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    题名 作者 年代 出处 被引量
1Nimodipine对脑外伤后脑水及脑皮质和血清钙含量的影响显示文摘本文观察了脑损伤后不同时间大鼠脑水含量和脑皮质及血清钙含量变化,以及Nimodipine对外伤性脑水肿和钙含量变化的影响。结果表明,脑损伤后6h脑白质水含量巳明显增多,为79.87±0.58(P<0.01),伤后48h达峰值,为81.02±0.51:脑皮质水含量稍有增加。脑皮质及血清钙含量均有不同程度升高,以脑皮质升高较为明显,伤后48h高达24.12±10.22mmol/kg干脑,为对照值的1.8倍.应用Nimodipine治疗,可显著降低脑皮质钙含量,伤后立即接受治疗组为16.78±4.98mmol/kg干脑(P<0.05),脑水肿明显减轻,为78.98±0.89(P<0.01)。徐如祥 易声禹 1992第一军医大学学报1992,12,3:23
2Nimodipine对冷冻伤性脑水肿的脑保护作用显示文摘本文观察了冷冻伤性脑水肿不同时间大鼠脑含水量和伊文思蓝(EB)含量的变化,脑含水量与EB含量之间的关系;以及尼莫地平(Nimodipine,Nim)对冷冻伤性脑水肿脑含水量和EB含量的影响。结果表明:冷冻伤脑含水量和EB含量明显升高,应用Nim治疗后,脑组织水分含量和EB含量明显降低,脑水肿减轻。这为临床颅脑损伤应用Nim治疗提供理论依据。陈立华 曹美鸿 秦天森 袁贤瑞 马建荣 李东升 张明宇 彭泽峰 1997临床神经科学1997,5,1:7
3The efficacy and safety of nimodipine in acute ischemic stroke patients with mild cognitive impairment: a double-blind, randomized,placebo-controlled trial显示文摘Nimodipine might be effective in subcortical vascular dementia(VaD). Its benefit in preventing further cognitive decline in patients with acute ischemic stroke(AIS) and vascular mild cognitive impairment(VaMCI) remains to be established. In this multicenter, double-blind trial, we randomly assigned 654 eligible patients to nimodipine 30 mg three times a day or placebo. The primary outcome was any cognitive decline defined by the changes on the Mini-Mental State Examination(DMMSE à3) or vascular AD assessment scale cognitive subscale(DADAS-cog ! 4) at 6 months. Secondary outcomes included any distribution shift of DADAS-cog, DMMSE or cognitive improvement defined by DADAS-cog à2, or DMMSE ! 0. The primary outcome in the nimodipine group and placebo group were similar for DMMSE à3(4.18% and 7.22%, respectively, P = 0.15) and DADAS-cog ! 4(8.36% and 8.93% respectively,P = 0.88). The distribution shift of DADAS-cog and DMMSE differed significantly between the two groups(P = 0.03 and P = 0.05 respectively). Cognitive improvement occurred in 55.4% in the nimodipine group and 43.6% in the placebo group measured by DADAS-cog à2(Odds Ratio, 1.54; 95% confidence interval[CI] 1.10–2.14, P < 0.01) or 84.0% and 74.6% respectively by DMMSE ! 0(Odds Ratio, 1.79; 95% CI 1.18–2.70, P < 0.01). Nimodipine was associated with better cognitive function in the memory domain. The adverse events rate was similar in two groups. This study is registered with ClinicalTrials.gov,NCT01220622. Nimodipine did not show benefit to prevent cognitive decline in AIS patients with VaMCI, but improved cognition moderately, especially measured in the memory domain.Huaguang Zheng Yilong Wang Anxin Wang Hao Li David Wang Xingquan Zhao Penglian Wang Haipeng Shen Lijun Zuo Yuesong Pan Zixiao Li Xia Meng Xianwei Wang Weixiong Shi Yi Ju Liping Liu Kehui Dong Chunxue Wang Rubo Sui Rong Xue Xiaoping Pan Xiaoyua Niu Benyan Luo Yi Sui Huali Wang Tao Feng Yongjun Wang 2019Science Bulletin2019,64,2:5
4Effect of age on the pharmacokinetics of polymorphic nimodipine in rats after oral administration显示文摘The previous investigation has proved that their existed pharmacokinetic difference between the different crystal forms of the polymorphic drugs after oral administration.However,no systemic investigations have been made on the change of this pharmacokinetic difference,resulted either from the physiological or from the pathological factors.In this paper,we used polymorphic nimodipine(Nim) as a model drug and investigated the effect of age difference(2- and 9-month old) on the pharmacokinetics after oral delivery in rats.As the results shown,for L-form of Nim(L-Nim),the AUC0–24 hin 2-month-old rats was 343.68747.15 ng h/m L,which is 23.36% higher than that in 9-month-old rats.For H-form of Nim(H-Nim),the AUC0–24 hin 2-monthold rats was 140.91719.47 ng h/m L,which is 54.64% higher than that in 9-month-old rats.The AUC0–24 h ratio between H-Nim and L-Nim was 2.44 in 2-month-old rats and 3.06 in 9-month-old rats.Since age difference could result in unparallelled change of the absorption and bioavailability of the polymorphic drugs,the results in this experiment are of value for further investigation of crystal form selection in clinical trials and rational clinical application of the polymorphic drugs.Wenli Liu Xiaona Wang Ruilian Chen Kaixuan Zhang Yao Li Yi Li Duanyun Si Junbo Gong Dianshu Yin Yongli Wang Zhenping Wei Mingshi Yang 2016Acta Pharmaceutica Sinica B2016,6,5:3
5EFFECTS OF NIMODIPINE ON PLATELET AGGREGATION AND THE ACTIVITY OF ENZYMES IN ARACHIDONIC ACID METABOLISM显示文摘The effects of nimodipine on platelet aggregation and arachidonic acid(AA)metabolismwere studied in order to explore its effect on patients with thrombosis or cardiovas-cular disease.The results indicate that nimodipine(50-350μmol/L)significantly inhibitsplatelet aggregation induced by ADP,AA,and ionophore A23187 in a dose dependentmanner.The inhibitory effects induced by ionophore A23187 could be partially antagonizedby calcium(1 mmol/L).When the substrate was AA and the enzyme was supplied bypig lung microsomes,nimodipine(50-400μmol/L)significantly reduced the generation ofTXB2 and 6-keto-PGF1a in parallel.When the substrate was prostaglandin endoperoxide,however,the levels of TXB2 and 6-keto-PGF1awere not significantly altered in the sameconcentration range.The results suggest that nimodipine is a cyclooxygenase inhibitor,andits ability to inhibit platelet aggregation is related to its calcium blocking effect.李箭 汪钟 1990Chinese Medical Sciences Journal1990,8,1:3
6星形胶质细胞存在L-型钙通道的新证据显示文摘以纯化培养的小鼠星形胶质细胞(Astrocyte,AS)为实验材料,采用激光共聚焦钙成像和荧光分光光度计技术,探讨钙激动剂Bay k8644和钙拮抗剂nimodipine对星形胶质细胞胞内钙离子浓度的影响。结果显示,Bay k8644在0.0001、0.001和0.01mmol/L浓度下均可显著增加星形胶质细胞的细胞内钙水平,而nimodipine在0.001、0.01和0.1mmol/L浓度下均可显著降低星形胶质细胞胞内钙水平,并阻止KCl引起的细胞内钙升高。上述结果表明星形胶质细胞对L-型钙通道激动剂和拮抗剂的反应与神经元的反应相似,提示星形胶质细胞胞膜上也存在L-型钙通道。王磊 蔡景霞 2007Zoological Research2007,28,5:2
7Solid dispersion in the development of a nimodipine delayed-release tablet formulation显示文摘Nimodipine(NMD)is a dihydropyridine calcium channel blocker with selectivity for cerebral blood vessels and the major therapeutic indication of NMD is for the prevention and treatment of delayed ischemic neurological disorders and other cerebrovascular disorders,such as stroke which is associated with biological rhythm.This study was mainly designed to solve the drawback of conventional NMD solid dosage form,low bioavailability and limited clinical efficacy,by preparing enteric solid dispersion(SD)and the SD was prepared via melting method.The physical state of the dispersed NMD in the polymer matrix was characterized by differential scanning calorimetry(DSC),powder X-ray diffraction(PXRD)and dissolution studies.Compared with pure drug and physical mixture,the dissolution of NMD-SD was enhanced dramatically(about 80%).Furthermore,in consideration of the biological rhythm of stroke,we first obtained a delayed-release tablet containing NMD-SD by a direct powder compression method.As shown in the dissolution studies,the tablet released less than 10%in the artificial gastric acid in the initial 2 h and released 32.1%,75%,more than 90%at 4,10 and 14 h respectively in the artificial intestinal fluid.This investigation has solved the problems of oral solid dosage forms of NMD,and it has the good industry prospect.Yang Zhao Tiegang Xin Tiantian Ye Xinggang Yang Weisan Pan 2014Asian Journal of Pharmaceutical Sciences2014,9,1:1
8Lamotrigine联合钙通道阻滞剂Nimodipine治疗局灶性脑缺血的实验研究显示文摘目的:观察同时应用钠通道阻滞剂和钙通道阻滞剂对鼠局灶性脑缺血的保护作用。方法:采用单尼龙线线栓法制备鼠大脑中动脉缺血3小时再灌流21小时模型,分别观察lamotrigine(20mg/kg ip),nimodipine(1μg/kg/min iv)以及两者联合应用对在鼠神经功能缺损的恢复、梗塞体积、突触体内游离钙浓度的影响。结果:联合应用lamotrigine和nimodipine缩小大鼠梗塞体积,恢复神经功能缺损较单独应用lamotrigine或nimodipine效果更明显(P<0.05)。结论:联合使用钠通道阻滞阻滞剂和钙通道阻滞剂优于单用其中一种药。承欧梅 胡常林 1998脑与神经疾病杂志1998,6,6:1
9新型钙拮抗剂Nimodipine的质谱研究显示文摘本文报告了新型钙拮抗剂Nimodipine的EIMS谱、HR -EIMS数据和1 3 CNMR(COM .INEPT)谱和数据。根据HREI数据讨论了主要特征碎片离子的可能裂解途径。其中许多碎片离子是由麦氏重排而得。余志立 胡来兴 胡琼莹 王占国 杨细文 曹廷富 周凤珍 2001质谱学报2001,22,2:1
10Research on the pathogenesis of cerebral vasospasm following subarachnoid hemorrhage显示文摘目的 :进一步研究脑血管痉挛的发生机理 ,为临床治疗服务。方法 :采用 1 4只成年家犬 ,实验组 9只 ,对照组 5只 ,通过 2次枕大池注血法建立蛛网膜下腔出血 (SAH)模型。观察痉挛血管的自由基变化、血管活性、血管造影像、超微结构变化。另外 2 0只犬用来观察血管扩张剂的作用。结果 :实验组较对照组自由基含量高 ,血管活性降低 ,血管狭窄 ,管壁损害重。结论 :尼莫地平对急性痉挛有效 ,对慢性痉挛无效 ;慢性血管痉挛是以管壁结构性狭窄为特点。Liu Baiyun Wang Chungcheng Wu Zhongxue Wu Jianzhong 2000白求恩医科大学学报2000,26,5:0
11Modeling the neuro-protection of theaflavic acid from black tea and its synergy with nimodipine via mitochondria apoptotic pathway显示文摘Ischemic stroke presents a leading cause of mortality and morbidity worldwide.Theaflavic acid(TFA)is a theaflavin isolated from black tea that exerts a potentially neuro-protective effect.However,the dynamic properties of TFA-mediated protection remain largely unknown.In the current study,we evaluated the function of TFA in the mitochondria apoptotic pathway using mathematical modeling.We found that TFA-enhanced B-cell lymphoma 2(Bcl-2)overexpression can theoretically give rise to bistability.The bistability is highly robust against parametric stochasticity while also conferring considerable variability in survival threshold.Stochastic simulations faithfully match the TFA dose response pattern seen in experimental studies.In addition,we identified a dose-and time-dependent synergy between TFA and nimodipine,a clinically used neuro-protective drug.This synergistic effect was enhanced by bistability independent of temporal factors.Precise application of pulsed doses of TFA can also promote survival compared with sustained TFA treatment.These data collectively demonstrate that TFA treatment can give rise to bistability and that synergy between TFA and nimodipine may offer a promising strategy for developing therapeutic neuro-protection against ischemic stroke.Dan MU Huaguang QIN Mengjie JIAO Shaogui HUA Tingzhe SUN 2021Journal of Zhejiang University-Science B(Biomedicine & Biotechnology)2021,22,2:0
12The changes of neuronal Ca^(2+) channel and its effects on BBB permeability and cerebral edema associated with brain injury显示文摘ThechangesofneuronalCa^(2+)channelanditseffectsonBBBpermeabilityandcerebraledema associatedwithbraininjuryXuRuxiang(徐如祥);YiSh?..徐如祥 易声禹 1994Journal of Medical Colleges of PLA(China)1994,9,1:0
13a Clinical Observation of Stellate Ganglion Block Used for Migraine张淑珍 高淑琴 王恩真 2001中国组织工程研究2001,15,9:0
14尼莫地平合并泰必利治疗偏头痛95例疗效观察显示文摘尼莫地平(Nimodipine)合并泰必利(Tlapridi)治疗偏头痛未见报道,现将我院使用两药治疗偏头痛的疗效报道如下: 1 资料与方法 1.1 病例选择 符合下列标准的患者作为观察对象:头痛呈周期性发作,发作间歇无头痛;多在青春期前起病;病程在3个月以上,每月发作2次以上;排除其它原因的头痛。 本组95例偏头痛患者,随机分为三组。尼莫地平治疗组30例,男性11例,女性19例,年龄20~55岁,平均年龄45岁;尼莫地平合并泰必利治疗组32例,男性10例。孙传兰 1999药学与临床研究1999,14,2:0
15Effects of calcium antagonist nimodipine on patients with severe craniocerebral trauma显示文摘The authors report the effects of a calcium antagonist, nimodipine, on severe craniocerebral trauma.A total of 488 cases of severe craniocerebral trauma with Glasgow Coma Scale (GCS) 3~8 score were recruited into the clinical study. The patients were divi徐如祥 杨俊 陈长才 1995Journal of Medical Colleges of PLA(China)1995,10,3:0
16Lercanidipine及其他钙离子阻断剂在高血压方面的使用显示文摘1882年Dr.Ringer发现肌肉收缩与体外钙离子浓度有关开始,科学家便想如果可以减少钙进入细胞,就应该能减少肌肉收缩。1962年Dr.AlbrechtFleckenstdn研究发展出第一个钙离子阻断剂-Verapamil,此后,陆陆继继有许多的华学分子被筛选为钙离子阻断剂,如1971年的Nffedipine,1973的Diltiazem。1982年verapamil正式临床许可应用子冠状动脉扩张。而nifedipine、diltiazem也陆续广泛的应用在治疗高血压和心绞痛。钙离子阻断剂大致可以分为dihydropyridinecalciumchannelblocker、benzothiazepines及chenylalkylamines。Nffedipine、diltiazem、verapamil目前仍是处方常用药,经由剂型的改良,发展出长效制剂以克服有效作用时间短和明显的副作用如心肌抑制作用、心跳加速、头痛、脸部潮红、足部水肿、昏睡、便秘等缺点。由nifedipine的结构衍生出的钙离子阻断剂,如felodipine、nimodipine等则是著重在加强心血管选择性,减少心肌抑制作用。但是仍然存在有效作用时间短和作用太快而易导致副作用的缺点。Lercanidipine是属于第三代dihydropyridine类的钙离子阻断剂,由于化学结构上带有巨大的bis-phenylalkylamine侧链,使午lercanidipine比amlodipine,nitrendipine、rimodipme脂溶性更强,能够快速的离开血中蛋自而溶入血管平滑肌的细胞膜中,藉著缓慢作用在细胞膜的L型钙离子通道,让细胞外钙离子无法进入细胞内。2007中国医药技术与市场2007,7,2:0
17钙拮抗剂与学习、记忆显示文摘钙拮抗剂是七十年代发展起来的一类以多种方式影响细胞内Ca2+代谢的药物。由于其作用机制不明,产生了多种命名如钙阻断剂、钙通道阻断剂、钙内流阻断剂、钙抑制剂等.其共同特征是选择性抑制Ca2+跨膜内流。经典的钙拮抗剂可分为苯烷.苯硫氮(艹卓)和双氢吡啶(DHP)三类,用于临床的代表药物分别是异搏定(Ver)。熊鹰 张长城 1995四川生理科学杂志1995,17,Z1:0
18多胺与缺血性神经元损伤的关系及三种药物对神经元的保护作用显示文摘本实验观察全脑缺血大鼠不同再灌流期脑部多胺含量与缺血性神经元损伤的关系,以及Ni-modipine、MK-801、Baclofen治疗对它们的影响。结果发现,腐胺与再灌流神经元损伤密切相关,三种药物均能保护神经元,减轻缺血性损伤,而且又使腐胺含量降低,讨论了作用机理。郑彩梅 黎红华 吕智勇 1995第三军医大学学报1995,17,3:0
19钠通道Na(v)1.6与缺血性脑损伤显示文摘目的通过观察大鼠缺血脑组织中Na(v)1.6表达探讨Na(v)1.6与缺血性脑损伤的关系。方法线栓法制作大鼠脑缺血模型,168只SD大鼠分为假手术组、脑缺血组和钠通道阻滞剂-riluzole、钙通道阻滞剂-ni-modipine治疗组。大鼠脑缺血后6h、1d、2d、3d取材,应用免疫组化检测Na(v)1.6表达,荧光法检测钙离子浓度,氯化三苯四唑染色检测脑梗死体积。结果 Na(v)1.6在脑缺血后6h~1d表达上调,2~3d表达下调;相同时间点nimodipine治疗组与缺血组相比较,Na(v)1.6表达变化不明显;riluzol治疗组Na(v)1.6表达变化明显,差异具有显著性(P<0.05)。riluzol治疗组和nimodipine治疗组钙离子浓度、脑梗死体积均比缺血组降低,riluzol治疗组降低最明显,差异具有显著性(P<0.05)。结论钠离子内流发生在脑缺血的早期阶段;脑缺血后Na(v)1.6表达上调,抑制Na(v)1.6表达可以减轻脑缺血损伤,Na(v)1.6参与了缺血性脑损伤。任丽 王玉凯 黄铭娜 龙赤 黄海鹰 2013中风与神经疾病杂志2013,30,6:0
20Cooperative effect of polyvinylpyrrolidone and HPMC E5 on dissolution and bioavailability of nimodipine solid dispersions and tablets显示文摘Solid dispersion(SD)systems have been extensively used to increase the dissolution and bioavailability of poorly water-soluble drugs.To circumvent the limitations of polyvinylpyrrolidone(PVP)dispersions,HPMC E5 was applied in the formulation process and scaling-up techniques,simultaneously.In this study,SD of nimodipine(NMP)and corresponding tablets were prepared through solvent method and fluid bed granulating one step technique,respectively.Discriminatory dissolution media were used to obtain reliable dissolution results.Meanwhile,the stability study of SDs was investigated with storage under high temperature and humidity conditions.Moreover,the solubility of SDs was measured to explore the effect of carriers.The preparations were characterized by DSC,PXRD,and FTIR.Dramatical improvements in the dissolution rate of NMP were achieved by the ingenious combination of the two polymers.Binary NMP/PVP/HPMC-SDs released steadily,while the dissolution of single NMP/PVP-SDs decreased rapidly in water.The fluid-bed tablets(FB-T)possessed a similar dissolution behavior to the commercial Nimotop TM tablets.The characterization patterns implied that NMP existed in an amorphous state in our SDs.Furthermore,the results of stability tests suggested a better stability of the binary SDs.A special cooperative effect of PVP and HPMC was discovered on dissolution characteristics of NMP SDs and tablets,which could be extended to other drugs henceforth.Finally,the bioavailability of FB-T was evaluated in beagle dogs with Nimotop TM as the reference,and the results showed a higher AUC 0–12h value for FB-T.Zhisu Sun Huicong Zhang Huiyang He Lingling Sun Xiaorui Zhang Qun Wang Kexin Li Zhonggui He 2019Asian Journal of Pharmaceutical Sciences2019,14,6:0
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