H—TdR前体掺入技术在复方中药抗癌制剂研究中的应用

将一种快速、灵敏、可靠、简便的抗癌活性微量测定技术——~3H—TdR前体掺入技术用于复方中药抗癌制剂制备工艺筛选,短期内即拟定出较合理的工艺,经临床及14项生物学指标综合评定,该制剂疗效好,无明显的毒副作用。表明把一些快速、灵敏的医学检测技术引入药物制备工艺、质量标准及稳定性研究,可克服由于活性成分不清楚带来的一些困难,拓宽了研究途径,提高了研究水平。     

T2毒素在灌流大鼠肠肝中的首过效应和代谢动力学

建立并用大鼠在体肠-肝灌流标本研究了T2毒素在大鼠肠肝中的首过效应和代谢转化动力学,T2毒素在大鼠肠肝中的主要代谢产物是HT2,3′-OHHT2和其葡萄糖醛酸结合物,T2毒素具有显著的肠肝首过效应,当毒素(42μg·ml~(-1))由上肠系膜动脉恒速单次灌流(8 ml·min~(-1))肠-肝标本时,穗态肝、肠抽提率分别为0.978和0.454,总有效清除率为7.91 ml·min~(-1),T2毒素在循环灌流大鼠肠-肝标本中的消除半衰期为6.5min,主要代谢产物HT2,3′-OHHT2的生成半衰期分别为8.5和38.5 min,结果表明,T2毒素经消化道中毒后,在肠和肝的首过代谢下能很快地转化为产物,因此,毒素在体内的毒效作用主要由其代谢产物表现出来。     

负压封闭吸引对糖尿病溃疡愈合的促进作用

目的 在"创而床准备(WBP)"理论指导下,观察负压封闭吸引局部处理糖尿病溃疡的疗效.方法 收集2000年1月至2005年1月间收治的27例糖尿病溃疡患者作对照组,2005年1月至2007年6月的8例糖尿病溃疡患者为试验组.两组患者均经常规系统的治疗,试验组在创面的黑、黄期采用清创后负压吸引治疗.观察两组创而各分期间的演进情况.比较两组手术Ⅰ期修复率、入院首次及实施负压治疗后1、2、3周创面细菌学检查结果 .观察各期创面组织标本的HE染色和黄、红两期Ⅰ、Ⅲ型胶原纤维苦味酸-天狼猩红染色结果 及对其含量进行图像分析.结果 试验组患者创面各分期的演进速度、于术Ⅰ期修复率均优于以照组(100%比46%,P<0.05).治疗2周后试验组创面末检出致病菌,对照组检出率为66.7%(P<0.05).HE染色显示试验组各期间的演进类似于急性创面愈合过程,且试验组黄期Ⅰ、m型胶原总含量为12.28%,对照组为24.77%(P<0.01).结论 基于WBP方案的负压吸引治疗能促进糖尿病溃疡的创面愈合过程.     

阿糖胞苷纳米粒的制备及其释药规律研究

采用乳化聚合法制备阿糖胞苷纳米粒，研究其体内外释药特性。结果表明阿糖胞苷纳米粒体外释药规律符合双指数方程，有明显的缓释作用。在家兔体内的药物动力学过程符合二室模型，与阿糖胞苷注射剂相比，t1／2β和MRT延长，CL降低，表明阿糖胞苷纳米粒可显著延长阿糖胞苷在体内存留时间，具有明显的缓释特征。     

Movement-related potentials preceding voluntary movement are modulated by the mode of movement selection

In two experiments movement-related cortical potentials preceding voluntary movement were recorded. In experiment 1, subjects performed four motor tasks involving joystick movements. The four tasks differed in complexity (single vs sequential movements) and in the mode of movement selection, i.e., whether a movement or movement sequence was made in fixed or in self-determined directions. The choice of these tasks was based, firstly, on previous electrophysiological studies suggesting an effect of task-complexity on the amplitude of the readiness potential (RP) and, secondly, on previous positron emission tomography (PET) studies showing that activity of the supplementary motor area (SMA) is influenced by the mode of movement selection. The results show that, for single movements, RP amplitude is higher preceding freely selected movements than preceding movements in a fixed direction. In experiment 2 this effect was replicated using button presses instead of joystick movements. The results converge with PET evidence obtained in similar tasks and establish that the RP is modulated by the mode of movement selection. This modulation is probably related to differential involvement of the SMA.     

宫颈细胞学ASCUS/LSIL的临床意义及处理

目的探讨宫颈不典型鳞状上皮，低度鳞状上皮内病变（ASCUS／LSIL）的临床意义及处理方法。方法对中国医学科学院肿瘤医院2004～2006年妇科门诊用TCT（宫颈液基细胞学）的方法检出的254例ASCUS／LSIL以病理结果为金标准进行回顾性分析，其中136例进行了阴道镜检查。结果在140例ASCUS中，宫颈上皮内瘤变（CIN）病变占51．5％，其中高度病变占22．9％，114例LSIL中CIN病变占59．6％，其中高度病变占30．7％，两组资料比较差异无统计学意义，P〉0．05。其中136例中阴道镜诊断炎症47例，低度宫颈上皮内病变53例，高度宫颈上皮内病变36例及病理检查结果炎症55例，低度宫颈上皮内病变41例，高度宫颈上皮内病变40例，阴道镜与病理对照进行了～致性检验，Kappa=0．314，U=0．064，P〈0．05，一致性好。病理证实人乳头状瘤病毒（HPV）阳性的妇女中CIN发生率79％（67／84），而HPV阴性者中CIN发生率43．5％％（74／170），结果显示两组资料比较差异有统计学意义，X^2=29．88，P〈0．05。本组资料中年龄在35～55岁的妇女占83．5％与HPV阳性的妇女年龄高峰一致。结论对ASCUS的患者应与LSIL同样重视，立即进行阴道镜检查以避免22．9％的高度病变的患者漏诊或失访，对35～55岁的HPV感染的妇女应更加重视。     

The adrenergic modulation of firings of respiratory rhythm-generating neurons in medulla-spinal cord preparation from newborn rat

We analysed the modulation of respiratory neurons by adrenaline or noradrenaline (NA) in a newborn rat brainstem-spinal cord preparation. Adrenaline or NA caused a dose-dependent depression of the respiratory rhythm and induced C4 spinal tonic discharges. The inhibitory effect of adrenaline (ED₅₀=0.5 μM) on the respiratory rhythm was stronger than NA (ED₅₀=5 μM). The adrenaline respiratory rhythm depression was partially blocked by the α₁-antagonist prazosin or by the α₂-antagonist yohimbine. The C4 tonic discharge elicited by adrenaline was blocked by the α₁-antagonist prazosin. The direct effects of adrenaline on pre-inspiratory (Pre-I) neurons were examined in a synaptic blockade solution (low Ca), and fifty-six percent of Pre-I neurons were found to continue firing. In low-Ca solution, Pre-I neurons were excited (n=29 of 39) or depressed (n=5 of 39) by adrenaline, and excited by α₁-agonist phenylephrine or depressed by α₂-agonist clonidine. These results suggest that the respiratory rhythm depression under intact network conditions is mediated by some other inhibitory system. The inhibitory effect of adrenaline on the respiratory rhythm was partially blocked by the GABA_A-antagonists bicuculline or picrotoxin, but not by the GABA_B-antagonist phaclofen. The present results suggest that: (1) respiratory rhythm generation is more sensitive to adrenaline than NA through α-adrenergic action of adrenaline; (2) the activity of Pre-I neurons could be directly regulated by excitation via α₁-receptors and inhibition via α₂-receptors; and (3) the depression of the respiratory rhythm by adrenaline is partly mediated by GABA_Aergic neurons. Received: 8 April 1997 / Accepted: 6 October 1997     

Retrospective multicentre study on mechanical and enzymatic preparation of fresh and cryopreserved testicular biopsies

BACKGROUND: Isolation of sperm suitable for ICSI from fresh or frozen-thawed testicular sperm extraction (TESE) can be facilitated by mechanical or enzymatic processing of the samples. METHODS: A retrospective multicentre study was initiated to compare these two approaches. Eleven German centres provided data on their TESE cycles performed during the period 1996/1997. Quality of retrieved sperm, fertilization rates of injected oocytes, embryo quality, resulting pregnancy rates and evolution of pregnancies were evaluated. RESULTS: The percentage of cycles with at least some motile sperm available for injection was higher after mechanical preparation. Independent of the preparation method, fertilization rates were higher for motile compared with immotile sperm or elongated spermatids in all groups and in general higher for cryopreserved versus fresh samples. Embryo quality was significantly better after injection of motile sperm for all treatments and in particular after enzymatic versus mechanical processing of biopsies. Pregnancy rates were identical for embryos derived from sperm prepared mechanically or enzymatically from fresh or cryopreserved testicular samples. The abortion rate (32/172, 18.6%) and the rate of multiple implantations (32/140, 22.9%) were not different from results reported in the literature for ICSI using ejaculated sperm. CONCLUSION: In this retrospective multicentre study, no unequivocal advantage of one over the other preparation method could be identified in 839 ICSI cycles using testicular sperm from 549 patients.     

Influence of Various Immunomodulators on the Induction of Experimental Autoimmune Encephalomyelitis in Lewis Rats

The effect of various immunomodulators on the induction of experimental autoimmune encephalomyelitis (EAE) is evaluated in the Lewis rat. Bordetella pertussis (BP) is the optimal inductor of EAE in this rat strain. Treatment of the animals with BP either before or after or simultaneously with guinea-pig spinal cord preparation (GpSC) resulted in an EAE about two weeks thereafter. Additional injection of living BCG, of CFA, IFA (incomplete Freund's adjuvant) or Vibrio cholerae neuraminidase (VCN) did not augment or mitigate the effect induced by BP or GpSC. Living BCG, IFA, VCN or Corynebacterium parvum (CP) did not induce EAE when given in combination with GpSC but without BP. CFA combined with GpSC only occasionally induced EAE. However, EAE could be induced by the combination of CFA and GpSC or IFA and GpSC in a part of the animals tested if they had been pretreated or simultaneously been injected with living BCG by intravenous route. EAE could not be enhanced by the additional injection of VCN. Surprisingly, most of the animals peracutely died after injection of CFA and BP in combination with GpSC when they had been pretreated with CP. This effect was most pronounced when pretreatment was done on day -4. No acute effect could be seen when CP was given simultaneously to CFA, BP and GpSC. Animals which did not peracutely succumb developed EAE similarly as those in the positive control groups. CP treatment simultaneously with BP but without CFA resulted in a reduction of the EAE specific mortality. This reduction could not be seen if treatment with CP was done after injection of GpSC and BP.     

药用辅料在制剂中的应用概述

药用辅料是药物制剂的基础材料的重要的组成部分,在制剂型和生产中起着关键作用,它不仅赋予药物一定剂型,并且与提高药物的疗效,降低毒副作用有很大的关系,因此,研究开发,合理应用辅仅可提高药物制剂质量和生产技术水平,而且可取得较大的社会及经济效益。