DONEPEZIL HYDROCHLORIDE
Donepezil hydrochloride
CAS: 120011-70-3;110119-84-1
Molecular Formula: C24H30ClNO3
DONEPEZIL HYDROCHLORIDE - Names and Identifiers
| Name | Donepezil hydrochloride |
| Synonyms | E-2020 ARICEPT AKOS 226-31 DonepezilHCL DONEPEZIL HCL Donepezil HCl Donepezil hydrochloride Donezepil hydrochloride DONEPEZIL HYDROCHLORIDE DonepezilHcl120011-70-3 An oxidized polyethylene wax Aricept, E-2020 Donepezil HCl DONEPEZIL (DONEPEZIL HYDROCHLORIDE) 2-(1-Benzylpiperidin-4-ylmethyl)-5,6-dimethoxyindan-1-one hydrochloride 2-[(1-Benzyl-4-piperidyl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one hydrochloride 2,3-dihydro-5,6-dimethoxy-2-{[1-(phemylmethyl)-4-piperidinyl]methyl}-1H-indan-1-one HCL 2,3-dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-1h-inden-1-one hydrochloride |
| CAS | 120011-70-3 110119-84-1 |
| EINECS | 1312995-182-4 |
| InChI | InChI=1/C24H29NO3.ClH/c1-27-22-14-19-13-20(24(26)21(19)15-23(22)28-2)12-17-8-10-25(11-9-17)16-18-6-4-3-5-7-18;/h3-7,14-15,17,20H,8-13,16H2,1-2H3;1H |
DONEPEZIL HYDROCHLORIDE - Physico-chemical Properties
| Molecular Formula | C24H30ClNO3 |
| Molar Mass | 415.95 |
| Boling Point | 527.9°C at 760 mmHg |
| Flash Point | 273.1°C |
| Solubility | DMSO : 6.2 mg/mL (14.91 mM) |
| Vapor Presure | 3.11E-11mmHg at 25°C |
| Appearance | White crystal |
| Storage Condition | 2-8℃ |
| Physical and Chemical Properties | White crystals. |
DONEPEZIL HYDROCHLORIDE - Risk and Safety
| Toxicity | 生殖毒性：大鼠给予10mg/kg/天（按体表面积折算，约为推荐人用最大剂量的8倍），生育力未受影响。妊娠大鼠和家兔分别给予多奈哌齐达16和10mg/kg/天（按体表面积折算，分别约为推荐人用最大剂量的13和16倍），未见明显致畸作用。另一试验中大鼠从妊娠第17天到分娩后第20天连续给予多奈哌齐10mg/kg/天（按体表面积折算，约为推荐人用最大剂量的8倍），死产数轻微升高，产后4天内子代的成活率轻微下降。 遗传毒性：在Ames细菌回复突变试验中未见多奈哌齐具有致突变性。中国仓鼠肺细胞染色体畸变试验中，可见多奈哌齐产生诱裂作用。小鼠微核试验中多奈哌齐未产生诱裂作用。致癌性：目前尚无多奈哌齐的致癌性研究资料。 |
DONEPEZIL HYDROCHLORIDE - Reference
| Reference Show more | 1. Xue Jiao, Gu Yewei, Han Yuqian. Effect of DHA Phosphatidylserine on Learning and Memory of Scopolamine Dementia Model Mice [J]. China Marine Drug 2020 039(001):26-30. 2. Yu Xiufang, Lei Xia, Cao Ling, et al. Effects of Buyang Huanwu Decoction on Hippocampal Apoptosis Factors and Learning and Memory Ability in Alzheimer's Disease Mice [J]. Chinese Journal of Experimental Prescription, 2018, 24(03):109-113. 3. Zhou Wei, Yu Guozhen, Liu Yamin, et al. Baicalin Regulates Apoptosis of HT22 Cells Induced by Aβ25-35 through IκBα/NF-κB Pathway [J]. Chinese Patent Medicine, 2019, 041(011):2765-2769. 4. Li Jie, Mao Yu, Jiang Kexin, Ma Lei, Wang Rui. Tanshinone ⅡA alleviates cognitive impairment in rats by improving mitochondrial function and oxidative stress [J]. Journal of East China University of Science and Technology (Natural Science Edition),2021,47(01):48-57. 5. [IF = 5.34] Dongli Li et al."Systems pharmacology approach uncovers the therapeutic mechanism of medicarpin against scopolamine-induced memory loss." Phytomedicine. 2021 Oct;91:153662 6. [IF = 5.076] Wan Ping et al."FA-97, a New Synthetic Caffeic Acid Phenethyl Ester Derivative, Protects against Oxidative Stress-Mediated Neuronal Cell Apoptosis and Scopolamine-Induced Cognitive Impairment by Activating Nrf2/HO-1 Signaling." Oxid Med Cell Longev. 2019;2 7. [IF = 3.038] Bing Cao et al."Amentoflavone Ameliorates Memory Deficits and Abnormal Autophagy in Aβ 25 35 -Induced MICE BY MTOR Signaling." Neurochem Res. 2021 Apr;46(4):921-934 8. [IF = 2.557] Hongyan Wang et al."Donepezil down-regulates propionylation, 2-hydroxyisobutyrylation, butyrylation, succinylation, and crotonylation in the brain of bilateral common carotid occlusion-induced vascular dementia ats." Clin Exp Pharmacol P. 2020 Oct; 9. [IF = 3.252] Mengnan Zeng et al."Adenosine ameliorated Aβ25 35-induced brain injury through the inhibition of apoptosis and oxidative stress via an ER α pathway." BRAIN RESEARCH. 2022 Aug;1788:147944 10. [IF = 5.34] Mengnan Zeng et al."Corallodiscus flabellata B .L. Burtt extract and isonuomioside A ameliorate Aβ25 − 35-induced brain injury by inhibiting apoptosis, oxidative stress, and autophagy via the NMDAR2B/CamKⅡ/PKG pathway." PHYTOMEDICINE. 2022 Jul;101:154114 |
DONEPEZIL HYDROCHLORIDE - Standard
Authoritative Data Verified Data
This product is (± )-2-[(1-benzyl-4-piperidinyl) methyl]-5, 6-dimethoxy-1-indanone hydrochloride. The content of C24H29N03 • HCl should be between 98.0% and 102.0% calculated on the dried product.
Last Update：2024-01-02 23:10:35
DONEPEZIL HYDROCHLORIDE - Trait
Authoritative Data Verified Data
- This product is white or off-white crystalline powder.
- This product is soluble in chloroform, soluble in water, slightly soluble in ethanol; Slightly soluble in hydrochloric acid solution (1-1000).
Last Update：2022-01-01 15:03:48
DONEPEZIL HYDROCHLORIDE - Differential diagnosis
Authoritative Data Verified Data
- take an appropriate amount of this product, add water to dissolve and dilute to make a solution containing about 20ug per lml, and measure by UV-visible spectrophotometry (General rule 0401) at 230nm, there is a maximum absorption at the wavelength of 271nm and 316nm, and a minimum absorption at the wavelength of 220nm, 245nm and 290nm.
- in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 1188).
- the aqueous solution of this product was chloride identification (1) of the reaction (General 0301).
- two items (1) and (2) above can be selected as one item.
Last Update：2022-01-01 15:03:48
DONEPEZIL HYDROCHLORIDE - Exam
Authoritative Data Verified Data
acidity
take 0.20g of this product, Add 10ml of water to dissolve, and measure according to law (General rule 0631). The pH value should be 4.5~6.0.
clarity and color of solution
take 0.20g of this product and add 10ml of water to dissolve. The solution should be clear and colorless. If it is turbid, it should not be more concentrated than the No. 2 Turbidity standard solution (General rule 0902 first method).
bromide
take this product l. Add 10ml of water, dissolve in water bath, cool, add 3 drops of hydrochloric acid and 1ml of chloroform, and add 2% chloramine T solution Dropwise while shaking (ready for use) 3 drops, chloroform layer such as color, with the standard potassium bromide solution (precision weighing at 105°C dry to constant weight of potassium bromide 0.1489g, dissolved in water and diluted to 100ml, shake, that is) 1.0, compared with the control solution prepared by the same method, no deeper (0.1%).
Related substances
take about 10mg of this product, put it in a 25ml measuring flask, add the mobile phase to dissolve and dilute to the scale, shake well, as a test solution; Take 1ml for precision measurement, put it in a 200ml measuring flask, dilute with mobile phase to the scale, shake, as a control solution; Precision take the control solution 2ml, 50ml flask, diluted with mobile phase to the scale, shake, as a sensitivity solution. According to the chromatographic conditions under the content determination item, the sensitivity solution 20 u1 is accurately measured and injected into the human liquid chromatograph, and the signal-to-noise ratio of the main component chromatographic peak is not less than 10; then 20 u1 of the test solution and the control solution are respectively injected into the liquid chromatograph, and the chromatogram is recorded to 2 times of the retention time of the main component chromatographic peak. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than 0.2 times (0.1%) the area of the main peak of the control solution, and the sum of the areas of each impurity peak shall not be greater than the area of the main peak of the control solution (0.5%). The peak less than the main peak area of the sensitivity solution in the chromatogram of the test solution is negligible (0.02%).
loss on drying
take this product, dry to constant weight at 105°C, weight loss shall not exceed 0.5% (General rule 0831).
ignition residue
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
Heavy metals
The residue left under the item of taking the ignition residue shall not contain more than 20 parts per million of heavy metal when examined by law (General rule 0821, Law II).
Last Update：2022-01-01 15:03:49
DONEPEZIL HYDROCHLORIDE - Content determination
Authoritative Data Verified Data
measured by high performance liquid chromatography (General 0512).
chromatographic conditions and system suitability test
silica gel bonded with octanoalkyl silane as filler (4.6mm X 150mm ,5um or equivalent); Sodium 1-decanesulfonate G dissolved in water, 350ml of acetonitrile and 1 ml of perchloric acid were added and mixed evenly as mobile phase. The detection wavelength was 271nm. The flow rate is adjusted so that the retention time of the main component chromatographic peak is about 11 minutes, the number of theoretical plates is not less than 3000 calculated by donepezil peak, and the separation degree between donepezil peak and adjacent impurity peaks shall meet the requirements.
assay
take about 25mg of this product, precision weighing, put in 25ml measuring flask, add mobile phase to dissolve and dilute to the scale, shake, take 5ml precision, put in 50ml measuring flask, dilute to scale with mobile phase, shake well, as a test solution, and inject 10u1 into liquid chromatograph with precise amount, record chromatogram; Take donepezil hydrochloride reference substance, and determine with the same method. According to the external standard method to calculate the peak area, that is.
Last Update：2022-01-01 15:03:50
DONEPEZIL HYDROCHLORIDE - Category
Authoritative Data Verified Data
acetylcholinesterase inhibitors.
Last Update：2022-01-01 15:03:50
DONEPEZIL HYDROCHLORIDE - Storage
Authoritative Data Verified Data
shade, seal, and store in a cool place.
Last Update：2022-01-01 15:03:50
DONEPEZIL HYDROCHLORIDE - Reference Information
| Treatment of Alzheimer's disease | Donepezil hydrochloride is a treatment of Alzheimer's disease. It is a second-generation cholinesterase (ChE) inhibitor. It is clinically used for the treatment of mild or moderate Alzheimer's dementia symptoms. Compared with similar drugs, it has the characteristics of low incidence of adverse reactions and obvious curative effect, it is the only drug that can meet the standards of the US Food and Drug Administration's dementia treatment guidelines, and it is also the only new drug approved by the US FDA and the UK MCA for the treatment of mild to moderate Alzheimer's disease. At present, it is believed that the pathogenesis of cognitive impairment in Alzheimer's disease is partly related to the low cholinergic neurotransmission function. Donepezil hydrochloride can play a therapeutic role by enhancing the function of cholinergic nerves. It reversibly inhibits the hydrolysis of acetylcholine by acetylcholinesterase, thereby increasing the concentration of acetylcholine at the receptor site. According to the above mechanism of action, as the course of the disease progresses, the functional cholinergic neurons gradually decrease, and the effect of donepezil may be weakened. There is no evidence that donepezil can alter the underlying course of dementia. |
| toxicity | reproductive toxicity: rats were given 10 mg/kg/day (calculated according to body surface area, about 8 times the maximum dose recommended for human use), and fertility was not affected. Pregnant rats and rabbits were given donepezil 16 and 10mg/kg/day respectively (calculated according to body surface area, about 13 and 16 times of the maximum dose recommended for human use, respectively), and no obvious teratogenic effect was found. In another experiment, rats were given donepezil 10mg/kg/day continuously from the 17th day of pregnancy to the 20th day after delivery (calculated by body surface area, about 8 times the maximum dose recommended for human use), and the number of stillbirths increased slightly, and the survival rate of offspring decreased slightly within 4 days after delivery. Genotoxicity: Donepezil was not mutagenic in Ames bacterial mutation test. In the chromosome aberration test of Chinese hamster lung cells, donepezil can be seen to induce cleavage. Donepezil did not induce cleavage in mouse micronucleus test. Carcinogenicity: There is no research data on the carcinogenicity of donepezil. |
| precautions | 1. patients who are highly sensitive to donepezil hydrochloride or piperidine derivatives are contraindicated. 2. It has an impact on patients with heart disease, asthma or obstructive pulmonary disease, and can also increase the risk of peptic ulcer. 3. Choline-like effect may cause urinary retention and convulsions (which may be related to the primary disease). Attention should be paid to observation during medication. 4. It has antagonistic effect with succinylcholine muscle relaxants and anticholinergic drugs, so it cannot be used together. |
Last Update：2024-04-09 20:48:19
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