与健康人相比,冠心病血瘀证人的t1/2z显著减小,Vz虽然下降较大,但是由于较大的标准差,没有达到统计学上的显著性差别。其他药代参数在两组间没有差别。结论:mlB在血瘀证患者中的药代特征与健康受试者明显不同,血液循环功能的下降可能是造成药物分布减少,进而使半衰期缩短的病理机制。对于冠心病血瘀证患者可适当提高剂量、延长滴注时间或增加给药次数。
Objective: To study the pharmacokinetics of lithospermate B (mlB), a major active ingredient of Danshen, in patients with coronary heart disease and blood stasis syndrome, and to provide a basis for clinical rational drug use. By comparing with the data of healthy people, Type of drug on the dynamic impact. Methods: The plasma concentration of mlB in different time points was determined by HPLC - electrochemical method after intravenous infusion of 200mg salvianolate injection. Pharmacokinetic parameters were calculated using Winnolin software. SPSS software was used to compare the pharmacokinetic parameters in patients with coronary heart disease and blood stasis syndrome and healthy subjects. Results: The established analytical method has the specificity, accuracy, precision and recovery rate to meet the requirements of clinical trials. (AUC (0-t)), mean retention time (MRT (0-t)), terminal elimination half-life (t1 / 2z), clearance (CLz) and volume of distribution ) Were 10.7 ± 5.58 mg / hL, 22.14 ± 8.78 h, 1.71 ± 0.78 h, 0.31 ± 0.12 L / kg.h and 0.78 ± 0.51 L / kg, respectively. Compared with healthy subjects, 2z significantly decreased, although Vz decreased significantly, but due to the larger standard deviation, did not reach a statistically significant difference. Other pharmacokinetic parameters did not differ between the two groups. Conclusion: The pharmacokinetic characteristics of mlB in patients with blood stasis syndrome are obviously different from those in healthy subjects. The decrease of blood circulation function may be the pathological mechanism of reducing the drug distribution and shortening the half-life. For patients with coronary heart disease with blood stasis may be appropriate to increase the dose to extend the infusion time or increase the number of dosing.