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??OBJECTIVE To identify a Yunnan herbal medicine-Corydalis Taliensis Herb. METHODS Pharmacognostic METHODS have been used on the original plant,macroscopic characteristics ,microscopic tissue structure and powder characteristics of Corydalis Taliensis Herb. RESULTS Corydalis Taliensis Herb is the dried herb of Corydalis taliensis.Its stems five prism,leaves 2- to 3-ternate divided, flowers, spurred,purple, violet or pink, starchy and bitter. The size of epidermal cells are not the same, and some of cell outer wall papillate;stone cells visiblly,fibres with various shapes. CONCLUSION Experimental RESULTS can be used for authenticity identification and quality control of Corydalis Taliensis Herb.     

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??OBJECTIVE To introduce and compare research support for rare disease and orphan drug innovation in China and United States, and provide reference for relevant policies in China.METHODS Data of main source of funding for rare disease research in two countries ie. National Institutes of Health, Food and Drug Administration in the United States and National Natural Science Foundation of China were analyzed and compared. RESULTS US NIH gives substantial support for rare disease research every year with funded capital growing. FDA Orphan Products Grants program provides incentives for sponsors to develop products for rare diseases. In China, however, there is no specific support project for rare disease research, and there is a huge gap in funding efforts for rare disease research between China and the United States. CONCLUSION China should establish rare disease research center to promote rare disease research and set up specific funding for rare diseases research, increase efforts to support research and innovation for rare diseases and orphan drugs, in order to protect the health interests of patients with rare diseases.     

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??OBJECTIVE To provide references for effective quality control of soft capsules and discuss the applicability of method for dissolution test of soft capsules. METHODS Based on analyzing dissolution requirements of soft capsules, we were compared the differences of METHODS for dissolution test in the pharmacopoeias of several countries with current correlative research from home and abord. RESULTS The dissolution characteristics of soft capsules are more complex than common oral solid dosage forms, and the requirments are different in the pharmacopoeias of several countries. The formula of contents, hydrophilicity, rupture test and crossliking have impacts on the dissolution characteristics as well as dissolution device and so on. CONCLUSION In order to develop the method for dissolution test of soft capsules, the dissolution device and medium, rupture test and in vitro-in vivo correlation etc. should be studied.     

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??OBJECTIVE To compare different pretreatment methods for determination of 10 metallic elements including Pb, Cd, As etc in Ganoderma extract. METHODS Microwave digestion, automatic wet digestion and electrical heating wet digestion methods were used to conduct pretreatment of Ganoderma extact, then the contents of Pb, Cd, Hg, As, Cu, Fe, Mn, Zn, Al, Zn and Cr were determined by inductively coupled plasma mass spectrometry(ICP-MS). RESULTS The contents of metallic elements determined by the three kinds of digestion methods were not statistically different except for Hg(P??0.05). The average recoveries of Hg in the Ganoderma samples were 65.28% and 70.39% when processed by automatic digestion and electrical heating digestion method, respectively, much lower than the value of microwave digestion method(98.31%). The recoveries of other metallic elements ranged from 92.19% to 103.26% by the three kinds digestion methods, with RSDs less than 5%. CONCLUSION Automatic digestion and electrical heating digestion methods are unable to meet the requirement for simultaneous determination of the 10 kinds of metallic elements in Ganoderma extract, however, microwave digestion method can. As the microwave digestion method is simple and rapid, so it is more suitable for the determination of heavy metals in Ganoderma. It is suggested to choose appropriate sample digestion method according to specific determination requirement on metallic elements in actual situation.     

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??OBJECTIVE To establish classifiers to predict genotoxic and non-genotoxic carcinogens using toxicogenomics methods, explore the effect of exposure time and validated the prediction performance of the classifiers. METHODS The primary mouse hepatocyte model was treated for 24 and 48 h with two genotoxic carcinogens, aflatoxin B1(AFB1), benzo(a)pyrene (BAP) and two non-genotoxic carcinogens, thioacetamide (TAA), wyeth-14643 (WY). The differentially expressed genes were input to prediction analysis for microarray (PAM) software to screen out classifiers. The functions and interrelations of genes in classifiers were studied by gene set enrichment analysis (GSEA) and the protein-protein interactions were predicted using STRING database. Two additional carcinogens to validate the prediction performance of the classifiers were used. Finally, the experiment of QuantiGene Multiplex assay (Q-GP) to validate the microarray data was used. RESULTS Forty-eight h classifiers had a better predicted capability than that of 24 h classifiers. p53 pathway, TNF-?? signaling pathway, fatty acid metabolism, PPAR signaling pathway involved in the classifires were enriched by GSEA. Carcinogenic protein-protein interaction network and metabolism-related protein-protein interaction network are obtained using STRING database. The predicted probability of the two additional carcinogens using 48 h classifiers was nearly 100% and data between QuantiGene Multiplex assay and microarray assay had a high conformity. CONCLUSION The classifiers which could be used to discriminate the potential genotoxic carcinogens and non-genotoxic carcinogens and to predict modes of action for unknown compounds, are successfully established and validated. This might be a promising candidate in vitro method for carcinogenicity study in the field of nonclinical safety evaluation of drugs.     

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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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??OBJECTIVE ??-Conotoxin LtIA (??-CTX LtIA, LtIA) is a specific inhibitor of ??3??2 nicotinic acetylcholine receptors (nAChRs) from Conus litteratus, a marine snail native to Hainan. The aim of this study was to evaluate the analgesic activity of ??-CTX LtIA. METHODS The analgesic effect of ??-CTX LtIA on pain models was evaluated using mice hot-plate and tail-flick models by intracerebroventricular (icv) injection. RESULTS In tail-flick test, the maximum analgesia percentage (PMAP) was 37.74% at 15 min after LtIA administration by icv injection with dose of 0.2 nmol per mouse. While in hot-plate test, PMAP was 48.81% at 60 min after LtIA administration by icv injection with same dose of 0.2 nmol per mouse. ??-CTX LtIA showed good analgesic activity in two pain models. CONCLUSION ??-CTX LtIA exhibits good analgesic activity by specific interaction with ??3??2 nAChRs subtype. These RESULTS have great significance for the research and development of LtIA painkiller in the future.     

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??OBJECTIVE To develop a method for simultaneous determination of six iridoid glycosides from Cymbaria dahurica.METHODS Cymbaria dahurica collected from different regions were determined by HPLC. The separation was performed on Inertsil ODS-SP column (4.6 mm??250 mm,5 ??m) at 30 ?? by gradient elution with CH₃OH-H₂O as the mobile phase, with the detection wavelength set at 210 nm.RESULTS Under the chromatographic conditions adopted in this study, all the calibration curves exhibited good linearity (r>0.999 4) in a relatively wide concentration range. The recovery of the method was within the range of 95.0%-98.0%, and the RSD was less than 3%. The contents of all the compounds (S1-S6) in samples from different habitats varied significantly.CONCLUSION The quantitative method for evaluating the quality of Cymbaria dahurica is established and can be used for the quality control of Cymbaria dahurica.     

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??OBJECTIVE To investigate the therapeutic effects metabolic mechanism of Schisandra chinensis polysaccharide (SCP) on chronic fatigue syndrome (CFS). METHODS CFS rat model was established in a variety of ways such as the bondage, excessive exercise, crowded and noise environment. The Morris water maze test, the open-field test and the tail-suspension test were performed to evaluate the CFS model. The gas chromatography-mass spectrometry (GC-MS) method was conducted to screen the different metabolites in rat urine and analyze the metabolic pathway. RESULTS The body weight of rats were increased and their space exploration and memory ability were strengthened after SCP supplement. The eleven diversity urine metabolites were detected and the involved metabolic pathways were the tricarboxylic acid cycle and the alanine, aspartic and glutamic acid metabolic pathways. CONCLUSION SCP could relieve the chronic fatigue syndrome. The metabolic mechanism is relative to the improvement of SCP on the tricarboxylic acid cycle and the alanine, aspartic and glutamic acid metabolic pathways.     

基于渗透压原理实现尼莫地平可控释药系统的研究

目的 制备基于渗透压原理的尼莫地平渗透泵胶囊,考察影响其释药行为的因素,优化处方并考察其释放机制。方法 根据尼莫地平渗透泵胶囊在体外累积释放度与零级方程拟合度,对囊壳、含药层、助推层的辅料种类和用量进行单因素考察,选出释放主要影响因素为致孔剂用量、含药层并检测其渗透压活性物质用量和膨胀剂用量,利用Box-Behnken设计法对其进一步优化,确定最优处方。制备3批尼莫地平渗透泵胶囊体外释放度与零级方程拟合考察其释药特性,再使用相似因子法(f₂)进行释放机制研究。结果 尼莫地平渗透泵胶囊最优处方为致孔剂(PEG 6000)用量14 mg、含药层渗透压活性物质(NaCl)用量33.7 mg、膨胀剂(PEO 800万)用量33.2 mg,制备的尼莫地平渗透泵胶囊在12 h内药物释放较完全,致孔剂为药物提供释药途径,渗透压活性物质为释药动力。结论 尼莫地平渗透泵胶囊控释效果良好,累积释放度大于90%,并且接近零级释放方程,符合预期。     

岩白菜素高载药量渗透泵型控释片的制备

目的:制备难溶性药物岩白菜素高载药量单室单层渗透泵型控释片。方法:以渗透泵片常用辅料为混合载体材料制备固体分散体,利用等渗原理优化片芯处方;以岩白菜素累积释放度为指标,采用星点设计-效应面法优化包衣处方。结果:PEG 1500质量分数1.30%,包衣增重9.5%时,制得的岩白菜素高载药量渗透泵片累积释放度接近80%,符合零级释药特征。结论:充分发挥辅料多种功能可有效提高渗透泵片载药量;优化片芯与衣膜处方的方法能显著缩短试验周期,为渗透泵制剂处方设计提供一种新思路。     

钩藤碱双层渗透泵控释片的制备及处方优化

目的 制备钩藤碱双层渗透泵控释片,并进行处方优化.方法 以释药线性和累积释放度为评价指标,单因素试验考察PEO N750用量、PEO Coagulant用量、PEG 4000用量、包衣增重对体外释药的影响,正交试验优化处方,对体外释药过程进行模型拟合.结果 最优处方为PEO N750用量165 mg,PEO Coagulant用量55 mg,PEG 4000用量8%,包衣增重7%,12 h内累积释放度为93.36%,体外释药符合零级模型(r=0.989 5).结论 双层渗透泵控释片可有效控制钩藤碱体外缓释.     

难溶性药物阿替洛尔单层芯渗透泵片的制备

 目的以阿替洛尔为模型药物,通过酸碱反应提高难溶性药物的溶解能力并制备单层芯渗透泵片。方法在处方中加入酒石酸使其与阿替洛尔的碱性基团反应从而增强药物的溶解性,用自行设计的带针冲头压制带孔片芯,以乙基纤维素为膜材包衣制备渗透泵片,采用相似因子作为指标筛选处方。结果在酒石酸溶液中阿替洛尔的溶解能力大幅度提高,制备的阿替洛尔单层芯渗透泵片能在24h内匀速释放药物,且释药行为不受桨转速和释放介质的影响。结论用酒石酸提高阿替洛尔的溶解能力并进而制备单层芯渗透泵片的方法是可行的。酸碱反应增溶药物的方法可望推广到其他难溶于水,但具有酸碱反应能力药物的增溶和渗透泵片的制备。     

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??OBJECTIVE To establish a determination method of the dissolution curves of albendazole tablets with differentiation ability and investigate the similarity of dissolution curves in vitro between reference preparation and generic preparations.METHODS Paddle method was adopted with rotation speed of 50 r??min^-1 and the dissolution medium volume was 900 mL. The dissolution media were pH 1.2 hydrochloric acid solution and water. The similarity factor (f₂) method was used to evaluate the comparability of dissolution curves.RESULTS The three established dissolution curves had good distinguishing ability. As shown by the similarity factor (f₂), the generic preparation from manufacture A was similar to the reference preparation, while those from the manufacture B and C were not similar.CONCLUSION The study provides the experimental basis for the consistency evaluation of the dissolution curves of abendazole tablets.     

星点设计-效应面法优选银杏叶双层渗透泵控释片处方工艺

目的:优选银杏叶双层渗透泵控释片的处方工艺,为改善该制剂的临床用药安全性和有效性提供参考。方法:以总黄酮醇苷的累积释放率为评价指标,通过单因素试验筛选含药层、助推层和包衣液处方,利用f2相似因子法进行相似性判断。选择包衣液中PEG4000用量、包衣增重及助推层PEO用量为自变量,药物释放曲线的相关系数和16 h内累积释放率为因变量,采用星点设计-效应面法优选银杏叶双层渗透泵控释片的处方。结果:最优处方为助推层中聚氧乙烯120 mg,包衣液聚乙二醇4000用量1.5 g,包衣增重11%;16 h内累积释放率90%。结论:制备的渗透泵控释制剂释放曲线符合要求,线性良好(r=0.996 4)。优选的处方工艺稳定可行,可推广于银杏叶双层渗透泵控释片的工业化生产。     

水蜈蚣总黄酮固体分散体微孔渗透泵控释片的处方优化研究

目的 制备水蜈蚣总黄酮固体分散体微孔渗透泵控释片,考察片芯及包衣处方对其体外释药行为的影响,并优选最佳片芯及包衣处方。方法 用以溶剂法制备的水蜈蚣总黄酮固体分散体作为含药片芯,以提高难溶性药物的体外溶出度;制备微孔渗透泵控释片,利用单因素考察和正交试验设计,优化筛选出最佳处方。结果 最佳处方为促渗透剂为氯化钠,用量为100 mg,聚乙二醇400(PEG 400)用量为150%,邻苯二甲酸二丁酯(DBP)用量为20%,包衣膜增重率为2%。结论 按最佳处方制得的水蜈蚣总黄酮固体分散体微孔渗透泵控释片,在12 h内可稳定释药且累积释药率大于90%,其体外释药行为符合零级释放规律。     

盐酸安非他酮微孔型渗透泵片的处方筛选及体外释药模型拟合

 目的 制备盐酸安非他酮微孔型渗透泵片,考察影响该制剂体外释药行为的因素。方法 以累积释药百分率为指标,采用单因素法优化盐酸安非他酮渗透泵片的衣膜处方、片芯组成、制备工艺和体外释放条件,并对优化处方的体外释药行为进行模型拟合。结果 盐酸安非他酮微孔型渗透泵片遵从以渗透压作为主要释药动力的释药模式,释药方程为：Q＝7.228 6t+1.200 0,r＝0.998 1,体外零级释放特征显著。结论 基于渗透压释药机制的盐酸安非他酮微孔型渗透泵片理论可行,结果可控,有利于渗透泵型控释片的产业化推广。     

磷酸川芎嗪微孔渗透泵游离膜扩散动力学研究及其处方优化

 目的 以磷酸川芎嗪为模型,拟合适用于微孔渗透泵控释片的经验公式,用于预测不同包衣膜处方下药物释放速度并优化磷酸川芎嗪微孔渗透泵控释片处方。方法 用游离膜扩散动力学方法,研究不同包衣液处方、游离膜厚度、溶液黏度与药物扩散速度的函数关系。用均匀设计优化磷酸川芎嗪微孔渗透泵处方。结果 以理论的经典公式为原型,以实验数据为根据拟合出适用于微孔渗透泵控释片的经验公式。用均匀设计软件处理磷酸川芎嗪微孔渗透泵释药数据,得到回归方程和优化处方,F检验显示回归方程显著有效,相关系数超过0.99。结论 拟合得到的经验公式能很好的预测药物的释放速度,能为进一步研究提供指导。最优处方药物释放均一性、重现性良好,符合零级释药规律,12 h药物释放90％以上。     

盐酸青藤碱单室单层渗透泵型控释片的制备及释放考察

 目的 研制盐酸青藤碱单室渗透泵型控释片,并考察体外释药行为。方法 采用湿法制粒制备片芯,包衣后激光打孔制备渗透泵片。考察不同辅料种类及用量、助溶剂及包衣增重等因素对药物释放的影响。考察优选处方在不同溶出条件下的释药行为。结果 渗透泵片片芯采用质量百分比为60% 的甘露醇-乳糖（2∶1）为渗透促进剂,10%酒石酸为酸性助溶剂;包衣膜采用醋酸纤维素为控释材料,聚乙二醇为增塑剂,包衣增重4%。所得控释片可体外控制释药16 h,药物释放曲线符合零级释药模型。结论 所研制的盐酸青藤碱控释片释药过程达到了预期的控释目的。