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??OBJECTIVE To study the chemical constituents of Fomes fomentarius (L.Ex.Fr.). METHODS The compounds were isolated by chromatography on silica gel column, Sephadex LH-20 column, and their structures were elucidated by spectral analysis. RESULTS Six compounds were obtained and identified as fomentarinin (1), 2-hydroxy hexacosanoic acid ethyl ester (2),syringic acid (3), syringyl alcohol (4), vanillin (5), and ergosta-7,22-diene-3,6-dione (6), respectively. CONCLUSION Compound 1 is a new compound, and compound 2-6 are isolated from the fungus for the first time.
     

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??OBJECTIVE To systematically evaluate the economics of saxagliptin for treatment of type 2 diabetes mellitus. METHODS PubMed, Embase, Cochrane Library, NHS EED, CNKI, Wanfang and CBM were systematically searched. Literatures were screened according to pre-defined inclusion criteria. The quality of included studies were evaluated by CHEERS statement and the economic RESULTS were systematically analyzed. RESULTS Eight cost-effectiveness analyses were included, one of which was conducted in China. Patients among the studies all had blood glucose non-adeguately controlled by monotherapy. When added on to metformin, saxagliptin was cost-effective compared with sulfonylureas (glipizide and glimepiride) and thiazolidinediones (pioglitazone and rosiglitazone). When added on to metformin or sulfonylureas, saxagliptin was cost-effective compared with NPH insulin. CONCLUSION Saxagliptin represents a cost-effective option in treatment of type 2 diabetes mellitus patients with non-adequately controlled blood glucose after monotherapy.     

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??OBJECTIVE To analyze the connotation and composition of the clinical value of drugs, and to build the index system for the evaluation of drug's clinical value, hence to provide references for its scientific evaluation. METHODS We designed the preliminary constructs index system referencingmedicine clinical evaluation indicatorsof German and French firstly. And then the expert interview and Delphi survey were used to analysis to determine the index system and index weight of medicine clinical evaluation. RESULTS The classified index system of the clinical value was established, which was composed of 2 first-grade indexes including clinical value and innovation value and 15 grade two indexes. Experts were invited to assess the value ranking according to the background information of rosuvastatin, atorvastatin and simvastatin statin drugs by their generic names. The expert's scoring results were summarized to determine the sequence. And it were compared with the average market prices in Germany, France, Britain, the United States, South Korea, Japan and analyzed. CONCLUSION The clinical value of drugs is an international standard for determining the reasonable price of drugs. This research method is feasible to determine the drug prices sequencing by the classified clinical value of drugs in the same kind of product. The price sequencing of some generic names of statin drugs did not correspond with its clinical value sequence, and the price can not reflect its value. The integrity and authenticity of the background data directly determine the classification of the clinical value. Various parties are needed to participate in providing detailed data and information.     

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??Polygonati Rhizoma as one of the most common Chinese herbal medicine and food was widely distributed in China. In TCM clinic, it was used for diabetes, hyperlipemia and rehabilitation therapy of cancer. Nowadays, with the rapid development of health industry, Polygonati Rhizoma shows excellent functions on healthcare, and then a surge of demands was coming. But there are so many species belongs to this genus and the classification criteria are not unified, so some important problems become urgently to be resolved, such as how to guarantee the quality and how to keep sustainable development. In this paper, the origin, distribution in China, chemical composition, pharmacological, and clinical application are reviewed. Its prospect is discussed to be helpful to promote the comprehensive development of Polygonatum.     

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??OBJECTIVE Blood tends to deposit in atrium to form thrombus in patients with atrial fibrillation. Patients with diabetes are in high coagulation state, for whom thrombosis is easy to occur. The number of diabetic patients with atrial fibrillation is large. Warfarin is one of the most widely used oral anticoagulants, which can cause major or fatal bleeding, so it is necessary to perform regular monitoring of international normalized ratio (INR) on all patients treated with warfarin. New kinds of antidiabetic drugs are widely used in clinic, among which a lot affect INR levels achieved with warfarin therapy. Clinical pharmacists should pay attention to drug interactions and monitor adverse drug reactions. As a new antidiabetic drug, exenatide has less reports of interaction with warfarin. The characteristic of the interaction between exenatide and warfarin was investigated, with the aim to optimize the rational and individualized medication. METHODS A case was introduced in which exenatide was administrated combined with warfarin, so that the possible mechanism of exenatide affecting to warfarin were analyzed. RESULTS INR declined from 2.13 to 1.57 after exenatide being added, and decreased further to 1.43 with concurrency of the increasing exenatide dose. On the contrary, INR was on rise as result of discontinuing exenatide. At last, INR returned to 1.78 when the patient discharged. CONCLUSION Exenatide inhibited the absorption of warfarin, which lead to INR decline attributed to its effect of slowing down the gastric emptying. When exenatide and warfarin are combined,the dose of warfarin must be adjusted based on INR under clinical monitoring.     

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??OBJECTIVE To study and collate the literature on rare diseases in domestic and abroad, and comparative analysis, provide a scientific basis for the domestic rare diseases research. METHODS Retrieved the Web of Science, China National Knowledge Infrastructure from January 2011 to June 2016 published literature about rare diseases. RESULTS Through the screening of literature, finally determine the 200 articles for analysis. It is divided into seven research directions:rare diseases policy research, rare diseases legal and regulatory research, rare diseases medical social security study, orphan drugs availability research, orphan drugs economic evaluation study, orphan drug development research, rare diseases defined standard research. CONCLUSION Rare diseases policy research is the focus of research both domestic and abroad. Compared with foreign countries, the domestic research on the availability and economic evaluation of orphan drug is less, especially the economic evaluation research is almost blank. It is suggested that the researchers study the multiple aspects of rare diseases and drugs, and to provide the basis and reference for build rare disease policy in China.In addition to the field of rare diseases research, rare diseases drugs face many difficulties in pharmaceutical research, production and supply.The precondition to solve these problems is the nation formulate specific policies and regulations for rare diseases,and then clear the official definition standards of rare diseases,establish relevant policies to encourage pharmaceutical companies to develop rare diseases drugs.     

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??OBJECTIVE To synthesize 5-substituted indole-3-deoxypodophyllotoxin derivatives and study their antitumor activity. METHODS The target compounds were synthesized through a series of reactions and their anti-tumor activity in vitro were evaluated against Hela, K562 and K562/A02 cell lines by MTT as assay. RESULTS Ten target compounds were synthesized and confirmed by ¹H-NMR, ¹³C-NMR, and HR-ESI-MS. All the target compounds had different degrees of cytotoxic activity in vitro. Most of the compounds had significant anti-MDR activity in vitro. CONCLUSION 5-Substituted indole-3-deoxypodophyllotoxin derivatives have good antitumor activity and worth of further study.     

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??OBJECTIVE To determine the effects of saxagliptin and exenatide on humerus cancellous bone of diabetes-induced osteopenia rats by histomorphometry. METHODS Thirty-five Cases of female SD rats were randomly divided into normal group (N group, n=7), control group (C group, n=7), and the remaining rats were used to establish the type 2 diabetic model by combination of high-fat&sugar-diet feeding for 4 weeks and then low-dose streptozotocin injection(STZ, 30 mg??kg^-1) . After 10 d, the oral glucose tolerance test and the fasting blood glucose were measured, rats with high OGTT(2 h) above 11.1 mmol??L^-1 and high FBG above 16.7 mmol??L^-1 were divided into model group (M group, n=5), saxagliptin group (G group, n=5) and exenatide group (D group, n=6), and continuously treated for 30 d. The left humerus (proximal humeru metaphometry, PHM) were fixed with 4% paraformaldehyde for 48 h, uncalcified embedded in methyl methacrylate after dehydrated and cleared, and sections were taken for bone histomorphometry after Masson-Goldner Trichrome stained. RESULTS In PHM, there was no statistical significance between N and C group, the trabecular bone area ratio( BV/TV) and trabecular quantity were significantly decreased (P??0.01) in M group, while the trabecular separation degree was increased, comparing with those in C group (P??0.01), and the trabecular bone area ratio( BV/TV) and trabecular quantity in G and D group were higher (P??0.01) than those of model rats, while the trabecular separation degree was decreased, comparing with those in M group (P??0.01). Cell parameters showed no statistical significance between N and C group, the osteocllast number and percentage of osteocllast surface perimeter were significantly reduced(P??0.05, P??0.01) in M group, while the osteoclast number and percent osteocllast surface perimeter were significantly increased (P??0.01) as compared with those in C group, saxagliptin and exenatide were found to significantly induce osteocllast number (P??0.01) and percentage of osteoblast surface perimeter (G group P??0.05, D group P??0.01), while reduce osteoclast number (P??0.01) and percent osteoblast surface perimeter (P??0.05) compared with M group. In growth-plate, there was no statistical significance between N and C group, the thickness of growth-plate and the diameter of the mast cells were reduced in M groups (P??0.01), while the thickness of growth-plate (P??0.01) and the diameter of the mast cells (P??0.05) were increased in G and D group,compared with M group. CONCLUSION Therapeutic effects of saxagliptin and exenatide on diabetes -induced osteopenia rats was showed, and the mechanism may be related to the improved growth rate of growth-plate and the changed bone turnover status.     

眼用制剂的前药及其药动学研究进展

前药是自身无活性,在体内经化学或酶代谢后释放出有药效活性的原药或代谢物的化合物。前药设计是一种改善眼用制剂不良性质,如水溶性差、生物利用度低、半衰期短和眼部刺激性的重要手段。眼用制剂的药动学主要研究眼对药物的吸收、分布、代谢和排泄的规律。笔者将按照结构修饰类型综述眼用前药的药动学研究进展,从而指导临床合理用药、减少不良反应、提高疗效。     

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??OBJECTIVE The aim of this study is to investigate labelings on dermatologic drugs for pregnant women and provide qualitative and quantitative pharmaceutical support for clinical use. METHODS Labelings and formularies on pregnancy of topical drugs were analyzed and sorted according to classification on pregnancy use. Transdermal abilities of the drugs not forbidden nor avoided were evaluated through ACD/LAB 6.0 software and Potts-Guy formulation. Through TOXNET database and dose conversion equation, toxicities on animals were collected and human doses for pregnant women were calculated. RESULTS In dermatologic drugs, there are 16 drugs forbidden, 8 not recommended/avoided/should not be used, 14 used with caution/weighed pros and cons, 7 used under instruction, 16 unclear or with no statement. In topical drugs not forbidden nor avoided, there are 9 drugs?? logKp above-5, butenafine and sertaconazole with strongest transdermal abilities, 7 drugs?? logKp influenced under pH5.5 or pH7.0, with a decline in logK??p compared with logKp, still 15 drugs not influenced by pH, 7 drugs?? toxicities on animals unknown, 14 drugs?? pregnancy human doses under 10 mgkg^-1. CONCLUSION Currently,only a few topical drugs?? instructions on pregnancy are clear. With properties and animal experiments, better pharmaceutical support can be provided for clinical use on qualitative or quantitative reference.     

中药谱效学溶度参数制样法的研究

[摘要] 目的 研究不同溶度参数的溶剂对中药复方成分溶出规律,为谱效学制样提供新思路及其理论依据。 方法 用不同溶度参数溶媒对补阳还五汤浸膏所得溶解物,通过HPLC方法获得其成分指纹图谱,结合总量统计矩原理,采用总量统计矩相似度法评价不同溶解度参数的溶剂对总方成分溶出液指纹图谱的差异性。 结果 样品的零阶矩AUCT、一阶矩 、二阶矩 的RSD%分别为58.2%、12.8%、24.8%,说明不同溶度参数溶媒溶解所得的化学成分及总量存在明显差异的,其总量统计矩标准相似度介于0.370～0.998之间,特别是S4、S5、S6(溶度参数18.33～20.60 J1/2?cm-3/2)与其他所有号样品的相似度,以及S7、S8(溶度参数21.73～22.87 J1/2?cm-3/2)与除了相邻的样品之外的相似度,都小于0.9,说明其溶媒对的总方溶出成分构成比基本不同。 结论 溶度参数制样法能得到具有显著差异性的中药复方成分组成比,不同溶度参数的溶剂对总分的溶出具有明显规律,可为谱效学体外制样提供一种全新的、可借鉴的思路,为谱效学制样建立完整的理论指导奠定基础。     

从人参药性历史记载的变化看单味药药性成因

总结人参药性成因及单味药药性研究的意义,为中药药性研究提供参考。通过本草学研究,考证历代中医药古籍文献对于中药人参药理药性与功效应用的论述,从“单味药药性成因假说”角度,辨析单味药人参药性历史变化过程,总结单味药人参药性成因。人参药性历史变化过程是中医学具体理论流派指导下的不同流派临床实践经验总结过程,是中药临床功效与临床用药倾向影响中药单味药药性形成过程的具体实例。单味药人参的复杂药性成因体现了中药单味药药性理论与药性实践形成过程中的科学性。     

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??OBJECTIVE To analyze the relationship between hygroscopicity and water solubility of chemical drugs by using nonparametric test. METHODS Dynamic vapor sorption (DVS) analysis was adopted to determine the hygroscopicity of 515 chemical drugs, and solubility test method was adopted to determine the water solubility of these drugs. All samples were divided into four levels according to their water solubility, and the relationship between hygroscopicity and water solubility was investigated by using Kruskal-Wallis ??Wilcoxon rank sum test. RESULTS There were significant differences in the hygroscopicity of drugs with different levels of water solubility, and the hygroscopicity of level 4 was significantly higher than that of level 1. Hygroscopicity was positively correlated with water solubility. CONCLUSION The hygroscopicity of chemical drugs is interpreted in terms of a physical property in this study, and the results provide an experimental foundation for further studies on the mechanism of hygroscopicity.     

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??PEGylated UOX is a kind of modified pharmaceuticals designed by coupling PEG with UOX to increase in vivo circulation half-life and reduce immunogenicity. UOX is modified by PEG at random multiple sites, which RESULTS in more complicated physical and chemical characteristics and in vivo and in vitro activities than UOX. At present, there is no standardized quality analysis method for such drugs. Through collecting and summarizing references about the quality control method of PEG-modified drugs in recent years, this article summarizes the analysis METHODS for three difficulties of the quality control of UOX namely the average extent of modification, consistency of modification and PEGylation sites so as to provide technical guidance for enterprises to develop the drug.     

中药谱效学溶度参数制样法考察

目的:研究不同溶度参数的溶剂对中药复方成分溶出规律,为谱效学制样提供新思路及理论依据。方法:用不同溶度参数溶媒溶解补阳还五汤浸膏,所得溶解物通过HPLC获得其成分的指纹图谱,结合总量统计矩原理,采用总量统计矩相似度法评价不同溶解度参数的溶剂对总方成分溶出液指纹图谱的差异性。结果:样品的零阶矩AUCT、一阶矩λT、二阶矩珚σ2T的RSD分别为58.2%,12.8%,24.8%,说明不同溶度参数溶媒溶解所得的化学成分及总量存在明显差异,其总量统计矩标准相似度介于0.370～0.998。S4,S5,S6(溶度参数18.33～20.60 J1/2.cm-3/2)与其他样品的相似度,以及S7,S8(溶度参数21.73～22.87 J1/2.cm-3/2)与除了相邻样品之外的样品相似度均<0.9,说明其溶媒对总方溶出成分构成比不同。结论:溶度参数制样法能得到具有显著差异性的中药复方成分组成比,不同溶度参数的溶剂对总方的溶出具有明显规律,可为谱效学体外制样提供一种全新的、可借鉴的思路,为谱效学制样建立完整的理论指导提供参考。     

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??To provide scientific and theoretical basis for the further study and reference for the development and efficient use of the medicinal plants, the extraction and separation technology of Celtis sinensis and its main chemical components and pharmacological effects were summarized. Literatures were reviewed, and the key information was classified and summarized. A large number of flavonoids, triterpenoids, phenols, anthraquinones and amides have been isolated from the plants. Extract of Celtis shows diversed pharmacological activities, such as antioxidant, anti-inflammatory, antibacterial, anti-tumor and so on. Further studies should be carried out on Celtis sinensis, which is abundant in our country and has high medicinal value and broad application prospect, for its better development and utilization.     

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??With the continuously clinical study of capsaicin, capsaicin-drug interaction has become increasingly prominent. In recent years, the studies indicate that capsaicin shows a significant inducing or inhibitory effect on a variety of drug metabolism enzymes and transporters, thereby leading to the occurrence of complex drug interactions and affecting the other drugs in vivo process. In this paper, the modulation effect of capsaicin on drug metabolizing enzymes and transporters by reviewing the relevant research at home and abroad in recent years were summarized, and the drug-drug interactions associated with capsaicin in order to provide theoretical guidance for clinical rational drug use were explored . Furthermore, complex drug-drug interaction studies can be provided with prior examples.     

“三要素”理念下药性实质的数学探索

中药药性理论是中药辨、采、制、用的理论指导,具有重要的理论价值和实践意义。课题组首次提出药性构成“三要素”理论,采用文献学、化学、药理学、数学相结合的方法展开研究,得出“药性是以化学成分为始动因素的,在特定机体状态上发生的复杂、多层次正/负生物效应的综合表达”的研究结论。该文从药性与化学成分要素的关联关系、药性与机体状态要素的关联关系、药性与生物效应要素的关联关系、药性构成“三要素”的整合研究4个方面,系统展示数理分析的研究内容,并提出展望,为中药药性的数学研究和数理解读提供参考。