消旋棉酚晶态结构的研究

目的:研究消旋棉酚晶形结构。方法:采用红外光谱(IR)、差示扫描量热法(DSC)、测定溶解度和粉末X射线衍射法(XRD)来研究消旋棉酚晶态结构。结果:消旋棉酚[(±)G]、左旋棉酚[(-)G]和右旋棉酚[(+)G]的红外谱图基本相同;DSC图谱及热特征数据不一致;在消旋棉酚的饱和溶液中加入光学活性棉酚,光学活性棉酚可以继续溶解,并且有旋光产生;(±)G与(-)G及(+)G的XRD图完全不同。结论:消旋棉酚晶体属于外消旋化合物。     

Copper thiocyanato complexes and cocaine – a case of ‘black cocaine’

The chemical composition of a black powder confiscated by German customs was elucidated. Black powders are occasionally used as a ‘transporter’ for cocaine and are obviously especially designed to cloak the presence of the drug. The material consisting of cocaine, copper, iron, thiocyanate, and graphite was approached by analytical tools and chemical modelling. Graphite is added to the material probably with the intention of masking the typical infrared (IR) fingerprints of cocaine and can be clearly detected by powder X‐ray diffraction (XRD) and Raman spectroscopy. Cu²⁺ and NCS^? ions, when carefully reacted with cocaine hydrochloride, form the novel compound (CocH)₂[Cu(NCS)₄] (CocH⁺ = protonated cocaine), which has been characterised by single crystal XRD, IR, NMR, UV/Vis absorption and EPR spectroscopy. Based on some further experiments the assumed composition of the original black powder is discussed. Copyright © 2014 John Wiley & Sons, Ltd.     

德都红花-7味散对大鼠肝再生过程的双向调节作用机制研究

目的 探讨在肝再生过程中德都红花-7味散对酪氨酸激酶(JAK)/信号转导及转录激活因子(STAT)信号通路的影响.方法 按照随机数字表法将SD大鼠分为4组:假手术组、模型组、阳性对照组和实验组,每组20只.阳性对照组灌胃护肝片(0.28 g·kg-1),实验组灌胃德都红花七味散(0.6 g·kg-1).大鼠部分肝切除术...     

降糖新药那格列奈的一种新晶型结构

目的：发现降糖药那格列奈另一种新的晶型结构,我们称之为S型。给出X射线衍射图谱和相关数据。方法：用X射线衍射物相分析法确定这种新的结构。用差示扫描量热仪测定它的熔点。结果：S型那格列奈具有与文献报道的H、B型完全不同的晶体结构。熔点为172．04℃,。结论：S型那格列奈是一种新型结构,X射线衍射法是药物晶型结构鉴定的有效方法。     

Optimization of the High-Shear Wet Granulation Wetting Process Using Fuzzy Logic Modeling

A fuzzy model has been developed for the optimization of high-shear wet granulation wetting on a plant scale depending on the characteristics of pharmaceutical active substance particles. The model optimized on the basis of experimental data involves a set of rules obtained from expert knowledge and full-scale process data. The skewness coefficient of particle size distribution and the tapped density of the granulated mixture were chosen as the model input variables. The output of the fuzzy ruled system is the optimal quantity of wetting liquid. In comparison to manufacturing practice, a very strong sensitivity of the optimal quantity of the added wetting liquid to the size and shape of the active substance particles has been identified by fuzzy modeling.     

Dry powder inhalations containing thymopentin and its immunomodulating effects in Wistar rats

Thymopentin (TP5), a synthetic pentapeptide, has been used in clinic as a modulator for immunodeficiences through intramuscular administration. The purpose of this study was to design and evaluate dry powder inhalations (DPIs) for pulmonary delivery of TP5. Dry powder inhalations containing leucine (a dispersibility enhancer), mannitol, and lactose (bulking agents) were prepared by spray-drying from aqueous formulations. The formulation components on the aerosolisation characteristics of spray-dried powders were investigated through the use of various amount of leucine, lactose and mannitol. Following spray-drying, resultant powders were characterized using scanning electron microscopy, laser diffraction and tapped density measurements, and the aerosolisation performance was determined using Twin Stage Impinger. The immunosuppression Wistar rats model was constructed to evaluate the immunomodulating effects of TP5 DPIs in vivo. The results of T-lymphocyte subsets (CD3+, CD4+, CD8+, CD4+/CD8+ ratio) analyses suggest that TP5 DPIs have modulating effects. On an overall evaluation, TP5 pulmonary delivery DPIs may be feasible for the future clinical application.     

沙美特罗替卡松粉复合吸入剂联合孟鲁司特治疗咳嗽变异性哮喘的疗效观察

目的探讨沙美特罗替卡松粉复合吸入剂联合孟鲁司特对咳嗽变异性哮喘（CVA）患者的临床疗效。方法100例CVA患者完全随机分为孟鲁司特组和联合治疗组各50例,孟鲁司特组给予孟鲁司特（默沙东公司,商品名：顺尔宁）10mg,每晚1次,疗程8周;联合治疗组吸人沙美特罗替卡松粉复合吸入剂（葛兰素史克公司,商品名：舒利迭）50μg／250μg,2次／d,口服孟鲁司特10mg,每晚1次,疗程均为8周。观察2组治疗前后临床症状、肺功能以及诱导痰中炎性细胞的变化。结果2组药物治疗后临床咳嗽症状改善明显,孟鲁司特组总有效率82％,联合治疗组总有效率94％,二者比较,差异有统计学意义（P〈0．01）;与孟鲁司特组比较,联合治疗组诱导痰中相关炎症细胞总数和嗜酸粒细胞百分比较治疗前减少明显（2．76±0．61vs3．02±0．55;10．2±2．9vs14．8±3．5,P〈0．05）,肺通气功能（FEV1,FEV1预计值和FEV1／FVC）改善明显（P〈0．05）,联合治疗组疗效优于孟鲁司特组。结论沙美特罗替卡松粉复合吸入剂联合孟鲁司特治疗CVA具有较好的疗效。     

湿感头痛散联合针灸康复治疗发作期紧张性头痛的临床疗效观察

目的：探讨湿感头痛散联合针灸康复治疗发作期紧张性头痛的临床疗效。方法选取我院120例急紧张性头痛患者,通过随机数字表法分为联合组和针灸组各60例,联合组采用湿感头痛散联合针灸治疗,针灸组单用针灸治疗,观察比较两组患者临床疗效。结果两组患者治疗后,联合组的临床疗效总有效率高于针灸组,差异有统计学意义（P＜0．05）;联合组的HAMD、HAMA评分优于针灸组（P均＜0．05）;联合组的头痛发作频率、持续时间（h）少于针灸组（P均＜0．05）;联合组的VAS（分）低于针灸组（P＜0．05）。结论采用湿感头痛散联合针灸治疗紧张性头痛有助于缓解患者的抑郁,减少发作次数,减少持续时间以及疼痛感,疗效显著,值得临床推广。     

Multi-walled carbon nanotube-induced inhalation toxicity: Recognizing nano bis-demethoxy curcumin analog as an ameliorating candidate

Human beings and ecosystems are being possibly exposed to CNTs, as there is a rise in global production rate of carbon nanotubes (CNTs). This may affect the health of humans and increases the environmental risk. We have already reported the pulmonary toxicity due to the inhalation of MWCNTs. We claim that a compound with anti-inflammatory and antioxidant activity may ameliorate the CNT-induced toxic effect. With this view, we have investigated the ameliorative effect of intravenously-administered nano bis-demethoxy curcumin analog (NBDMCA) against MWCNTs-induced inhalation toxicity by examining the lung histopathology for inflammatory cell dynamics, pulmonary remodeling and estimating the inflammatory biomarkers in the broncho-alveolar lavage fluid. We observed that NBDMCA could ameliorate the injury as evidenced by the decline in the levels of markers of inflammation, cell damage, and the histopathological changes induced by MWCNTs. We conclude that NBDMCA may be used to reduce the risk of MWCNTs-induced inhalation toxicity.     

高效液相色谱法同时测定三七伤药片中新北美圣草苷和柚皮苷的含量

目的 建立三七伤药片中同时测定新北美圣草苷和柚皮苷含量的方法.方法 以甲醇为溶剂,进行超声提取;色谱柱:Agilent C18(250 mm×4.6 mm,5 μm);流动相:乙腈-0.1%磷酸溶液(17:83),流速:1 mL·min-1,检测波长:283 nm,柱温35 ℃.结果 新北美圣草苷在87.55~1 313.25 ng范围内线性关系良好(r=0.999 4),平均回收率为99.13%,RSD=1.21% (n =6),柚皮苷在80.4~1 206 ng范围内线性关系良好(r=0.999 6),平均回收率为96.78%,RSD=3.34%(n=6).结论 高效液相色谱法(HPLC)可以同时测定新北美圣草苷和柚皮苷的含量,方法简便、准确、灵敏度高、重现性好,可用于三七伤药片中骨碎补的质量控制.