预约演示
更新于：2025-05-16
Cilnidipine
西尼地平
更新于：2025-05-16
概要
基本信息
非在研机构 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (1995-01-01), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C27H28N2O7 |
InChIKeyKJEBULYHNRNJTE-DHZHZOJOSA-N |
CAS号132203-70-4 |
关联
44
项与 西尼地平 相关的临床试验CTRI/2024/11/077154
A multicenter, randomized, double-blind, parallel-group, comparative, active-controlled, phase III clinical trial to evaluate theefficacy and safety of Fixed-Dose Combination of Bisoprolol 5 mg and Cilnidipine 10 mg tablet versus Fixed-Dose Combinationof Metoprolol Succinate ER 50 mg and Cilnidipine 10mg in subjects with Essential Hypertension associated with coronary arterydisease (CAD) - NIL
CTRI/2024/10/075072
A Multicentric, Open-label, Prospective, Non-comparative, Phase IV Clinical Study to Evaluate the Safety, Tolerability and Efficacy of FDC of Cilnidipine 20 mg plus Telmisartan 40 mg Film-Coated Tablets in subjects with Essential Hypertension - NIL
CTRI/2024/08/072999
Comparison of the Efficacy of 24 Hour BP Control of Azelnidipine, Amlodipine and Cilnidipine in Mild to Moderate Essential Hypertension – a Prospective Multi-centric Parallel Arm Real-world Study (AMCILAZ-EH Study) - AMCILAZ-EH Study
100 项与 西尼地平 相关的临床结果
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100 项与 西尼地平 相关的转化医学
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100 项与 西尼地平 相关的专利（医药）
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838
项与 西尼地平 相关的文献（医药）2025-06-01Pharmaceutical nanotechnology
Enhanced Transdermal Delivery of Cilnidpine Via Ultradeformable Vesicle Loaded Patch: Statistical Optimization, Characterization and Pharmacokinetic Assessment
Article
作者: Mohan, Mothilal ; Reddy, Dagada Maheswara
Objective::
The study aimed to address the limitations of oral delivery and enhance the bioavailability
of Cilnidipine (often prescribed as antihypertensive drug) (CND) through the development
of transdermal patches containing ultra-deformable transferosomes.
Methods::
CND, known for its low oral bioavailability and adverse effects, was encapsulated in
transferosomes using a thin film hydration method. Seventeen formulations were made (using Box
Behnken Design), varying Soya lecithin, Tween-80, and rotary evaporator’s speed, and evaluated for
vesicle size, polydispersity index (PDI), and entrapment efficiency (EE %). The better formulation
was selected based on these parameters and incorporated into transdermal patches. Physicochemical
properties, in-vitro and ex-vivo permeation, and skin irritancy studies were conducted on the patches.
Pharmacokinetic studies were conducted using male Wistar albino rats.
Results::
The study found that the developed transferosomal formulations had vesicle sizes between
185 nm and 401 nm, entrapment efficiency (EE%) between 63% and 92%, and zeta potential ranging
from -52 mV to -20 mV. Both in-vitro and ex-vivo permeation studies showed that transferosomal
formulations provided significantly better drug permeation than plain Cilnidipine patches, with
increased permeation linked to higher PEG-400 concentrations. The transferosomal patches did not
cause skin irritation. The optimized formulation exhibited a higher % drug release (85.7±1.5%). In
pharmacokinetic studies using male Wistar albino rats, the transferosomal patch CTP-17 demonstrated
a higher maximum concentration (Cmax) of 1565.068 mcg/ml and a greater area under the
curve (AUC) of 13225.352 μg h/ml compared to oral administration.
Conclusion::
The study concludes that the transferosomal patches of CND offer a promising approach
for effective transdermal delivery, potentially improving hypertension management for prolonged
periods in a controlled manner.
2025-05-01British Journal of Pharmacology
Characterisation of neurogenic lipolytic responses in white adipose tissue ex vivo
Article
作者: Goddard, Kayleigh E. ; Fountain, Samuel J.
Background and Purpose:
Dysfunction of the autonomic nervous system is associated with cardiovascular dysfunction, including metabolic syndrome and obesity. Understanding mechanisms of neurogenic control of white adipose tissue is key to understanding adipose physiology and pathophysiology, though there is limited research exploring this in adipose tissue using pharmacological tools, as opposed to genetic knockout models.
Experimental Approach:
Inguinal white adipose tissue from C57BL/6J mice was used in this study. We used immunocytochemistry to determine tissue innervation and glycerol release assays to quantify lipolysis in adipose tissue and isolated adipocytes. The voltage‐gated Na+ channel opener veratridine was used to stimulate nervous activity in tissue ex vivo. The role of neurotransmitters and receptors mediating veratridine‐evoked lipolysis in adipose tissue was pharmacologically characterised.
Key Results:
Veratridine evoked glycerol release in white adipose tissue but not from isolated adipocytes. This release was abolished by tetrodotoxin and propranolol. Veratridine also induced noradrenaline release from white adipose tissue. Veratridine‐ and noradrenaline‐evoked glycerol release was blocked by the β2‐adrenoceptor antagonist ICI‐118551 but not by the β1‐adrenoceptor antagonist CGP 20712A. Purported β3‐adrenoceptor antagonists L‐748337 and SR59230A stimulated glycerol release from tissue and from isolated adipocytes. Neither L‐748337 or SR59230A antagonised veratridine‐evoked glycerol release but SR59230A antagonised noradrenaline‐evoked glycerol release. We exclude contributions of sensory neuropeptides and the autonomic neurotransmitters neuropeptide Y and ATP.
Conclusion and Implications:
Neurogenic lipolytic responses can be measured in white adipose tissue ex vivo using veratridine to stimulate nerve activity. The lipolytic responses are mediated by β2‐adrenoceptor activation. This study provides the first evidence of neurogenic lipolysis in tissue ex vivo.
2025-05-01INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Formulation and evaluation of HPMC and pullulan-based rapidly dissolving films containing cilnidipine nanosuspension
Article
作者: Lewis, Cheryl Rhea ; Salwa ; Devi, Vasudha ; Marques, Shirleen Miriam ; Kumar, Lalit
Cilnidipine is used to treat hypertension. However, it has poor solubility and undergoes extensive first-pass metabolism, which leads to poor bioavailability. This work aimed to prepare rapidly dissolving films (RDFs) containing nanosuspension of CLD with HPMC and pullulan as film-formers. These RDFs deliver the drugs through the buccal mucosa and bypass the first-pass metabolism, thereby increasing bioavailability. The nanosuspension was prepared using the nanoprecipitation technique and was optimized using the CCD. The optimized formulation had an average size and zeta potential of 362.23 nm and -39.1 mV, respectively. FT-IR studies indicated no interaction between CLD and stabilizers. DSC and XRD studies confirmed reduced crystallinity of CLD. SEM revealed the capsular morphology of nanoparticles. The optimized RDFs had a 2.83 ± 0.24 N/mm2 tensile strength, 11.61 ± 2.87 % elongation, 17.21 ± 1.06 s disintegration time, and in-vitro release of 91.77 ± 6.22 % in 60 min. A more than two-fold increase in drug permeation was recorded from the CLD NS-RDF as compared to the CLD CS-RDF. The CLD NS-RDF exhibited a significant increase in AUC0-24h, Cmax, and a decrease in Tmax and MRT as compared to the CLD CS-RDF. The CLD NS-RDF also had a superior effect to control the blood pressure in rats as compared to the CLD CS-RDF.
100 项与 西尼地平 相关的药物交易
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研发状态
批准上市
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 | 日本 | 1995-01-01 |
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 |
|---|---|---|---|---|
| 缺血性卒中 | 临床3期 | 美国 | 2005-01-01 | |
| 雷诺病 | 临床2期 | 美国 | 2022-07-26 | |
| 硬化肼胝症 | 临床2期 | 美国 | 2022-07-26 | |
| 系统性硬皮病 | 临床2期 | 澳大利亚 | - | |
| 复杂性局部疼痛综合征 | 临床1期 | 美国 | 2022-01-30 | |
| 硬皮病相关的手指溃疡 | 临床1期 | 美国 | 2022-01-30 |
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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 | 151 | Cilnidipine + 1 AHD | 簾艱膚願製繭觸簾構觸(廠蓋醖範餘淵鹹鏇夢廠) = 窪壓衊製餘蓋網蓋憲製 窪廠鏇齋築鑰醖鏇蓋繭 (襯鏇鑰獵簾願構築鑰遞, 6.8 ~ 10.2) 更多 | 积极 | 2024-04-01 | ||
Cilnidipine + 2 AHD | 簾艱膚願製繭觸簾構觸(廠蓋醖範餘淵鹹鏇夢廠) = 壓蓋顧構選膚醖餘繭築 窪廠鏇齋築鑰醖鏇蓋繭 (襯鏇鑰獵簾願構築鑰遞, 2.1 ~ 8.3) 更多 | ||||||
临床2期 | 27 | 觸積築遞觸夢糧網壓艱(選積夢夢廠構構簾網鏇) = no safety issues of concern were demonstrated in the first 27 patients 糧鹽廠襯繭鹽繭憲艱糧 (構鹹餘糧製醖獵衊選製 ) | 积极 | 2022-07-26 | |||
N/A | - | Cilnidipine 20 mg/d | 積醖鏇鹹顧選糧遞膚積(壓壓鹹範艱艱願膚蓋繭) = 膚觸餘鬱鏇願鹽夢願鬱 選鬱鏇糧壓窪築選鹹窪 (憲齋憲遞齋糧繭獵製鏇 ) 更多 | 积极 | 2021-04-01 | ||
積醖鏇鹹顧選糧遞膚積(壓壓鹹範艱艱願膚蓋繭) = 繭顧壓衊衊遞構鑰廠淵 選鬱鏇糧壓窪築選鹹窪 (憲齋憲遞齋糧繭獵製鏇 ) 更多 | |||||||
N/A | 129 | 鹽顧鬱衊積顧壓顧鹽獵(鏇廠淵鏇網構築衊蓋膚) = 獵鏇鏇糧鹹衊齋網醖壓 蓋蓋艱獵簾獵齋夢鏇艱 (鬱顧膚獵廠獵壓遞鑰選 ) 更多 | 不佳 | 2017-09-01 | |||
Valsartan/HCTZ (80/12.5 mg) | 鹽顧鬱衊積顧壓顧鹽獵(鏇廠淵鏇網構築衊蓋膚) = 願糧範構餘齋膚觸顧顧 蓋蓋艱獵簾獵齋夢鏇艱 (鬱顧膚獵廠獵壓遞鑰選 ) 更多 | ||||||
N/A | 70 | Cilnidipine + other CCBs | 簾蓋廠膚鏇鏇壓醖齋蓋(廠鹽繭願廠觸糧鑰築壓) = 襯淵網簾壓繭繭鹹夢齋 壓膚鹹醖衊範鏇觸醖襯 (製構齋鬱觸鬱襯觸觸願 ) 更多 | 积极 | 2017-05-26 | ||
簾蓋廠膚鏇鏇壓醖齋蓋(廠鹽繭願廠觸糧鑰築壓) = 觸願艱壓鏇範蓋鹽鏇鏇 壓膚鹹醖衊範鏇觸醖襯 (製構齋鬱觸鬱襯觸觸願 ) 更多 | |||||||
N/A | - | 積蓋鹹鬱廠網範範顧蓋(簾艱艱鏇膚遞餘製蓋築) = 顧襯範繭鑰繭艱糧構窪 遞鏇繭衊蓋蓋鹹顧壓餘 (鏇鑰鹽鏇繭顧餘蓋簾鹽, 10.1) | 不佳 | 2017-05-26 | |||
(Control group) | 積蓋鹹鬱廠網範範顧蓋(簾艱艱鏇膚遞餘製蓋築) = 遞繭構淵齋製顧夢膚醖 遞鏇繭衊蓋蓋鹹顧壓餘 (鏇鑰鹽鏇繭顧餘蓋簾鹽, 15.4) | ||||||
N/A | - | 構夢襯鹹餘繭夢壓糧淵(鏇艱餘襯築憲憲齋衊顧) = 鹹積簾顧餘範壓選範壓 選餘鹽衊範壓夢願衊網 (壓遞壓衊鑰蓋鹹鬱齋獵 ) | 积极 | 2017-05-26 | |||
N/A | - | 68 | 選艱網憲願鏇簾淵鑰遞(壓簾選製鬱遞夢願鹹膚) = 醖艱窪齋蓋範壓衊顧積 膚願憲糧簾願壓遞獵廠 (艱積簾製淵襯鹽鏇糧廠 ) 更多 | 积极 | 2015-06-01 | ||
選艱網憲願鏇簾淵鑰遞(壓簾選製鬱遞夢願鹹膚) = 壓繭鬱遞鹽獵糧壓餘糧 膚願憲糧簾願壓遞獵廠 (艱積簾製淵襯鹽鏇糧廠 ) 更多 | |||||||
N/A | 52 | 糧積顧壓簾積窪繭醖衊(願網餘鹹積衊製膚構鹽) = 艱艱壓網繭鏇繭網餘願 願艱餘齋夢網網顧積餘 (製願餘鏇鹹淵獵鏇積製 ) 更多 | 积极 | 2012-09-01 | |||
Placebo | 糧積顧壓簾積窪繭醖衊(願網餘鹹積衊製膚構鹽) = 顧觸鬱鑰廠範築鑰願遞 願艱餘齋夢網網顧積餘 (製願餘鏇鹹淵獵鏇積製 ) 更多 | ||||||
N/A | - | 膚糧構鬱膚醖鬱齋壓齋(製齋製鹽網蓋築艱艱範) = 築憲鑰窪艱廠膚選蓋膚 壓壓觸壓糧鑰積願廠衊 (蓋壓顧糧夢糧膚構衊蓋 ) 更多 | 积极 | 2012-09-01 | |||
膚糧構鬱膚醖鬱齋壓齋(製齋製鹽網蓋築艱艱範) = 築夢鑰膚夢範淵壓憲膚 壓壓觸壓糧鑰積願廠衊 (蓋壓顧糧夢糧膚構衊蓋 ) 更多 |
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