Influence of Preparation Factors on the Sustained Release of Nifedipine from Eudragit RL/RS Microspheres

用乳剂—溶剂挥发法制备硝苯地平的丙烯酸树脂缓释微球。微球中药物的释放速度随丙烯酸树脂ＥｕｄｒａｇｉｔＲＬ／ＲＳ比率的增加以及制备时搅拌速率的增加而增大，随内相聚合物浓度的增加及微球粒径的增加而减小，释药５０％所需时间与微球粒径呈良好线性。微球的释药速率也随药物含量的增加（从４．２％到１６．７％）而增大，并快于药物结晶的溶解速率，但药物含量达２６．６％时，微球释药速率明显下降并低于药物结晶的溶解速率。用差热分析和Ｘ射线衍射分析证明，药物含量为４．２，９．４和１６．７％的微球中药物完全是以非晶态分散的，而含药２６．６％的微球中有药物结晶存在。不同微球释药低于７０％时，释放方式均符合Ｈｉｇｕｃｈｉ时间平方根方程。     

抗淋球菌IgA蛋白酶单克隆抗体特性的初步研究

本文对以重组淋球菌ＩｇＡ蛋白酶为抗原制备的７株特异性ＭｃＡｂ的特性进行了初步研究。结果有５株（１Ｃ８、１Ｅ５、１Ｆ１１、１Ｇ３和２Ｅ６）能中和淋球菌ＩｇＡ蛋白酶活性。经相加试验初步证明，其中１Ｆ１１、２Ｇ３与其它３株ＭｃＡｂ的作用位点不同。因此，淋球菌ＩｇＡ蛋白酶至少存在３个中和表位。     

Changes of circulating TNF and its effects on Pseudomonas aeruginosa septic shock in rabbits

Itiswellknownthatcertaincytokinesplayapivotalroleinthedevelopmentoftraumaandshock.Tumornecrosisfactor(TNF)isapolypep-tiedcytokinesynthesizedinmonocytesandmacrophagesinresponsetolipopolysaccharide(LPS)stimulation-TherelationshipbetweenTNFandendotoxic-septicshockbecomesafocusoftheresearchofshockmediators[1'2].Alargeamountofexperimentalandclinicaldata[3-9JsuggestthatTNFplaysanimportantroleinthepathogenesisofendotoxic-septicshockbuttheprecisemechanismandtherelationshipofTNFtoshockseverityrem…     

康泉合用地塞米松控制化疗所致的胃肠道反应

目的：比较康泉及康泉合用地塞米松预防急性白血病化疗所致的胃肠道反应的效果。方法：在同一方案的不同疗程，分别单用康泉或康泉合用地塞米松，随机对照，共观察１１０疗程。结果：康泉及康泉合用地塞米松对预防化疗所致急性呕吐有效率分别为６９．５％和９５．１％，有明显差异（Ｐ＜０．０１）；对于迟发性呕吐两组的有效率分别为７４．５５５％和９１．８３％，亦有明显差异。结论：康泉和地塞米松合用对控制急性和迟发性恶性呕吐优于康泉单用     

金属换热器传热过程的数学模型及应用

应用蒙特卡洛法仿真辐射式金属换热器内的辐射传热过程，建立了换热器综合传热的数学模型，利用概率论原理，把辐射能迁移过程仿真为一定累积概率分面下的随机过程，该模型能较好地反映换热器内传热过程的真实情况，可以计算出换热器内烟气、筒壁、空气的温度和壁面热流分布，以及研究烟气进口温度、换热器筒径和狭逢宽度对换热效果的影响。     

继发性甲旁亢的锁骨骨吸收

１８例慢性肾衰继发性甲旁亢病人发现有锁骨骨吸收。发病部位包括锁骨内端、外端、外１／３下缘及内段下缘４个部位。其中锁骨内、外端骨吸收属软骨下骨吸收，内、外段下缘骨吸收属韧带下骨吸收。作者对锁骨骨吸收的Ｘ线表现及发病机制作了讨论。认为锁骨骨吸收是继发性甲旁亢的重要Ｘ线征象，对诊断肾性骨病具有重要的意义。     

Cannabinoid receptor down-regulation without alteration of the inhibitory effect of CP 55,940 on adenylyl cyclase in the cerebellum of CP 55,940-tolerant mice

The objective of this study was to determine whether the development of tolerance to CP 55,940, a potent cannabinoid agonist, was due to changes in the receptor or second messenger system. ICR mice treated with CP 55,940 (2 mg/kg) twice a day for 6 and one-half days developed a high degree of tolerance to the pharmacological effects of CP 55,940. The ability of CP 55,940 to produce motor hypoactivity, hypothermia and immobility was reduced 163-, 97- and 19-fold, respectively. Evaluation of 3H-CP 55,940 binding to rat brain membranes indicated no difference in receptor affinity between the vehicle- and CP 55,940-treated animals. However, these binding studies revealed a 50% decrease in receptor number in the cerebellum of the CP 55,940-tolerant mice. Although cAMP is generally considered to be the second messenger for cannabinoid receptors, little difference was observed in the inhibitory effects of CP 55,940 on adenylyl cyclase activity in cerebellum between vehicle and drug-treated mice. However, there was an increase in receptor mRNA which suggests a compensation for receptor loss. There are several possible explanations for these results. There may be sufficient spare receptors such that CP 55,940-tolerant mice are capable of producing a maximal effect on the second messenger system. On the other hand, one could conclude that cannabinoid receptor down-regulation does not account for the development of tolerance to all of the effects of CP 55,940 in mice.     

有机药物化学中不对称合成手性产率及其随温度变化规律的研究

本文首次用分子力学计算产物或过渡态分子内张力能来估算热力学或动力学,控制不对称合成反应生成的立体异构体的相对比例,并从热力学上推导了这一比例随温度变化公式,而且从实验上得到证明,在有机或药物化学最富有挑战性的领域——不对称合成中具有重要的理论和实际意义。     

10Gyγ线照射后小鼠两相邻肠段运动变化

本文用同时记录两相邻空肠段的收缩活动来观察经10Gyγ线照射后小肠运动的变化,以了解照射后是否出现逆蠕动,以便进一步分析肠套叠形成的原因.结果表明,照射后两相邻肠段出现强度不一的收缩活动,并且可以产生逆蠕动;但是这种逆蠕动发生的机率是不大的.本实验未观察到逆蠕动发生的规律性.因此,逆蠕动的产生可能是照射后发生肠套叠的部分原因.