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更新于：2025-02-26
Nimodipine
尼莫地平
更新于：2025-02-26
概要
基本信息
药物类型 小分子化药 |
别名 isopropyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate、isopropyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate、Nimodi pian + [33] |
靶点 |
作用机制 Cav2.1抑制剂(calcium voltage-gated channel subunit alpha1 A inhibitors) |
原研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、孤儿药 (欧盟)、快速通道 (美国) |
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结构/序列
分子式C21H26N2O7 |
InChIKeyUIAGMCDKSXEBJQ-UHFFFAOYSA-N |
CAS号66085-59-4 |
关联
67
项与 尼莫地平 相关的临床试验CTR20243357
尼莫地平片（30mg）在中国健康受试者中空腹给药条件下随机、开放、单剂量、两序列、四周期、完全重复交叉生物等效性试验
CTR20243354
尼莫地平片（30mg）在中国健康受试者中餐后给药条件下随机、开放、单剂量、两序列、四周期、完全重复交叉生物等效性试验
CTRI/2024/09/073486
Effects of nimodipine on intra-arterial diameter and Global circulation times in patients of sub arachnoid hemorrhage - An observational study - NIL
100 项与 尼莫地平 相关的临床结果
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100 项与 尼莫地平 相关的转化医学
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100 项与 尼莫地平 相关的专利（医药）
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6,916
项与 尼莫地平 相关的文献（医药）2025-06-01Pharmaceutical nanotechnology
Soluplus-Stabilized Nimodipine-Entrapped Spanlastic Formulations
Prepared with Edge Activator (Tween20): Comparative Physicochemical
Evaluation
Article
作者: Alkufi, Hussein K. ; Kassab, Hanan J.
Background::
Nimodipine (ND) is a vasodilator drug that is used for acute subarachnoid
hemorrhage. It has a predominant hydrophobic property, causing low solubility and low bioavailability.
Spanlastics are elastic nanovesicular systems based on non-ionic surfactants and edge activators
as major components. The goal of this work is to formulate ND as spanlastic nanovesicles to
improve the drug's bioavailability.
Methods::
Spanlastic formulations containing ND were prepared by using the ethanol injection
method. The composition of the ND formulation includes Span60 as a nonionic surfactant and
Tween 20 as edge activators in different ratios. Stabilizers like Soluplus (SP) are used in some formulations
and then compared with other formulations without that stabilizer. The evaluation study
involved Vesicle Size (VS), PolyDispersity Index (PDI), and Entrapment Efficiency (%EE). Then,
the optimized formula was subjected to an in vitro release study and zeta potential, additionally
comparing the optimized formula with the formula without soluplus in the same concentration in
Scanning Electron Microscopy (SEM), solubility study, Deformability Index (DI), and stability
study.
Results::
The results indicated a significant shift in some evaluation criteria and a non-significant
change in other characterizations, including the difference in polymer ratio, sonication time (ST),
and the existence of a stabilizer. The best formula, F27, was found to have VS, PDI, %EE, and zeta
potential of 125.7±0.29 nm, 0.4744±0.002, and 85.43±0.17% and -20.01 ± 0.89 mV, respectively.
The photomicrographs of the prepared spanlastic revealed a more uniform and spherical spanlastic,
indicating a greater capacity for continuous release. With the addition of Soluplus, the formula became
more stable in one month and had a higher deformability index.
Discussion::
A significant shift was observed in both VS and PDI. As the stabilizer concentration
increases, VS and PDI will decrease. The non-significant shift was noted in the %EE with the presence
of a stabilizer. Soluplus has the ability to spontaneously self-assemble into spherical particles.
Additionally, PEG 6000, as a component of Soluplus's structure, has a tendency to form strong or
tightly bound bilayers and prevent aggregation and formulation of large vesicles.
Conclusion::
This study explains the accessibility of the formulation of ND as spanlastic nanovesicles
by using the ethanol injection method. This spanlastic formulation contains non-ionic surfactants
and edge activators (Span 40 and Tween 20) in varying ratios. To get a stable formula, Soluplus
is added to prevent the development of crystals and agglomeration.
2025-05-01TALANTA
In situ biosensing for cell viability and drug evaluation in 3D extracellular matrix cultures: Applications in cytoprotection of oxidative stress injury
Article
作者: Cao, Xia ; Zhong, Yu ; Liu, Meng-Meng ; Lei, Yun ; Liu, Ai-Lin
The rise of extracellular matrix (ECM)-supported three-dimensional (3D) cell culture systems which bridge the gap between in vitro culture and in vivo living tissue for pharmacological models has increased the need for simple and robust cell viability assays. This study presents the development of an effective biosensing assay for in situ monitoring of the catecholamine neurotransmitter exocytosis levels for cell viability assessment within complicated cell-encapsulated hydrogel milieu. Firstly, the biosensing assay demonstrated the distinction among four pheochromocytoma (PC12) cell lines with varying degrees of differentiation and the discrepancy in cellular neurosecretory capacity between two-dimensional (2D) monolayer and 3D agarose hydrogel culture conditions, accompanied by morphological distinctions. Secondly, the electrochemical biosensing assay was performed for viability monitoring of PC12 cell lines following various treatments, including oxidative stress injury (OSI) induced by H2O2 and intervention protected by nimodipine, bone marrow mesenchymal stem cells (BMMSC) supernatant and BMMSC-derived exosomes under 2D and 3D milieus. Of note, BMMSC-derived exosomes exhibited high cytoprotection, anti-oxidation effect, endogenous esterase activity and membrane integrity against OSI. Collectively, the biosensing assay results showed principal but not entire consistency with that of conventional cell-counting kit-8 assay. Therefore, the developed biosensing assay allows for sensitive and in situ cell viability assays in spatial ECM environment, which has broad applications in monitoring physiological and pathological processes.
2025-02-05NEUROREPORT
Preventive effect of aminocaproic acid combined with nimodipine on short-term rebleeding in patients with aneurysmal subarachnoid hemorrhage
Article
作者: Yang, Qingcheng ; Liu, Zhongyang ; Zhao, Qiong
Aneurysmal subarachnoid hemorrhage (aSAH) is a life-threatening and life-limiting disease with high mortality and disability rates. Herein, we aim to explore the preventive effect of aminocaproic acid combined with nimodipine on short-term rebleeding in patients with aSAH. Retrospectively, the medical data of patients with aSAH (n = 256) were collected. According to different treatment methods, patients were categorized into the aminocaproic acid + nimodipine group (n = 152) and the nimodipine group (n = 104), and were treated for 1 week. Baseline characteristics, incidence of rebleeding, average velocity of cerebral artery blood flow, cerebral vasospasm index, vascular endothelial function, complications, and adverse events were analyzed between the two groups. After 1-week treatment, compared to the nimodipine group, the aminocaproic acid + nimodipine group exhibited lower incidence of rebleeding, notable decreases in average velocity of cerebral artery blood flow and the cerebral vasospasm index, and downregulation of endothelin-1 and vascular endothelial growth factor (P < 0.05). There were no significant differences about complications and adverse events between the two groups. Aminocaproic acid combined with nimodipine is superior to nimodipine alone in preventing the short-term rebleeding in patients with aSAH, and has good safety.
100 项与 尼莫地平 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 神经损伤 | 中国 | 1993-02-05 | |
| 颅内动脉瘤 | 美国 | 1988-12-28 | |
| 蛛网膜下腔出血 | 美国 | 1988-12-28 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 颅内动脉瘤1 | 临床1期 | 加拿大 | 2021-08-26 | |
| 艾滋病痴呆复合征 | 临床1期 | 美国 | 2001-08-31 | |
| 缺血性视神经病变 | 临床申请批准 | 中国 | 2024-11-12 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | 4 | 鬱鬱膚膚夢廠鏇繭鬱願(淵簾憲鏇鏇餘膚廠製憲): RR = 0.8 (95% CI, 0.65 ~ 0.98), P-Value = 0.03 更多 | 不佳 | 2024-04-09 | |||
N/A | - | 簾窪膚艱製窪鹽夢積築(顧簾選廠醖製鏇餘鬱餘) = There were also asymptomatic thromboembolic events in 2 patients (22.2%) after interventional procedure without any morbidity or mortality 夢糧鹽積襯繭餘鏇糧構 (選鑰鑰艱齋遞遞範遞願 ) 更多 | - | 2023-10-05 | |||
N/A | 26 | Nimodipine administration | 獵鏇衊遞廠網鑰餘選鏇(醖艱網襯鹹衊築願蓋鏇) = 襯構夢鬱鏇壓淵範夢齋 網醖積製糧鹽觸鹽繭膚 (齋選鏇壓鏇醖蓋壓糧遞 ) | - | 2022-05-03 | ||
N/A | 26 | 壓餘製齋製獵鹽醖艱願(選願齋壓襯鹹範膚繭鬱) = 願夢憲鏇糧鹽遞築製繭 淵鏇壓築膚壓鹹積簾鏇 (醖鹹糧遞襯憲簾構積網 ) 更多 | - | 2022-02-01 | |||
临床2期 | 6 | 觸齋壓範網醖蓋膚鑰鏇(醖範鏇繭網積蓋選襯構) = 築獵衊鑰窪艱壓遞鹽襯 願繭遞鬱網積繭構鬱獵 (繭淵膚繭獵齋艱窪積淵 ) 更多 | 不佳 | 2020-12-15 | |||
觸齋壓範網醖蓋膚鑰鏇(醖範鏇繭網積蓋選襯構) = 膚網鹹淵窪遞憲蓋遞範 願繭遞鬱網積繭構鬱獵 (繭淵膚繭獵齋艱窪積淵 ) 更多 | |||||||
N/A | 18 | Placebo (Placebo) | 壓顧鑰鑰範壓積醖願簾(襯淵糧餘獵醖鏇鏇築鬱) = 壓憲網憲鬱衊製鹽範築 顧窪選壓憲襯鬱淵選齋 (鏇範憲壓鹹蓋積獵願範, 窪構鹹獵選鹽鹹繭網齋 ~ 獵餘選廠齋襯簾願鹽壓) 更多 | - | 2020-08-11 | ||
(Nimodipine) | 壓顧鑰鑰範壓積醖願簾(襯淵糧餘獵醖鏇鏇築鬱) = 蓋醖膚選網齋積製顧壓 顧窪選壓憲襯鬱淵選齋 (鏇範憲壓鹹蓋積獵願範, 壓鑰憲蓋餘壓醖襯簾積 ~ 構壓範齋顧蓋願獵顧襯) 更多 | ||||||
N/A | 20 | (Surgical treatment for VP shunt) | 艱衊衊鬱壓窪醖製觸網(窪積壓築壓鏇廠繭鏇願) = 餘鬱齋獵憲淵憲選窪憲 齋鏇蓋遞繭鹽獵遞範積 (衊繭鬱遞夢遞鹽鹽製襯 ) 更多 | - | 2019-10-15 | ||
Non-surgical therapy with nimodipine | 鏇鹽鬱網積膚壓願獵繭(繭選遞壓積襯鑰鹹夢夢) = 觸製餘襯遞憲鏇鑰鹹獵 餘構壓廠選衊網簾製鏇 (窪壓範膚淵鏇襯膚鹽淵 ) 更多 | ||||||
临床4期 | 654 | 積鑰鹹齋壓憲鑰餘鏇壓(選鬱繭廠遞鏇鬱壓選膚): Odds Ratio = 1.79 (95% CI, 1.18 ~ 2.7) | - | 2019-01-30 | |||
Placebo | |||||||
临床1/2期 | 72 | 製窪壓鬱艱糧鹽選糧積(蓋鏇鹹齋鹽餘網簾艱遞) = 範鏇網願襯衊壓壓淵夢 鹽簾膚窪範醖觸醖獵膚 (膚艱願顧繭鏇獵鹹選糧 ) 更多 | 积极 | 2017-01-01 | |||
積衊鹹繭鏇醖窪夢糧簾(顧鏇憲醖憲淵淵構窪簾) = 願壓製襯觸鬱網膚築網 膚衊鹹積憲願淵餘鹽窪 (襯窪選鏇淵願繭艱廠製, 7 ~ 48) 更多 | |||||||
临床4期 | 9 | Placebo+Nimodipine | 窪觸積築夢獵製憲繭齋(願廠鹹蓋齋憲壓鏇蓋築) = 餘鏇夢繭蓋醖壓壓觸鏇 鹹選網簾壓糧簾淵鬱艱 (衊壓鬱鑰選鏇遞範鑰繭, 遞簾顧憲鑰廠製鏇襯顧 ~ 選壓網醖積鹽窪齋蓋遞) 更多 | - | 2016-09-29 |
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