注射用促肝细胞生长素辅料的研究

寻找一种注射用促肝细胞生长素（ＨＧＦ）适用的辅料。方法：以三批不同批次的ＨＧＦ原料液为实验对象,分别通过 Ｆｏｌｉｎ－酚和~３Ｈ－ＴｄＲ掺入法研究了三种辅料： ３％右旋糖酐, ８％甘露醇, ２％右旋糖酐＋ ８％甘露醇对ＨＧＦ多肽含量及活性的影响。结果：８％甘露醇作为辅料时使ＨＧＦ多肽含量测定显著增高,而右旋糖酐则不影响测定结果。三种辅料对ＨＧＦ活性均无显著影响。结论：最终选用３％右旋糖酐作为ＨＧＦ的辅料。     

A novel approach to prepare tripolyphosphate/chitosan complex beads for controlled release drug delivery

A novel approach was developed to improve the mechanical strength of tripolyphosphate (TPP)/chitosan beads prepared under coagulation condition at 4 degrees C in the presence of gelatin. Cross-sectional analysis indicated that the beads had a homogeneous crosslinked structure, as a result the beads were strengthened greatly (the mechanical strength increased more than ten times). Furthermore sodium alginate (a polyanion) can interact with cationic chitosan on the surface of these TPP/chitosan beads to form polyelectrolyte complex film for the improvement of the drug sustained release performances. The loading efficiency of model drugs (brilliant blue and FITC-dextran) in these beads was very high (more than 90%). Crosslinking time, TPP solution pH and other preparation factors had an effect on the drug release performance of beads. The release period of brilliant blue (a poor water soluble dye) was more than 2-months at a fairly constant rate in 0.9% NaCl, 10 mM PBS pH 7.4. However, for FITC-dextran (a water soluble polysaccharide) only 1-2 days in the same conditions. It seems that TPP/chitosan bead prepared by the novel method is a promising formulation for drug delivery.     

氯吡格雷和沙格雷酯联用致血小板减少

1例74岁女性患者行人工血管旁路移植术,术后给予肝素,约8．33U·Kg^-1·min^-1静脉泵入;氯吡格雷50mg,1次／d口服;沙格雷酯100mg,3次／d口服;华法林3mg／d口服。手术次日停用肝素,改为达肝素钠0．4ml,1次／12h皮下注射。术后第7天血小板301×10^9／L,停用达肝素钠,同时加用辛伐他汀20mg／d,氯吡格雷、沙格雷酯及华法林按原剂量口服。术后6个月停用华法林,继续口服其他3种药物,此时复查血小板计数为240×10^9／L。术后9个月复查,血小板计数降至1×10^9／L,白细胞及血红蛋白水平正常。立即停用氯吡格雷和沙格雷酯,继续口服辛伐他汀。停药4周,血小板计数恢复至156×10^9／L。     

Inhibition of human Na(v)1.5 sodium channels by strychnine and its analogs

Strychnine and brucine from the seeds of the plant Strychnos nux vomica have been shown to have interesting pharmacological effects on several neurotransmitter receptors. In this study, we have characterized the pharmacological properties of strychnine and its analogs on human Na_v1.5 channels to assess their potential therapeutic advantage in certain arrhythmias. Among the eight alkaloids, only strychnine and icajine exhibited inhibition potency on the Na_v1.5 channel with the half-maximum inhibition (IC₅₀) values of 83.1 μM and 104.6 μM, respectively. Structure–function analysis indicated that the increased bulky methoxy groups on the phenyl ring or the negatively charged oxygen atom may account for this lack of inhibition on the Na_v1.5 channel. Strychnine and icajine may bind to the channel by cation–π interactions. The substitution with a large side chain on the phenyl ring or the increased molecular volume may alter the optimized position for the compound close to the binding sites of the channel. Strychnine and icajine bind to the Na_v1.5 channel with a new mechanism that is different from TTX and local anesthetics. They bind to the outer vestibule of the channel pore with fast association and dissociation rates at resting state. Strychnine and icajine had little effect on steady-state fast inactivation but markedly shifted the slow inactivation of Na_v1.5 currents toward more hyperpolarized potentials. The property of icajine influencing slow-inactivated state of Na_v1.5 channel would be potential therapeutic advantages in certain arrhythmias.     

注射用头孢哌酮钠-舒巴坦钠致严重迟发型过敏反应1例

1例72岁男性患者因右下肺感染入院,静脉滴注头孢哌酮钠-舒巴坦钠后出现严重迟发型过敏反应。通过对头孢哌酮钠-舒巴坦钠致不良反应的原因进行探讨,为临床合理用药提供参考。     

赖诺普利与依那普利对高血压的疗效比较

９２例原发性Ⅰ和Ⅱ期高血压病人采用随机、单盲方法，分２组治疗。一组用赖诺普利，ｐｏ，２０－８０ｍｇ／ｄ，另一组用依那普利，ｐｏ，１０－４０ｍｇ／ｄ，疗程均为４ｗｋ。降压总有效率和降压幅度：赖诺普利是８９％和２．９／２．０ｋＰａ，依那普利是９７％和３．１／２．１ｋＰａ，２药降压均显著（Ｐ＜０．０１），降压疗效相仿（Ｐ＞０．０５）。不良反应发生率是２９％和３４％，其中最多是干咳。结果提示赖诺普利治疗轻、中度高血压有效、安全。     

小脑皮层神经细胞的体外原代培养

本文探讨了神经细胞培养的方法,建立了稳定的神经细胞培养模型。对培养各阶段的神经细胞进行了观察且系统地描述了它们的形态特征。并对培养的神经细胞的来源、轴突的形成、生长锥的形态和特点、神经细胞和突起聚集的原因等方面进行了讨论。     

解剖钢板和压力螺栓治疗跟骨骨性毁损伤的生物力学稳定性的研究

目的 探讨解剖钢板和压力螺栓(Anatomic Plate and CompressionBolts,APCB)治疗跟骨骨性毁损伤的生物力学稳定性的应用效果.方法 选取经确诊为跟骨粉碎、关节面显著的碎裂移位、跟骨变宽、高度显著的丢失、Bohler角及Gissane角显著的改变的单侧跟骨关节内严重粉碎骨折的患者102例,随机临床对照试验(randomized controlled trials,RCT)分为两组,观察组应用解剖钢板和加压螺栓治疗,对照组采用经标准的外侧L形切口AO解剖钢板和螺钉治疗.结果 观察组的手术时间明显短于对照组(P＜0.05),而Bohler角较对照组改善明显,但两组未发现统计学差异(P＞0.05),手术后负重时间显著地短于对照组(P＜0.05),观察组患者发生术后并发症发生率明显的低于对照组(P＜0.05),而两组患者距下关节炎、AOFAS评分及住院时间均差异无统计学意义(均P＞ 0.05).结论 应用小切口微创解剖钢板及加压螺栓进行加压固定、能够减少手术相关并发症,进行早期功能锻炼治疗跟骨骨性毁损伤是一个合理、稳定性较强,能够获得较为理想有效的治疗效果.     

西立伐他汀降脂治疗及对血小板活化功能、胰岛素抵抗的影响

目的：探讨西立伐他汀对高胆固醇血症患者血脂、血小板活化功能、胰岛素抵抗（IR）的干预作用。方法：对88例高胆固醇血症患者用西立伐他汀治疗4－8wk治疗前后观察血小板颗粒膜蛋白（GMP－140）、空腹血糖（FPG）、空腹胰岛素（FINS）、总胆固醇（TC）、高密度脂蛋白－胆固醇（HDL－C）、低密度脂蛋白－胆固醇（LDL－C）、三酰甘油（TG）,并计算胰岛素敏感指数（ISI）,结果：西立伐他汀能有效降低FBG、FINS、LDL－C、TC、TG、GMP－140,升高ISI（P＜0．05）,但对HDL－C无显著变化（P＞0．05）。结论：西立伐他汀治疗高胆固醇血症或混合性高脂血症患者,在调脂的同时,可抑制血小板活性,改善胰岛素抵抗。     

口腔溃疡豚鼠血清中谷胱甘肽过氧化物酶活性的研究

目的：研究口腔溃疡豚鼠血清中谷胱甘肽过氧化物酶（GSH-PX）的活性。方法：用90%苯酚溶液灼烧豚鼠左侧面颊,造成口腔溃疡模型,观察豚鼠口腔溃疡模型的溃疡面积、溃疡程度及溃疡组织病理变化,测定血清中GSH-PX活性。结果：用苯酚溶液造豚鼠口腔溃疡模型成功,d1～d5,模型组与空白组相比,口腔溃疡程度显著,血清中GSH-PX活性显著降低（P<0.01）。口腔溃疡豚鼠随着时间的变化溃疡面积逐渐缩小,血清中GSH-PX活性逐渐增强。结论：血清中GSH-PX对口腔溃疡的自愈有促进作用。