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国外医药.合成药.生化药.制剂分册 1984年第5期 310-311页

作者：王建华

异名 Perisalol、SG-75、Sigma 75化学名 N-(2-羟乙基)菸酰胺硝酸酯(?)药效分类抗心绞痛药开发单位 (日)中外制药、三菱油化药品上市厂商 (日)三菱油化药品1984年3月

关键词：高剂量大鼠 nicorandil 本品

nicorandil pretreatment inhibits myocardial apoptosis and improves cardiac function after coronary microembolization in rats

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Journal of Geriatric Cardiology 2018年第9期15卷 591-597页

作者： Wen-Kai HE Qiang SU Jiao-Bao LIANG Xian-Tao WANG Yu-Han SUN Lang LI Department of Cardiology the First Affiliated Hospital of Guangxi Medical University Nanning China

Background nicorandil （NIC） is a vasodilatory drug used to treat angina. However, its efficacy of cardioprotection in coronary mi- croembolization （CME） is largely unknown. This study was undertaken to determine whether nicorandil pretreatment could attenuate myo- cardial apoptosis and improve cardiac function after CME in rats. Methods Forty-five rats were randomly divided into a Sham group, a CME group and a CME ＋ NIC （NIC） group （n = 15 per group）. CME was established by injecting plastic microspheres （42 pm in diameter） into the left ventricle of the rats in all of the groups except the Sham group. The NIC group received nicorandil at 3 mg/kg per day for seven days before the operation. Cardiac fimction was assessed by echocardiography, the expression levels of cleaved caspase-9/8/3 were detected by Western blot, microinfarction area was measured by haematoxylin-basic fuchsin picric acid staining, and myocardial apoptosis was de- tected by TUNEL staining. Results Compared to that in the Sham group, cardiac fimction in the CME group was significantly decreased （P 〈 0.05）. However, compared to the CME group, the NIC group showed improved cardiac function （P 〈 0.05）. The expression levels of cleaved caspase-9/8/3 protein and myocardial apoptosis were dramatically increased in the CME group compared to those in the Sham group （P 〈 0.05）, while the NIC pretreatment group had significantly decreased expression levels of cleaved caspase-9/8/3 protein as well as a de- creased apoptotic rate （P 〈 0.05）. Conclusions NIC pretreatment inhibited CME-induced myocardial apoptosis and improved cardiac func- tion through blockade of the mitochondrial and death receptor-mediated apoptotic pathways.

关键词： Apoptosis Coronary microembolization Cardiac function nicorandil

Bilayer nicorandil-loaded small-diameter vascular grafts improve endothelial cell function via PI3K/AKT/eNOS pathway

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Bio-Design and Manufacturing 2021年第1期4卷 72-86页

作者： Zheng Xing Chen Zhao Chunchen Zhang Yubo Fan Haifeng Liu Key Laboratory for Biomechanics and Mechanobiology of Ministry of Education School of Biological Science and Medical EngineeringBeijing Advanced Innovation Centre for Biomedical EngineeringBeihang UniversityXue Yuan Road No.37Haidian DistrictBeijing 100191China School of Pharmaceutical Sciences Tsinghua UniversityBeijing 100084China Key Laboratory of Biomedical Engineering of Ministry of Education Zhejiang UniversityHangzhou 310027China Zhejiang Provincial Key Laboratory of Cardio-Cerebral Vascular Detection Technology and Medicinal Effectiveness Appraisal Zhejiang UniversityHangzhou 310027China

For the surgical treatment of cardiovascular disease(CVD),there is a clear and unmet need in developing small-diameter(diameter<6 mm)vascular *** our previous work,sulfated silk fibroin(SF)was successfully fabricated ... 详细信息

For the surgical treatment of cardiovascular disease(CVD),there is a clear and unmet need in developing small-diameter(diameternicorandil(NIC),an FDA-approved drug with multi-bioactivity,was loaded in the BLVG to fabricate NIC-loaded *** morphology,chemical composition and mechanical properties of NIC-loaded BLVG were *** results showed that the bilayer structure of NIC-loaded BLVG endowed the graft with a biphasic drug release *** in vitro studies indicated that NIC-loaded BLVG could significantly increase the proliferation,migration and antioxidation capability of endothelial cells(ECs).Moreover,we found that the potential biological mechanism was the activation of PI3K/AKT/eNOS signaling ***,the results effectively demonstrated that NIC-loaded BLVG had a promising in vitro performance as a functional small-diameter vascular graft.

关键词： Bilayer vascular grafts nicorandil Sulfated silk fibroin Endothelial cell function PI3K/AKT/eNOS pathway

Effects of intracoronary injection of nicorandil and tirofiban on myocardial perfusion and short-term prognosis in elderly patients with acute ST-segment elevation myocardial infarction after emergency PCI

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World Journal of Emergency Medicine 2020年第3期11卷 157-163页

作者： Guo-xiong Chen Hong-na Wang Jin-lin Zou Xiao-xu Yuan Department of Cardiology Zhoushan Hospital of Zhejiang ProvinceZhoushan 316000China

BACKGROUND:This study investigated the effects of the intracoronary injection of nicorandil and tirofiban on myocardial perfusion and short-term prognosis in elderly patients with acute ST-segment elevation myocardial infarction(STEMI)after emergency percutaneous coronary intervention(PCI).METHODS:Seventy-eight STEMI patients with age>65 years who underwent emergency PCI were consecutively *** patients received conventional PCI and were randomly divided into a control group and a treatment group(n=39 per group).The control group received an intracoronary injection of tirofiban followed by a maintenance infusion for 36 hours after *** treatment group received intracoronary injection of tirofiban and nicorandil,and then intravenous infusion of tirofiban and nicorandil 36 hours after *** following parameters were measured:TIMI grade,corrected TIMI frame count(c TFC),TIMI myocardial perfusion grade(TMPG),STsegment resolution(STR)rate 2 hours post-operatively,resolution of ST-segment elevation(STR)at 2 hours postoperatively,peak level of serum CK-MB,left ventricular end diastolic diameter(LVEDD)and left ventricular ejection fraction(LVEF)at 7–10 days postoperatively,and major adverse cardiac events(MACEs)in-hospital and within 30 days ***:Compared with the control group,more patients in the treatment group had TIMI 3 and TMPG 3,and STR after PCI was significantly *** treatment group also had significantly lower c TFC,lower infarction relative artery(IRA),lower peak CK-MB,and no reflow ratio after *** treatment group had significantly higher LVEDD and LVEF but lower incidence of MACEs than the control ***:The intracoronary injection of nicorandil combined with tirofiban can effectively improve myocardial reperfusion in elderly STEMI patients after emergency PCI and improve shortterm prognoses.

关键词： Acute ST-elevation myocardial infarction Elderly Emergency coronary intervention nicorandil Tirofiban Myocardial reperfusion

nicorandil as a promising therapeutic option for ventricular arrhythmia:A case report and review of literature

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World Journal of Cardiology 2024年第12期16卷 768-775页

作者： Ling-Yu Bai Ming Zhao Kui-Ying Ma Department of Cardiovascular Medicine Affiliated Hospital of Inner Mongolia University for NationalitiesTongliao 028000Inner Mongolia Autonomous RegionChina

BACKGROUND Ventricular arrhythmia is a common type of arrhythmia observed in clinical *** is primarily characterized by premature ventricular contractions,ventricular tachycardia,and ventricular *** formation or transmission of cardiac electrical impulses in patients affects cardiac ejection *** may present with symptoms such as palpitations,dyspnea,chest discomfort,and reduced exercise *** severe cases,ventricular arrhy-thmia can even lead to ***,prompt treatment is very much essential upon *** symptoms did not improve after previous conventional drugs and electrical defibrillation treatment,but the ventricular arrhythmia was prevented after the addition of *** SUMMARY A 75-year-old female patient was admitted to the hospital because of intermittent chest tightness,shortness of breath for 10 days,and fainting once for 7 *** with laboratory tests and auxiliary examination,the patient was tentatively diagnosed with coronary heart disease or arrhythmia-atrial *** admission,the patient had intermittent ventricular arrhythmia,which was uncontrolled with lidocaine,defibrillation,and ***,when she was treated with nicorandil,the ventricular arrhythmia *** mitigates the action potential duration by facilitating the opening of potassium ion channels,thereby regulating the likelihood of premature and delayed depolar-ization in two distinct phases and subsequently averting the onset of malignant ventricular *** may inhibit ventricular arrhythmia by dilating coronary arteries,improving coronary microcirculation and reducing myocardial *** option for inhibiting ventricular arrhythmias.

关键词： nicorandil Ventricular arrhythmia Electrical storm Phase 2 early after-depolarization Amiodarone Microcirculation Myocardial fibrosis Lidocaine Case report

Effects of nicorandil on myocardial infarct size in patients with ST-segment elevation myocardial infarction undergoing primary percutaneous coronary intervention:study design and protocol for the randomized controlled trial

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Journal of Geriatric Cardiology 2020年第8期17卷 519-524页

作者： Xiao-Si JIANG Li-Chao TIAN Zi-Chao JIANG Yu-Ting ZOU Ping LI Xin-Chun YANG Xi SU Jin-Wen TIAN Bei SHI Zong-Zhuang LI Yong-Jun LI Ren-Qiang YANG Geng QIAN Yun-Dai CHEN Department of Cardiology the First Medical Center of Chinese PLA General HospitalBeijingChina The School of Medicine Nankai UniversityTianjinChina Department of Cardiology the First People's Hospital of YunlinGuangxiChina Department of Cardiology Beijing Chaoyang HospitalCapital Medical UniversityBeijingChina Department of Cardiology Wuhan Asia Heart HospitalWuhanChina Department of Cardiology Hainan Hospital of PLA General HospitalHainanChina Department of Cardiology Affiliated Hospital of Zunyi Medical CollegeGuizhouChina Department of Cardiology Guizhou Provincial People's HospitalGuizhouChina Department of Cardiology the Second Hospital of Hebei Medical UniversityHebeiChina Department of Cardiology the Second Affiliated Hospital of Nanchang UniversityJiangxiChina

Previous studies have shown that nicorandil has a protective effect on ***,there is no study to investigate whether perioperative intravenous nicorandil can further reduce the myocardial infarct size in patients with ST-segment elevation myocardial infarction(STEMI)compared to the current standard of percutaneous coronary intervention(PCI)*** CHANGE(China-Administration of nicorandil Group)study is a multicenter,prospective,randomized,double-blind and parallel-controlled clinical study of STEMI patients undergoing primary PCI in China,aiming to evaluate the efficacy and safety of intravenous nicorandil in ameliorating the myocardial infarct size in STEMI patients undergoing primary PCI and provide evidence-based support for myocardial protection strategies of STEMI patients.

关键词： Cardiovascular disease Myocardial infarct size nicorandil Primary percutaneous coronary intervention ST-segment elevation myocardial infarction

Identification and Determination of nicorandil and its Degradation Products by HPLC and GC/MS

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Chinese Chemical Letters 2006年第8期17卷 1057-1060页

作者： Zhong Zhou CHENG Ze Hui JIA Yan CHEN Li Ying CHEN Hua LI Institute of Analytical Science Northwest University Xi＇an 710069 Xi＇an Libang Pharmaceuticals Co. Ltd Xi＇an 710075

A rapid and sensitive HPLC-DAD method is developed for simultaneous determination of nicorandil and its degradation products, N-（2-hydroxyethyl） nicotinamide, nitrate ion and nicotinic acid, using nicotinamide （NT） as internal standard, at wavelength 204 nm. Nicotinic acid is identified by HPLC and GC/MS. The method can also be applied to study kinetic of degradation processes of nicorandil in storage.

关键词： nicorandil degradation HPLC GC/MS UV.

Design and evaluation of nicorandil extended-release tablet

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Asian Journal of Pharmaceutical Sciences 2015年第2期10卷 108-113页

作者： Ju-Young Kim Chun-Woong Park Beom-Jin Lee Eun-Seok Park Yun-Seok Rhee College of Pharmacy Woosuk UniversityWanju-gun 565-701Republic of Korea College of Pharmacy Chungbuk National UniversityCheongju 361-763Republic of Korea College of Pharmacy Ajou UniversitySuwon 443-749Republic of Korea School of Pharmacy Sungkyunkwan UniversitySuwon 440-746Republic of Korea College of Pharmacy and Research Institute of Pharmaceutical Sciences Gyeongsang National UniversityJinju 660-701Republic of Korea

The aim of this study was to design and evaluate extended-release formulations of a model drug,nicorandil,in order to achieve the desired steady-state plasma concentration of drug in *** was employed to estimate optimum dissolution and absorption rate of *** dissolution test was employed using pH 1.2,4.0,6.8 buffer solution,or water,to measure the in vitro release behaviors of nicorandil formulations.A single dose(15 mg)of each formulation was orally administered to four beagle dogs under fasted conditions,and the pharmacokinetic parameters were *** in vitro/in vivo relationship of the extended-release formulation was confirmed using in vitro dissolution profiles and plasma concentrations of drug in beagle *** was released completely within 30 min from the immediate-release tablets and released for 24 h from the extended-release *** nicorandil plasma concentration could be modified by adjusting the drug release rate from the extended-release *** release rate of nicorandil was the rate-limiting step in the overall absorption of drug from the extendedrelease *** results highlight the potential of a nicorandil extended-release formulation in the treatment of angina pectoris.

关键词： nicorandil In vitro In vivo Pharmacokinetic Extended-release

Cerebral protective effect of nicorandil premedication on patients undergoing liver transplantation

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Hepatobiliary & Pancreatic Diseases International 2012年第2期11卷 132-136页

作者： Yun-Fei Xia,Zheng-Ping Wang,Ya-Chun Zhou,Tao Yan and Shi-Tong Li Department of Anesthesiology, Shanghai First People’s Hospital, Medical College, Shanghai Jiaotong University, Shanghai 200080, China Department of Anesthesiology Shanghai First People's Hospital Medical College Shanghai Jiaotong University Shanghai 200080 China Shanghai China

BACKGROUND:Neurological injury is a common complication in the early period after liver transplantation,posing an enormous obstacle to treatment efficiency and patient *** is a mitochondrial ATP-sensitive potassium channel(mitoK ATP) *** has been reported to be effective in reducing brain injury in recent ***,it is still unclear whether nicorandil has cerebral protective effect in patients undergoing liver ***:Fifty patients scheduled for liver transplantation were randomly divided into a nicorandil group(group N)(n=25),in which patients received 10 mg nicorandil through a nasogastric tube 30 minutes before induction of anesthesia,and a control group(group C)(n=25) who received 10 mL normal *** Mini-Mental State Examination(MMSE) was performed before anesthesia(day 0),and on days 3 and 7 after *** samples were obtained before induction of anesthesia(T1),and at 12(T2) and 36 hours(T3) after surgery for determination of serum neuron-specific enolase(NSE) and S100β protein(S100β) ***:During surgery,5 patients in each group were eliminated due to severe reperfusion or renal ***,20 patients remained in each *** MMSE scores after operation were significantly lower than those before operation in group ***,there was no difference at days 3 and 7 compared with day 0 in group *** NSE concentrations after surgery were significantly higher than baseline(at T1) in both groups,except at T3 in group *** S100β concentration after surgery was significantly higher than baseline(at T1) in both *** MMSE scores at days 3 and 7 in group N were significantly higher than those in group *** concentrations of serum NSE and S100β at T2 and T3 in group N were significantly lower than those in group ***:Oral nicorandil,as a premedication before liver transplantation,improves postoperative MMSE *** also attenuates the increase of NSE and S100β

关键词： nicorandil premedication liver transplantation cerebral protection

Efficacy and prognostic impact of Pericarpium Trichosanthis injection combined with nicorandil for intractable angina pectoris in elderly patients: A retrospective study

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World Journal of Cardiology 2023年第12期15卷 633-641页

作者： Jun Li Mo-Wei Kong Yu-Yu Xie Ze-Bi Wang Li Xu Guo-Xiang He Department of Cardiology Guiqian International General HospitalGuiyang 550018Guizhou ProvinceChina Department of Dermatology Guiqian International General HospitalGuiyang 550018Guizhou ProvinceChina

BACKGROUND Coronary artery disease(CAD)is a leading cause of global cardiovascular *** angina pectoris,a manifestation of CAD,requires effective drug *** Trichosanthis injection,a traditional Chinese medicine,improves cardiovascular symptoms,while nicorandil alleviates spasms and *** have potential in treating *** To investigate the therapeutic effects of combining Pericarpium Trichosanthis injection and nicorandil in elderly patients suffering from refractory angina caused by coronary heart *** A retrospective analysis was conducted on the data of 130 patients diagnosed with refractory coronary heart *** on the different treatment regimens administered during hospitalization,the patients were divided into a control group(58 cases)and a study group(72 cases).The control group received conven-tional treatment,which included aspirin,statins,and nitrate *** addition to the conventional medication,the study group received a combination treatment of Pericarpium Trichosanthis injection and *** After treatment,the study group showed significantly higher left ventricular ejection fraction and cardiac output,and lower brain natriuretic peptide and C-reactive protein levels compared to the control *** study group also exhibited improvements in angina,quality of life,exercise endurance,and lipid *** logistic regression analysis revealed a relationship of lipid levels and heart function with the combined *** patients in the study group experienced headaches during treatment,but no significant adverse reactions were ***-up showed that the treatment was well-tolerated,with no drug-related adverse reactions *** Combination of Pericarpium Trichosanthis injection and nicorandil is more effective than conventional treatment in improving symptoms and heart function in elderly patients with refractory angina pectoris.

关键词： Pericarpium Trichosanthis injection Coronary heart disease Intractable angina pectoris nicorandil