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     

HPLC测定氨茶碱片中的无水茶碱

目的 采用HPLC法测定氨茶碱片中茶碱的含量.方法 采用Shim-pack VP-ODS C_(18)柱(150 mm×4.6 mm,5 μm),流动相为甲醇-0.05 mol·L~(-1)磷酸二氢钾溶液-三乙胺(25:75:0.2),流速1 mL·min~(-1),检测波长271 nm,柱温30 ℃.结果 无水茶碱7.935～79.35 mg·L~(1-)与峰面积的线性关系良好(r=0.9999,n=6),平均回收率为99.2%,RSD=0.5%(n=6).结论 该方法简便、准确、重复性好,可用于氨茶碱片的质量控制.     

Advances in the Management of Pediatric Asthma: A Review of Recent FDA Drug Approvals and Label Updates

Children have the highest prevalence of asthma of any age group. In the United States during 2001, there were 12.6 million physician and hospital outpatient visits for asthma treatment, of which almost 5 million involved children 18 years and younger. Therapeutic advances in pediatric asthma could improve patient outcomes and potentially reduce the burden on health care systems. Efforts to obtain efficacy and safety data in pediatric populations and develop pediatric formulations of asthma treatments have been encouraged by the FDA and clinicians. This article reviews the newest additions to asthma therapies approved for use in children, including an inhaled corticosteroid, some long-acting β₂-agonists, some leukotriene-receptor blockers, and a single-isomer, short-acting β₂-agonist.     

吸入性糖皮质激素联合茶碱对支气管哮喘患者的疗效

目的 探讨吸入性糖皮质激素(ICS)联合小剂量茶碱对未控制支气管哮喘的治疗效果.方法 筛选郑州大学人民医院门诊2011年1至12月门诊未控制支气管哮喘患者280例,用简单随机化分组平均分为试验组和对照组.试验组吸入布地奈德,200μg/吸,2吸/d,联合口服氨茶碱片0.1g,3次/d;对照组吸入布地奈德福莫特罗粉吸入剂(160 μg/4.5 μg)/吸,2吸/d;疗程均为6个月.比较两组患者治疗前后第1秒用力呼气容量占预计值百分比(FEV1％预计值)、外周静脉血白细胞介素(IL)-4、IL-5、IgE值的变化.结果 对照组(134例)及试验组(132例)患者平均年龄分别为(46±13)、(47±12)岁,男女构成比为1∶1.两组治疗前和治疗6个月后的FEV1％预计值、IL-4、IL-5、IgE值:试验组分别为68％±6％和76％±6％,(14.5±4.4)和(7.2±2.6) ng/L,(27.4±6.2)和(24.2±5.9)ng/L,(771±130)×103和(592±104) ×103 U/L,对照组分别为66％±8％和77％±6％,(13.7±4.3)和(7.7±4.0)ng/L,(26.9±5.8)和(24.6±4.8)ng/L,(752±154)×103和(604±122) ×103 U/L;两组治疗前比较差异均无统计学意义(均P＞0.05),治疗后两组组内比较差异均有统计学意义(均P＜0.05),组间比较差异均无统计学意义(均P＞0.05).结论 ICS联合茶碱,在改善哮喘患者肺功能、控制气道炎症方面与ICS联合长效β2受体激动剂有相似的疗效.     

福莫特罗干粉联合茶碱缓释片治疗中度支气管哮喘58例的疗效观察

目的：探讨小剂量的福莫特罗干粉联合茶碱缓释片治疗中度支气管哮喘的疗效、安全性以及药物经济学。方法：选取58例中度支气管哮喘患者,按照随机抽样的方法将其分成A、B两组,每组29例。A组的治疗方式为：福莫特罗干粉吸入（80、4.5μg/吸）早、晚各1次,茶碱缓释片0.2 g/次、1次/12 h口服;B组为：单纯福莫特罗干粉吸入（160、4.5μg/吸）早、晚各1次;两组疗程均为12周。观察两组患者的临床症状、肺功能、药物反应情况。结果：两组治疗后临床基本控制率、哮喘控制测试评分、第1秒用力呼气容积（FEV1）和FEV1占预计值的百分比均优于治疗前（P<0.01）,而两组治疗后比较差异、不良反应产生率的差异均无统计学意义（P>0.05）。在费用上, A组的治疗人均药物治疗费用比B组低（P<0.05）。结论：福莫特罗干粉吸入剂联合茶碱缓释片治疗中度支气管哮喘疗效好,不良反应少,且费用相对较低。     

Development of Enteric-coated Timed-release Matrix Tablets for Colon Targeting

A new oral drug delivery system for colon targeting has been developed based on enteric-coated matrix tablets which suitably exploits both pH-sensitive and time-dependent functions. Matrix-tablets were prepared by direct compression of mixtures of hydroxyethylcellulose (HEC), a hydrophilic swellable polymer, with the inert insoluble ethylcellulose (EC) or micro-crystalline cellulose (MCC) polymers, in which theophylline, selected as model drug, was dispersed. Eudragit S100, a methacrylic acid copolymer soluble at pH 7, was used as pH-sensitive coating polymer. The influence of varying the cellulose-derivative combinations and their relative ratios as well as the level of the coating polymer was investigated. Surface morphology of the tablets was monitored by SEM analysis before and after the release test. The results of release studies, performed according to the USP basket method using a sequence of dissolution media simulating the gastrointestinal physiological pH variation, indicated that the Eudragit S100 enteric-coated matrix tablets were successful in achieving gastric resistance and timed-release of the drug, assuring an adequate lag time for the intended colonic targeting, followed by a controlled-release phase. The enteric-coating level emerged as the critical factor in determining the duration of the lag-phase, whereas the release rate mainly depended on the matrix composition. Formulations with higher HEC content showed a faster drug release rate than those with greater content in inert polymer and the MCC–HEC combinations were more effective than the corresponding EC–HEC ones. The best results were given by the 27% coated 1:0.3:0.7 (w/w) drug/MCC/HEC tablets, which, after a 260 min lag time, regularly released the drug, achieving about 90% of release after 10 h.     

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.     

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。     

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.