广义估计方程GEE2与GEE1的比较

在纵向资料分析中，当我们既要阐明因变量对自变量的依从关系，又要描述因变量间的相互关系时，可以用广义估计方程ＧＥＥ２来分析。本文简介了ＧＥＥ２的基本原理和应用特点，比较了ＧＥＥ２与ＧＥＥ１的异同及适用范围。     

头孢克肟治疗68例尿路感染临床疗效

头孢克肟治疗６８例尿路感染临床疗效ＴＨＥＲＡＰＥＵＴＩＣＡＬＯＢ５ＥＲＶＡＴＩＯＮＯＦＣＥＦＩＸＩＭＥＩＮＴＨＥＴＲＥＡＴＭＥＮＴＯＦＵＲＩＮＡＲＹＴＲＡＣＴＩＮＦＥＣＴＩＯＮＩＮ６８ＣＡＳＥＳ余瑛，孙铎，谢文练，杨周灼，王一锋，陈如恒，何柏林ＹｕＹ...     

7α－芳基－6，14－内亚乙烯基四氢蒂巴因的合成

７α－芳基－６，１４－内亚乙烯基四氢蒂巴因的合成仇缀百，曾一斌，杨杰（上海医科大学药学院，上海２０００３２）ＳＹＮＴＨＥＳＥＳＯＦ７α－ＡＲＹＬ－６，１４－ＥＮＤＯＥＴＨＥＮＯ－ＴＥＴＲＡＨＹＤＲＯＴＨＥＢＡＩＮＥ￥ＱＩＵＺｈｕｉ－Ｂａｉ；ＺＥＮＧＹ...     

非氨酯中间体2－苯基－1，3－丙二醇的合成

非氨酯中间体２－苯基－１，３－丙二醇的合成张灿，张惠斌，黄海燕，黄文龙（中国药科大学药物化学研究室，南京２１０００９）ＳＹＮＴＨＥＳＩＳＯＦ２－ＰＨＥＮＹＬ－１，３－ＰＢＯＰＡＮＥＤＩＯＬ，ＡＮＩＮＴＥＲＭＥＤＩＡＴＥＦＯＲＦＥＬＢＡＭＡＴＥ￥ＺＨＡ...     

酸处理的表皮生长因子对小鼠胎肝细胞BNL CL.2生物活性的影响

目的 探讨酸抑制剂对表皮生长因子（ＥＧＦ）活性的保护机理。方法用含有胃蛋白酶的盐酸培养重组人ＥＧＦ，用高压液相分析酸和胃蛋白酶中ＥＧＦ的稳定性，用３Ｈ－ＴｄＲ法测定酸降解的ＥＧＦ对胎肝细胞的体外生物活性的影响，用ＦＡＣＳ检测小鼠胎肝细胞经酸降解的ＥＧＦ诱导４８ｈ后ＥＧＦ的变化。结果所有含胃蛋白酶的标本中，当ｐＨ＜４．０时，ＥＧＦ被降解成为分子量较小的形式。经盐酸降解的该因子受体（ＥＧＦ）对小鼠胎肝细胞的增殖效应明显低于未用酸降解的ＥＧＦ处理组，未用酸降解的ＥＧＦ处理的小鼠胎肝细胞的ＥＧＦＲ表达也明显高于酸降解的ＥＧＦ处理组。结论 在ｐＨ＜４．０时，经酸处理的ＥＧＦ稳定性较差，能被迅速降解成分子量较小的形式，其活性也大大减弱，对小鼠胎肝细胞的促增殖作用明显低于未经酸降解的ＥＧＦ组。用抑酸药调节胃液中适当的ｐＨ值，对维持ＥＧＦ的稳定性，促进对胃粘膜的保护有一定作用。     

盐酸黄连素片的一阶导数光谱测定

盐酸黄连素片的一阶导数光谱测定许桢灿，林绍乐，陈其银（三明市药品检验所，福建３６５０００）ＤＥＴＥＲＭＩＮＡＴＩＯＮＯＦＢＥＲＢＥＲＩＮＥＨＹＤＲＯＣＨＬＯＲＩＤＥＴＡＢＬＥＴＳＢＹＦＩＲＳＴＯＲＤＥＲＤＥＲＩＶＡＴＩＶＥＳＰＥＣＴＲＯＰＨＯＴＯＭＥ...     

无载体固定化细胞制备6－氨基青霉烷酸

无载体固定化细胞制备６－氨基青霉烷酸ＴＨＥＰＲＥＰＡＲＡＴＴＩＯＮＯＦ６－ＡＭＩＮＯＰＥＮＩＣＩＬＬＡＮＩＣＡＣＩＤＢＹＣＡＲＲＩＥＲ－ＦＲＥＥＩＭＭＯＢＩＬＩＺＥＤＣＥＬＬＳ刘光荣，虞和慈，姜云龙，张捷，袁剑萍，陈俊琳ＬｉｕＧｕａｎｇ－ｒｏｎｇ；Ｙ...     

石杉碱甲,他克林和E2020对离体小鼠神经肌肉接头胆碱能传递作用的比较(英文)

目的：比较石杉碱甲，他克林和Ｅ２０２０对胆碱能传递的作用．方法：在小鼠的膈神经肌肉标本上用胞内记录的方法研究了石杉碱甲（ＨｕｐＡ），他克林（ｔａｃｒｉｎｅ）和Ｅ２０２０对自发释放的小终板电位（ＭＥＰＰ），终板电位（ＥＰＰ）的量子含量，以及肌细胞的静息膜电位的作用．结果：ＨｕｐＡ，ｔａｃｒｉｎｅ和Ｅ２０２０１０μｍｏｌ·Ｌ－１可增强ＭＥＰＰ的振幅、上升相和半下降相，其作用强度为Ｅ２０２０＞ＨｕｐＡ＞ｔａｃｒｉｎｅ．ＨｕｐＡ对ＭＥＰＰ的频率，以及ｇＭＥＰＰ和ｓＭＥＰＰ的出现率无显著影响．它对ＥＰＰ的量子含量和肌细胞的静息膜电位亦无显著作用．结论：ＨｕｐＡ是一种高选择性的ＡＣｈＥ抑制剂，由此促进神经肌肉接头处的胆碱能传递．     

垂体腺苷酸环化酶活化多肽对垂体细胞内钙调素活性的作用

垂体腺苷酸环化酶活化多肽对垂体细胞内钙调素活性的作用范明，李东亮，ＥｒｉｋＴＥＵＧＥＬＳ２ＥｌｉｓａｂｅｔｈＨＯＯＰＨＥ－ＰＥＴＥＲＳ２甘思德（军事医学科学院基础医学研究所，北京１００８５０；新乡医学院生理教研室，新乡４５３００３；Ｄｅｐａｒｔｍｅｎ...     

乙氧亚甲基丙二酸二乙酯的合成

乙氧亚甲基丙二酸二乙酯的合成张爱华，张荣久，吴国沛（南京药物研究所，江苏２１０００９）ＳＹＮＴＨＥＳＩＳＯＦＤＩＥＴＨＹＬＥＴＨＯＸＹＭＥＴＨＹＬＥＮＥＭＡＬＯＮＡＴＥ￥ＺＨＡＮＧＡｉ－Ｈｕａ，ＺＨＡＮＧＲｏｎｇ－Ｊｉｕ，ＷＵＧｕｏ－Ｐｅｉ（Ｎａｎｊ...     

用大孔离子交换树脂从人尿中提取尿激酶

筛选得到一种大孔离子交换树脂（ＨＤ－２），用于从新鲜人尿提取尿激酶，树脂用量为０．１２％（ｗ／ｖ），收率为８５．０％，所得粗酶比活为５７３．０ＩＵ／ｍｇ。整个提取工艺简单、快速，成本低，有较大的推广潜力。     

提纯孕马血清促性腺激素的中试生产研究

孕马血清经偏磷酸、乙醇分级沉淀得比活为409IU／mg的粗品，回收率为47．3％。粗品经离子交换层析得到比活为1455IU／mg的精品，回收率达97.4％。再过柱层析得比活为2400IU／mg的产品。     

Antithrombotic and hemorrhagic activities of fucoidan isolated from Fucus evanescens brown algae

The antithrombotic and hemorrhagic activities of fucoidan with molecular weight within 20 - 40 kD isolation from Fucus evanescens seaweed have been investigated. The antithrombin activity of fucoidan is 41 +/- 9 aIIa IU/mg and the anti-factor Oà activity is 38 +/- 8 aOà IU/mg. The antithrombin and anti-factor Oà activities of plasma, antithrombotic activity (100% prevention of formation of a blood clot observed at a dose of 10 mg/kg), and hemorrhagic activity (to a lesser degree, than that of unfractionated heparin in comparable antithrombotic activity doses) increase as the doses of fucoidan increases from 2.5 to 10 mg/kg at intravenous injection in rats.     

Defibrotide is equipotent to urokinase in stimulating arterial and venous thrombolysis

The action of iv. defibrotide (100 mg/kg bolus injection, followed by 30 mg/kg x h) on arterial and venous thrombus formation was studied in rabbits and compared with iv. urokinase (4,000 IU/kg bolus injection, followed by 1,500 IU/kg x h). In comparison with saline treated controls, defibrotide reduced the thrombus weight by 43% in veins and 76% in arteries (P less than 0.01), while urokinase reduced the thrombus weight by 50% in veins and 71% in arteries. The data suggest a potent thrombolytic activity of defibrotide which is comparable to that of urokinase.     

Dependence of the anticoagulant activity of starch and inulin on their degree of sulfonation

We have studied a relationship between the degree of sulfonation and anticoagulant activity of starch from Solanum tuberosum (molecular weight, 25000-30000 Da; sulfonation degree, 0.4-2.5) and inulin from Helianthus tuberosus (molecular weight, 7000-8000 Da; sulfonation degree, 0.6-1.6). Starch and inulin sulfates (i) increased the time of appearance of fibrin clots in plasma in coagulometric tests and (ii) reduced (via antithrombin) the rate of thrombin-induced hydrolysis of a chromogen substrate. The antithrombin (aIIa) activity of starch sulfates reached 16.8-70.0 IU/mg and the activity against factor Xa (aXa activity) was 2.3-16.6 IU/mg. The antithrombin activity of inulin sulfates was within 5.5-11.4 IU/mg and the activity against factor Xa (aXa activity) was within 0-1.4 IU/mg. An increase in the degree of sulfonation led to a growth in the anticoagulant activity of starch sulfates. The anticoagulant activity of starch sulfates and inulin sulfate with sulfonation degree 1.0 is mediated by antithrombin, which is the plasma inhibitor of serine proteases.     

Evaluation of self-dissolving needles containing low molecular weight heparin (LMWH) in rats

Feasibility study of self-dissolving needles containing polysaccharide was performed. Low molecular weight heparin (LMWH) was used as a representative polysaccharide. Using chondroitin, dextran and dextrin as the base, self-dissolving needles (SDN) were prepared. The obtained SDNs were evaluated in rat absorption experiment, where pharmacological availability (PA) was calculated by comparing the plasma anti-Xa activity vs. time curves between SDNs and i.v. solution. After the insertion of SDNs to rats skin where the doses of LMWH were 25, 50 and 100 IU/kg, plasma samples were collected for 6h and anti-Xa activity was measured as the pharmacological index of LMWH. The anti-Xa level was maintained above 0.2 IU/ml, the therapeutic level, for about 2h at a dose of 100 IU/kg. Almost the same PAs of LMWH were obtained with dextran and dextrin SDNs, 97.7% and 102.3%, though lower PA was obtained with chondroitin SDN, 81.5%. In vitro dissolution experiment showed that LMWH was released from dextran, dextrin and chondroitin SDNs within 10 min. The T(50%)s were 0.84+/-0.06 min for dextran SDN, 1.07+/-0.12 min for chondroitin SDN and 2.11+/-0.31 min for dextrin SDN, respectively. Plasma anti-Xa activity vs. time profiles showed good dose-dependency in the 25-100 IU/kg range and high PAs were obtained, 90.0% for 25 IU/kg, 95.4% for 50 IU/kg and 97.7% for 100 IU/kg from dextran SDNs. Stability experiment was performed with dextran SDNs for 3 months. Above 97% of LMWH were remained in SDNs under three different conditions, -80, 4 and 40 degrees C. These results suggest the usefulness of SDN to polysaccharide drug.     

Antithrombotic activity of para-aminobenzoic acid

Mechanisms of the anticoagulant activity of p-aminobenzoic acid (PABA) were studied. The specific antithrombin activity of PABA is aIIa = 7.00 +/- 0.32 IU/mg and the specific antiactivated factor Xa activity is aXa = 6.70 +/- 0.12 IU/mg. Study of the antithrombotic activity of PABA in rats with a model of venous stasis showed that intravenous injection of PABA at a dose of 1.5 mg/kg prevented the experimental thrombosis development 1.5 h after injection. The activity exhibited a peak 3 h after drug injection and ceased by the 5th hour. Equal antithrombotic activity in the rat blood plasma was observed for fraxiparin at a dose of 40 aXa IU/kg and PABA at 25 aXa IE/kg (1.5 mg/kg). At the same time, PABA affected neither the number of thrombocytes nor their response to the thrombocyte aggregation factors (ADP or adrenaline).     

Monomeric destetrapeptide human insulin from a precursor expressed in Saccharomyces cerevisiae

Abstract: Destetrapeptide insulin (DTI, human insulin with B27–30 removed) was obtained from a monomeric precursor (MIP) expressed in Saccharomyces cerevisiae through tryptic transpeptidation in the presence of synthetic tetrapeptide Gly‐Phe‐Phe‐Tyr. The in vivo biological activity of DTI, determined by mouse convulsion assay, is 22 IU/mg. Its binding activity with insulin receptor on human placental membrane is 80% and its in vitro biological activity, determined by free fat cell assay, is 77%. Compared with native insulin, DTI molecules do not associate in solution but exist in the monomeric form, thus leading to its rapid utilization in vivo.     

Influence of histamine in a liver injury model induced by Propionibacterium acnes and lipopolysaccharide

In normal mice, plasma histamine levels were 29.4+/-10.1 pmol/ml. When 0.1 microg of lipopolysaccharide (LPS) was intravenously injected into Propionibacterium acnes (P. acnes)-primed ICR mice, histamine levels increased remarkably to 61.2+/-15.9 pmol/ml (p<0.001). An increase was also observed in liver tissues. Oral administration of histidine at 200 mg/kg once daily for 5 d before intravenous LPS injection increased the plasma alanine aminotransferase (ALT) activity to 2936.5+/-356.3 IU/l, a significant change compared with the controls (2244.8+/-425.5 IU/l, p<0.05). The 24 h survival rate after LPS injection was 72.7% in the mice treated with 50 mg/kg of ranitidine, in contrast with 50% in the control group although the treatment did not significantly decrease the plasma ALT activity. On the other hand, 50 mg/kg of pyrilamine significantly reduced plasma ALT activity (p<0.001). The results suggested that histamine levels are related to hepatic damage in the P. acnes plus LPS induction of liver injury.     

组织纤溶酶原激活物的分离纯化

用亲和层析法从猪心组织分离纯化纤溶酶原激活物(tissue type plasminogen activator,t-PA),以纤维蛋白-sepharose-4B 和 lys-sepharose-4B 两种亲和胶,从5 kg 新鲜猪心组织中分离出 t-PA1.46mg,比活性为235000 IU/mg,得率为34%,SDS 聚丙烯酰胺凝胶电泳测定为一条带,分子量为68000。