RP-HPLC测定长春西汀冻干乳剂的含量及其有关物质

目的建立RP-HPLC进行长春西汀冻干乳剂的含量及有关物质测定方法,为原料与制剂的质量控制提供有效的分析方法。方法采用C18色谱柱（4.6mm×250mm,5μm）,流动相：甲醇-0.5%三乙胺溶液（84∶16,pH8）;检测波长：273nm;流速：1.0ml/min;柱温：室温。结果在选定的色谱条件下,长春西汀与有关物质分离完全;长春西汀在5～50μg/ml内,峰面积与质量浓度线性关系良好,相关系数r2=0.9998,检测限为20ng/ml;冻干乳中平均回收率为100.79%,相对标准差为0.67%（n=9）。结论本法简便、准确、专属性强,可用于长春西汀的有关物质检查及其冻干乳剂的含量测定。     

前列地尔联合长春西汀对后循环缺血性眩晕患者DHI评分、血流流变学及血管内皮功能的影响

目的 探讨前列地尔联合长春西汀治疗后循环缺血性眩晕患者的临床效果.方法 选取2020年1月至2021年1月我院神经内科收治的86例后循环缺血性眩晕患者作为研究对象,随机将其分为对照组与观察组,各43例.对照组给予长春西汀治疗,观察组给予前列地尔联合长春西汀治疗.比较两组患者的临床效果.结果 观察组的治疗总有效率高于对照...     

Preventive effect of vinpocetine on calcifications: atherosclerosis in experimental rabbits

The action of vinpocetine (14-ethoxycarbonyl-(3 alpha, 16 alpha-ethyl)-14, 15 eburnamine) on calcifications in liver, kidney, and CNS tissues from cholesterol-induced atherosclerosis in 16 experimental rabbits was studied. Three of 4 groups (4 rabbits each group) feeding on a cholesterol-rich diet developed atherosclerosis after 3 months. Two of the 4 groups were also fed vinpocetine supplements and analysis by neutron activation method showed a decrease in calcium content in CNS tissues and in liver and kidney. Results suggest that vinpocetine acts to decalcify cholesterol-induced atherosclerotic lesions in these tissues.     

长春西汀对突发性耳聋患者血小板及血液流变学相关指标的影响

目的 探讨长春西汀对突发性耳聋患者血液流变学和血小板相关指标的影响.方法 选择2012年1月至2015年12月收治的突发性耳聋患者54例,按照随机数字法分为对照组和观察组,每组27例.观察组采用长春西汀治疗,20 mg/次/d,静脉滴注;对照组采用丹参注射液治疗,20 ml/次/d,静脉滴注.连续7 d为1个疗程,2组患者均治疗3个疗程.观察治疗前、治疗后7 d、14 d和21 d患者血液流变学指标与血小板相关指标的变化.结果 治疗7 d、14 d、21 d后,观察组患者全血高切黏度、全血低切黏度和血浆黏度显著小于对照组,差异有统计学意义(P<0.05).治疗7 d、14 d、21 d后,观察组患者红细胞聚集指数、血沉方程K值和红细胞电泳指数显著小于对照组,差异有统计学意义(P<0.05).治疗7 d、14 d、21 d后,观察组患者CD62p、CD61、VWF和PAR显著小于对照组,差异有统计学意义(P<0.05).结论 长春西汀用于治疗突发性耳聋能有效改善患者血液流变学和血小板相关指标,对改善耳部微循环发挥着积极的作用.     

长春西汀的大鼠在体肠吸收研究

采用单向灌流技术考察长春西汀的大鼠在体肠吸收性质.结果表明,灌流速度对药物吸收速率常数(Ka)和表观吸收系数(Papp)有极显著影响(P＜0.01);药物浓度对Ka和Papp无显著影响(P＞0.05);药物在全肠道吸收较好,吸收窗主要在小肠,且小肠内无明显的特定吸收部位;羟丙基-β-环糊精在1%～4%范围内对药物的肠吸收无显著影响.     

PET studies on the brain uptake and regional distribution of [11C]vinpocetine in human subjects

OBJECTIVES: Vinpocetine is a compound widely used in the prevention and treatment of cerebrovascular diseases. It is still not clear whether the drug has a direct and specific effect on neurotransmission or its effects are due to extracerebral actions, such as changes in cerebral blood flow. The main objective of the present investigation was to determine the global uptake and regional distribution of radiolabelled vinpocetine in the human brain in order to explore whether it may have direct central nervous system effects. MATERIAL AND METHODS: Three healthy subjects were examined with positron emission tomography and [11C]vinpocetine. The regional uptake was determined in anatomically defined volumes-of-interest. The fractions of [11C]vinpocetine and labelled metabolites in plasma were determined using high pressure liquid chromatography. RESULTS: The uptake of [11C]vinpocetine in brain was rapid and 3.7% (mean; n = 4) of the total radioactivity injected was in brain 2 min after radioligand administration. The uptake was heterogeneously distributed among brain regions. When compared with the cerebellum, an a priori reference region, the highest regional uptake was in the thalamus, upper brain stem, striatum and cortex. Following an initial peak, the total concentration of radioactivity in blood was relatively stable with time, whereas the concentration of the unchanged compound decreased with time in an exponential manner. CONCLUSION: Vinpocetine, administered intravenously in humans, readily passes the blood-brain barrier and enters the brain. Its regional uptake and distribution in the brain is heterogeneous, indicating binding to specific sites. The brain regions showing increased uptake in the human brain correspond to those in which vinpocetine has been shown to induce elevated metabolism and blood flow. These observations support the hypothesis that vinpocetine has direct neuronal actions in the human brain.     

对大鼠在体肠单向灌流技术中重量法的评价

目的:评价重量法在大鼠在体肠单向灌流技术中的应用.方法:以长春西汀为模型药物,采用大鼠在体肠单向灌流技术,对重量法和酚红法计算的净水流量值(NWF)、药物吸收速率常数(Ka)和药物表观吸收系数(Papp)进行比较,并对重量法中收集液在密度修正前后的NWF和Papp值进行比较.结果:重量法计算所得的NWF值显著高于酚红法(P＜0.05),前者计算所得的Ka和Papp值略高于后者(P＞0.05);重量法能显著减少实验误差;对收集液密度进行修正可以进一步提高实验数据的准确性.结论:重量法可以作为大鼠单向灌流在体肠吸收实验中校正灌流液体积的有效方法,它避免了加入"标示物"给实验带来的一系列问题.     

生物样品中长春西汀的测定

本文建立了用反相高效液相色谱法分离并鉴定生物样品中长春西汀的方法。与文献报道方法相比，较为简单，灵敏度、特异性也较高。生物样品标准曲线在５０～８０００ｎｇ／ｍｌ之间有良好线性关系，药物最低检测极限５０ｎｇ／ｍｌ。各生物样品中药物回收率约在９６．１３～１０３．６９％之间，测定结果的变异系数为：日内ＣＶ小于５％，日间ＣＶ小于６％。     

长春西汀双层渗透泵控释片的制备及体外释放度考察

目的制备难溶性药物长春西汀单室双层渗透泵控释片,并对其体外释药影响因素进行考察。方法利用正交设计优化了渗透泵处方,根据不同时间累积释放度对药物的释放情况进行了考察。结果渗透泵控释片的最优处方为长春西汀15 mg、HPMC 140 mg、PEO 65 mg、氯化钠14 mg,包衣增质量24 mg。其体外释药特征符合控释制剂的要求。结论本渗透泵片以渗透压差为释药动力,能在14 h内良好的控制长春西汀零级释放。