脑血管药CBN注射剂药代动力学研究——对植物药药代动力学研究方法学的探讨

Study on Pharmacokinetics of CBN Injection--- Study on Methodology of Pharmacokeinetics of Plant Medicinces

药学界一直普遍关注从植物中研究和发现新的药物,多数情况下,植物中的总成分较单一成分药效表现得更强更全面。因此,我们需要对于这种总成分的体内过程有一个全面的了解。对于这种多成分组成的药物的代谢过程,以往较少有人去系统地研究。我们以脑血管二类新药CBN注射剂为例,对其在体内的动力学过程进行了研究。目的是阐明和发现CBN的药代动力学特点,同时也为植物药药代动力学的研究方法进行探索。我们从葛根素和人参皂苷Rg1两个代表成分对CBN的动力学进行考察,结果表明静脉注射CBN后,葛根素代谢较快,平均注留时间(MRT)为26min,人参皂苷Rg1的MRT为3.3h。两者相比有显著差异(P<0.05)。我们体会到,植物药总成分的药代动力学研究的关键在于测试指标的选择,首选含量高的活性成分,最好选做2-3个。其次应尽可能做总成分测定。对于在测试过程中出现的未知成分,只要有消长变化的,也应就其峰面积-时间变化规律进行拟合,即所谓药代动力学指纹图(finger-printinkinetic)。这样有利于较全面地阐明所研究对象的药代规律。

In the medical circle of China people always show much solicitude for the discovery of new drugs from plants in recent years.It should be noticed that in most cases the total constituents of plants have more effectiveness than the single ones and therefore it is necessary to make an overall undersranding of the process in vivo of the said total constituents.By now quite few studies on the metabolic process of such medicines as made up of multi-constituents have been carried out systematically.The authors have studied the kinetic process in vivo of CBN(a complex injection form the active parts of herbal medicines,which are effective for stroke)in order to know and expound the characteristics of pharmacokinetics of herbal medicines and also to explore the methodology of the study on their pharmacokinetics.They have made a test of the pharmacokinetics of puerarin and ginsenoside Rg1in CBN,which showes that after the injection of CBN into the vein(100mg /kg)puerarin quickly metabolizes in26minutes of mean retention time (MRT),while the MRT of ginsenoside Rg1takes about 3.3hours,here assuming their great difference(P<0.05).Therefore,it should be indicated that the key to the study on the pharmacokinedtics of the total constituents of herbal medicines lies in the selection of the index of test,in which it would be best to select two or three active ones with high content for test first and then everything possible should be done to test their total components.For the unknown parameters which appear in the test and the changeable laws of their changing peak and time should be fitted,i.e.,fingerprint in kine,tics.By this way it is helpful to clarify the pharmacokinetic laws of studied objects overally.