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1.
程雪龙 《黑龙江医药》2011,24(5):712-714
中药药代动力学对研究中药作用及现状、设计以及研发新药、剂型的改进有重要意义.本文对中药药代动力学的研究现状及问题分析做了综述.  相似文献   

2.
Xiang Z  Cai XJ  Zeng S 《药学学报》2012,47(5):558-564
药物研发模式的转变推动了药物评价技术体系的革新。中药药代动力学研究是中药现代化研究的重要组成部分,对于创新中药及现代中药复方研发具有重要意义。中药药代动力学理论近些年虽然取得了进步,但目前尚缺乏符合中药自身特征的药代动力学研究与评价技术体系。本文扼要介绍了中药药代动力学的研究现状、代谢组学及复杂网络理论,并在此基础上提出应用代谢组学和复杂网络方法来研究多组分药代动力学(网络药动学)的设想,以期揭示中药药效物质基础和作用机制。  相似文献   

3.
马昕 《北方药学》2011,8(11):18-19
从中药复方药代动力学的概念入手,对有效成分明确和不明确的中药及其复方制剂的研究方法及应用进行了论述和比较,指出了各种研究方法的特点;强调应进一步加强对中药复方药理学和药物动力学的研究,用科学的语言阐明中药复方的作用过程和机理;此举将对中医药实现现代化产生重要影响。  相似文献   

4.
目前中药药代动力学研究尚处于探索阶段,从上个世纪80年代起中药药动学有了很大的发展。本文综述了一些临床常用中药有效成分的药动学研究进展,从中药特点和研究现状入手,指出了各种研究方法存在的不足,强调应进一步加强对中药的药理学和药物动力学的研究。阐明中药的作用过程和机理,对中医药的现代化目标产生重要影响。关键词中药药代动力学中医药现代化,同时指出了今后中药药动学研究中应该解决的问题。  相似文献   

5.
中药药代动力学的研究方法   总被引:2,自引:0,他引:2  
李东  王敏  谢静  张雁  聂中越 《中国药业》2006,15(11):25-27
中药的作用特点是多成分、多途径、多环节、多靶点,研究中药药代动力学的关键是探索新的理论和方法.该文回顾了中药药代动力学的研究方法,并着重介绍了一些新理论和新方法.  相似文献   

6.
中药注射剂的安全性问题正受到越来越多的关注。药代动力学研究是揭示中药注射剂效应物质基础及其体内过程的重要途径,对于临床合理用药、提高中药注射液质量控制标准与临床用药的有效性、安全性具有十分重要的意义。本文简要分析了中药注射剂药物代谢动力学研究相关进展,指出对中药注射液药代动力学的重视程度尚有待提高。随着近年来中药药代动力学研究技术方法的进步,已逐步具备条件开展中药注射液的体内过程研究,中药注射液的质量控制、安全性评价、工艺优化以及临床合理用药研究等方面应充分利用和结合中药注射液体内过程的研究结果,以保障和提高中药注射液临床用药的有效性与安全性。  相似文献   

7.
代谢组学高通量、整体性的研究技术和研究思路,对中药中活性物质的分析方法及其代谢产物的药代动力学分析提供了新思路,有助于揭示中医证候的科学内涵和开展中药现代化研究。生命体.疾病.中药作用是一个动态的、紧密联系的整体过程,代谢组学则是连接的枢纽和中心,其全景式、整体互动性的特点与中医药的整体观念、证候的复杂体系及动态连贯性、中药作用的多靶点和突出整体效应不谋而合,是中医药现代化的最佳切入点。中药进入生命体后,起效的是中药中的原形成分或代谢产物,或与机体作用形成的新成分,三者构成体内中药成分的代谢物组。而中药代谢物组通过多靶点、多系统,协调干预人体内源性代谢物组来治疗疾病,所产生的一系列变化实质上仍然是代谢动力学变化,如能科学阐明原方成分与体内代谢成分的规律,自然能揭示中药成分的代谢规律,因此推动与基因组学——蛋白质组学相关联的代谢组学和成分组学的研究,从根本上解决中药的药动学问题。  相似文献   

8.
中药药代动力学研究的难点和热点   总被引:35,自引:3,他引:35  
刘昌孝 《药学学报》2005,40(5):395-401
中药的药物代谢动力学(简称中药药代动力学)是借助于动力学原理,研究中草药活性成分、组分、中药单方和复方体内吸收、分布、代谢和排泄(ADME)的动态变化规律及其体内时量.时效关系,并用数学函数加以定量描述的一门边缘学科。它是中药药理学与药物代谢动力学相互结合、相互渗透而形成的。它借助于药代动力学的基本理论和方法研究中草药,中草药药代动力学的研究也为药代动力学提出了新的课题。中药特别是中药方剂十分复杂,其药代动力学的研究较通常的化学药物的药代动力学更为困难,中药药代动力学必将大大促进药代动力学向更深层次的发展。  相似文献   

9.
滴眼剂的人眼部药代动力学研究对眼科药物的开发及评价具有重要意义。本文对滴眼剂的眼部药代动力学特征、眼部药代动力学研究的设计要点、泪液及房水中药代动力学研究的设计及实施方法进行探讨。  相似文献   

10.
王丽 《儿科药学杂志》2004,10(5):5-6,11
临床基础科研必须强调理论与实用性并重,国际合作与交流的选题和合作伙伴很重要。国际学术会议是最新信息交流的最好场所,短期交换是加速实质性合作的有力措施。当前形势下,建议基金委将抗癫痫中药现代化研究、群体药代动力学、药代动力学,药效动力学模式研究立项,定期组织小型专家座谈会及医学论坛,多多支持在华举办国际性或区域性专业会议。  相似文献   

11.
Natural medicines(NMs)are indispensable sources for the development of modern drugs.However,the targets for most natural compounds are unknown and the current pharmacokinetic evaluation systems developed for target-defined drugs may not be directly applicable to NM-based drug discovery,which is a major bottleneck in bringing natural compounds to the clinic.We propose the concept of "reverse pharmacokinetics" and discuss how a "reverse pharmacokinetics" perspective could help clarify key questions in modern drug discovery from NMs with validated clinical benefits,thereby strengthening the translational potential.Reverse pharmacokinetics can provide physiologically relevant clues to the target identification and mechanistic study of NMs,which may also innovate drug discovery for complex diseases.We anticipate that an evolving deep understanding of the novel mode of action of natural compounds with a reverse pharmacokinetic insight may improve discovery of both single ingredient and multiple-component modern drugs from NMs.  相似文献   

12.
The commercially available herbal products as the form of extract were usually mixtures containing various compounds. In spite of the purported efficacy in each active constituent, the coexisting constituents in the herbal extract might interfere with the efficacy and safety and affect the pharmacokinetic properties of active constituents. To compare for the pharmacokinetic properties of α-mangostin, a major bioactive compound, in mangosteen extract and pure α-mangostin, the pharmacokinetics as well as tissue distribution, in vitro metabolism, plasma protein binding and safety evaluation were conducted in mice because a mouse model is required a small amount of compounds and useful to develop disease models. The absorption of α-mangostin was increased and hepatic metabolism of α-mangostin was decreased in mice treated with mangosteen extract. However, the intestinal metabolism α-mangostin is comparable and still extensive in mice treated with α-mangostin and mangosteen extract. Intraperitorial LC50 of α-mangostin and mangosteen extract was 150 and 231 mg/kg, respectively. These findings may be valuable to explain the different pharmacokinetics and safety of α-mangostin and mangosteen extract. Furthermore, these findings are useful to design the efficacy and safety investigation of α-mangostin or mangosteen extract in mice with disease models or combination therapies to extrapolate into the clinical levels.  相似文献   

13.
Traditional Chinese medicines (TCMs) have a long history for safely treating human diseases. Unlike western medicine, TCMs usually contain multiple components synergistically and holistically acting on the diseases. It remains a big challenge to represent rationally the in vivo process of multiple components of TCMs for understanding the relationship between administration and therapeutic effects. For years, efforts were always made to face the challenge, and the achievements were obvious. Here, we give an comprehensive overview of the recent investigation progress (from 2015 to 2017, except the part of ‘integrated pharmacokinetics of TCMs’ from 2014 to 2017 and the part of ‘reverse pharmacokinetics in drug discovery from natural medicines’ in 2014) on pharmacokinetics of TCMs, mainly referring to the following six aspects: (1) classical pharmacokinetic studies on TCMs; (2) absorbed components and metabolites identification of TCMs; (3) pharmacokinetic herb–drug interactions and herb–herb interactions with TCMs; (4) integrated pharmacokinetics of TCMs; (5) pharmacokinetic and pharmacodynamic combination studies to dissect the action mechanisms of TCMs; and (6) reverse pharmacokinetics in drug discovery from natural medicines. Finally, based on the insights from the recent progress and our latest efforts, we propose new perspectives on the integrated pharmacokinetics of TCMs.  相似文献   

14.
Meldonium is a metabolic drug whose inclusion in the 2016 List of Prohibited Substances and Methods followed the analysis of data collected under the 2015 World Anti‐Doping Agency Monitoring Program. In the early months of 2016, anti‐doping laboratories reported an unusually high number of cases in which urine samples contained high concentrations of meldonium. Consequently, the meldonium excretion period in healthy athletes and the substance's long‐term urine and blood (plasma) pharmacokinetics became central questions for the anti‐doping community to address, to ensure appropriate assessment of the scientific and medical situation, and also fair treatment of athletes from a result management and legal standpoint. At the present time, data on meldonium pharmacokinetics is limited to a few studies, with no known data available on long‐term excretion of high oral doses. The primary objective of this open‐label study was to determine long‐term urine and plasma pharmacokinetic parameters of meldonium in healthy volunteers. Study design included single and repeated functional load testing and assessment of L‐carnitine administration on meldonium excretion and pharmacokinetics. Thirty‐two volunteers were equally divided into two groups receiving either 1.0 g or 2.0 g of oral meldonium daily for 3 weeks. The study found meldonium takes several days to attain a steady state in blood and displays an elimination period over several months after cessation of treatment. Moreover, findings demonstrate that the daily dose, periodicity and duration of treatment with meldonium are the most important factors to consider in calculating the substance's elimination and complete body clearance.  相似文献   

15.
中药复方药代动力学研究进展   总被引:6,自引:0,他引:6  
目的对中药复方的药动学研究进展进行综述.方法查阅10余年来有关中药复方药动学研究的国内外文献.结果中药复方的药代动力学研究方法主要有血药浓度测定法和生物效应法,中药复方的药动学研究有自己的特殊性,并仍存在不少问题.结论要加强中药复方药动学的方法学研究.  相似文献   

16.
Although dexibuprofen (S-ibuprofen) was marketed in Austria and Switzerland, the racemate at various formulations is still extensively used worldwide, and there are no indications that the racemate will be replaced by the single enantiomer. Thus, elucidation of the characteristics and involved mechanisms of the chiral pharmacokinetics of racemic ibuprofen is of special importance for the understanding of the pharmacological and toxicological consequences, and for prediction of the clinically potential drug interactions and influence of the pathological states. Stereoselective pharmacokinetics and metabolism are common features for chiral nonsteroidal antiinflammatory drugs (NSAIDs) and especially for 2-arylpropionic acid derivatives characterized with a chiral center adjacent to the carboxyl group. Although the enantioselective pharmacokinetic characteristics of different NSAIDs should be treated case by case, they share similar mechanisms underlying the protein binding, metabolism and chiral inversion. Ibuprofen was the most extensively researched drug in terms of chiral characteristics and mechanisms. Therefore, elucidation of the mechanisms derived from research on ibuprofen may provide better understanding and prediction of other chiral drugs. This article attempts to elucidate the chiral pharmacokinetics and involved mechanisms of ibuprofen in comparison with other NSAIDs based on recent developments. Topics on history of ibuprofen, enantioselective analysis method, absorption, protein binding, conventional metabolism, metabolic chiral inversion, gene polymorphism, and biochemical developments were included. It is worth mentioning that some underlying biochemical mechanisms, especially for the metabolic chiral inversion and ethnic differences still remain to be seen. Further research is required to develop human-resourced researching model and to provide more evidence concerning the site of inversion, species variation, CYP450 gene polymorphisms, and biochemical mechanisms.  相似文献   

17.
Introduction  Chronic kidney disease is a common, progressive illness that is becoming a global public health problem. In patients with kidney dysfunction, the renal excretion of parent drug and/or its metabolites will be impaired, leading to their excessive accumulation in the body. In addition, the plasma protein binding of drugs may be significantly reduced, which in turn could influence the pharmacokinetic processes of distribution and elimination. The activity of several drug-metabolizing enzymes and drug transporters has been shown to be impaired in chronic renal failure. In patients with end-stage renal disease, dialysis techniques such as hemodialysis and continuous ambulatory peritoneal dialysis may remove drugs from the body, necessitating dosage adjustment. Methods  Inappropriate dosing in patients with renal dysfunction can cause toxicity or ineffective therapy. Therefore, the normal dosage regimen of a drug may have to be adjusted in a patient with renal dysfunction. Dosage adjustment is based on the remaining kidney function, most often estimated on the basis of the patient's glomerular filtration rate (GFR) estimated by the Cockroft–Gault formula. Net renal excretion of drug is a combination of three processes: glomerular filtration, tubular secretion and tubular reabsorption. Therefore, dosage adjustment based on GFR may not always be appropriate and a re-evaluation of markers of renal function may be required. Discussion  According to EMEA and FDA guidelines, a pharmacokinetic study should be carried out during the development phase of a new drug that is likely to be used in patients with renal dysfunction and whose pharmacokinetics are likely to be significantly altered in these patients. This study should be carried out in carefully selected subjects with varying degrees of renal dysfunction. In addition to this two-stage pharmacokinetic approach, a population PK/PD study in patients participating in phase II/phase III clinical trials can also be used to assess the impact of renal dysfunction on the drug's pharmacokinetics and pharmacodynamics. Conclusion  In conclusion, renal dysfunction affects more that just the renal handling of drugs and/or active drug metabolites. Even when the dosage adjustment recommended for patients with renal dysfunction are carefully followed, adverse drug reactions remain common.  相似文献   

18.
Introduction: The elucidation of the toxicological mechanisms of herbal medicines is becoming more and more important with the increasing application of herbal medicines, for treatment of various diseases and the promotion of health. Furthermore, it is widely recognized that as herbal components undergo bioactivation, there is a critical need for a greater understanding of herbal toxicity induction. Areas covered: This article summarizes the current understanding of structural alerts present in herbal remedies as well as the herbs' and individuals' factors, complicating the interpretation of herbal toxicity via bioactivation. Medline (by means of PubMed up to July 2010) has been searched using proper relevant terms. The reader is provided with reported examples of herbal bioactivation based on toxicophores, which are summarized in an extended list. The article also discusses the factors which influence the herbal bioactivation study, including herbal complexity, competitive detoxification metabolism pathways as well as the individual and species difference of drug metabolizing enzymes and intestinal factors. Expert opinion: The early evaluation of the bioactivation potential of herbal components is helpful for providing alerts of herbal toxicity. However, the potential toxic effects should be considered in the context of the complex systems of herbs and the individual patient.  相似文献   

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