Synthetic Zeolites as Controlled‐Release Delivery Systems for Anti‐Inflammatory Drugs

Scientists have always been trying to use artificial zeolites to make modified‐release drug delivery systems in the gastrointestinal tract. An ideal carrier should have the capability to release the drug in the intestine, which is the main area of absorption. Zeolites are mineral aluminosilicate compounds with regular structure and huge porosity, which are available in natural and artificial forms. In this study, soaking, filtration and solvent evaporation methods were used to load the drugs after activation of the zeolites. Weight measurement, spectroscopy FTIR, thermogravimetry and scanning electronic microscope were used to determine drug loading on the systems. Finally, consideration of drug release was made in a simulated gastric fluid and a simulated intestinal fluid for all matrixes (zeolites containing drugs) and drugs without zeolites. Diclofenac sodium (D) and piroxicam (P) were used as the drug models, and zeolites X and Y as the carriers. Drug loading percentage showed that over 90% of drugs were loaded on zeolites. Dissolution tests in stomach pH environment showed that the control samples (drug without zeolite) released considerable amount of drugs (about 90%) within first 15 min when it was about 10–20% for the matrixes. These results are favorable as NSAIDs irritate the stomach wall and it is ideal not to release much drugs in the stomach. Furthermore, release rate of drugs from matrixes has shown slower rate in comparison with control samples in intestine pH environment.     

臭氧联合玻璃酸钠关节腔注射治疗膝骨关节炎的疗效分析

目的：探讨臭氧联合玻璃酸钠关节腔注射治疗膝骨关节炎的临床疗效。方法：将124例膝骨关节炎患者随机分为治疗组和对照组,治疗组72例,对照组52例,治疗组采用臭氧联合玻璃酸钠关节腔注射治疗,对照组采用单纯玻璃酸钠关节腔注射治疗。记录治疗前、首次治疗后1周、末次治疗后1周及治疗后6个月时的VAS评分、Lysholm膝关节评分及有效率。结果：经治疗后,2组患者VAS疼痛评分均降低,Lysholm膝关节评分均提高（P<0.05）。组间比较,治疗组疼痛较对照组显著减轻,Lysholm膝关节评分及有效率较对照组显著提高。结论：臭氧联合玻璃酸钠关节腔注射是治疗膝骨关节炎的有效方法,且疗效优于单纯玻璃酸钠关节腔注射疗法。     

头孢西丁钠致过敏性休克一例

目的 1例73岁女性患者因上呼吸道感染合并慢性阻塞性肺病,入院给予头孢西丁2.0 g溶于0.9%氯化钠注射液250 mL中静脉滴注。输液约5 min时患者出现呼吸、心跳骤停,意识不清。立即停药,行心肺复苏和药物对症治疗,1.5 h后好转。     

Leptin and post-prandial satiety: acute central leptin more potently reduces meal frequency than meal size in the rat

Rationale Many attempts to understand ingestion have sought to clarify the control of meals. Little is known about the effects of the anorexogenic hormone leptin on meal patterning.Objective The present study sought to perform a dose–response analysis of the effects of acute central leptin administration on meal patterning using a validated, objective meal definition and to compare these results to those obtained with a previously used, subjective meal definition.Methods To validate the objective meal definition pharmacologically, the microstructural effects of the well-studied compound fenfluramine (SC 0, 1, 2, 4 mg/kg) on spontaneous nocturnal intake were determined in mature, non-deprived male Wistar rats (n=8) using a full Latin square design. The effects of intracerebroventricular leptin administration (0, 0.3, 1, 3, 6.25 g; n=10) were also examined, and perceived meal patterns obtained from the objective and subjective definitions were compared.Results Fenfluramine reduced meal size and eating rate at doses that did not reduce meal frequency or duration. In contrast, comparably anorectic doses of leptin had potent post-meal satiety-like effects, reducing meal frequency and prolonging the intermeal interval without reducing average meal size, a finding opposite to that suggested by the previously used subjective meal definition. Unlike comparably and more anorectic doses of fenfluramine, leptin non-specifically reduced both prandial and non-prandial drinking.Conclusions Acute increases in central leptin levels may potently augment post-prandial satiety and influence body-fluid homeostasis. The results reveal unappreciated central modes of action for the ob protein which qualitatively differ from the intra-meal satiating-like effects of fenfluramine.     

磷酸肌酸钠对缺血缺氧新生儿血浆脑钠肽及心肌营养素-1的影响

目的观察磷酸肌酸钠对缺血缺氧新生儿血浆脑钠肽（BNP）及心肌营养素-1（CT-1）的影响。方法 86例缺血缺氧新生患儿随机分为治疗组和对照组,每组43例。两组采用常规治疗外,治疗组加用磷酸肌酸钠治疗,分别于出生后24 h和治疗10 d后抽取患儿静脉血,评价临床疗效,采用双抗体夹心酶联免疫吸附法（ELISA）测定检测患儿血浆中BNP以及CT-1。结果经磷酸肌酸钠给药治疗后,其临床有效率达87.6%,与对照组（62.8%）相比,差异有统计学意义（P〈0.05）;ELISA法检测结果显示,治疗前,治疗组与对照组血浆BNP、CT-1的含量差异无统计学意义;经10 d治疗后,与治疗前相比治疗组患儿血浆BNP、CT-1含量显著下降（P〈0.05）;且治疗后,对照组与治疗组相比,血浆BNP、CT-1的含量均有显著性差异（P〈0.05）。结论磷酸肌酸钠治疗缺血缺氧新生儿的作用靶点可能与降低患儿血浆中BNP以及CT-1有关。     

木糖醇注射液与临床常用五种抗菌药物的配伍稳定性考察

目的模拟临床常用静滴浓度,研究阿奇霉素、氨苄青霉素钠、羟氨苄青霉素钠、头孢曲松钠、加替沙星五种常用抗菌药物与木糖醇注射液的配伍稳定性。方法采用紫外分光光度法测定8 h内配伍液中五种药物的含量变化,同时观察室温(25℃)下的外观及pH变化。结果阿奇霉素、加替沙星、头孢曲松钠和木糖醇注射液配伍后在室温下8 h内外观、含量、pH值没有明显变化,保持稳定状态。但氨苄青霉素钠、羟氨苄青霉素钠和木糖醇注射液配伍后在室温下2 h后含量明显下降。结论在上述条件下,木糖醇注射液可与阿奇霉素、加替沙星和头孢曲松钠配伍应用。但与氨苄青霉素钠、羟氨苄青霉素钠配伍不稳定。     

复方地塞米松鼻用凝胶的制备与质量控制

目的:制备复方地塞米松鼻用凝胶,并建立质量控制方法.方法:以卡波姆934作为凝胶基质,运用高效液相色谱同时测定盐酸麻黄碱、呋喃西林、地塞米松磷酸钠的含量,并进行稳定性考察.结果:该制剂为淡黄色澄明黏稠凝胶,盐酸麻黄碱、呋喃西林、地塞米松磷酸钠平均回收率分别为99.69%,98.57%,99.00%,RSD分别为1.19%,2.68%,2.30%.加速实验稳定.结论:该制剂制备工艺简便,稳定性良好,质量控制方法快速、准确.     

硝苯地平联合依诺肝素钠对重度子痫前期术后患者妊娠期高血压的影响

目的探讨联合应用硝苯地平与依诺肝素钠治疗对重度子痫前期术后患者血压、凝血功能及对血清D-二聚体的影响。方法选取2015年6月-2017年10月期间行宫剖产术进行分娩的203例重度子痫前期孕妇,依据随机对照表分为对照组(101例)和观察组(102例)。对照组采用硝苯地平治疗,观察组采用硝苯地平联合依诺肝素钠治疗,比较2组患者采用不同方式治疗后血压、凝血功能的变化情况,以及对血清D-二聚体的影响,并统计不良妊娠结局。结果观察组总体有效率为95.10%,显著高于对照组(87.13%),具有统计学差异(P<0.05)。观察组治疗后FIB、D-二聚体、PAI-1、HB、PLT显著降低,而PT、APTT、t-PA均显著增加,各指标水平显著优于对照组(P<0.05)。治疗后2组患者的收缩压、舒张压均显著降低,且治疗后观察组各血压水平显著低于对照组(P<0.05)。治疗后2组患者的血清vWF、PAPP-A水平均显著降低,其中观察组各水平显著低于对照组(P<0.05)。观察组平均妊娠时间、胎儿体质量均显著优于对照组,24 h蛋白尿水平显著低于对照组,主要不良妊娠结局为胎儿窘迫、早产、产后出血、新生儿窒息,其中观察组不良妊娠发生率(9.80%)显著低于对照组(18.81%),具有统计学差异(P<0.05)。结论硝苯地平联合依诺肝素钠对重度子痫前期治疗效果显著,可有效降低患者术后血压,改善凝血功能,调节血清D-二聚体水平,从而降低不良妊娠结局发生率。     

二巯丙磺钠对百草枯急性中毒大鼠肺组织基质金属蛋白酶-9 mRNA及其金属蛋白酶组织抑制剂-1 mRNA表达的影响

目的探讨二巯丙磺钠(DMPS)救治百草枯(PQ)急性中毒大鼠作用机制。方法120只雄性SD大鼠随机分为正常对照组,DMPS(200mg.kg-1,ip)对照组,PQ急性中毒(20mg.kg-1,ip)1,3,7,14和28d组以及DMPS干预(先给DMPS,15min后再给PQ)1,3,7,14和28d组。应用RT-PCR技术检测PQ急性中毒组大鼠及DMPS干预组大鼠肺组织中基质金属蛋白酶9(MMP-9)mRNA和金属蛋白酶1组织抑制剂(TIMP-1)mRNA的表达。结果PQ急性中毒组早期肺组织毛细血管扩张充血,炎症细胞浸润,后期出现较大范围慢性炎症病灶,纤维组织增生。与正常对照组比,MMP-9mRNA明显升高,分别为1.13±0.06,1.32±0.04和1.10±0.06,0.85±0.06和0.75±0.05,TIMP-1mRNA明显升高,分别为1.14±0.08,1.29±0.05,1.61±0.09,1.83±0.13和1.73±0.08;7,14和28d MMP-9mRNA/TIMP-1mRNA比值明显低于正常对照,分别为0.68±0.03,0.46±0.04和0.43±0.06;DMPS干预后,MMP-9mRNA1,3和7d和TIMP-1mRNA1,3,7,14和24d表达低于PQ中毒组,MMP-9mRNA分别为1.05±0.03,1.17±0.05和0.93±0.09;TIMP-1mRNA分别为10.0±0.07,1.15±0.09,1.09±0.06,1.16±0.08和1.23±0.09;MMP-9mRNA/TIMP-1mRNA比值略低于DMPS对照组,但高于PQ中毒组,分别为0.85±0.05,0.63±0.04和0.58±0.02(均P<0.05)。结论DMPS可能通过下调大鼠肺组织MMP-9mRNA和TIMP-1mRNA表达,上调肺组织MMP-9mRNA/TIMP-1mRNA比值发挥救治PQ中毒作用。     

磷霉素钠与加替沙星氯化钠注射液配伍的稳定性考察

目的考察磷霉素钠与加替沙星氯化钠注射液配伍变化,为临床合理用药提供参考依据。方法在室温条件下观察及测定配伍液8h内的pH及外观变化,并用紫外光谱法监测配伍液中加替沙星的图谱和含量变化。结果两药配伍后,在8h内配伍液的pH及外观无明显变化,而配伍液中加替沙星的紫外图谱和含量均有明显变化。结论磷霉素钠不宜和加替沙星氯化钠注射液配伍使用。