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Journal of Zhejiang University-Science B(Biomedicine & Biotechnology) 2021年第2期22卷 123-135页

作者： Dan MU Huaguang QIN Mengjie JIAO Shaogui HUA Tingzhe SUN School of Life Sciences the Province Key Laboratory of the Biodiversity Study and Ecology Conservation in Southwest AnhuiAnqing Normal UniversityAnqing 246133China

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.

关键词： Theaflavic acid(TFA) Nimodipine Ischemic stroke Apoptosis Synergy

The efficacy and safety of Nimodipine in acute ischemic stroke patients with mild cognitive impairment: a double-blind, randomized,placebo-controlled trial

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Science Bulletin 2019年第2期64卷 101-107页

作者： 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 Beijing Tiantan Hospital Capital Medical University China National Clinical Research Center for Neurological Diseases OSF Saint Francis Medical Center Peoria Faculty of Business and Economics University of Hong Kong The First Hospital Liao Ning Medical College The General Hospital Tianjin Medical University Guangzhou First People’s Hospital School of Medicine South China University of Technology The First Hospital of Shanxi Medical University The First Hospital Zhejiang Medical University Shenyang First People’s Hospital Shenyang Medical College Dementia Care & Research Center Peking University Institute of Mental Health

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 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.

关键词： Nimodipine Acute ischemic stroke Mild cognitive impairment Cognitive decline Prevention

Effect of age on the pharmacokinetics of polymorphic Nimodipine in rats after oral administration

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Acta Pharmaceutica Sinica B 2016年第5期6卷 468-474页

作者： Wenli Liu Xiaona Wang Ruilian Chen Kaixuan Zhang Yao Li Yi Li Duanyun Si Junbo Gong Dianshu Yin Yongli Wang Zhenping Wei Mingshi Yang School of Chemical Engineering and Technology Tianjin University State Key Laboratory of Drug Delivery Technology and Pharmacokinetics Tianjin Institute of Pharmaceutical Research Pharmaceutical Research Institute Shijiazhuang No.4 Pharmaceutical Company Faculty of Pharmaceutical Science University of Copenhagen

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.

关键词： Nimodipine Age difference Polymorphic drug Pharmacokinetics Crystal form

Cooperative effect of polyvinylpyrrolidone and HPMC E5 on dissolution and bioavailability of Nimodipine solid dispersions and tablets

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Asian Journal of Pharmaceutical Sciences 2019年第6期14卷 668-676页

作者： Zhisu Sun Huicong Zhang Huiyang He Lingling Sun Xiaorui Zhang Qun Wang Kexin Li Zhonggui He Wuya College of Innovation Shenyang Pharmaceutical UniversityShenyang 110016China School of Pharmacy Shenyang Pharmaceutical UniversityShenyang 110016China Examination and Certification Center Liaoning InspectionShenyang 110036China

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.

关键词： Solid dispersion Nimodipine HPMC E5 Fluid-bed Bioavailability

Clinical efficacy and mechanism of action of hyperbaric oxygen therapy combined with Nimodipine in the treatment of gestational hypertension in pregnant women

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Chinese Journal of Nautical Medicine and Hyperbaric Medicine 2024年第2期31卷 237-240页

作者： Xu Q. Lu L. Bai B. Department of Obstetrics Linyi People’s Hospital Linyi 276003 China Department of Reproductive Medicine Linyi People's Hospital Linyi 276003 China

Objective To investigate the clinical efficacy and mechanism of action of hyperbaric oxygen（HBO）therapy combined with Nimodipine in the treatment of gestational hypertension in pregnant women.Methods A total of 98 pregnant women with gestational hypertension admitted to the Department of Obstetrics of Linyi People’s Hospital from July 2020 to May 2021 were selected as the study subjects. They were divided into an observation group and a control group according to the random number table method，with 49 cases in each group. The patients in the control group were given treatment with intravenous injection and oral administration of Nimodipine，while the patients in the observation group received HBO therapy in addition to the treatments of the control group. The clinical efficacy，blood pressure，pregnancy outcome，and occurrence of adverse reactions were compared between the two groups. Enzyme-linked immunosorbent assay was used to detect the levels of serum T-bet and pregnancy-associated plasma protein-A（PAPP-A）before and after treatment in both groups. Results The clinical total effective rate of the observation group was significantly higher than that of the control group（χ2=5.018，P=0.025）. The diastolic blood pressure（DBP），systolic blood pressure（SBP），and levels of serum T - bet and PAPP - A in the observation group were significantly lower than those in the control group after treatment（P0.05）. Conclusion HBO therapy combined with Nimodipine can improve the clinical total effective rate in the treatment of gestational hypertension in pregnant women，reduce blood pressure，improve pregnancy outcome，b

关键词： Gestational hypertension Hyperbaric oxygen Nimodipine Pregnancy outcome

Solid dispersion in the development of a Nimodipine delayed-release tablet formulation

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Asian Journal of Pharmaceutical Sciences 2014年第1期9卷 35-41页

作者： Yang Zhao Tiegang Xin Tiantian Ye Xinggang Yang Weisan Pan Department of Pharmaceutics School of PharmacyShenyang Pharmaceutical University103 Wenhua RoadShenyang 110016China

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.

关键词： Nimodipine Solid dispersion Delayed-release Dissolution test

Effect of baicalin and berberine on transport of Nimodipine on primarycultured,rat brain microvascular endothelial cells

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Acta Pharmacologica Sinica 2007年第4期28卷 573-578页

作者： Dong-mei ZHANG Hai-yan LIU Lin XIE Xiao-dong LIU Center of Drug Metabolism and Pharmacokinetics,China Pharmaceutical University,Nanjing 210009,China CenterofDrugMetabolismandPharmacokinetics ChinaPharmaceuticalUniversityNanjing210009China

Aim:To investigate whether baicalin and berberine affects the transport ofNimodipine (NMD) across the blood-brain barrier (BBB).Methods:Primary-cultured,rat brain microvascular endothelial cells (rBMEC) were used as an invitro model of the BBB.When cells became confluent,the steady-state uptake ofNMD by rBMEC with or without baicalin and berberine was measured.The ef-fects of baicalin and berberine on the efflux of NMD from rBMEC were also studied.Results:Baicalin (2-5 μg/mL) increased the uptake of NMD,and baicalin (10-20μg/mL) decreased the uptake.The steady-state uptake of NMD was higher thanthat of control group in the presence of 0.01-1 μg/mL berberine,but was lower inthe presence of 2-10 μg/mL berberine.Conclusion:The bidirectional effect ofbaicalin and berberine on the uptake of NMD by rBMEC was found.Higherconcentration showed an inhibitory effect,and lower concentration demonstratedan increasing effect.

关键词： Nimodipine baicalin berberine P-glycoprotein

Distribution of Nimodipine in brain following intranasal administration in rats

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Acta Pharmacologica Sinica 2004年第4期25卷 124-129页

作者： Qi-zhi ZHANG, Xin-guo JIANG2, Chun-hua WU Department of Pharmaceutics, School ofPharmacy, Fudan University, Shanghai 200032, China Department of Pharmaceutics School of Pharmacy Fudan University

AIM: To determine whether nasally applied Nimodipine (NM) could improve its systemic bioavailability and be transported directly from the nasal cavity to the brain. METHODS: NM was administered nasally, intravenously (iv), and orally to male Sprague-Dawley rats. At different times post dose, blood, cerebrospinal fluid (CSF), and brain tissue samples were collected, and the concentrations of NM in the samples were analyzed byHPLC. RESULTS: Oral systemic bioavailability of NM in rats was 1.17 %, nasal dosing improved bioavailibility to 67.4 %. Following intranasal administration, NM concentrations in olfactory bulb (OB) within 30 min post dose were found significant higher than in the other brain tissues. However, similar NM levels in different brain regions were observed after iv injection. AUC in CSF and OB from the nasal route was 1.26 and 1.39 fold compared with the iv route, respectively. The brain-to-plasma AUC ratios were significantly higher after nasal administration than after iv administration (P<0.01). CONCLUSION: Nasally administered NM could markedly improve the bioavailability and a fraction of the NM dose could be transported into brain via the olfactory pathway in rats.

关键词： intranasal administration Nimodipine olfactory bulb olfactory pathways

Effects of glutamate and Nimodipine on survival rate of embryonic rat neuronal stem cells cultured in vitro

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Neural Regeneration Research 2008年第12期3卷 1286-1289页

作者： Xiaohong Lu Hailong Fu Qiang Sun Li Cui Dihui Ma Weihong Lin Department of Neurology First Hospital Jinlin University Changchun 1300021 Jilin Province China

BACKGROUND： At least three types of calcium ion channel （T, N, and L） have been recognized in nerve ceils, but only the L type of channel is sensitive to drugs. Theoretically, Nimodipine can lead to L-type channel inactivation and prevent calcium ion inflow, thereby exhibiting protective effects on nerve cells. OBJECTIVE： To observe the protective effects of Nimodipine on glutamate-induced injury to embryonic rat neural stem cells, and to make a comparison with MK-801, a nonselective glutamate receptor antagonist. DESIGN, TIME AND SETTING： The present in vitro experiment pertaining to neural stem cells was performed at the Department of Neurology, First Hospital, Jilin University between January 2005 and December 2006. MATERIALS： Glutamate was sourced from the Shanghai Biological Research Institute of the Chinese Academy of Sciences. Nimodipine was provided by Bayer Company, Germany. Brain tissue was taken from Wistar rats on day 15 of gestation for isolation and culture of neural stem cells. METHODS： Passage 2 neural stem cell spheres were taken for preparation of single cell suspension. The prepared single cell suspension was divided into 4 groups：（1） Normal control, normally cultured. （2） Glutamate, cultured with 50, 100, 200, 500, and 1 000 μmol/L glutamate. （3） Nimodipine, received a 30- minute Nimodipine [1×（10^-8-10^-2） g/L] culture followed by a glutamate （200 μmol/L） treatment step. （4） MK-801, given as 30- minute MK-801 （100 μmol/L） culture, followed by a glutamate （200 μmol/L） treatment step. MAIN OUTCOME MEASURES： Determination of glutamate-induced cell death by methyl thiazolyl tetrazolium （MTT） assay; calculation of neural stem cell survival rate following addition of Nimodipine. RESULTS： The survival rate of neural stem cells was approximately 25.26% following 24 hour 50 μmol/L glutamate culture and gradually decreased as the glutamate dose increased （P 〈 0.05 0.01）. Only 9.27% of neural stem cells survived when the glutamate dose was 1000 μmol/L. The survival rate of neural stern cells was signif

关键词： neural stem cells culture glutamate injury Nimodipine protective effects

Nimodipine Modulates Bcl-2 and Bax mRNA Expression after Cerebral Ischemia

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Journal of Huazhong University of Science and Technology(Medical Sciences) 2004年第2期24卷 170-172页

作者：刘昌勤周瑞祥孙圣刚 Department of Neurology Union Hospital Tongji Medical College Huazhong University of Science and Technology

In order to explore whether the member of Bcl-2 gene family, for example, Bcl-2 and Bax, are induced after cerebral ischemia, and whether expression of genes can be modulated by calcium-antagonist, the rat cerebral ischemic models were made by occluding left middle cerebral artery. The expression of Bcl-2 and Bax mRNA was measured by RT-PCR method. After middle cerebral artery occlusion (MCAO), the expression of both Bcl-2 and Bax mRNA were induced. Level of Bcl-2 mRNA increased steadily and level of Bax mRNA increased gradually at first, reached a peak after 24 h, then decreased slowly. After administration of Nimodipine, Bcl-2 mRNA was up-regulated in the hippocampus 6 and 24h after ischemia, while Bax mRNA was down-regulated 6 and 24 h after ischemia. Focal cerebral ischemia can induce proto-oncogenes to express, which was associated with apoptosis. Calcium-antagonist can up-regulate Bcl-2 mRNA and down-regulate Bax mRNA. The increased ratio of Bcl-2 and Bax mRNA may contribute to the anti-apoptic effect of Nimodipine. The study indicates that pharmacological modulation of Bcl-2 family member expression could become a new strategy to manage neuronal damage.

关键词： cerebral ischemia Nimodipine modulate Bcl-2 and Bax mRNA