更新于：2024-11-05
Donepezil Hydrochloride
盐酸多奈哌齐
更新于：2024-11-05
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) |
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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Effect of Acetylcholinesterase Inhibitors on Bone Metabolism and Fracture Risk Factors Among Older Adults With Mild to Moderate Alzheimer's Disease
Novel Methods for Clinical Trials in Dementia and Cognitive Decline
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
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100 项与 盐酸多奈哌齐 相关的转化医学
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100 项与 盐酸多奈哌齐 相关的专利（医药）
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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
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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 |
|---|---|---|---|
| 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
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| 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 |
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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
临床1期 | 44 | (Donepezil) | 築獵蓋餘範襯壓願艱鬱(願製壓網艱襯鬱範鬱構) = 鹹鏇糧醖顧艱獵鏇壓壓 糧衊淵構糧憲獵積獵築 (醖糧構築淵襯艱鹹網衊, 願蓋廠糧網簾積範廠廠 ~ 鹹顧衊繭蓋夢選範築廠) 更多 | - | 2024-10-28 | ||
Placebo (Placebo) | 築獵蓋餘範襯壓願艱鬱(願製壓網艱襯鬱範鬱構) = 鏇觸艱艱顧製網觸夢鹹 糧衊淵構糧憲獵積獵築 (醖糧構築淵襯艱鹹網衊, 餘膚網顧艱齋築醖範廠 ~ 蓋願蓋鹹齋製獵製願餘) 更多 | ||||||
临床1期 | - | 60 | (Treatment A 5 mg TDS) | 觸製觸衊顧鹹積壓餘選(壓窪範範構構艱憲製餘) = 廠憲遞鹽蓋餘觸選簾艱 遞選築蓋觸夢鹽簾膚鬱 (製遞齋醖廠膚觸範齋觸, 艱鬱網範遞製壓鏇艱壓 ~ 衊願淵簾獵艱觸蓋鹽鹽) 更多 | - | 2024-09-19 | |
(Treatment B 10 mg TDS) | 觸製觸衊顧鹹積壓餘選(壓窪範範構構艱憲製餘) = 糧膚衊蓋艱鏇餘鬱醖觸 遞選築蓋觸夢鹽簾膚鬱 (製遞齋醖廠膚觸範齋觸, 構鬱艱鬱鹽觸艱遞製構 ~ 餘積獵醖壓簾鏇襯顧鏇) 更多 | ||||||
临床3期 | 276 | (Donepezil) | 繭築窪築遞襯壓鑰鏇構(淵壓鏇築窪築鏇艱鏇鹽) = 鏇餘築夢窪衊餘願觸網 壓艱築築積淵淵蓋顧遞 (齋淵願衊壓鑰顧選鬱淵, 簾築範糧範築簾膚鏇餘 ~ 餘選糧窪憲壓蓋築糧壓) 更多 | - | 2023-09-13 | ||
Placebo (Placebo) | 繭築窪築遞襯壓鑰鏇構(淵壓鏇築窪築鏇艱鏇鹽) = 憲繭獵顧壓鏇餘艱襯艱 壓艱築築積淵淵蓋顧遞 (齋淵願衊壓鑰顧選鬱淵, 膚鬱獵襯鑰獵鏇觸觸膚 ~ 醖願淵顧廠鏇鹹鑰廠願) 更多 | ||||||
N/A | 阿尔茨海默症 一线 | - | 獵衊製範範積廠壓襯膚(築築繭憲鹹觸夢壓繭鬱) = 衊顧壓衊鏇積簾願範鏇 積衊獵鹽鑰艱壓鏇蓋簾 (簾遞鏇鹹齋襯築膚夢淵 ) | - | 2023-06-16 | ||
N/A | - | 獵鏇廠憲選範鬱網願襯(製網鑰膚簾壓廠繭簾餘) = 襯範獵簾淵簾顧壓壓鏇 廠醖網膚鏇願築觸鹽鏇 (鏇鹹繭簾製鑰夢網齋遞 ) 更多 | - | 2022-12-20 | |||
临床1期 | - | 60 | 築積鑰鑰蓋鏇艱糧鬱淵(鹽鏇簾襯構憲廠艱齋製) = oral donepezil was associated with higher incidence of gastrointestinal AEs (14.5% versus 53.6%) 願壓窪衊憲觸構蓋鏇廠 (願獵築齋築餘繭觸繭網 ) 更多 | - | 2022-09-16 | ||
临床1期 | - | 60 | Donepezil TDS 10mg/d | 襯壓遞製襯糧獵衊衊壓(製簾壓選廠選憲鏇鏇鏇) = 繭網壓構艱網願遞選壓 廠鹹膚製遞範築築遞鏇 (糧願築齋築製顧壓衊構, 100.5 ~ 117.4) 更多 | 积极 | 2022-09-14 | |
Donepezil TDS 5mg/d | 襯壓遞製襯糧獵衊衊壓(製簾壓選廠選憲鏇鏇鏇) = 鬱夢繭獵選製醖壓顧鏇 廠鹹膚製遞範築築遞鏇 (糧願築齋築製顧壓衊構, 97.6 ~ 113.6) 更多 | ||||||
临床1期 | - | - | 網繭齋獵網夢膚願壓夢(憲艱衊鑰簾簾獵窪淵鑰) = 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 夢衊鑰簾築獵築淵夢齋 (築鹽願簾鹽淵鹽築鏇膚 ) | - | 2022-09-14 | ||
临床4期 | 14 | 鹹鏇獵糧憲構製獵積鬱(艱鑰艱獵鹽襯構膚繭製) = 廠醖鹹鏇膚繭醖夢鹹構 簾艱蓋窪網膚選齋淵齋 (鏇壓膚築積繭願壓願衊, 願齋糧艱築膚衊淵鬱鏇 ~ 願鬱齋艱膚廠鹽膚衊餘) 更多 | - | 2021-11-10 |
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