甲硝唑口颊片的工艺研究

采用正交试验设计,考察处方工艺中羧甲基纤维素钠的用量、筛网的大小和片剂的硬度对甲硝唑口颊片的质量影响,从而优选甲硝唑口颊片的最佳处方和制备工艺。制备的甲硝唑口颊片各项指标均符合质量标准,20、50和90min的释放度分别为33．4％、54．3％和74．1％。     

葛根黄豆苷元分散片的制备及其溶出度测定

对葛根黄豆苷元片进行工艺改进,制成分散片,以提高其溶出度,并通过探讨葛根黄豆苷元片溶出度检查方法的稳定性、均一性、重现性、回收率试验等,确立测定葛根黄豆苷元片溶出度的最佳条件。     

尼莫地平固体分散片溶出度比较

以进口尼莫地平薄膜包衣片为参考 ,比较国内两厂家的尼莫地平固体分散片溶出度。以乙醇∶水 (15∶85 )为溶出介质 ,在 (37± 0 5 )℃下 ,浆法 ,进行溶出实验 ,采用紫外分光光度法测定并计算结果。各厂家尼莫地平片 30min内溶出度不低于 70 %。经t检验 ,3种样品组间 4 5min溶出度无显著性差异 (P >0 0 5 )。     

饮片细粉对肠炎宁半浸膏片压缩成型的影响研究

目的 研究半浸膏颗粒中饮片细粉含量对其物理性质和压缩性能的影响。方法 以肠炎宁片为模型药物,测定含不同饮片细粉比例的肠炎宁颗粒的粉体学性质、压缩过程参数、抗张强度等指标,采用不同压缩方程对片剂抗张强度-压力、孔隙率-压力、抗张强度-孔隙率的变化规律进行拟合,阐明肠炎宁半浸膏片的成型机制,并用主成分分析对粉体学性质、压缩过程参数及拟合系数之间的相关性进行分析。结果 当肠炎宁颗粒中的饮片细粉含量小于6%时,随着饮片细粉含量的增加,粒子间的结合力增强,粉体的成型性增强;当含量超过6%后,饮片细粉弹性作用增强,粒子间结合力减弱,抑制成型。结论 从压缩成型角度说明了肠炎宁半浸膏片中饮片细粉含量的临界值为6%,可为半浸膏片的处方工艺优化提供较好的理论和实验依据。     

探讨服用复方丹参片和VE胶囊对治疗椎动脉型颈椎病的疗效

目的探讨复方丹参片和VE对于治疗椎动脉型颈椎病的疗效。方法比较,对35例中年女患者(37～53岁)口服复方丹参片和VE1个月,服药前后,对椎基底动脉血流及临床病症前后对比。结论口服复方丹参片和VE胶囊可治疗颈椎病,特别是椎动脉型颈椎病效果更显著。     

盐酸二甲双胍缓释片在健康受试者餐后条件下的生物等效性研究

评价盐酸二甲双胍缓释片受试制剂和参比制剂在健康受试者餐后单次给药条件下的生物等效性和安全性。试验采用单中心、随机、开放、单剂量、两周期、两序列、双交叉设计,32例健康受试者在餐后状态下单次服用受试制剂或参比制剂0.5 g,在给药前(0 h)至给药后1、3、4、4.5、5、5.5、6、7、8、9、10、12、15、24、36和48 h采集静脉血4 mL,检测血浆样本中二甲双胍的浓度,用Win Nonlin 7.0软件计算药代动力学参数,当受试制剂与参比制剂的c_max、AUC_0-t、AUC_0-∞几何均值比的90%置信区间均在80.00%～125.00%等效区间内,证明两制剂生物等效。有1例受试者因不良事件脱落。受试制剂和参比制剂的主要药代动力学参数：c_max为(0.68±0.14)和(0.65±0.11) mg/L,AUC_0-t为(7.33±1.65)和(7.00±1.89) h·mg/L,AUC_0-∞为(7.39±1.67)和(7.06±1.91) h·mg...     

Discontinuation of Phenytoin, Carbamazepine, and Valproate in Patients with Active Epilepsy

The effects of discontinuing individual antiepileptic drugs (AEDs) in patients with active epilepsy who are receiving combination therapy have not been studied systematically. We report a double-blind, prospective study of discontinuation of phenytoin (PHT), carbamazepine (CBZ), and valproate (VPA) in 70 patients with chronic active epilepsy. Each drug discontinuation was randomized to one of two relatively fast rates of reduction, and a control group of 25 patients continued with stable therapy. Patients who had CBZ removed had a significant increase in seizures that was maintained for 4 weeks after the end of drug reduction, and 10 of these 23 patients had to restart therapy with CBZ. There was no significant change in seizure numbers in the other groups. Two patients discontinued from VPA had to restart the drug; none had to restart PHT. The optimal rates of reduction of CBZ remain uncertain. There was no evidence for a clinically or temporally distinct burst of "discontinuation seizures" in any group. Any marked increase in seizures always resolved on reintroduction of the discontinued drug.     

羟丙基甲基纤维素（HPMC）在盐酸洛美沙星片生产中的应用

目的：考查羟丙基甲基纤维素合剂对盐酸洛美沙星片溶出度的影响,选择出最佳粘合剂浓度。方法：实验选用5种浓度的HPMC制备盐酸洛美沙星片,用RC－2型药物溶出仪测定咄度,从中选出最佳粘合剂浓度。并采用两种处方、三种粘合剂制片,。进行溶出度及片面比较。结果：用5％HPMC作粘合剂不仅可改善片剂出度,而且片面明显优于加有吐温－80者。结论：羟丙基甲基纤维素可改善片剂溶出度,效果明显。     

互聚物复合形成对口腔粘膜粘附片释放的影响

通过测量ＨＰＭＣ和ＣａｒｂｏｐｏＤ１９７４Ｐ在不同ｐＨ值的缓冲液中的混合溶液浊度变化的方法证实了互聚物复合形成。复合的程度在酸性ｐＨ条件下高,当两者比例为１：１时最强,然后随着ｐＨ值的长吭而减弱。以非洛地平为模型药物,采用直接压片工艺制备了口腔粘膜粘附片。体外释放实验表明,互聚物复合形成对药物的释放有很大影响,能够有效控制药物释放。粘附片中加入不同酸碱度的物质可调节药物的释放速率。聚合物间的这种特     

Effects of chronic treatment with valproate on serotonin-1A receptor binding and function

Valproate is effective in treating bipolar disorder characterized by rapid cycling or acute mania, although the mechanism of action is unclear. In contrast to other treatments for depression, 21 days of treatment in rats with valproate (100, 200 or 400 mg/kg) did not significantly alter the hypothermia induced by 8-hydroxy-2-(di-n-propyl)aminotetralin (8-OH-DPAT), an agonist at serotonin-1A receptors. Treatment with valproate also had no effect on radioligand binding to serotonin-1A, serotonin-2 or -adrenergic receptors. Based on these animal studies in frontal cortex and hippocampus, the therapeutic benefit of valproate in mood disorders does not appear to involve adaptive changes in serotonin-1A, serotonin-2 or -adrenergic receptor number.