HPLC测定替卡西林钠及注射用替卡西林钠克拉维酸钾中的有关物质

目的 建立测定替卡西林钠及注射用替卡西林钠克拉维酸钾中有关物质的高效液相色谱梯度洗脱法。方法 采用HPLC梯度洗脱法,色谱柱为Waters XBridgeTM C18柱(4.6 mm×250mm,5μm);以0.01mol/L磷酸氢二铵溶液(pH7.0) 为流动相A,0.01mol/L磷酸氢二铵溶液(pH7.0)-甲醇（50:50）为流动相B,梯度洗脱;流速为1.0mL/min;检测波长为220nm;柱温为30℃。结果 与等度洗脱法比较,梯度洗脱法具有更强的分析杂质的能力,样品中各成分的分离度及检出灵敏度均满足有关物质测定要求。替卡西林杂质A与破坏条件下产生的降解杂质与主成分峰分离较好;替卡西林的最低检出限为4.8ng,克拉维酸的最低检出限为7.3ng;原料药与制剂样品中替卡西林杂质A均＜1.5%,最大单个杂质均＜2.0%,总杂质均＜4.0%。结论 本方法专属性好,灵敏度高,可用于替卡西林钠原料药和注射用替卡西林钠克拉维酸钾中有关物质的测定。     

人喉癌Hep-2细胞膜钾离子通道与RNA编辑酶1的相关性

目的研究人喉癌细胞系Hep-2细胞膜钾离子通道特性及其与RNA编辑酶1(RNA-dependent adenosinedeaminase1,ADAR1)的相关性.方法以Hep-2细胞为研究对象,采用穿孔膜片钳全细胞记录法研究钾离子通道特性,用逆转录聚合酶链反应检测四乙胺(tetraethylammonium,TEA)阻断钾离子通道前后Hep-2细胞ADAR1 mRNA的表达.结果 Hep-2细胞膜的静息膜电位为(-29.8±1.9)mV,在钳制电压-40 mV,阶跃电压在-80～ 80 mV,记录到一种跨膜电流,该跨膜电流具有电压依赖、外向整流特性,该电流在延迟25ms后最大激活,800 ms内不失活,可被阻断剂TEA阻断.Hep-2细胞钾离子通道被TEA阻断前后ADAR1mRNA相对表达量存在显著性差异.结论 Hep-2细胞膜上存在延迟整流钾离子通道,此钾离子通道可能和ADAR1 mRNA的表达密切相关.     

阿莫西林克拉维酸钾不同给药方法治疗慢性支气管炎急性发作的临床疗效对比研究

目的对比并探讨阿莫西林克拉维酸钾序贯疗法和静脉滴注2种不同给药方法治疗慢性支气管炎急性发作的临床疗效。方法将88例慢性支气管炎急性发作患者随机分为观察组和对照组各44例。观察组采用阿莫西林克拉维酸钾序贯疗法给药方案治疗,对照组采用阿莫西林克拉维酸钾静脉滴注给药方案治疗。对2组临床疗效、不良反应发生情况及平均住院时间进行比较。结果观察组临床总有效率为88.64%,对照组为86.36%,2组比较差异无统计学意义(P>0.05)。观察组不良反应发生率为4.55%,低于对照组的13.64%;观察组平均住院时间为(4.27±2.15)d,短于对照组的(11.12±2.43)d,差异均有统计学意义(P<0.05)。结论阿莫西林克拉维酸钾序贯疗法治疗慢性支气管炎急性发作,具有安全、有效、经济实用的优点,值得临床推广应用。     

妥卡尼对豚鼠心室肌细胞钙电流和钾电流的抑制作用

利用酶分散的成年豚鼠心室肌细胞和全细胞电压钳技术,研究了妥卡尼(tocainide)对心室肌细胞钙电流(I_ca)、延迟整流钾电流(I_k)和ATP敏感性钾电流(Ik,ATP)的作用。结果表明,妥卡尼对I_ca和I_k均显示浓度相关的抑制作用,妥卡尼50umol·L^-1对I_ca和I_k的抑制率分别为16%和3%。这可能是妥卡尼有效抑制室上性心动过速和缩短心肌动作电位平台期的重要机制。     

Stimulation of aldosterone production in vitro and its inhibition by spironolactone

Summary The synthesis of aldosterone was stimulated in vitro by ACTH, dibutyryl-cyclic AMP, potassium ions and angiotensin II. Aldosterone was determined by a method involving two thin layer chromatographies (TLC), a periodic acid oxidation step, and a final esterification with heptafluorobutyric anhydride to prepare the aldosterone--lactone-heptafluorobutyrate for gas chromatographic quantification with electron-capture detection. The method is described in detail.Spironolactone (6×10^–5–1×10^–4M) added to the incubation medium inhibited the synthesis of aldosterone in a dose-dependent manner, while the production of corticosterone was not affected.It is concluded that spironolactone inhibits the conversion of corticosterone to aldosterone.     

Activators of potassium channels enhance calcium influx into endothelial cells as a consequence of potassium currents

Summary Ca²⁺ influx into stimulated endothelial cells is attenuated by depolarization. We hypothesized that Ca²⁺ influx is driven by the membrane potential and may be enhanced by hyperpolarizing drugs like activators of K⁺ channels. Therefore we studied the effects of pinacidil, cromakalim, and cicletanine on membrane currents and on the intracellular free calcium concentration ([Ca²⁺]i) in cultured endothelial cells from porcine aorta. In patch-clamped cells, pinacidil (1 mol/l) and cromakalim (1 mol/l) elicited outward currents carried by K⁺ and significantly prolonged the Ca²⁺-dependent K⁺ currents induced by bradykinin and ATP. Peak currents in response to bradykinin were not affected. In cells loaded with the fluorescent Ca²⁺ indicator indo-1 and prestimulated with thimerosal, pinacidil (0.1–1 mol/l elicited long-lasting increases in [Ca²⁺)_i from 100 ± 10 to 550 ± 110 nmol/l. These effects were completely abolished in a medium containing 90 mmol/l K⁺. Similar results were obtained with cromakalim. Likewise, in cells stimulated with bradykinin, pinacidil raised [Ca²⁺]_i when applied during the decline of [Ca²⁺]_i after the initial peak. Cicletanine elicited K⁺ currents in resting and attenuated K⁺ currents in bradykinin-stimulated cells. It elevated [Ca²⁺]_i even in the absence of extracellular Ca²⁺ and in K⁺-rich medium. Hence, the effects of cicletanine cannot be explained by direct actions on K⁺ channels. However, our studies demonstrate that pinacidil and cromakalim elevate [Ca²⁺]_i secondary to their activation of K⁺ channels by inducing hyperpolarization and augmenting the driving force for potential-dependent Ca²⁺ influx. In this way, the two drugs may promote Ca²⁺-dependent formation of endothelium-derived relaxing factor. Send offprint requests to A. Lückhoff at the above address     

青霉素V钾片中水分和有关物质的相关性研究

目的 对青霉素V钾中的水分和有关物质进行相关性研究,以考察青霉素V钾片有关物质存在差异的原因.方法 采用《中国药典》2010年版中青霉素V的有关物质的测定方法测定制剂中总杂质含量,采用卡氏水分法测定制剂中水分,采用干燥失重法测定制剂减失重量.结果 水分和有关物质的总杂质含量成正相关,平均片重大时水分有增大的趋势.结论 有必要对青霉素V钾片的水分进行控制,限度可拟定为含水分不得过2.0％.     

Differential flow cytometric detection of intracellular cytokines in peripheral and peritoneal mononuclear cells of women with endometriosis

OBJECTIVE: The pathogenesis of endometriosis is related to functional changes in CD3+ and CD14+ cells observed both at the local and systemic level. Here we investigated whether, and if so, how the body compartment influences cytokine expression in stimulated peritoneal and peripheral CD3+ and CD14+ cells of women with endometriosis. STUDY DESIGN: Isolated peripheral blood (PB) and peritoneal fluid (PF) mononuclear cells from women with endometriosis were cultured under non-adherent conditions and stimulated with PMA and ionomycin for 6h to induce intracellular cytokine synthesis of TNF-alpha, IFN-gamma, and IL-8 by CD3+ cells or with LPS for 9h to produce TNF-alpha, IL-6, IL-10, MCP-1, and IL-8 by CD14+ cells. RESULTS: The percentages of positive CD3+ cells stained for TNF-alpha and IFN-gamma were significantly higher and those stained for IL-8 were significantly lower in PF compared with PB, this being independent of the stage of endometriosis. In contrast, the percentages of CD14+ cells producing TNF-alpha, IL-6, IL-10, MCP-1, and IL-8 were significantly higher in PB than PF of women with endometriosis. CONCLUSIONS: Monocytes/macrophages and lymphocytes derived from the peripheral and peritoneal compartments of women with endometriosis differentially respond to stimulated cytokine synthesis induction. However, it is difficult to state whether the observed phenomenon is more related to body compartment influence per se or to the presence of endometriosis.     

ICU应用微量泵中心静脉高浓度补钾有效性及安全性评价

目的探讨ICU-应用微量泵中心静脉高浓度补钾的有效性及安全性。方法回顾性分析ICU发生低钾血症78例患者的临床资料。随机分为常规组和高浓度组,每组各39例,补钾均在心电监护下进行。常规组钾浓度为40mmol／L,补钾速度为10～20mmol／h;高浓度组钾浓度为100～300mmol／L,补钾速度为加～200mmol／h,同时计算达到目标血钾浓度所需补钾量,监测两组血钾浓度、每小时尿量、达到目标血钾浓度所需时间及患者局部不良反应。结果两组患者治疗前均存在低钾血症,设定目标血钾浓度为4．0mmol／L,两组治疗前血钾浓度、所需补钾量比较差异无统计学意义,分别为（2．9±0．2）、（3．0±0．2）mmol／L和（85．2±8．7）、（92．3±7．6）mmol。常规组与高浓度组相比达到目标血钾浓度所需时间较长[（17.25±4．49）h比（5．67±0．75）h,P〈0．01]。结论在ICU严密监护下应用微量泵中心静脉高浓度补钾安全、有效．有一定的临床廊用价值。     

维生素C注射液与门冬氨酸钾镁注射液配伍稳定性考察

目的 考察维生素C注射液与门冬氨酸钾镁注射液在0.9％氯化钠注射液中配伍的稳定性.方法 考察常温下24 h内维生素C注射液与门冬氨酸钾镁注射液在0.9％氯化钠注射液中配伍后,其配伍液的外观、pH及药物的含量.结果与结论 维生素C注射液和门冬氨酸钾镁注射液在0.9％氯化钠注射液中配伍后,24 h内药物的含量、pH及外观均无明显变化.