更新于：2024-11-15
Nitrendipine
尼群地平
更新于：2024-11-15
概要
基本信息
原研机构- |
在研机构 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (1987-01-01), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C18H20N2O6 |
InChIKeyPVHUJELLJLJGLN-UHFFFAOYSA-N |
CAS号39562-70-4 |
关联
6
项与 尼群地平 相关的临床试验The Effect of Nitrendipine/Atenolol Combination on Blood Pressure Variability of Patients With Grade 1 Hypertension Compared With Nitrendipine or Atenolol Monotherapy.
尼群地平片（10 mg）人体生物等效性研究
A Randomized, Open-label, Positive Drug Controlled Clinical Trials to Compare the Efficacy of Nitrendipine and Hydrochlorothiazide , Captopril Plus Hydrochlorothiazide and Beijing Hypotensive No.0 in Tibetan Hypertension
100 项与 尼群地平 相关的临床结果
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100 项与 尼群地平 相关的转化医学
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100 项与 尼群地平 相关的专利（医药）
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2,619
项与 尼群地平 相关的文献（医药）2024-11-01INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Enhanced drug release through nitrendipine/hydroxypropyl methylcellulose solid dispersion via supercritical antisolvent technique
Article
作者: Zhu, Ning ; Hong, Hailong ; Hao, Jianxia ; Song, Lijun
The poor water solubility of nitrendipine (NT) results in low oral bioavailability, which hinders its practical application. Hydroxypropyl methylcellulose (HPMC) is a prominent drug carrier that has been applied in the biomedical field due to its significant characteristics, such as large surface area, biocompatibility and biodegradability. In this study, an efficient drug delivery system based on the preparation of NT/HPMC solid dispersion using supercritical antisolvent (SAS) technology was proposed. The effect of different operating parameters such as solvent, host guest ratio, concentration, temperature, and pressure on NT/HPMC was optimized to obtain dispersed particles with maximum solubility. The formed solid dispersion presents non-static spherical particles with a high surface area and small particle size. Importantly, in vitro drug release studies have demonstrated that the dissolution and solubility of NT in solid dispersion are significantly enhanced compared to pure drug. In vitro bioactivity experiments showed that the NT/HPMC solid dispersion has good biocompatibility and antibacterial performance. Thus, this study indicates that solid dispersion prepared using SAS technology are considered a promising drug delivery system.
2024-07-01CURRENT DRUG METABOLISM
Carboxylesterase 1-Based Drug-Drug Interaction Potential of Remimazolam: In-Vitro Studies and Literature Review
Article
作者: Petersen, Karl-Uwe ; Stöhr, Thomas ; Schmalix, Wolfgang ; Pesic, Marija
Background::
The ultra-short-acting benzodiazepine remimazolam, approved for procedural sedation
and general anesthesia, is inactivated by carboxylesterase 1 (CES1).
Objective::
Remimazolam´s involvement in CES1-mediated drug-drug interactions (DDIs) was investigated.
Methods::
Possible interactions of remimazolam were studied in co-exposure experiments with eleven different
drugs. Further, substrates and inhibitors of CES1, identified in the literature, were evaluated for possible
in-vivo inhibition using pharmacokinetic and Ki or IC50 values. Compounds with only one published inhibitory
concentration and CES1 substrates lacking inhibition data were assigned conservative Ki values.
Results::
In human liver homogenates and/or blood cells, remimazolam showed no significant inhibition of
esmolol and landiolol metabolism, which, in turn, at up to 98 and 169 μM, respectively, did not inhibit remimazolam
hydrolysis by human liver homogenates. In human liver S9 fractions, IC50 values ranged from 0.69
μM (simvastatin) and 57 μM (diltiazem) to > 100 μM (atorvastatin) and, for the remaining test items (bupropion,
carvedilol, nelfinavir, nitrendipine, and telmisartan), they ranged from 126 to 658 μM. Remifentanil
was ineffective even at 1250 μM. Guidance-conforming evaluation revealed no relevant drug-drug interactions
with remimazolam via CES1. The algorithm-based predictions were consistent with human study data.
Among CES1 inhibitors and substrates identified in the literature, only dapsone and rufinamide were found to
be possible in-vivo inhibitors of remimazolam metabolism.
Conclusion::
Data and analyses suggest a very low potential of remimazolam for pharmacokinetic DDIs mediated
by CES1. The theoretical approach and compiled data are not specific to remimazolam and, hence,
applicable in the evaluation of other CES1 substrates.
2024-06-14MEDICINE
A network meta-analysis comparative the efficacy of angiotensin-converting enzyme inhibitors and calcium channel blockers in hypertension
Article
作者: Cai, Shi-Kang ; Yao, You-Jian ; Gui, Mei
Background::
Currently, most studies primarily focus on directly comparing the efficacy and safety of angiotensin-converting enzyme inhibitors (ACEIs) and calcium channel blockers (CCBs), the two major classes of antihypertensive drugs. Moreover, the majority of studies are based on randomized controlled trials and traditional meta-analyses, with few exploring the efficacy and safety comparisons among various members of ACEIs and CCBs.
Methods::
ACEIs and CCB were searched for in randomized controlled trials in CNKI, Wanfang, VIP, China Biology Medicine Disc (Si-noMed), PubMed, EMbase, and Cochrane Library databases. The search can be conducted till November 2022. Stata software (version 16.0) and R 4.1.3 was used for statistical analysis and graphics plotting, applying mvmeta, gemtc, and its packages. Meta-regression analysis was used to explore the inconsistencies of the studies.
Results::
In 73 trials involving 33 different drugs, a total of 9176 hypertensive patients were included in the analysis, with 4623 in the intervention group and 4553 in the control group. The results of the analysis showed that, according to the SUCRA ranking, felodipine (MD = −12.34, 95% CI: −17.8 to −6.82) was the drug most likely to be the best intervention for systolic blood pressure, while nitrendipine (MD = −8.01, 95% CI: −11.71 to −4.18) was the drug most likely to be the best intervention for diastolic blood pressure. Regarding adverse drug reactions, nifedipine (OR = 0.32, 95% CI: 0.14–0.74) was the drug most likely to be the safest.
Conclusion::
The research findings indicate that nifedipine is the optimal intervention for reducing systolic blood pressure in hypertensive patients, nitrendipine is the optimal intervention for reducing diastolic blood pressure in hypertensive patients, and felodipine is the optimal intervention for safety.
100 项与 尼群地平 相关的药物交易
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研发状态
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 高血压 | 中国 | 1987-01-01 |
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临床结果
临床结果
适应症
分期
评价
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N/A | 59 | Combined antihypertensive treatment with nitrendipine | 製築簾壓憲積齋壓衊遞(艱簾積餘簾遞鹹醖壓繭) = 簾遞夢積齋獵蓋鏇衊鏇 鹽壓範艱構構壓膚壓餘 (積憲築鬱顧簾襯願醖艱 ) | - | 2023-08-27 | ||
临床4期 | 1,405 | 繭遞繭築觸繭蓋夢觸艱(顧觸衊願夢鬱糧餘製願) = 膚築窪範膚製廠窪繭餘 夢鬱淵衊觸蓋鹹鹹築顧 (糧繭窪淵鬱範鹹鹽夢選 ) | - | 2005-06-01 | |||
繭遞繭築觸繭蓋夢觸艱(顧觸衊願夢鬱糧餘製願) = 積蓋糧構蓋襯蓋獵繭鹽 夢鬱淵衊觸蓋鹹鹹築顧 (糧繭窪淵鬱範鹹鹽夢選 ) |
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