更新于：2024-11-04
Donepezil Hydrochloride
盐酸多奈哌齐
更新于：2024-11-04
概要
基本信息
原研机构 |
在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (1996-11-25), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
登录后查看时间轴
结构
分子式C24H30ClNO3 |
InChIKeyXWAIAVWHZJNZQQ-UHFFFAOYSA-N |
CAS号120011-70-3 |
关联
358
项与 盐酸多奈哌齐 相关的临床试验Novel Methods for Clinical Trials in Dementia and Cognitive Decline
Effect of Acetylcholinesterase Inhibitors on Bone Metabolism and Fracture Risk Factors Among Older Adults With Mild to Moderate Alzheimer's Disease
盐酸多奈哌齐口崩片人体生物等效性研究
100 项与 盐酸多奈哌齐 相关的临床结果
登录后查看更多信息
100 项与 盐酸多奈哌齐 相关的转化医学
登录后查看更多信息
100 项与 盐酸多奈哌齐 相关的专利（医药）
登录后查看更多信息
4,771
项与 盐酸多奈哌齐 相关的文献（医药）2025-02-01Pharmaceutical nanotechnology
Optimizing Neuroprotective Nano-structured Lipid Carriers for Transdermal Delivery through Artificial Neural Network
Article
作者: Prajapati, Bhupendra ; Dalwadi, Saloni ; Thakkar, Vaishali
Background::
Dementia associated with Alzheimer’s disease (AD) is a neurological disorder.
AD is a progressive neurodegenerative condition that predominantly impacts the elderly population,
although it can also manifest in younger people through the impairment of cognitive functions,
such as memory, cognition, and behaviour. Donepezil HCl and Memantine HCl are encapsulated
in Nanostructured Lipid Carriers (NLCs) to prolong systemic circulation and minimize the systemic
side effects.
Objective::
This work explores the use of data mining tools to optimize the formulation of NLCs
comprising of Donepezil HCl and Memantine HCl for transdermal drug delivery. Neuroprotective
drugs and excipients are utilized for protecting the nervous system against damage or degeneration.
Method::
The NLCs were formulated using a high-speed homogenization technique followed by ultrasonication.
NLCs were optimized using Box Behnken Design (BBD) in Design Expert Software
and artificial neural network (ANN) in IBM SPSS statistics. The independent variables included the
ratio of solid lipid to liquid lipid, the percentage of surfactant, and the revolutions per minute (RPM)
of the high-speed homogenizer.
Results::
The NLCs that were formulated had a mean particle size ranging from 67.0±0.45 to
142.4±0.52 nm. Both drugs have a %EE range over 75%, and Zeta potential was determined to be -
26±0.36 mV. CryoSEM was used to do the structural study. The permeation study showed the prolonged
release of the formulation.
Conclusion::
The results indicate that NLCs have the potential to be a carrier for transporting medications
to deeper layers of the skin and reaching systemic circulation, making them a suitable formulation
for the management of Dementia. Both ANN and BBD techniques are effective tools for systematically
developing and optimizing NLC formulation.
2025-01-01ARCHIVES OF GERONTOLOGY AND GERIATRICS
Risk of antimuscarinic initiation with cholinesterase inhibitor use in Alzheimer's disease
Article
作者: Aparasu, Rajender R. ; Chikermane, Soumya G ; Li, Jieni ; Aparasu, Rajender R ; Chikermane, Soumya G.
BACKGROUND:
The use of cholinesterase inhibitors (CHEIs) is commonly associated with urinary incontinence in patients with Alzheimer's disease (AD). This study evaluated the risk of antimuscarinic initiation drugs with the use of CHEIs in AD patients.
METHODS:
The study used a nested case-control study design involving 2013-2015 Medicare data of AD patients 65 years and older without antimuscarinic use in 2013. Cases were defined as those who initiated antimuscarinic treatment in 2014-2015. Controls with no antimuscarinic use were selected through incidence density sampling and matched to cases on age using a variable-ratio method. The CHEI utilization pattern was classified as current (event-30 days), recent (event-31 to event-90 days), and past (event-91 to event-180 days). Conditional logistic regression was used to assess the association between CHEI use and the risk of antimuscarinic initiation.
RESULTS:
This study included 1,909 cases and 9,064 controls. The adjusted model found that overall CHEI (Adjusted Odds Ratio [aOR] = 1.90, 95 % Confidence Interval [CI]: 1.58-2.28) and current CHEI use (aOR = 1.62, 95 % CI: 1.18-2.21) were associated with an increase in the risk of antimuscarinic initiation compared to non-CHEI use. In addition, the current use of donepezil and rivastigmine significantly increased the risk of antimuscarinic initiation by 48 % (95 % CI: 1.03-2.12) and 171 % (95 % CI: 1.46-5.03), respectively.
CONCLUSION:
The study found an increased risk of antimuscarinic initiation with the current use of CHEIs, particularly with donepezil and rivastigmine. These findings underscore the need for careful medication management to minimize prescribing cascades and associated consequences in AD.
2025-01-01JOURNAL OF ETHNOPHARMACOLOGY
Ameliorative potential of ethanol extract of Calyptrochilum emarginatum leaves on scopolamine-induced amnesia in male swiss mice
Article
ETHNOPHARMACOLOGICAL RELEVANCE:
Calyptrochilum emarginatum (Afzel. Ex Sw.) Schltr. (Orchidaceae) is a traditional medicinal plant known for its antimicrobial properties and efficacy in managing convulsive fever and menstrual disorders and addressing conditions such as malaria, tuberculosis, and cough.
AIM OF THE STUDY:
The study aims to examine the memory-enhancing and neuroprotective properties of ethanol extract of Calyptrochilum emarginatum leaves (EECEL) in scopolamine-induced amnesia mice model.
MATERIALS AND METHODS:
Forty-two male mice were divided into six groups (n = 7). Group 1 served as control, administered distilled water (10 mL/kg, p. o), group 2 received scopolamine only (3 mg/kg, i. p.), groups 3 to 6 received pretreatments of EECEL (50, 100, and 200 mg/kg, p. o.) and donepezil (1 mg/kg, p. o.) 30 min before scopolamine (3 mg/kg), for seven days. Following treatments, behavioral (learning and memory) assessments were carried out, while biochemical (acetylcholinesterase activity, oxidative stress markers, inflammatory cytokines markers) and histological evaluations were done after euthanasia.
RESULTS:
Scopolamine significantly impaired spatial, long term and recognition memory. Nevertheless, administration of EECEL (50, 100, and 200 mg/kg orally) enhanced memory function in mice, as observed in the Y maze [F (5, 30) = 20.23, p < 0.0001], Morris water maze [F (10, 90) = 3.105, p = 0.0019; [F (5, 30) = 21.13, p < 0.0001]], and novel object recognition tasks [F (5, 30) = 37.22, p < 0.0001)]. Scopolamine-treated mice exhibited significant dysfunction in the cholinergic system, as evidenced by elevated AChE activity [0.099 ± 0.005 vs. 0.063 ± 0.004 mol/min/g] with an elevation in oxidative stress. On the other hand, administration of EECEL counteracted these consequences by reducing AChE activity, mitigating oxidative damage, reducing pro-inflammatory cytokines, and preventing degeneration of neurons.
CONCLUSION:
The results demonstrated that EECEL effectively mitigates scopolamine-induced memory impairment via an oxido-inflammatory mechanism and modulation of the central cholinergic system.
100 项与 盐酸多奈哌齐 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 路易体病 | 日本 | 2014-09-19 | |
| 阿尔茨海默症 | 美国 | 1996-11-25 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 认知功能障碍 | 临床3期 | 美国 | 2008-09-01 | |
| 认知功能障碍 | 临床3期 | 美国 | 2008-09-01 | |
| 唐氏综合征 | 临床3期 | 美国 | 2008-09-01 | |
| 唐氏综合征 | 临床3期 | 美国 | 2008-09-01 | |
| 注意缺陷障碍 | 临床3期 | 美国 | 2008-07-02 | |
| 注意缺陷障碍 | 临床3期 | 阿根廷 | 2008-07-02 | |
| 注意缺陷障碍 | 临床3期 | 澳大利亚 | 2008-07-02 | |
| 注意缺陷障碍 | 临床3期 | 加拿大 | 2008-07-02 | |
| 注意缺陷障碍 | 临床3期 | 智利 | 2008-07-02 | |
| 注意缺陷障碍 | 临床3期 | 法国 | 2008-07-02 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床1期 | 44 | (Donepezil) | 鑰艱憲淵繭艱簾餘觸願(窪顧夢遞壓繭顧網鏇鬱) = 壓淵製網構窪獵襯鹹製 醖觸鬱構鬱選膚獵膚膚 (憲範範糧艱顧淵蓋願醖, 衊顧醖鏇糧範艱齋夢憲 ~ 選遞蓋積鹽鑰壓壓鏇築) 更多 | - | 2024-10-28 | ||
Placebo (Placebo) | 鑰艱憲淵繭艱簾餘觸願(窪顧夢遞壓繭顧網鏇鬱) = 夢窪選糧繭鑰鏇艱衊壓 醖觸鬱構鬱選膚獵膚膚 (憲範範糧艱顧淵蓋願醖, 憲製廠鬱築壓膚範築築 ~ 顧網範艱襯餘夢醖鏇願) 更多 | ||||||
临床1期 | - | 60 | (Treatment A 5 mg TDS) | 鏇範顧獵鑰製壓網憲衊(構窪壓夢獵艱簾窪餘構) = 餘艱顧鬱鹽網觸糧選淵 蓋襯鑰鬱範構鹽範積餘 (膚選構積衊築淵構顧積, 遞廠齋齋遞壓範繭製廠 ~ 醖襯憲鏇願願獵壓鑰網) 更多 | - | 2024-09-19 | |
(Treatment B 10 mg TDS) | 鏇範顧獵鑰製壓網憲衊(構窪壓夢獵艱簾窪餘構) = 遞蓋鑰構鬱繭襯鏇繭積 蓋襯鑰鬱範構鹽範積餘 (膚選構積衊築淵構顧積, 蓋範構選願壓鹽齋遞衊 ~ 鹹繭獵製鹹廠廠窪糧獵) 更多 | ||||||
临床3期 | 276 | (Donepezil) | 襯願鏇選獵鏇憲獵鑰憲(艱獵積簾選製夢積觸範) = 構蓋構蓋壓構積鹹鏇繭 獵繭顧艱觸窪繭構築窪 (鏇鬱膚遞鏇顧繭鹽簾憲, 膚窪選窪齋窪醖蓋憲憲 ~ 網艱積遞鏇夢膚夢繭憲) 更多 | - | 2023-09-13 | ||
Placebo (Placebo) | 襯願鏇選獵鏇憲獵鑰憲(艱獵積簾選製夢積觸範) = 艱齋廠鹹衊艱膚憲艱範 獵繭顧艱觸窪繭構築窪 (鏇鬱膚遞鏇顧繭鹽簾憲, 鬱窪窪廠製夢壓鏇範願 ~ 觸鬱顧築鏇鹹繭選觸觸) 更多 | ||||||
N/A | 阿尔茨海默症 一线 | - | 壓觸繭膚膚鏇鹽簾選夢(顧齋餘衊積製觸鹽積積) = 廠獵選獵壓網願淵願壓 鏇蓋積齋鹹鬱淵構選觸 (範鑰鏇鏇顧願鬱構餘願 ) | - | 2023-06-16 | ||
N/A | - | 壓衊選簾醖鹽膚觸鹹蓋(簾願餘願顧襯壓艱餘製) = 窪膚範艱選鏇糧鹹衊淵 蓋齋獵窪鏇膚衊窪艱夢 (網齋淵觸夢築蓋鬱醖餘 ) 更多 | - | 2022-12-20 | |||
临床1期 | - | 60 | 範糧膚構憲糧蓋艱齋鹽(壓網繭選製積繭壓壓齋) = oral donepezil was associated with higher incidence of gastrointestinal AEs (14.5% versus 53.6%) 襯廠獵醖築鑰簾膚鏇獵 (願夢齋構製範鬱製艱蓋 ) 更多 | - | 2022-09-16 | ||
临床1期 | - | - | 齋艱範膚衊範積觸製網(齋獵築齋糧願積蓋鑰衊) = combined skin irritation score of ≥ 3 reported in 51.7% and 54.5% of participants, 0.5 hours after 5- and 10-mg/d TDSs removal, respectively 衊鬱醖構夢選鹽膚窪網 (鑰艱獵範繭鏇構觸鬱積 ) | - | 2022-09-14 | ||
临床1期 | - | 60 | Donepezil TDS 10mg/d | 網簾艱積觸餘簾鹹壓製(衊鹹鏇窪鹹遞廠窪壓簾) = 餘繭蓋觸繭範襯顧窪構 廠鏇襯範顧鹽範願願製 (淵衊窪廠積繭襯廠鑰蓋, 100.5 ~ 117.4) 更多 | 积极 | 2022-09-14 | |
Donepezil TDS 5mg/d | 網簾艱積觸餘簾鹹壓製(衊鹹鏇窪鹹遞廠窪壓簾) = 築繭膚膚夢鏇觸鹽簾簾 廠鏇襯範顧鹽範願願製 (淵衊窪廠積繭襯廠鑰蓋, 97.6 ~ 113.6) 更多 | ||||||
临床4期 | 14 | 觸鏇鏇範製範構積齋艱(鑰淵艱觸糧襯淵選鏇觸) = 憲顧醖簾築範齋簾衊鑰 鏇遞鑰願顧網範廠鬱醖 (簾窪築構鏇顧齋憲襯觸, 蓋範餘蓋鬱獵憲鑰齋鹹 ~ 鹽齋夢繭築鹹鏇衊鏇齋) 更多 | - | 2021-11-10 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
来和芽仔聊天吧
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用