注射用丹参多酚酸中主要成分的降解动力学分析

目的:探索注射用丹参多酚酸中主要活性成分(丹酚酸B和迷迭香酸)在不同pH和温度下的降解规律.方法:采用HPLC测定迷迭香酸、丹酚酸B含量,研究二者在不同pH(1～13)和温度(60,70,80,90℃)下含量变化,通过化学动力学法计算降解动力学参数.结果:丹酚酸B与迷迭香酸在不同pH和温度下降解反应均属于一级动力学反应,降解速率随pH及温度的升高而增加.丹酚酸B和迷迭香酸在水溶液中的降解活化能(Ea)分别为48.54,49.83 kJ· mol-1,在注射用丹参多酚酸中则分别为95.19,83.56 kJ· mol-1.结论:丹酚酸B与迷迭香酸在碱性条件及高温条件下易降解,与对照品相比较,二者在注射用丹参多酚酸中更为稳定.     

30例注射用双黄连（冻干）不良反应分析及思考

目的了解注射用双黄连（冻干）临床应用的安全性,探讨其不良反应表现,为临床使用提供参考。方法对笔者所在医院2008年6月～2010年12月使用注射用双黄连（冻干）发生不良反应的患者情况进行分类统计、分析。结果注射用双黄连（冻干）不良反应临床主要表现为全身性损害、呼吸系统损害及多器官多系统损害,程度轻重不一、预后良好。结论药品生产企业加强上市后的安全监测,并开展生产工艺和质量研究,完善药品说明书;医生、患者应严格按照药品说明书的规定合理用药,以减少药品不良反应的发生。     

葛根素纳米粉体的制备及质量评价

目的制备葛根素纳米冻干粉,并对其进行质量评价。方法通过对冻干保护剂、冻干时间、预冻温度等的单因素考察,选择葛根素纳米冻干粉的最佳制备工艺,并对冻干粉的理化性质、纳米形态和质量进行评价。结果葛根素纳米粉体的最佳成型工艺为:以甘露醇为冻干保护剂,置-80℃冰箱中预冻12h,然后在-40℃、5Pa下真空冷冻干燥36h升华水分。制备的纳米粉体具有良好的溶解性能,平均粒径为108nm,表面电位为-24.3mV,平均含量约为140mg/g。结论采用冻干技术制备葛根素纳米粉体技术可行。     

口服葛根总黄酮固体脂质纳米粒冻干粉的制备及其4种成分释放度考察

目的制备口服葛根总黄酮固体脂质纳米粒冻干粉并考察其主要有效成分3′-羟基葛根素、葛根素、大豆苷和大豆苷元的释放度。方法采用高压均质法制备葛根总黄酮固体脂质纳米粒混悬液,以甘露醇为冻干保护剂制备冻干粉,以人工胃液(pH 1.2)为溶出介质,考察葛根总黄酮固体脂质纳米粒冻干粉中4种有效成分的释放度。结果正交试验优选制备工艺:脂质-表面活性剂比例及用量为2∶1及2.0%、葛根总黄酮用量2.5%、150 MPa均质15次,并制备葛根总黄酮固体脂质纳米粒冻干粉,其粒径、多分散指数及Zeta电位分别为(517.1±10.3)nm、0.484±0.210及(-21.91±2.03)mV。葛根总黄酮固体脂质纳米粒冻干粉中4种有效成分的释放速率显著低于其物理混合物,具有明显的缓释特征。结论葛根总黄酮固体脂质纳米粒冻干粉制备方法简便,能显著延缓主要有效成分的释放速率,有望成为葛根总黄酮的新型纳米给药系统。     

大蒜冻干粉高效液相色谱指纹图谱研究

目的建立大蒜冻干粉HPLC指纹图谱,为整体控制和评价大蒜冻干粉质量提供依据。方法采用高效液相色谱法,以甲醇-1％无水甲酸水溶液为流动相进行梯度洗脱,检测波长254nm,流速1mL／min,分别对10个批次大蒜冻干粉进行检测,采用药典委员会指定的指纹图谱相似度软件（2004A版）进行相似度评价,计算不同批次大蒜冻干粉的相似度。结果建立了大蒜冻干粉HPLC指纹图谱,确定9个共有峰,10个批次的大蒜冻干粉的色谱图与对照指纹图谱的相似度〉0．96。结论本法准确可靠,精密度、稳定性及重复性试验均符合指纹图谱的技术要求。     

Biochemical and pathological evidences on the benefit of a new biodegradable nanoparticles of probiotic extract in murine colitis

Efficacy of probiotics in the management of human inflammatory bowel disease (IBD) has been approved in the recent years. In the present work, the efficacy of a new biodegradable nanoparticles (NPs) of encapsulated and lyophilized probiotic extract (LPE) was examined in murine colitis. Colitis was induced by rectal instillation of trinitrobenzen sulfonic acid to male Wistar rats. The safety and effective dose of LPE was determined in a pilot study. To ease delivery into colon, LPE was encapsulated in chitosan‐coated‐poly (lactide co glycolide acid) NPs. After induction of colitis, animals in different groups received test compound in three doses by gavage for 10 days. Groups of sham, control (saline), and standard (dexamethasone) were also assigned. Colonic pathological examination, tumor necrosis factor alpha, interlukin (IL)‐1β, myeloperoxidase (MPO), and lipid peroxidation (LPO) were performed. LPE at all doses (273, 545, and 1100 mg/kg) had positive effects in reduction of pro‐inflammatory cytokines, LPO, and MPO in a dose‐dependent manner. The formulated compound containing medium dose of LPE was more efficient in mitigating the experimental colitis in comparison with that of high‐dose LPE. It is concluded that LPE and its nanoparticle‐encapsulated form are very much effective in control of colitis. Regarding safety of this compound, further studies can be conducted in patients with IBD.     

蚯蚓冻干粉对高血脂小鼠羟甲基戊二酸单辅酶A还原酶基因的调节作用

以高脂饲料饲喂昆明种小鼠构建高血脂小鼠模型,灌胃给予高、中、低剂量(0.4、0.2和0.1 g/kg)蚯蚓冻干粉,每天1次,同时饲喂高脂饲料,共饲养10周.提取小鼠肝脏总RNA,应用反转录基因扩增(RT-PCR)技术检测羟甲基戊二酸单辅酶A还原酶(HMG-CoAR)信使核糖核酸(mRNA)水平.结果表明,试验组小鼠HMG-CoAR mRNA相对含量显著低于高脂饲料组小鼠,提示蚯蚓冻干粉能够降低高血脂小鼠血浆胆固醇水平,可能与下调肝HMG-CoAR mRNA表达有关.     

利巴韦林脂质体吸入粉雾剂的研制与初步评价

目的 为解决利巴韦林存在的明显不良反应问题,研制利巴韦林脂质体吸入粉雾剂,并初步评价其质量特性。方法 采用薄膜分散法制备利巴韦林脂质体,再冻干制备成利巴韦林脂质体粉雾剂,并考察制剂的外观形态、流动性、松密度、包封率、复溶液粒径、聚合物分散指数、电位及亲水性。结果 利巴韦林脂质体粉雾剂形态、粒径、电位、流动性与亲水性均较好,能满足粉雾剂給药的基本要求。结论 应用该方法制备利巴韦林脂质体粉雾剂的制剂技术是可行的,为后续体内外研究提供制剂学技术依据。     

Comparison of the specificity of rheumatoid factor detected by latex fixation with that of regulatory rheumatoid factor

BackgroundRheumatoid factor (RF), originally defined as pathological autoantibodies to IgG that are detected in rheumatoid arthritis, turned out to be multi‐specific antibodies, some of which exhibit immunoregulatory properties. Recently, we identified a RF, the production of which confers resistance to experimental autoimmune diseases and is associated with the remission of autoimmune diseases. To differentiate the RF, we discovered from the one associated with rheumatic disease onset or progression and to reflect its immunoregulatory properties, we named it regulatory rheumatoid factor (regRF). Immunization with conformers of Fc fragments that expose regRF neoepitopes reduces collagen‐induced arthritis in rats. Certain information about the specificity of classical RF and regRF indicates that these populations may be one and the same. Therefore, the aim of this study was to determine whether there is a difference between the classical RF and regRF.MethodsClassical RF was measured in diseased blood by the latex fixation method, and regRF was detected by the agglutination of human IgG‐loaded tanned erythrocytes. Competitive analysis was used to determine the specificity of rheumatoid factors.ResultsIt was found that regRF and pathology‐associated RF constitute different antibody populations. Pathology‐associated RF is specific for lyophilized IgG. RegRF does not interact with IgG. RegRF is specific to conformers of IgG Fc fragments that have a reduced hinge. In latex‐positive rheumatoid arthritis sera, regRF may be present in addition to pathology‐associated RF. The latex fixation method detects both rheumatoid factor populations.ConclusionRegRF and classical pathology‐associated RF have different specificity.     

冻干重组人脑利钠肽对急性心力衰竭临床疗效

目的针对急诊治疗急性心衰实施冻干重组人脑利钠肽治疗的举措,观察及分析效果情况。方法在本院2017年8月—2018年8月期间选取治疗的150例急性心衰病患,随机数字法均分为两个组别,其中对照组心衰患者采用常规药物治疗,试验组在对照组治疗基础上加上冻干重组人脑利钠肽,观察两组患者心率和左心室射血分数(LVEF)、临床疗效及不良反应情况。结果治疗后,试验组患者心率、LVEF水平及总有效率均优于对照组(P<0.05),且不良反应明显低于对照组(P<0.05)。结论冻干重组人脑利钠肽用于治疗急性心力衰治竭疗效果明显,增强患者生活质量水平,在临床治疗中具有重要参考价值及意义。