聚苯乙烯磺酸钠树脂中的残留单体苯乙烯的GC-MS法测定

建立了顶空GC-MS法测定聚苯乙烯磺酸钠树脂中苯乙烯单体的含量.以苯乙烯-d8为内标,采用石英毛细管色谱柱,以选择离子监测法定量.苯乙烯在0.5～15μg/ml浓度范围内线性关系良好(r=0.999 5),检测限为1 ng/g(1 ppb).     

Sodium Zirconium Cyclosilicate (ZS‐9): A Novel Agent for the Treatment of Hyperkalemia

Hyperkalemia is a potentially life‐threatening electrolyte abnormality that may be caused by select medications, underlying organ dysfunction, or alterations in potassium homeostasis. Treatment for this condition has remained largely unchanged since the release of sodium polystyrene sulfonate (SPS) in 1958. Despite its widespread use, the safety and efficacy of SPS remains controversial. Two novel potassium‐binding resins have emerged in recent years. Patiromer was the first of these to receive U.S. Food and Drug Administration approval for the treatment of hyperkalemia in October 2015. A second potassium‐binding resin, a zirconium cyclosilicate currently known as ZS‐9, may provide yet another alternative to the archetypal treatment with SPS. ZS‐9 is an orally administered nonabsorbed inorganic compound that selectively binds potassium ions in vivo. Two phase III multicenter, randomized, placebo‐controlled, double‐blind trials have evaluated ZS‐9 for the treatment of acute hyperkalemia. In this review, we discuss the pharmacology, clinical efficacy, safety, and potential place in therapy of ZS‐9 for the enhanced elimination of potassium in the setting of hyperkalemia.     

降血钾树脂的临床应用

降血钾树脂适用于各种高血钾增高症及肾功能衰竭引起的氮质血症。根据大量国内外资料表明,其作用时间持久、安全、副作用轻而少,具有较好的应用前景,特别适用于基层广大无透析设备的医疗单位。     

Development and Characterization of Bioadhesive Vaginal Films of Sodium Polystyrene Sulfonate (PSS), a Novel Contraceptive Antimicrobial Agent

No HeadingPurpose. Polystyrene sulfonate (PSS) is a novel noncytotoxic antimicrobial contraceptive agent. A gel formulation of PSS was found safe for vaginal administration in phase I clinical trials. The purpose of the current study was to develop and evaluate novel bioadhesive vaginal film formulations of PSS.Methods. PSS films were prepared by solvent evaporation and optimized for various physical, mechanical, and aesthetic properties. Further, films were evaluated for various biological activities and safety.Results. Vaginal films containing 300 mg PSS per unit have been developed, using generally regarded as safe (GRAS) listed excipients. The films are colorless, transparent, thin, soft, and tough, dissolve rapidly in physiologic fluid to form a smooth, viscous and bioadhesive solution that could be retained in the vagina for prolonged intervals. Sperm function inhibition (hyaluronidase and cervical mucus penetration) and antimicrobial activities against human immunodeficiency virus (HIV) and herpes simplex virus (HSV) by PSS films were found comparable to PSS. Also, films did not inhibit normal vaginal microflora (Lactobacillus) and were noncytotoxic as indicated by negligible sperm immobilization and cytotoxicity to host cell assays.Conclusions. Rapidly dissolving bioadhesive vaginal film formulation of PSS with desired physical, mechanical, aesthetic, and biological properties is a suitable candidate vaginal microbicide for prevention of sexually transmitted disease (STDs) and is ready for toxicological and clinical evaluation.     

高效液相色谱法测定注射用卡络磺纳中卡络磺纳的含量

目的:建立以高效液相色谱法测定注射用卡络磺钠含量的方法。方法:色谱柱为C18,流动相为0.12%磷酸二氢铵缓冲液-无水乙醇(925∶75),流速为0.8ml/min,检测波长为363nm,进样量为10μl,柱温为25℃。结果:卡络磺钠检测浓度在0.08865～0.4432mg/ml范围内线性关系良好(r=0.9999,n=5),平均回收率为99.89%(RSD=1.53%,n=9)。结论:本方法简便、快捷、准确、精密度高,可用于注射用卡络磺钠的质量控制。     

卡络磺钠注射液含量测定方法研究

目的用高效液相色谱（HPLC）法测定卡络磺钠注射液的含量。方法采用C18柱，流动相为醋酸及醋酸钠缓）中液（取醋酸钠10．2g，加冰醋酸40mL，再加水稀释至500mL）-甲醇（90：10），检测波长为363nm。结果方法平均回收率及RSD分别为99.82％和0.49％（n=6）。结论HPLC法简便、准确，适用于该产品的质量分析。     

注射用头孢唑林钠与丹皮酚磺酸钠注射液配伍稳定性研究

目的：观察注射用头孢唑林钠与丹皮酚磺酸钠注射液在0.9%氯化钠注射液中的配伍稳定性。方法模拟临床使用条件,用高效液相色谱法测定头孢唑林钠与丹皮酚磺酸钠配伍后6 h内的相对百分含量,并观察其外观、不溶性微粒数及pH变化。结果头孢唑林钠与丹皮酚磺酸钠配伍后,在室温下放置6 h,配伍液的外观、不溶性微粒数、pH及含量均无明显变化。结论注射用头孢唑林钠与丹皮酚磺酸钠注射液在0.9%氯化钠注射液中配伍后,室温下6 h内可使用。     

卡络磺钠氯化钠注射液的细菌内毒素检查法的建立

目的建立卡络磺钠氯化钠注射液的细菌内毒素检查的方法。方法按《中国药典》2000年版(二部)附录收载的细菌内毒素检查方法及指导原则进行实验。结果将卡络磺钠氯化钠注射液经2倍稀释可消除干扰因素,用标示灵敏度为0.25EU.mL-1的鲎试剂检测细菌内毒素是有效的。结论可以用细菌内毒素检查法代替家兔法控制卡络磺钠氯化钠注射液的质量。     

毛细管气相色谱法测定阿仑膦酸钠原料药中甲烷磺酸乙酯的残留量

目的:建立测定阿仑膦酸钠原料药中甲烷磺酸乙酯残留量的方法。方法:采用毛细管气相色谱法。色谱柱为HP-5毛细管色谱柱,载气为氮气,柱温为100℃保持8 min,流速为1.0 ml/min,进样量为1.0μl,分流比为10∶1,进样口温度为220℃,检测器为氢火焰离子化检测器,检测器温度为300℃。结果:甲烷磺酸乙酯检测质量浓度在3.92²7.44μg/ml范围内与峰面积积分值呈良好的线性关系(r=0.999 7);精密度、稳定性、重复性试验的RSD≤2.30%;平均回收率为97.94%,RSD=1.48%(n=9)。3批样品中均未检出甲烷磺酸乙酯。结论:该方法简便、灵敏、可靠,可用于阿仑膦酸钠原料药中甲烷磺酸乙酯残留量的测定。     

卡络磺钠注射液与注射用加替沙星的配伍稳定性考察

目的:考察卡络磺钠注射液与注射用加替沙星在0.9%氯化钠注射液中的配伍稳定性。方法:采用反相高效液相色谱法-二极管阵列检测器同时测定卡络磺钠注射液与注射用加替沙星在0.9%氯化钠注射液中配伍后,分别在25、37℃放置12h内各时间段的含量,并测定pH值,观察配伍液的外观变化。结果:在25、37℃下、12h内,配伍液外观、pH值及含量均无明显变化。结论:在25、37℃下,卡络磺钠注射液与注射用加替沙星在0.9%氯化钠注射液中在12h内可配伍使用。     

卡络磺钠片的处方工艺研究

目的优选卡络磺钠片的处方工艺。方法以单因素试验筛选填充剂、黏合剂和崩解剂,正交试验优化主要辅料用量,湿法制粒制备卡络磺钠片。结果优化后的处方为每片含卡络磺钠10 mg、淀粉20 mg、乳糖20 mg、微晶纤维素60 mg、羟丙甲纤维素5 mg、交联聚维酮4 mg、硬脂酸镁1 mg。优化后的工艺为,将淀粉于100℃干燥成含水量5%～8%的干淀粉,与卡络磺钠等量递加混合,粉碎,过筛;再与乳糖、微晶纤维素、羟丙甲纤维素、内加交联聚维酮混合,过筛;加乙醇适量,16目筛制粒2次,湿颗粒60℃左右干燥,14目筛整粒,外加交联聚维酮和硬脂酸镁,混合,压片。结论本处方工艺制备的卡络磺钠片,质量检查符合要求,溶出度较市售卡络磺钠片高,达到了设计要求。     

LCMS-QTOF鉴定卡络磺钠原料药的有关物质

目的 检测卡络磺钠原料药中有关物质,并进行结构鉴定,为工艺优化和质量控制提供参考。方法 采用Shim-pack Scepter C₁₈(4.6 mm×250 mm,5 µm)色谱柱,以50 mmol·L^–1乙酸铵水溶液为流动相A、乙腈为流动相B对卡络磺钠强制降解溶液中的有关物质进行分离。采用四极杆飞行时间高分辨质谱在m/z 100~800内进行正负离子扫描,数据依赖性采集获取二级质谱图。结合有关物质精确质量数、质谱裂解规律及卡络磺钠合成工艺推测其可能的结构。结果 卡络磺钠原料药经强制降解破坏得到8个主要的杂质,2种为已报道杂质,6种为本研究首次报道。强制降解试验表明卡络磺钠对高温和氧化相对较为稳定,光照、强酸和强碱条件对卡络磺钠影响较大。卡络磺钠原料药中检出杂质5,6和8,高温破坏的主要降解产物是杂质8。结论 本研究建立的液相色谱-四极杆飞行时间质谱联用法具有良好的分离能力,可有效地鉴定卡络磺钠原料药中有关物质,为其生产工艺和质量控制提供了参考。     

An evaluation of sodium zirconium cyclosilicate as a treatment option for hyperkalemia

ABSTRACT

Introduction

Hyperkalemia, defined as serum potassium level > 5.0 mEq/l, is associated with serious cardiac dysrhythmias, sudden death and increased mortality risk. It is common in patients with chronic kidney disease (CKD), diabetes (DM) and heart failure (HF), particularly in those treated with the renin-angiotensin-aldosterone system (RAAS) inhibitors or potassium-sparing diuretics. Although these drugs have documented renal and cardiac protective benefits, frequent hyperkalemia associated with their use often dictates administration of suboptimal doses or their discontinuation altogether. Treatment for chronic hyperkalemia in these settings has been challenging; however, the recent introduction of two new potassium-binding resins has revolutionized our approach to treating hyperkalemia.     

鱼腥草素钠类化合物的构效关系研究现状

综述国内外鱼腥草素钠类化合物构效关系的研究进展,探讨该类化合物碳链的长度、饱和度及取代对其抗菌、免疫调节、抗高血压、抗癌等药理活性的影响。     

RP-HPLC变波长同时测定复方谷氨酰胺颗粒中L-谷氨酰胺与薁磺酸钠的含量

目的：建立同时测定复方谷氨酰胺颗粒中L-谷氨酰胺和薁磺酸钠含量的方法。方法：采用Eclipse XDB-C18色谱柱（4.6 mm ×150 mm,5μm ）,以乙腈（A）-0.08％辛烷磺酸钠溶液（用磷酸调pH至3.0）为流动相,梯度洗脱（0～5 min,90％A;5～10 min,90％A→72％A;10～18 min,72％A）,检测波长为210 nm （0～10 min）、290 nm （10～18 min）。结果：L-谷氨酰胺在250.6～1503.6μg· mL^-1,薁磺酸钠在0.7575～4.5450μg· mL^-1范围内有良好的线性关系（相关系数均为1.0000）,平均回收率分别为99.94％和100.04％。结论：本方法同时测定复方谷氨酰胺颗粒中2种组分的含量,快速、简便、准确,可用于该制剂的含量测定。     

丁苯肽注射液联合丹参酮ⅡA磺酸钠注射液在脑梗死患者溶栓治疗中的效果探讨

目的:探讨丁苯肽注射液联合丹参酮IIA磺酸钠注射液在脑梗死患者溶栓治疗中的效果。方法:将2015年12月~2017年12月在某院神经内科治疗的116例脑梗死溶栓治疗患者随机分为两组。对照组单用爱通立溶栓治疗,在此基础上观察组使用丁苯肽注射液联合丹参酮IIA磺酸钠注射液,比较两组患者的临床疗效、神经功能及生活能力变化、神经损伤因子水平、炎性因子水平。结果:观察组治疗有效率为93.10%,明显高于对照组的77.59%(P<0.05);观察组治疗后NIHSS评分明显低于对照组,而BI指数明显高于对照组(P<0.05);观察组治疗后TNF-α、hs-CRP、IL-6水平明显低于对照组(P<0.05)。结论:丁苯肽注射液联合丹参酮IIA磺酸钠注射液在脑梗死患者溶栓治疗中的效果显著,能促进脑部受损神经功能的修复,改善脑部血液循环,抑制炎性因子对脑组织的损害,提升治疗效果。     

聚苯乙烯磺酸钠理化性质的考察

目的:考察新型药用辅料-聚苯乙烯磺酸钠的基本理化性质.方法:测定聚苯乙烯磺酸钠不同粒径下含水量,湿真密度,交换容量,溶胀率等基本理化性质.结果:聚苯乙烯磺酸钠粒径减小,含水量增大,湿真密度减小,交换容量增大,溶胀率增大.结论:聚苯乙烯磺酸钠的基本理化性质均受粒径影响.     

一种新型药用辅料——聚苯乙烯磺酸钠离子交换树脂的合成与表征

目的：制备一种新型药用辅料聚苯乙烯磺酸钠离子交换树脂并对其进行表征。方法：采用自由基聚合及磺化反应制备药用级聚苯乙烯磺酸钠离子交换树脂，并运用红外光谱法、差示扫描量热仪、X-射线衍射仪、激光衍射粒径分析仪等分析仪器对所制得的树脂及药物树脂复合物进行鉴别。结果：成功制备了粒径范围在60-200μm的聚苯乙烯磺酸钠离子交换树脂，并且证明药物与树脂通过化学键结合。结论：成功地制备了聚苯乙烯磺酸钠阳离子交换树脂。