马来酸依那普利片的人体生物等效性研究

目的考察两种马来酸依那普利片的相对生物利用度,评价两者的生物等效性。方法采用双周期自身随机交叉试验设计。20名健康男性志愿者单剂量口服受试制剂或参比制剂,血药浓度采用高效液相色谱-串联质谱测定。结果受试制剂及参比制剂马来酸依那普利实测平均血药峰浓度Cmax分别为（32.74±9.01）、（35.48±11.44）μg.L-1;实测平均达峰时间Tmax分别为（0.76±0.17）、（0.87±0.17）h;受试制剂及参比制剂t1/2分别为（2.52±2.95）、（3.10±5.79）h;AUC（0-48h）平均值分别为（59.22±20.46）、（64.43±23.42）mg·h·L-1;AUC（0-∞）平均值分别为（60.01±20.39）、（65.09±23.43）mg·h·L-1;以AUC计算,受试制剂的相对生物利用度为（97.8±34.1）%。结论受试制剂和参比制剂具有生物等效性。     

药品数粒机碎片剔除系统三维检测模型的构建

介绍在全自动药品数粒机上如何利用光电技术、物理学及微积分等原理构建三维检测模型,实现药品数粒过程碎片的检测和分类剔除。     

硝苯地平缓释片联合依那普利治疗高血压病48例疗效观察

目的观察硝苯地平缓释片联合依那普利的降压作用、不良反应及对代谢的影响。方法将96例原发性高血压病患者随机分为治疗组和对照组各48例,治疗组服用硝苯地平缓释片及依那普利,对照组单纯服用依那普利,疗程4周,由固定医生测坐位血压,于治疗前后测血糖、血脂、电解质、肝功能、肾功能,并行心电图检查。结果治疗组和对照组在服药4周后显效率分别为45．8％、25．O％,总有效率分别为95．8％、68．7％,两组比较差异有统计学意义（P〈0．05或P〈0．01）,而两组治疗对糖代谢、脂代谢、电解质、肝功能、肾功能及心电图并无明显影响。结论硝苯地平联合依那普利降压效果好,副作用小,值得临床推广应用。     

雷公藤多苷片对佐剂性关节炎大鼠血清SOD含量影响的实验研究

目的：研究雷公藤多苷片对佐剂性关节炎大鼠血清中超氧化物歧化酶（SOD）含量的影响。方法：将40只Wistar大鼠随机分成正常对照组、模型组、雷公藤多苷片治疗组（雷公藤组）、泼尼松治疗组（泼尼松组）4组,每组10只。造模后第8天、第12天、第16天、第20天、第24天测量大鼠左后踝关节周径,计算关节炎指数;第28天取血,检测血清中超氧化物歧化酶（SOD）含量。结果：与模型组比较,雷公藤组大鼠左足跖肿胀度及关节炎指数显著降低（P〈0．05,P〈0．01）,血清中SOD含量显著升高。结论：雷公藤多苷片除具有较强的抗炎及免疫抑制作用外,还具有抗氧化作用。     

大黄控释片的研制及其体外溶出特性的研究

 目的制备大黄控释片。方法采用正交设计以体外溶出为指标,以羟丙基甲基纤维素为阻滞剂,进行处方筛选。结果优化后的处方可达到美国药典对缓释制剂体外溶出的要求。结论该片剂处方合理,制备工艺简单易行,适合工业化生产。     

扶正化瘀胶囊/片治疗肝纤维化和肝硬化的临床研究进展

本文综述2010—2013年发表的扶正化瘀胶囊/片临床研究论文。扶正化瘀胶囊/片临床治疗肝纤维化和肝硬化疗效明确,用以治疗肝硬化并发症,也取得较好疗效。数十项临床研究证实,扶正化瘀胶囊/方与抗乙肝病毒的核苷类(核苷类似物)药物、普通干扰素或聚乙二醇干扰素、熊去氧胆酸以及其他药物联用,治疗慢性乙型肝炎和其他慢性肝病所致肝纤维化和肝硬化,提高了疗效。此外,也开展了利用人体样本揭示扶正化瘀胶囊的临床作用机制的研究。扶正化瘀胶囊/片的未来研究,可能会有如下趋势:1)扩大适应证;2)进一步联合应用其他药物以提高临床疗效;3)优化组方;4)开展新剂型的研究;5)进一步揭示扶正化瘀复方的作用机制。     

高效液相色谱法测定排毒清脂片中大黄素、大黄酚的含量

目的：建立高效液相色谱法（HPLC）测定排毒清脂片中的大黄素、大黄酚的含量。方法：色谱柱：UItimate XB－C18柱（250mm×4.6mm,5?滋m）;流动相：甲醇－磷酸溶液（85∶15）;流速：1mL·min-1;检测波长：254nm。结果：大黄素、大黄酚分离良好,进样量分别在0.007984~0.047904?滋g和0.01002~0.06012?滋g范围内与峰面积是良好线性关系,r值分别为0.9991和0.9998,平均回收率分别为99.18%和99.94%,RSD分别为1.19%和1.16%（n=5）。结论：该方法简便、精确、分离效果好、专属性强,可作为排毒清脂片中大黄成分的质量控制方法。     

5个企业枸橼酸他莫昔芬片的体外溶出度考察

目的对国内5个企业枸橼酸他莫昔芬片进行体外溶出度考察,为临床合理用药提供依据。方法以紫外分光光度法测定含量,浆法测定溶出度。利用Excel软件的VBA编写宏命令,在计算机上快速算出枸橼酸他莫昔芬片的累积溶出百分率和溶出参数,并对各组之间的溶出参数进行方差分析。结果所测产品的体外溶出均达到中国药典规定的30min溶出应大于标示量75%的要求,但各企业枸橼酸他莫昔芬片的溶出参数（m、t50、td、t80）间存在着高度显著性差异（P〈0.01）。结论不同企业枸橼酸他莫昔芬片的溶出参数存在着显著差异,临床用药时应加以注意。     

Studies on Formulation and In Vitro Evaluation of Floating Matrix Tablets of Domperidone

Floating matrix tablets of domperidone were developed to prolong gastric residence time and thereby increased drug bioavailability. Domperidone was chosen as a model drug because it is poorly absorbed from the lower gastrointestinal tract. The tablets were prepared by wet granulation technique, using polymers such as hydroxypropylmethylcellulose K4M, carbopol 934P, and sodium alginate, either alone or in combination, and other standard excipients. Tablets were evaluated for physical characteristics viz. hardness, % friability, floating capacity, weight variation and content uniformity. Further, tablets were evaluated for in vitro release characteristics for 24 h. In vitro release mechanism was evaluated by linear regression analysis. Floating matrix tablets based on combination of three polymers namely; hydroxypropylmethylcellulose K4M, carbopol 934P and sodium alginate exhibited desired floating and prolonged drug release for 24 h. Carbopol loading showed negative effect on floating properties but were found helpful to control the release rate of drug.     

The effect of chemical heterogeneity of HPMC on polymer release from matrix tablets

Polymer release from hydrophilic matrix tablets, composed of hydroxypropyl methylcellulose, was studied for seven different polymer batches. A time difference of more than 80 h between fully dissolved tablets was noticed although the batches were of the same pharmaceutical substituent (USP 2208) and viscosity (100 cps) grade. To find the functionality related parameters for polymer release from hydrophilic matrix tablets the polymer samples were characterised according to size and chemical composition. The size of the polymers was characterised by size-exclusion chromatography with multi-angle light scattering and refractive index detection. The average amount of substituents was measured with nuclear magnetic resonance and the distribution of the substituents along the cellulose chain was determined with high-performance anion-exchange chromatography with pulsed amperometric detection after acid and enzymatic hydrolysis. The results indicated that other types of interactions apart from entanglements were present between the polymer chains, which seemed to affect the polymer release. Most importantly, this study has shown a correlation between the polymer release and the substituent pattern, where the samples with slow release also were more heterogeneously substituted along the polymer chain. From this we can conclude that polymer release is very sensitive to alterations in chemical composition.