注射用益气复脉（冻干）冲管液安全剂量测定

目的 测定注射用益气复脉（冻干）（YQFM）冲管液安全剂量。方法 以YQFM为研究对象,以0.9%氯化钠注射液为稀释剂和冲管溶液,采用紫外-可见分光光度法测定冲管液中主药成分残留,确定冲管液的安全剂量;收集各段冲管液,在冲管液中加入常用配伍药物呋塞米注射液,采用紫外-可见分光光度法对冲管安全剂量进行验证;在冲管液中加入注射用环磷酰胺,采用不溶性微粒检查法对冲管液安全剂量进行验证。结果 YQFM 0.9%氯化钠溶液特征吸收波长为203和283 nm,浓度-吸收趋势拟合显示线性良好;在0~300 min内稳定性较好;冲管速度为40滴/min（2 mL/min）时,YQFM冲管液安全剂量为32.0 mL/min,经验证冲管效果符合要求。结论 为保证临床用药的安全性,建议YQFM冲管液用剂量应不少于32.0 mL。     

Study of the water structure in poly(methyl methacrylate-block-2-hydroxyethyl methacrylate) and its relationship to platelet adhesion on the copolymer surface

The water structure and platelet compatibility of poly(methyl methacrylate (MMA)-block-2-hydroxyethyl methacrylate (HEMA)) were investigated. The molecular weight (Mn) of the polyHEMA segment was kept constant (average: 9600), while the Mn of the polyMMA segment was varied from 1340 to 7390. The equilibrium water content of the copolymers was found to be mainly governed by the HEMA content. The water structure in the copolymers was characterized in terms of the amounts of non-freezing and freezing water (abbreviated as W_nf and W_fz, respectively) using differential scanning calorimetry. It was found that the W_nf for the copolymers were higher than those estimated from the W_nf for the HEMA and MMA homopolymers and that the amount of excess non-freezing water depended on the polyMMA segment length. In addition, X-ray diffraction analysis revealed that some of the copolymers had cold-crystallizable water. These facts suggested that the polyMMA segments were involved in determining the water structures in the copolymers. Furthermore, the platelet compatibility of the copolymers was improved as compared to that of the HEMA homopolymer. It was therefore concluded that the platelet compatibility of the copolymer was related to the amount of excess non-freezing water.     

Modification of Polyurethane with Polyethylene Glycol–Corn Trypsin Inhibitor for Inhibition of Factor Xlla in Blood Contact

Abstract

In previous work using gold as a model substrate, we showed that modification of surfaces with poly(ethylene glycol) (PEG) and corn trypsin inhibitor (CTI) rendered them protein resistant and inhibitory against activated factor XII. Sequential attachment of PEG followed by CTI gave superior performance compared to direct attachment of a preformed PEG-CTI conjugate. In the present work, a sequential method was used to attach PEG and CTI to a polyurethane (PU) substrate to develop a material with applicability for blood-contacting medical devices. Controls included surfaces modified only with PEG and only with CTI. Surfaces were characterized by water contact angle and X-ray photoelectron spectroscopy. The surface density of CTI was in the range of a monolayer and was higher on the PU substrate than on gold reported previously. Biointeractions were investigated by measuring fibrinogen adsorption from buffer and plasma, factor XIIa inhibition and plasma clotting time. Both the PU–PEG surfaces and the PU–PEG–CTI surfaces showed low fibrinogen adsorption from buffer and plasma, indicating that PEG retained its protein resistance when conjugated to CTI. Although the CTI density was lower on PU–PEG–CTI than on PU modified only with CTI, PU–PEG–CTI exhibited greater factor XIIa inhibition and a longer plasma clotting time, suggesting that PEG facilitates the interaction of CTI with factor XIIa. Thus sequential attachment of PEG and CTI may be a useful approach to improve the thromboresistance of PU surfaces.     

Blood compatibility of polypropylene surfaces in relation to the crystalline-amorphous microstructure

Blood-contacting properties of polypropylene surfaces with different crystalline states at the surface layer were examined in terms of plasma protein adsorption and changes in cytoplasmic free Ca²⁺ levels in platelets. Though the wettability of polypropylene surfaces was almost constantly independent from the surface layer crystallinity and interlamellar spacing, an increase in adhesiveness was observed with decreasing surface layer crystallinity and interlamellar spacing. It is suggested that the surface properties of the sheets varied in relation to the crystalline-amorphous microstructure. Minimum magnitudes in albumin and fibrinogen adsorption were observed on the polypropylene surface with a particular surface layer crystallinity (c. 55 wt%). A decrease in interlamellar spacing resulted in enhancing albumin adsorption and diminishing fibrinogen adsorption. Transient phenomena in plasma protein adsorption were observed on their surfaces with a plasma concentration. It is considered that the polypropylene surface with a particular crystalline-amorphous microstructure reduces the denaturation of adsorbed proteins. An increase in cytoplasmic free Ca²⁺ levels in platelets was prevented at the polypropylene surface with a surface layer crystallinity of 55 wt%: the particular crystalline-amorphous microstructure of such apolar surfaces as polypropylenes acts to reduce platelet activation. Thus, it is concluded that the blood compatibility of polypropylene surfaces is greatly improved by controlling a crystalline-amorphous microstructure at the surface layer.     

Surface studies of albumin immobilized onto PE and PVC films

The aim of this study is to evaluate the thrombogenic behaviour of the low density polyethylene and poly(vinyl chloride) modified by radiation-grafting technique. After copolymerization with acrylic acid by y-rays from a ⁶⁰Co source, BSA was immobilized onto functionalized graft copolymers. The biological interaction between these materials and blood was studies by in vitro methods. The BSA immobilization effectively suppressed the adhesion and activation of platelets when it contacted whole blood.     

基于活血化瘀理论的中药配伍防治脑缺血再灌注损伤炎症反应的作用机制

[目的]以丹红注射液为例,研究活血化瘀中药防治脑缺血再灌注损伤(cerebral ischemia-reperfusion injury,CIRI)炎症反应的作用机制。[方法]通过对以往研究文献的整理复习,从CIRI与炎症反应的相关性及瘀血证与炎症反应的相关性出发,重点分析以丹红注射液为代表的活血化瘀中药防治CIRI炎症反应的作用机制。[结果]炎症反应在CIRI的病理生理过程中起到重要作用,基于中医活血化瘀理论的瘀血证与炎症反应的关系密不可分。瘀血证的病理实质包括了多种致炎细胞因子造成组织器官水肿、血栓形成及相关炎症通路激活等一系列的病理变化,而活血化瘀疗法可以从不同方面通过不同途径调节CIRI过程中的炎症反应,如活血化瘀的代表药物丹红注射液能抑制CIRI中肿瘤坏死因子-α(tumor necrosis factor-α,TNF-α)、白细胞介素-1β(interleukin-1β,IL-1β)和IL-10的分泌,从而减轻炎症反应,有利于缓解脑组织损伤,防止病情进展,改善患者预后。[结论]对活血化瘀中药防治CIRI炎症反应的作用机制进行探讨,可以为临床防治CIRI的新药开发提供理论基础。     

基于关联规则的中药组分配伍治疗脑缺血再灌注损伤规律研究

目的探讨治疗脑缺血再灌注损伤(cerebral ischemia reperfusion injury,CIRI)的高频用药,并揭示用药与证型、组分与组分的关系,从组分层面解析中药治疗CIRI的配伍规律。方法收集中国知网(1998-08-25至2018-08-25)20年期刊文献数据库中治疗CIRI的中药及相关组分的研究,采用关联规则Apriori计算方法,对治疗CIRI的中药复方及相关组分的研究结果进行挖掘分析。结果高频次药物包括补阳还五汤、川芎嗪注射液、黄芪提取物等,印证及推测出构成丹参、三七等单味中药的活性成分及血栓通注射液和脑心通胶囊等中药复方的药效物质基础,并发现了芍药苷-阿魏酸、黄芪甲苷-藁本内酯-阿魏酸等新的组分配伍形式。结论基于关联规则,为CIRI中药组分配伍治疗挖掘高频用药、用药与证型、组分与组分的关联关系,可为组分配伍研发提供依据与参考。     

参麦注射液的质量控制、毒性及临床配伍研究进展

参麦注射液是由红参、麦冬制得的中药注射剂,具有益气固脱、养阴生津、生脉的功效。临床上用于治疗气阴两虚型之休克、冠心病、病毒性心肌炎、慢性肺心病、粒细胞减少症。主要从影响参麦注射液安全的热原、溶血、过敏、细菌内毒素、有机试剂残留的质量控制;与化学成分及辅料相关的毒性研究;与稀释剂、常用药物和不建议配伍药物的临床配伍研究3个方面加以综述,为提高产品安全质量控制、降低不良反应发生率提供参考。     

四君子汤抗胃癌活性部位配伍作用及其对细胞周期的影响

[目的]研究四君子汤抗胃癌活性部位的配伍作用及其对细胞周期的影响.[方法]以SGC-7901胃癌细胞为细胞模型,以接种SGC-7901细胞的裸鼠为动物模型,通过体内、体外方法筛选四君子汤抗胃癌活性部位的最佳配伍;流式细胞仪观察四君子汤活性部位配伍对SGC-7901细胞周期的影响.[结果]四君子汤挥发油部位、萜类部位、黄酮部位在体内、体外均体现出配伍协同作用,活性部位配伍组对SGC-7901细胞的药物半数抑制浓度(IC50)为1.574mg/ml,其高、低剂量组体内抑瘤率分别为55.48％和44.52％;四君子汤活性部位配伍组处理后G2/M期SGC-7901细胞显著增加,为12.84％.[结论]四君子汤挥发油部位、萜类部位、黄酮部位具有协同配伍作用,能将SGC-7901细胞阻滞于G2/M期.