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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。
The pharmaceutical industry has always been concerned about the research and discovery of new drugs from plants. In most cases, the total composition of plants is more powerful and comprehensive than the efficacy of single ingredients. Therefore, we need a comprehensive understanding of the in vivo process of this total composition. For the metabolic process of this multi-component drug, few people have systematically studied it in the past. We take CBN injection, a new type of cerebrovascular drug, as an example to study its in vivo kinetics. The purpose is to elucidate and discover the pharmacokinetic characteristics of CBN, and also to explore the research methods of pharmacokinetics of botanicals. We examined the kinetics of CBN from two representative components of puerarin and ginsenoside Rg1. The results showed that after intravenous injection of CBN, the metabolism of puerarin was rapid, the average retention time (MRT) was 26 min, and the MRT of ginsenoside Rg1 was 3.3. h. There was a significant difference between the two (P<0.05). We have realized that the key to the pharmacokinetics study of the total composition of botanical drugs is the selection of test indicators. The active ingredient with the highest content is preferred. It is best to choose 2-3. Second, the total composition should be determined as much as possible. For unknown components that appear in the test process, as long as they change, they should fit the peak area-time variation law, which is the so-called pharmacokinetic fingerprint (finger-printinkinetic). This is conducive to a more comprehensive elucidation of the pharmacokinetics of the subjects studied.