Compressional Characterization of Two Dextrose-Based Directly Compressible Excipients Using an Instrumented Tablet Press

The main objective of this work was to evaluate the compaction behavior and record the work and the force involved in the compaction of blends and granules of two dextrose-based directly compressed excipients using a single-punch instrumented tablet press. The second objective was to identify the predominant form of deformation for the two different directly compressible excipients. Anhydrous theophylline (10% w/w) was used as a drug model, Emdex and/or Maltrin M 510 (89.5% w/w) were used as diluent, and magnesium stearate (0.5% w/w) was used as lubricant. All formulations were compressed at four different compressional forces and at a target tablet weight of 450 mg ± 5%. Results show that compacts prepared from Emdex using the direct compression method produced the lowest elastic work and die wall friction, and the best degree of lubrication. Wet granulation for Maltrin M 510 decreased elastic work, frictional work, and ejection force, and enhanced both net work and degree of lubrication. In general, wet granulation for both Emdex and Maltrin M 510 decreased the crushing strength of the tablets and enhanced the degree of lubrication, compared to direct compression formulations. All formulations showed similar shape pattern for plastic deformation, suggesting that the predominant mechanism of deformation is plastic deformation type a Heckel plots.     

慢性阻塞性肺炎患者内科治疗方法的临床疗效探究

目的：探究内科治疗方法治疗阻塞性肺炎患者的临床疗效。方法选取我院2014年1月～2015年1月收治的64例患者，随机分成两组，观察组患者用多索茶碱治疗，对照组患者用氨茶碱治疗，均治疗一周后，比较两组患者的有效率，得出结论。结果观察组患者的有效率为（30/32）93.8%，对照组的有效率为（21/32）65.6%，两组患者的差异具有统计学意义（P＜0.05）。结论多索茶碱治疗慢性阻塞性肺炎的临床疗效优于氨茶碱，有明显的临床效果，能够有效降低不良反应的发生，提高治愈率。     

Inhibitory effects of hypoxia and adenosine on N-methyl-d-aspartate-induced pial arteriolar dilation in piglets

Our previous studies have indicated that oxygen radicals, produced during reoxygenation following short-term arterial hypoxia, lead to sustained suppression of cerebral arteriolar responses to N-methyl-

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-aspartate (NMDA). However, whether arteriolar dilator responses to NMDA are reduced during arterial hypoxia has never been examined. In this study, we determined whether hypoxia or hypoxia-related metabolites such as adenosine or nitric oxide (NO) will reduce NMDA-induced arteriolar dilation. We have also determined the location of NMDA receptor- and brain nitric oxide synthase (bNOS)-positive neurons in the cerebral cortex. In anesthetized piglets, pial arteriolar diameters were determined using intravital microscopy. Baseline arteriolar diameters were 100 μm. Topical application of NMDA at concentrations of 10⁻⁵, 5×10⁻⁵ and 10⁻⁴ M resulted in dose-dependent vasodilation (9±2, 18±2 and 29±2% above baseline, respectively, n=21). Administration of theophylline (20 mg/kg, i.v.) had no effect on NMDA-dependent vasodilation, but it did block dilation to hypoxia (inhalation of 8.5% O₂). In theophylline-treated animals, NMDA responses were completely abolished during hypoxia (28±2 vs. 2±1%, respectively to 10⁻⁴ M, n=7) while sodium nitroprusside (SNP, 10⁻⁴ M) still dilated pial arterioles normally. NMDA-induced vasodilation was not modified after application and removal of adenosine (10⁻⁴ M; n=5) or SNP (10⁻⁵ M; n=4), or when SNP (10⁻⁷ M) was coapplied with NMDA (n=6). Conversely, coapplication of adenosine (10⁻⁶ M) attenuated NMDA responses (31±5 vs. 20±3%, n=7). We also found that NMDA receptor- and bNOS-containing neurons were located predominantly in layers II/III of the cortex. Proximity of these neurons to the cortical surface is consistent with diffusion of NO to pial arterioles as the mechanism of dilation to NMDA. We conclude that NMDA-induced cerebral arteriolar dilation is inhibited by hypoxia alone and by exogenous adenosine, but not by NO.     

Modulation of thyroidal radioiodine uptake by theophylline

Diagnostic and therapeutic use of radioiodine in the management of thyroid disorders depends on the ability of thyroid cells to concentrate radioiodine, a process regulated by thyrotropin and dependent on the intracellular increase in cAMP. We tested the ability of theophylline, a drug known to increase intracellular cAMP via inhibition of phosphodiesterase, to modulate the thyroidal radioiodine uptake in FRTL-5 cells, in mice and in humans. In FRTL-5 cells, theophylline increased the uptake of radioactive iodine and intracellular cAMP only at low concentrations (1 microM). In mice, theophylline increased slightly the radioiodine uptake, although this increase varied from 1.5- to 6.6-fold. In humans, theophylline decreased slightly the radioiodine uptake, a decrease that became more pronounced with time after radioiodine administration. These studies suggest that theophylline modulates the radioiodine uptake in a dose-dependent fashion, although the modulation is mild and probably not applicable to the clinical setting.     

茶碱缓释片联合噻托溴铵对稳定期COPD患者夜间睡眠低氧的临床疗效研究

目的 探讨噻托溴铵联合茶碱缓释片对稳定期COPD患者夜间睡眠低氧的疗效.方法 随机选择2015年3月至2016年3月本院收治的慢性阻塞性肺疾病睡眠低氧患者82例作为本次研究对象,将其平均分为对照组41例和观察组41例.对照组噻托溴铵治疗,观察组噻托溴铵联合茶碱缓释片治疗,观察比较两组夜间睡眠血氧饱和度、血气分析及肺功能指标.结果 观察组治疗后夜间睡眠血氧饱和度与治疗前比较,差异具有统计学意义(均P＜ 0.05);治疗后,观察组夜间睡眠血氧饱和度与对照组比较,差异具有统计学意义(均P＜ 0.05).观察组治疗后血气分析与治疗前比较,差异具有统计学意义(P＜ 0.05)治疗后,观察组和对照组血气分析比较,差异具有统计学意义(均P＜ 0.05).观察组治疗后肺功能与治疗前比较,差异具有统计学意义(均P＜ 0.05);治疗后,观察组肺功能与对照组比较,差异具有统计学意义(均P＜ 0.05).结论 噻托溴铵联合茶碱缓释片可进一步改善稳定期COPD患者的夜间睡眠低氧、血气分析和肺功能,且安全性高.     

286例血清茶碱浓度监测结果分析

目的：分析本院2006年8月～2008年8月间286例血清茶碱浓度监测结果。方法：利用荧光偏振免疫法测定血清茶碱浓度。结果：大部分患者血药浓度处于5～15μg·ml。范围内,且随着患者年龄的增加,血药浓度值增大;而血药浓度值越大,不良反应发生率越高。结论：应根据患者基本情况,个体化使用茶碱类药物,并监测血药浓度,使茶碱类药物得到更安全、合理、有效的应用。     

RP-HPLC法同时测定人血浆中茶碱和多索茶碱的浓度

目的:建立以反相高效液相色谱法同时测定人血浆中茶碱和多索茶碱浓度的方法。方法:色谱柱为XterraRP18,流动相为甲醇-水(35:65),流速为1.0mL·min-1,检测波长为269.9nm,柱温为35℃,内标为非那西丁。结果:茶碱和多索茶碱浓度分别在1.563～50μg·mL-1(r=0.9995)、0.3125～10μg·mL-1(r=0.9999)范围内线性关系良好;茶碱、多索茶碱提取回收率分别为32.53%～35.08%、31.88%～34.55%,方法回收率分别为92.82%～109.41%、90.68%～102.72%,日内、日间RSD均<15%。结论:本方法快速、灵敏、准确,可用于同时测定人血浆中茶碱和多索茶碱的浓度。关键词茶碱;多索茶碱;反相高效液相色谱法;血药浓度监测     

The quinolone,flumequine, has no effect on theophylline pharmacokinetics

The kinetics of a single i. v. dose of theophylline given either alone or with flumequine was studied in eight healthy volunteers. No statistically significant differences were observed in the pharmacokinetic parameters of theophylline (volume of distribution, elimination half-life, AUC, plasma clearance) following the two treatments.Pretreatment for 5 days with oral flumequine (400 mg, three times daily) had no significant effect on the disposition of a single i. v. dose of theophylline in healthy volunteers.     

关于药物溶出度自身对照法应用的探讨

目的通过实验．探讨自身对照法在药物溶出度测定中的实际应用价值。方法分别采用自身对照法和对照品法两种方法计算同一药物不同剂型的溶出度值。结果自身对照法与对照品法对药物溶出度值的计算没有煤显著差异。结论自身对照法在药物溶出度的一般检验中有较大的应用价值。     

多索茶碱及其片剂的高效液相色谱分析

多索茶碱及其片剂的高效液相色谱分析刘春胜，何秀峰，王云萍，谷士杰，周同惠（中国医学科学院、中国协和医科大学药物研究所，北京１０００５０）多索茶碱（ｄｏｘｏｆｙｌｌｉｎｅ）是用于治疗支气管哮喘合并支气管痉挛的慢性阻塞性肺部疾病的新一代黄嘌吟衍生物，其药...