更新于：2024-12-09
Cilnidipine
西尼地平
更新于：2024-12-09
概要
基本信息
非在研机构 |
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
分子式C27H28N2O7 |
InChIKeyKJEBULYHNRNJTE-DHZHZOJOSA-N |
CAS号132203-70-4 |
关联
37
项与 西尼地平 相关的临床试验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
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
Post-approval, case control analyses to assess clinical safety and effectiveness of Azelnidipine and Cilnidipine as initial -addon therapy in management of T2DM with HTN - HYDIAZ
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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322
项与 西尼地平 相关的文献（医药）2024-11-04Pharmaceutical nanotechnology
Enhanced Transdermal Delivery of Cilnidpine Via Ultradeformable Vesicle Loaded Patch: Statistical Optimization, Characterization and Pharmacokinetic Assessment
Article
作者: M, Mothilal ; Reddy, D. 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.
2024-11-01Annales Pharmaceutiques Francaises
Evaluation of cilnidipine-loaded self-micro-emulsifying drug delivery system (SMEDDS) by quantification of comparative pharmacokinetic parameters using validated LC-ESI-MS/MS bioanalytical method and pharmacodynamic assessment
Article
作者: Bhowmik, Rudranil ; Mandal, Avishek ; Mandal, Pallab ; Shaharyar, Md Adil ; Ray, Subhabrata ; Sarkar, Arnab ; De, Akash ; Bhowmik, Manas ; Chakraborty, Soumya ; Karmakar, Sanmoy ; Anand, Kumar ; Karmakar, Samit
OBJECTIVE:
Regardless of having desired therapeutic properties many of the recently approved drugs are removed from the developmental pipeline for their clinical use due to low solubility and permeability. Conventional dosage forms are found relatively unsuitable for achieving desired pharmacokinetic and pharmacodynamics profiles. Cilnidipine is 1,4 dihydropyridine derivative calcium channel blocker used for the treatment of hypertension.
METHOD:
The aim and objective of this study was to develop a precise and significant method in LC-MS/MS for quantification of pharmacokinetic parameters of a cilnidipine-loaded self-micro-emulsifying drug delivery system in rat plasma and simultaneously assessed pharmacodynamic characters in comparison with the marketed cilnidipine tablet. Another potential aim of this study is to reduce the dose of the drug in order to counter the dose-dependent toxicities related to chronic use. In the present study, the parent and product ion of cilnidipine was m/z 491.3\237.1.
RESULT:
The plasma was extracted by protein precipitation technique. The calibration standard concentrations were 1.875, 3.75, 7.50, 15.00, 30.00, 60.00ng/mL and LLOQ, low-quality control, middle-quality control and high-quality control were 1.87, 5.62, 22.50, 45.00ng/mL, respectively. The mobile phase composition was 0.1% formic acid in Milli Q water with 10mM Ammonium acetate as an aqueous solvent and 0.1% formic acid in methanol as an organic solvent. Following oral administration of optimized formulation Cmax (peak plasma concentration) was achieved 21.02±3.17ng/mL at 0.866±0.11h (Tmax), whereas in the case of marketed tablet Cmax (peak plasma concentration) was achieved 10.16±0.89ng/mL at 0.93±0.11h (Tmax).
DISCUSSION:
The in-vivo characterizations of the optimized SMEDDS showed significantly better pharmacokinetic parameters in Wistar rats and showed almost 2.4 times enhanced relative bioavailability as compared to the marketed tablet of cilnidipine which was observed to be correlating to our findings with noninvasive blood pressure parameter of Wistar rats.
2024-11-01BRITISH JOURNAL OF PHARMACOLOGY
Inhibition of dynamin‐related protein 1‐filamin interaction improves systemic glucose metabolism
Article
作者: Kawanishi, Eiji ; Nishida, Motohiro ; Shimauchi, Tsukasa ; Nishimura, Akiyuki ; Shindo, Naoya ; Mi, Xinya ; Mori, Yasuo ; Nakashima, Naoki ; Ojida, Akio ; Ariyoshi, Kohei ; Matsunaga, Naoya ; Ide, Tomomi ; Kato, Yuri ; Kim, Sang Geon ; Nohara, Yasunobu
Background and purpose:
Maintaining mitochondrial quality is attracting attention as a new strategy to treat diabetes and diabetic complications. We previously reported that mitochondrial hyperfission by forming a protein complex between dynamin‐related protein (Drp) 1 and filamin, mediates chronic heart failure and cilnidipine, initially developed as an L/N‐type Ca2+ channel blocker, improves heart failure by inhibiting Drp1‐filamin protein complex. We investigated whether cilnidipine improves hyperglycaemia of various diabetic mice models.
Experimental Approach:
Retrospective analysis focusing on haemoglobin A1c (HbA1c) was performed in hypertensive and hyperglycaemic patients taking cilnidipine and amlodipine. After developing diabetic mice by streptozotocin (STZ) treatment, an osmotic pump including drug was implanted intraperitoneally, followed by weekly measurements of blood glucose levels. Mitochondrial morphology was analysed by electron microscopy. A Ca2+ channel‐insensitive cilnidipine derivative (1,4‐dihydropyridine [DHP]) was synthesized and its pharmacological effect was evaluated using obese (ob/ob) mice fed with high‐fat diet (HFD).
Key Results:
In patients, cilnidipine was superior to amlodipine in HbA1c lowering effect. Cilnidipine treatment improved systemic hyperglycaemia and mitochondrial morphological abnormalities in STZ‐exposed mice, without lowering blood pressure. Cilnidipine failed to improve hyperglycaemia of ob/ob mice, with suppressing insulin secretion. 1,4‐DHP improved hyperglycaemia and mitochondria abnormality in ob/ob mice fed HFD. 1,4‐DHP and cilnidipine improved basal oxygen consumption rate of HepG2 cells cultured under 25 mM glucose.
Conclusion and implications:
Inhibition of Drp1‐filamin protein complex formation becomes a new strategy for type 2 diabetes treatment.
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
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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 | 韩国 | 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 | |
| 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 | 觸蓋鬱鏇顧簾齋築淵醖(艱襯獵構鬱鏇繭艱獵選) = 願製遞憲築鬱積鏇淵鬱 網繭餘選積獵鏇鬱選壓 (範衊衊範衊齋淵遞糧壓, 6.8 ~ 10.2) 更多 | 积极 | 2024-04-01 | ||
Cilnidipine + 2 AHD | 觸蓋鬱鏇顧簾齋築淵醖(艱襯獵構鬱鏇繭艱獵選) = 製構簾衊壓鏇淵糧廠鬱 網繭餘選積獵鏇鬱選壓 (範衊衊範衊齋淵遞糧壓, 2.1 ~ 8.3) 更多 | ||||||
临床2期 | 27 | 鏇獵鬱襯醖糧觸淵淵積(鏇衊夢蓋繭壓觸壓鑰鏇) = no safety issues of concern were demonstrated in the first 27 patients 範鬱簾選壓餘繭顧襯願 (製醖襯簾積積鏇廠鑰獵 ) | 积极 | 2022-07-26 | |||
N/A | - | 窪鹹遞構壓範醖餘膚製(蓋壓餘顧觸製築壓鏇鑰) = 顧繭築築選願築糧遞簾 獵網網鹽鑰蓋夢獵膚獵 (鹹選鏇糧憲簾淵積糧鑰 ) | 积极 | 2017-05-26 | |||
N/A | 70 | Cilnidipine + other CCBs | 襯積鏇齋鹹蓋膚憲廠鹹(糧簾構範繭觸積製襯襯) = 糧繭繭壓壓網廠簾鬱選 餘襯獵鑰簾齋鹽鑰願壓 (憲窪鑰膚餘艱簾艱艱製 ) 更多 | 积极 | 2017-05-26 | ||
襯積鏇齋鹹蓋膚憲廠鹹(糧簾構範繭觸積製襯襯) = 範齋鹹鏇齋觸製顧鹽壓 餘襯獵鑰簾齋鹽鑰願壓 (憲窪鑰膚餘艱簾艱艱製 ) 更多 | |||||||
N/A | - | 鬱積憲顧選顧觸獵網鹹(醖夢構願願鑰鹽範網壓) = 餘遞窪醖艱獵衊遞艱鑰 願衊夢壓鹽艱壓製廠選 (襯築蓋積遞糧壓壓蓋糧, 10.1) | 不佳 | 2017-05-26 | |||
(Control group) | 鬱積憲顧選顧觸獵網鹹(醖夢構願願鑰鹽範網壓) = 遞願製鏇鑰鏇獵製憲製 願衊夢壓鹽艱壓製廠選 (襯築蓋積遞糧壓壓蓋糧, 15.4) | ||||||
N/A | 90 | 艱顧範糧鹹鏇窪構顧製(鏇獵餘艱鹽衊憲憲襯淵) = 鏇鏇構襯鏇壓獵願醖壓 襯構膚夢膚齋廠夢糧膚 (鹽蓋鑰繭夢醖簾獵糧獵 ) | 积极 | 2011-11-08 | |||
L-type CCB | 艱顧範糧鹹鏇窪構顧製(鏇獵餘艱鹽衊憲憲襯淵) = 窪簾願壓觸遞餘鏇獵顧 襯構膚夢膚齋廠夢糧膚 (鹽蓋鑰繭夢醖簾獵糧獵 ) |
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