Artemetero
Artemether
CAS: 71963-77-4
Molecular Formula: C16H26O5
Artemetero - Names and Identifiers
Artemetero - Physico-chemical Properties
| Molecular Formula | C16H26O5 |
| Molar Mass | 298.37 |
| Density | 1.0733 (rough estimate) |
| Melting Point | 86-88°C |
| Boling Point | 359.79°C (rough estimate) |
| Specific Rotation(α) | D19.5 +171° (c = 2.59 in CHCl3) |
| Solubility | Easily soluble in acetone or chloroform. Soluble in ethanol or ethyl acetate, almost insoluble in water. |
| Appearance | Colorless crystalline powder |
| Color | off-white to light brown |
| Merck | 14,815 |
| Storage Condition | room temp |
| Refractive Index | 1.6200 (estimate) |
| MDL | MFCD00866205 |
| Physical and Chemical Properties | White granular crystal, soluble in methanol, ethanol, DMSO and other organic solvents, derived from Artemisia annua leaves. |
| Use | Used as an antimalarial drug |
Artemetero - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 22 - Harmful if swallowed |
| Safety Description | 24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
| RTECS | KD4165000 |
| HS Code | 29329930 |
| Toxicity | LD50 i.m. in mice: 263 mg/kg (China Cooperative Research Group on Qinghaosu) |
Artemetero - Reference
| Reference Show more | 1. Zhu Chunyan, Xu Qiong, Mao Zhiyun, etc. Comparison of effects of three artemisinin derivatives on pain co-emotion disorder in mice with neuropathic pain [J]. Chinese Journal of Traditional Chinese Medicine 2018(15). 2. Wu Xuan, Su Xiaohui, Meng Xianghe, Wang Xin, Kong Xiangying, Lin Na. Comparative analysis of artemisinin and its derivatives on osteoclast differentiation [J]. Chinese Journal of Experimental prescriptions, 2018,24(04):84-89. 3. Zhuang Bintao, Ma Yuanyuan, Xie Shichen, Peng Junjie, Liang panhong, Zhu Xingquan, Yang Xiaoye, He Junjun. Effect Analysis of monensin sodium, sulfadiazine and artemether against Toxoplasma gondii RH strain tachyzoites in vitro and in vivo [J]. Chinese veterinary science, 2020,50(05):624-630. |
Artemetero - Compound Artemether Tablets
This product contains artemether (C16H2605) should be 90.0% ~ 105.0% of the label amount, containing the fluorenyl alcohol (C30H32Cl3NO) should be 95.0% ~ 105.0% of the label children.
prescription
artemether 20g
Benflumetol 120g
Appropriate amount of excipients
Made into 1000 tablets
trait
This product is yellow.
identification
- take an appropriate amount of fine powder of this product (about 20mg of artemether), add 20ml of acetone, shake, filter, and take the continued filtrate as the test solution; take appropriate amounts of artemether and benflumetol as reference, add acetone to dissolve and dilute to prepare solutions containing 6mg of artemether and benflumetol per 1 ml, as artemether control solution with benfluorenol control solution. According to the thin layer chromatography (General 0502) test, absorb the above three solutions of 10 u1, respectively, on the same silica gel GF254 thin layer plate, with n-hexane-ethyl acetate-glacial acetic acid (20:5:2.5) for the development of the solvent, expand, dry, set the UV light (254nm) under the view. The position and color of the main spot displayed by the test solution should be consistent with that of the main spot of the reference solution of benfluminol; After spraying with 20% sulfuric acid methanol solution and heating at 140°C for 10 minutes, the positions and colors of the two main spots in the test solution should be consistent with the main spots in the artemether reference solution and the fluorenyl alcohol reference solution.
- in the chromatogram recorded under the content determination item, the retention time of the two main peaks of the test solution should be consistent with the retention time of the corresponding two main peaks of the control solution.
- two items (1) and (2) above can be selected as one item.
examination
- Related substances I take 3 tablets of this product, grind them, heat them at 90°C for 1 hour, take them out, let them cool, add 5ml of water and 5ml of acetonitrile, sonicate them for 15 minutes, and centrifuge them at 4000 rpm, take the supernatant and add 1 ml of a solution containing 0.6mg of dihydroartemisinin per 1 ml [with water-acetonitrile (1:1) as solvent], 1 ml of a solution containing 0.2mg of artemether [Water-acetonitrile (1:1) as a solvent] was added per 1 ml, and the solution was shaken to be a system-suitable solution. Take 3 tablets of this product, add 6ml of water to disintegrate, add 6mL of acetonitrile, ultrasonic 15 minutes, centrifuge at 4000 rpm, take the supernatant as the test solution; Take artemether, artemether, the appropriate amount of dihydroartemisinin and artemether impurity n control was accurately weighed, and the appropriate amount of water-acetonitrile (1:1) was added to dissolve and quantitatively dilute to prepare each 1 ml containing 0 each of the above four control substances. lmg mixed solution was used as the reference stock solution; The reference stock solution was quantitatively diluted with the above solvents to prepare each lml containing artemether, artemether, dihydroartemisinin and artemether impurity II, 5ug, 10ug, 10ug respectively, 15ug, 25ug, 50ug and 75ug solution, as a control thin layer chromatography (General 0502) test, absorb the above eight kinds of solution 20 u1, respectively, on the same silica gel GF254 thin layer plate, dry in cold air, using n-hexane-ethyl acetate-glacial acetic acid (20:5:2.5) as the developing solvent (the chromatography cylinder should be saturated for 15 minutes before deployment), spread in the dark for 12cm, and dry in cold air, spray with 5% vanillin sulfuric acid solution, dry, system applicability solution should show 6 clear separation of spots (according to the size of the order from large to small artemether, unknown impurities, a- Artemether, artemether impurity I, dihydroartemisinin, artemether impurity II). Test solution such as impurity spots, a-artemether, dihydroartemisinin and Artemisia acid impurity II, and the reference solution of a-artemether, dihydroartemisinin and artemether impurity II spots shall not exceed 0.3%, 1.0% and 1.5%, respectively; Artemether impurity I, other individual impurities and the total amount of other impurities, artemether spots in the control solution were less than 0.5%, 0.2% and 0.5%, respectively.
- Related substances II take 5 tablets of this product, put them in a 500ml measuring flask, add 30ml of water, shake to disintegrate, add 100ml of N-propanol, and sonicate for 15 minutes, add ion pair solution (take sodium hexanesulfonate 5.65g and sodium dihydrogen phosphate 2.75g, add water to dissolve 800ml, adjust pH to 2.3 with phosphoric acid, dilute to 1000ml with water, shake well) 100ml and acetonitrile 200ml, sonicate for 30 minutes, cool, dilute to the scale with acetonitrile, shake well, centrifuge at 4000 rpm for 5 minutes, and take the supernatant as the test solution, quantitatively dilute with mixed solvent (take 100ml of ion-Pair Solution, add 30ml of water, mix well, add 100ml of N-propanol, and dilute to 500ml with acetonitrile to obtain) to prepare a solution containing about 1.2ug per 1 ml, as a control solution. According to the high performance liquid chromatography (General 0512) test, silica gel bonded with eighteen alkyl silane was used as the filler (Agilent Nucleosil 100-5 C18,4.OmmX125mm,5um or equivalent chromatographic column); With ion-Pair Solution-water-acetonitrile-N-propanol (20:50:25:5) as mobile phase A, ion Pair Solution-water-acetonitrile-N-propanol (20:10:65:5) was used as mobile Phase B, and gradient elution was carried out according to the following table; The detection wavelength was 300mn. Take appropriate amounts of benfluorenyl alcohol and benfluorenyl alcohol impurity I, add mixed solvent to dissolve and dilute to prepare a mixed solution containing about 1.2mg of benfluorenyl alcohol and 10.02mg of benfluorenyl alcohol impurity per 1 ml, as the system applicable solution, take 5u1 injection liquid chromatograph, record the chromatogram, the tailing factor of benfluorenol should be between 0.8 and 5.0, the resolution between the present fluorenyl alcohol peak and the present fluorenyl alcohol impurity T peak should be greater than 0.5. 5 u1 of each of the control solution and the test solution were accurately measured and injected into the human liquid chromatograph respectively, and the chromatogram was recorded. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than the area of the main peak of the control solution (0.1%), and the sum of each impurity peak area shall not be greater than 3 times the area of the main peak of the control solution (0.3%).
- The content uniformity shall be calculated according to the content of artemether and benflumetol in each tablet measured under the content determination item, and shall conform to the regulations (General rule 0941).
- the dissolution of artemether take this product, according to the dissolution and release determination method (General 0931 second method), with water as the dissolution medium, the speed is 100 rpm, according to the law, after 1 hour and 3 hours, take about 10ml of each solution, stand still for 3 minutes, filter, and take the continued filtrate as the test solution, an appropriate amount of water-acetonitrile (1:1) was added, dissolved by sonication and quantitatively diluted to prepare a solution containing about 20ug per 1 ml as a control solution. According to the high performance liquid chromatography (General 0512) test, silica gel bonded with eighteen alkyl silane was used as filler; Water-acetonitrile-N-propanol-trifluoroacetic acid (400:500:100:1) was used as mobile phase; the detection wavelength was 210nm, and the number of theoretical plates was not less than 3000 according to the calculation of artemether peak. Take 100 u1 of each of the reference solution and the test solution, respectively inject the human liquid chromatograph, and record the chromatogram. The dissolution amount of Artemether in each tablet was calculated by the peak area according to the external standard method. The limits of 45% and 65% of the labeled amount at 1 hour and 3 hours, respectively, shall be as specified.
- This fluorenyl alcohol take this product, according to the dissolution and release determination method (General 0931 second method), with 1% benzyl chloride dimethyl alkyl amine 0.lmol / L hydrochloric acid solution 1000ml as the dissolution medium, the speed is 100 rpm, according to the operation, after 45 minutes, take the solution about 10ml, stand for 3 minutes, filter, 2ml of the continuous filtrate was accurately measured, placed in a 10ml measuring flask, diluted to a scale with a dissolution medium, and shaken to be used as a test solution. The absorbance was measured at a wavelength of 0401 NM according to ultraviolet-visible spectrophotometry (General 300.8), and the amount of benfluorenyl alcohol dissolved in each tablet was calculated as the absorption coefficient of C30H32Cl3NO was. The limit is 60% of the labeled amount and shall be in accordance with the provisions.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
Content determination
- measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica gel as filler; Ion pair solution-acetonitrile (70:30) as mobile phase A, ion pair solution-acetonitrile (30:70) as the mobile phase B, the gradient elution was carried out according to the following table; The detection wavelength of artemether was 210nm, and the detection wavelength of benfluorenyl alcohol was 380mn. The number of theoretical plates shall not be less than 3000 based on the calculation of the peak of this fluorenyl alcohol, and the separation degree between the artemether peak and the peak of this fluorenyl alcohol shall be greater than 5.0.
- determination Method: Take 10 tablets of this product, put them in 100ml measuring flask respectively, add 6ml water to disintegrate, add 20ml N-propanol, sonicate for 15 minutes, add 20ml ion pair solution and 40ml acetonitrile, sonicate for 30 minutes, cool, dilute to the scale with acetonitrile, shake well, centrifuge at 4000 rpm for 5 minutes, take the supernatant as the test solution, take 20 u1 with precision, and inject human liquid chromatograph, record the chromatogram; Take the appropriate amount of artemether and benflumetol for precision weighing, A mixed solvent was added to dissolve and quantitatively dilute to prepare a solution containing about 0.2mg of artemether and 1.2mg of benflumetol per 1 ml, respectively, which was measured by the same method. The content of each tablet is calculated by peak area according to external standard method, and the average content of 10 tablets is obtained.
category
antimalarial drugs.
storage
shade, seal, and store in a cool and dry place.
attached
artemether, artemether impurity I, artemether impurity II see under artemether.
This fluorenyl alcohol impurity I see under this fluorenyl alcohol.
Last Update：2024-04-10 22:29:15
Artemetero - Reference Information
| introduction | artemether and bifluorenol are two new antimalarial drugs with different structures and functions successfully developed in recent years. Both drugs are usually treated with a single drug. The function of artemether is characterized by rapid killing of malaria parasites, but incomplete killing of insects, and the recovery rate of protozoa remaining in the patient's blood after treatment is high. |
| traits | white crystal or crystalline powder, bitter and odorless. |
| properties | this product is easily soluble in acetone and chloroform, soluble in ethanol or ethyl acetate, and almost insoluble in water. |
| use | artemether has a direct killing effect on the red inner phase of plasmodium, has no effect on the tissue phase, has low toxicity to experimental animals, absorbs blocks in the body, has wide distribution and fast excretion. Electron microscope observation shows that the main part of the action of this product on Plasmodium murine is the membrane structure, and its anti-malarial mechanism is believed to interfere with the function of the surface membrane of Plasmodium. A methyl ether derivative of artemisinin. Used as antimalarial drug |
| chemical properties | white granular crystal, soluble in methanol, ethanol, DMSO and other organic solvents, derived from Artemisia annua leaves. |
| category | toxic substances |
| toxicity classification | poisoning |
| acute toxicity | oral-mouse LD50: 1000 mg/kg; Subcutaneous-mouse LD50: 390 mg/kg |
| flammability hazard characteristics | combustible; combustion produces stimulating smoke |
| storage and transportation characteristics | ventilation and low temperature drying |
| fire extinguishing agent | dry powder, foam, sand, carbon dioxide, mist water |
| toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |
Last Update：2024-04-09 19:05:04
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Product Name: Artemether Request for quotation
CAS: 71963-77-4
Tel: 0086-551-65418684
Email: sales@tnjchem.com
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Mobile: 0086 189 4982 3763
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CAS: 71963-77-4
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
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Product List: View Catalog
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Product Name: Artemether Visit Supplier Webpage Request for quotationCAS: 71963-77-4
Tel: 18301782025
Email: 3008007409@qq.com
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QQ: 3008007409
Wechat: 18301782025
Spot supply
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Tel: +86-(0)731-84213302
Email: sales@staherb.cn
Mobile: +86 13875855783
QQ: 484702402
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