银杏内酯注射液联合胞磷胆碱钠片对脑梗死恢复期患者脑血流动力学、氧化应激和血清MCP-1、Lp-PLA2的影响

摘要 目的：研究银杏内酯注射液联合胞磷胆碱钠片对脑梗死恢复期患者脑血流动力学、氧化应激和血清单核细胞趋化蛋白-1（MCP-1）、脂蛋白相关磷脂酶A2（Lp-PLA2）的影响。方法：按照随机数字表法,将安徽中医药大学第一附属医院146例脑梗死恢复期患者分为对照组（n=73,采用常规治疗和胞磷胆碱钠片治疗）和研究组（n=73,对照组基础上结合银杏内酯注射液）。对比两组临床疗效、Barthel指数（BI）评分、美国国立卫生研究院卒中量表（NIHSS）评分、脑血流动力学指标、血清氧化应激指标、MCP-1、Lp-PLA2和用药安全性。结果：与对照组的82.19%临床总有效率对比,研究组的97.26%更高（P<0.05）。治疗后,研究组BI评分、平均血流速度（Vm）、血清超氧化物歧化酶（SOD）、过氧化氢酶（CAT）较对照组更高,NIHSS评分、搏动指数（PI）、阻力指数（RI）、血清活性氧（ROS）、血清MCP-1、Lp-PLA2较对照组更低（P<0.05）。两组不良反应发生率组间对比未见差异（P>0.05）。结论：银杏内酯注射液联合胞磷胆碱钠片可减轻脑梗死恢复期患者的神经功能损伤,改善患者的脑血流动力学,减轻氧化应激,调节血清MCP-1、Lp-PLA2水平,且用药安全性良好。     

Stereoselective drug release from Ketoprofen and Ricobendazole matrix tablets

Crystalline characteristics of racemic, pure R and S enantiomers and physical mixtures of Ketoprofen (KET) have been studied by DSC and X‐ray diffractometry. Aqueous solubilities were 182.6 ± 9.1 μg/ml for racemic KET, 259.6 ± 6.6 μg/ml for R‐KET, and 304.3 ± 2.7 μg/ml for S‐KET. Matrix tablets made with racemic and physical mixtures of KET show stereoselective drug release, which is faster for S‐KET than for R‐KET. This effect is more marked when the chiral excipient hydroxypropylmethylcellulose (HPMC) is used in place of the achiral Eudragit RL. Stereoselectivity of release is also affected by the amount of KET. Similar results were obtained when another chiral drug with low solubility, Ricobendazole (RBZ), is used. Depending on the excipient and drug dosage, more or less marked stereoselective drug release is obtained in RBZ matrix tablet formulations. Chirality 11:611–615, 1999. © 1999 Wiley‐Liss, Inc.     

亚健康状态大鼠的神经-免疫-内分泌机制的研究

目的探讨亚健康状态大鼠的神经-免疫-内分泌的机制。方法取雄性SPF级Wistar大鼠36只,按体重随机分成6组,即多因素组（MF）、多因素干预组（MFT）、热水游泳组（WS）、睡眠不足组（SD）、单纯束缚组（PC）和正常对照组（C）,每组6只。分别采用热水游泳、饮食限制、睡眠剥夺、束缚等方式建立亚健康大鼠模型,多因素干预组每日经口给予300 mg/kg的抗衰老片,在造模5 d后处理动物,并取大鼠血,分别测定血清5-羟色胺（5-HT）、多巴胺（DA）、甲状腺激素T3和T4、睾酮（T）、皮质酮（CORT）、促肾上腺皮质激素（ACTH）、白介素IL-1β、IL-2、IL-6、IL-8和IFN-γ含量以及T淋巴细胞亚群的变化,并取脾脏测定T、B淋巴细胞增殖能力和NK细胞活性变化。结果 （1）与正常对照组比,①造模结束后多因素组大鼠血清5-HT明显降低（P〈0.05）,而热水游泳组和单纯束缚组5-HT含量却升高显著（P〈0.01）,且睡眠不足组和单纯束缚组血清DA含量降低显著（P〈0.05）;同时各亚健康模型大鼠的血清T3、T4、CORT和ACTH含量均显著升高（P〈0.01）,T/C比值降低显著（P〈0.01）,且睡眠不足组血清T降低明显（P〈0.05）;②造模结束后多因素组的大鼠IL-8含量降低显著（P〈0.01）,而热水游泳组和单纯束缚组IL-1β、IL-2、IL-6、IL-8和IFN-γ含量以及睡眠不足组IL-1β、IL-2、IL-6含量均显著升高（P〈0.05,P〈0.01）,同时显著降低各亚健康模型大鼠淋巴细胞增殖转化能力和T淋巴细胞亚群CD3＋、CD4＋和CD4＋/CD8＋比值和NK细胞活性（P〈0.05,P〈0.01）。（2）与多因素组比,抗衰老片干预后多因素干预组大鼠血清DA含量明显升高（P〈0.05）,并能显著提高机体T淋巴细胞亚群CD3＋、CD4＋数目和CD4＋/CD8＋比值（P〈0.01）,降低血清CORT含量。结论亚健康状态能引起大鼠HPA轴反应性失衡,皮质醇释放过度,引起内分泌的紊乱,并能引起淋巴细胞功能降低,出现明显机体免疫抑制现象;而抗衰老片具有抗应激,提高T细胞免疫功能,改善情绪和内分泌紊乱的作用,从而达到改善亚健康体质的目的。     

血栓通注射液联合阿托伐他汀对急性脑梗死患者血脂和血液流变学的影响

目的:研究阿托伐他汀片与血栓通注射液联合治疗对脑梗死患者血脂及血液流变学的影响。方法:选取我院从2012年2月到2014年2月收治的急性脑梗死患者100例,分成两组,每组各50例。对照组静脉滴注血栓通注射液,试验组静脉滴注血栓通注射液加口服阿托伐他汀片治疗。14天后观察两个组的治疗效果,并且进行血脂(TC、TG、LDL-C、HDL-C)、血液流变学(血浆粘度、全血高切粘度、全血低切粘度、全血还原黏度、纤维蛋白原、细胞刚性指数)等指标的检测,以及疗效及不良反应情况。结果:治疗后试验组TC、TG、LDL-C低于对照组,HDL-C高于对照组,且具有统计学意义(P0.05)。治疗后,试验组血浆粘度、全血高切粘度、全血低切粘度、全血还原黏度、纤维蛋白原、细胞刚性指数均低于对照组,且具有统计学意义(P0.05)。试验组总有效率为88.0%(44/50),高于对照组的66.0%(33/50)(P0.05)。试验组发生不良反应发生率与对照组比较无统计学意义(P0.05)。结论:阿托伐他汀片联合血栓通注射液对于脑梗死患者的血脂和血液流变学的影响疗效显著,且具有明显的降脂效果。     

黑果枸杞提取物泡腾片的制备及其质量评价

为了解决黑果枸杞中花青素稳定性问题,本文采用Box-Behnken设计对黑果枸杞提取物泡腾片配方进行优化,并对其进行质量评价。采用酸碱混合制粒压片法,通过单因素实验,筛选出片剂所需的辅料:崩解剂、填充剂、润滑剂以及甜味剂。采用响应面试验,结合感官评价进行处方优化,从而确定最优配方:柠檬酸32%、黑果枸杞提取物25%、碳酸氢钠24%、乳糖15%、甜蜜素3%、聚乙二醇6000 1%;对最优配方进行质量评价,各项指标均符合规定,其中花青素含量为8.06 mg/g。该泡腾片表面光滑,泡腾效果好,具有黑果枸杞香气,为实际生产提供理论依据。     

Derivative emission spectrofluorimetry: Application to the analysis of newly approved FDA combination of ibuprofen and famotidine in tablets

A new combination of ibuprofen (NSAID) and famotidine (H₂ receptor antagonist) was recently approved by the FDA. It was formulated to relief pain while decreasing the risk of ulceration, which is a common problem for patients receiving NSAID. A rapid and simple derivative emission spectrofluorimetric method is proposed for the simultaneous analysis of this combination in their pharmaceutical preparation. The method is based upon measurement of the native fluorescence intensity of the two drugs at λ_ex = 233 nm in acetonitrile. The emission data were differentiated using the first (D1) derivative technique. The plots of derivative fluorescence intensity versus concentration were rectilinear over a range of 2–35 and 0.4–8 µg/mL for both ibuprofen (IBU) and famotidine (FAM), respectively. The method was sensitive as the limits of detection were 0.51 and 0.12 µg/mL and limits of quantitation were 1.70 and 0.39 µg/mL, for IBU and FAM respectively. The proposed derivative emission spectrofluorimetric method was successfully applied for the determination of the two drugs in their synthetic mixtures and tablets with good accuracy and precision. The proposed method was validated as per ICH guidelines. Copyright © 2014 John Wiley & Sons, Ltd.     

心可舒治疗频发早搏疗效观察

目的：应用心率变异性的方法观察心可舒片对旱搏的治疗效果及其影响。方法：将96例频发旱搏患者随机分成治疗组（51例）和对照组（45例）。对照组给予倍他乐克缓释片口服,47．5mg／次,1次／日,治疗组在口服倍他乐克缓释片基础上加用心可舒片4片／次,3次／日。在服药前及服药后1个月各行1次动态心电图及普通心电图检查,并进行临床观察。结果：治疗组在消除旱搏,改善临床症状方面较对照纽明显有效（P〈0．05）,治疗组较对照组心率变异性改善有明显差异（P〈0．05）。结论：心可舒片与倍他乐克舍用可有效增加其治疗早搏的作用,同时改善心率变异性和改善倍他乐克引起的窦性心动过缓副作用,有较好的临床疗效。     

三种药物联合治疗假丝酵母菌性阴道炎的临床疗效评价

目的:研究克霉唑阴道片、硝夫太尔制霉素阴道软胶囊联合定君生栓治疗复发性假丝酵母菌性阴道炎的临床疗效,为临床治疗提供依据。方法:选取2014年9月到2015年6月我院就诊的复发性假丝酵母菌性阴道炎患者60例,按照随机数字表法将患者分为实验组和对照组,每组30例,实验组给予克霉唑阴道片、硝夫太尔制霉素阴道软胶囊联合定君生栓治疗,对照组给予克霉唑阴道片和定君生栓治疗,治疗前检测所有患者病原菌分布情况,治疗后随访3个月,分析两组临床疗效和不良反应。结果:细菌培养结果共分离出158株假丝酵母菌,其中白色假丝酵母菌最多,占66.46%;实验组总有效率为93.33%,显著高于对照组的76.67%,两组比较差异具有统计学意义(P0.05);两组不良反应发生率比较无统计学意义(P0.05)。结论:克霉唑阴道片、硝夫太尔制霉素阴道软胶囊联合定君生栓治疗复发性假丝酵母菌性阴道炎具有较好的临床疗效,且无明显不良反应。     

Formulation and optimization of mouth dissolve tablets containing rofecoxib solid dispersion

The purpose of the present investigation was to increase the solubility and dissolution rate of rofecoxib by the preparation of its solid dispersion with polyvinyl pyrrolidone K30 (PVP K30) using solvent evaporation method. Drug-polymer interactions were investigated using differential scanning calorimetry (DSC), x-ray diffraction (XRD), and Fourier transform infrared spectroscopy (FTIR). For the preparation of rofecoxib mouth dissolve tablets, its 1∶9 solid dispersion with PVP K30 was used with various disintegrants and sublimable materials. In an attempt to construct a statistical model for the prediction of disintegration time and percentage friability, a 3² randomized full and reduced factorial design was used to optimize the influence of the amounts of superdisintegrant and subliming agent. The obtained results showed that dispersion of the drug in the polymer considerably enhanced the dissolution rate. The drug-to-carrier ratio was the controlling factor for dissolution improvement. FTIR spectra revealed no chemical incompatibility between the drug and PVP K30. As indicated from XRD and DSC data, rofecoxib was in the amorphous form, which explains the better dissolution rate of the drug from its solid dispersions. Concerning the optimization study, the multiple regression analysis revealed that an optimum concentration of camphor and a higher percentage of crospovidone are required for obtaining rapidly disintegrating tablets. In conclusion, this investigation demonstrated the potential of experimental design in understanding the effect of the formulation variables on the quality of mouth dissolve tablets containing solid dispersion of a hydrophobic drug.     

Enhancement of dissolution profile by solid dispersion (kneading) technique

This article investigates enhancement of the dissolution profile of valdecoxib using solid dispersion with PVP. The article also describes the preparation of fast-dissolving tablets of valdecoxib by using a high amount of superdisintegrants. A phase solubility method was used to evaluate the effect of various water-soluble polymers on aqueous solubility of valdecoxib. Polyvinyl pyrrolidone (PVP K-30) was selected and solid dispersions were prepared by the method of kneading. Dissolution studies, using the USP paddle method were performed for solid dispersions of valdecoxib. Infrared (IR) spectroscopy, differential scanning calorimetry (DSC), and x-ray diffractometry (XRD) were performed to identify the physicochemical interaction between drug and carrier, hence its effect on dissolution. Tablets were formulated containing solid dispersion products and compared with commercial products. IR spectroscopy, XRD, and DSC showed no change in the crystal structure of valdecoxib. Dissolution of valdecoxib improved significantly in solid dispersion products (<85% in 5 minutes). Tablets containing solid dispersion exhibited better dissolution profile than commercial tablets. Thus, the solid dispersion technique can be successfully used for improvement of dissolution of valdecoxib. Published: August 18, 2006