qinghausau
artemisinin
CAS: 63968-64-9
Molecular Formula: C15H22O5
qinghausau - Names and Identifiers
qinghausau - Physico-chemical Properties
| Molecular Formula | C15H22O5 |
| Molar Mass | 282.33 |
| Density | 1.0984 (rough estimate) |
| Melting Point | 156-157 °C (lit.) |
| Boling Point | 344.94°C (rough estimate) |
| Specific Rotation(α) | 76 º (c=0.5,MeOH) |
| Flash Point | 171.953°C |
| Solubility | Soluble in chloroform and acetone, insoluble in water |
| Vapor Presure | 0mmHg at 25°C |
| Appearance | White needle crystal |
| Color | Needles |
| Merck | 14,817 |
| Storage Condition | -20°C |
| Stability | Stable. Combustible. Incompatible with strong oxidizing agents, acids, acid chlorides, acid anhydrides. May absorb, and react with, carbon dioxide from the air. |
| Refractive Index | 75 ° (C=0.5, MeOH) |
| MDL | MFCD00081057 |
| Physical and Chemical Properties | melting point 156-157°C |
| Use | Used as an antimalarial drug |
qinghausau - Risk and Safety
| Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 2 |
| RTECS | KD4170000 |
| HS Code | 29322985 |
| Toxicity | LD50 in mice (mg/kg): 5105 orally; 2800 i.m.; 1558 i.p. (Koch); LD50 in mice, rats (mg/kg): 4228, 5576 orally; 3840, 2571 i.m. (China Cooperative Research Group on Qinghaosu) |
qinghausau - Reference
| Reference Show more | 1. Cui Yuchao, Zhu Qinghe, Wang Likun, etc. Screening of extraction methods for effective components of Artemisia annua L. [J]. Chinese Journal of Veterinary Medicine, 2018, v.52(04):46-51. 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. Liu Juan, Wu Shiman. Regulatory mechanism of artemisinin on peripheral blood Treg/Th17 in bronchial asthma [J]. Chinese Journal of clinicians (Electronic Edition), 2014, 000(012):2250-2255. 4. Feng Bing-yu, Zhu Yuan-gang, Wei Liang, etc. Inhibitory effect of artemisinin-β-Cyclodextrin Inclusion Complex combined with disulfiram on liver metastasis of colorectal cancer in vivo [J]. Specialty research, 2020, 042(001):6-10. 5. Jian Chen, Zhen Guo, Hai-Bao Wang, Jia-Jia Zhou, Wei-Jie Zhang, Qian-Wang Chen, Multifunctional mesoporous nanoparticles as pH-responsive Fe2 reservoirs and artemisinin vehicles for synergistic inhibition of tumor growth, Biomaterials, Volume 35, Issue 24 6. Chen, Jiajun, Lei Zhang, and Miao Hao. "Effect of artemisinin on proliferation and apoptosis-related protein expression in vivo and in vitro." Saudi journal of biological sciences 25.7 (2018): 1488-1493.https://doi.org/10.1016/j.sjbs.2018.04.003 7. Wang, Dongdong, et al. "Controllable synthesis of dual-MOFs nanostructures for pH-responsive artemisinin delivery, magnetic resonance and optical dual-model imaging-guided chemo/photothermal combinational cancer therapy." Biomaterials 100 (2016): 27-40.htt 8. [IF=12.479] Jian Chen et al."Multifunctional mesoporous nanoparticles as pH-responsive Fe2 reservoirs and artemisinin vehicles for synergistic inhibition of tumor growth."Biomaterials. 2014 Aug;35:6498 9. [IF=10.317] Dongdong Wang et al."Controllable synthesis of dual-MOFs nanostructures for pH-responsive artemisinin delivery, magnetic resonance and optical dual-model imaging-guided chemo/photothermal combinational cancer therapy."Biomaterials. 2016 Sep;100:27 10. [IF=7.79] Jian Chen et al."Mn(II) mediated degradation of artemisinin based on Fe3O4@MnSiO3-FA nanospheres for cancer therapy in vivo."Nanoscale. 2015 Jul;7(29):12542-12551 11. [IF=2.802] Jiajun Chen et al."Effect of artemisinin on proliferation and apoptosis-related protein expression in vivo and in vitro."Saudi J Biol Sci. 2018 Nov;25:1488 12. [IF=5.81] Li Peng et al."Detection of Vasodilators From Herbal Components by a Transcriptome-Based Functional Gene Module Reference Approach."Front Pharmacol. 2019 Oct;0:1144 13. [IF=6.953] Wen Zhu et al."Artemisinin hydroxypropyl-β-cyclodextrin inclusion complex loaded with porous starch for enhanced bioavailability."INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES. 2022 Jun;211:207 14. [IF=5.811] |
qinghausau - Nature
Open Data Verified Data
White needle-like crystals. The molecular weight was 282. 34, the melting point was 156-157 ℃, and the specific optical rotation was 66.3. (Chloroform). Almost insoluble in water, soluble in ethanol and ether, soluble in chloroform, acetone and ethyl acetate.
Last Update：2024-01-02 23:10:35
qinghausau - Preparation Method
Open Data Verified Data
take Artemisia annua leaf powder with 5 times the amount of Ether 3 times, extract concentrated to a small volume; And then 2% NaOH solution to remove acidic components, distilled to ether, the neutral ether extract was obtained (the yield was 2%~ 3%); The neutral ether extract was mixed with polyamide powder, percolated with 47% ethanol, and the percolation solution was concentrated to a small volume; then extracted with diethyl ether, combined with ether liquid concentration after silica gel column chromatography, with petroleum ether-10% ethyl acetate elution, 10% ethyl acetate-petroleum ether eluent concentration after crystallization, namely artemisinin (yield 0.2%).
Last Update：2022-01-01 11:15:09
qinghausau - Standard
Authoritative Data Verified Data
The content of C15H2205 shall be 98.0% to 102.0% based on the dry product.
Last Update：2024-01-02 23:10:35
qinghausau - Trait
Authoritative Data Verified Data
- This product is colorless needle-like crystal.
- This product is soluble in acetone, ethyl acetate, chloroform, dissolved in methanol, ethanol, dilute ethanol, ether and petroleum ether, almost insoluble in water; Soluble in glacial acetic acid.
melting point
The melting point of this product (General rule 0612 first method) is 150~153°C.
specific rotation
take this product, precision weighing, plus absolute ethanol dissolution and quantitative dilution to make a solution containing 10 mg per lml, determination according to law (General 0621), the specific rotation was 75 ° to 78 °.
Last Update：2022-01-01 13:32:42
qinghausau - Use
Open Data Verified Data
It is a highly effective antimalarial drug and also has a killing effect on schistosomiasis.
Last Update：2022-01-01 11:15:09
qinghausau - Differential diagnosis
Authoritative Data Verified Data
- take about 5mg of this product, add anhydrous ethanol 0.5ml to dissolve, add potassium iodide test solution 0.4ml, dilute sulfuric acid 1.5ml and starch indicator solution 4 drops, immediately purple.
- take about 5mg of this product, add 0.5ml of anhydrous ethanol to dissolve, add 0.5ml of hydroxylamine hydrochloride test solution and 0.25ml of sodium hydroxide test solution, set in water bath to slightly boil, after cooling, 2 drops of hydrochloric acid and 1 drop of ferric chloride solution were added.
- 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 220).
Last Update：2022-01-01 13:32:42
qinghausau - Exam
Authoritative Data Verified Data
Related substances
take this product, add acetone to dissolve and dilute to make a solution containing 15mg per lml as a test solution; Take 0.5 for precision measurement and put it in a 100ml measuring flask, dilute to the scale with acetone as the control solution (1); Take 5ml of the control solution (l) with precision, put it in a 10ml measuring flask, dilute with acetone, as a control solution (2); Take the artemisinin control and the dihydroartemisinin control, and add acetone to dissolve and dilute to prepare 10 mg of artemisinin and dihydroartemisinin per 1 ml. A mixed solution of 1 mg is used as a system-applicable solution. According to the thin layer chromatography (General 0502) test, absorb the above four solutions of 10 u1, respectively, on the same silica gel G thin layer plate, with petroleum ether (boiling range 60~90°C)-Acetone-glacial acetic acid (8:2:0.1) as the developing solvent, spread more than 15cm, take out, dry, spray with 20% sulfuric acid ethanol solution containing 2% vanillin, heating at 85°C for 10-20 minutes until the spots are clear, the system applicable solution should show clear spots of artemisinin and dihydroartemisinin respectively. Test solution such as impurity spots, deep in the control solution (2) main spot color (0.25%) and not deep in the control solution (1) main spot color (0.5%) no more than 1 spot, other impurity spots should not be deep in the control solution (2) show the main spot color (0.25%).
loss on drying
take this product, dry to constant weight at 80°C, weight loss shall not exceed 0.5% (General rule 0831).
ignition residue
not more than 0.1% (General rule 0841).
Last Update：2022-01-01 13:32:43
qinghausau - Content determination
Authoritative Data Verified Data
measured by high performance liquid chromatography (General 0512).
chromatographic conditions and system suitability test
silica gel bonded with eighteen alkyl silane was used as the filler; Acetonitrile-water (60:40) was used as the mobile phase; The detection wavelength was 210Nm. Take the appropriate amount of this product and the reference substance of dihydroartemisinin, add methanol to dissolve and dilute to make a mixed solution containing about 1 mg in each lml, take 20u1 and inject it into human Liquid Chromatograph. Dihydroartemisinin shows two chromatographic peaks, the degree of separation between artemisinin peak and adjacent dihydroartemisinin peak should be greater than 2.0; The number of theoretical plates should not be less than 3000 according to artemisinin peak.
assay
take about 25mg of this product, accurately weigh, put it in 25ml measuring flask, add methanol to dissolve and dilute to the scale, shake, as a test solution, accurately take 20M1 injection liquid chromatography, record chromatogram; Take artemisinin reference, the same method. According to the external standard method to calculate the peak area, that is.
Last Update：2022-01-01 13:32:44
qinghausau - Category
Authoritative Data Verified Data
antimalarial drugs.
Last Update：2022-01-01 13:32:44
qinghausau - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update：2022-01-01 13:32:44
qinghausau - Artemisinin piperaquine tablets
Authoritative Data Verified Data
This product contains artemisinin (C15H22O5) and piperaquine (C29H32C12N6) should be 90.0% ~ 110.0% of the label amount.
trait
This product is a film-coated tablet, white to light yellow after removing the coating.
identification
- take an appropriate amount of fine powder of this product (about 10mg of artemisinin), add 3ml of dichloromethane, dissolve, filter, and take the continued filtrate as the test solution; Take an appropriate amount of artemisinin reference, add anhydrous ethanol to dissolve and dilute to prepare a solution containing 3mg per 1 ml as artemisinin reference solution; Take an appropriate amount of piperaquine reference, add methylene chloride to dissolve and dilute to prepare a solution containing 18mg per 1 ml, as a piperaquine control solution. According to the thin layer chromatography (General 0502) test, absorb the above three solutions each 5 u1, respectively, on the same silica gel GF254 thin layer plate, with dichloromethane-n-hexane-diethylamine (5:5:1) for the development of the opening agent (the thin layer plate is pre-saturated for 20 minutes), after deployment, dry, set the UV light (254mn) under the inspection. The position and color of the main spot of the test solution should be consistent with the main spot of the piperaquine reference solution; Then spray with anisaldehyde methanol solution (take 10ml of glacial acetic acid and 5ml of concentrated sulfuric acid, slowly add to 55ml of methanol, cool, add this solution to 30ml of methanol containing ml of anisaldehyde, shake, protect from light), heated at 110°C for 3-5 minutes to develop color, the position and color of the main spot displayed by the test solution should be consistent with the main spot of the artemisinin control solution.
- in the chromatogram recorded under the content determination of artemisinin and piperaquine, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the control solution.
- take an appropriate amount of the fine powder of this product (about 60mg of artemisinin), add 2ml of acetone, shake to dissolve, filter, evaporate the filtrate in a 60°C water bath, and dry at 80°C for 30 minutes, determined by infrared spectrophotometry (General 0402). Except for a small set of absorption peaks at 220-1, the infrared absorption spectrum of this product should be consistent with the control spectrum (Spectrum set).
- take an appropriate amount of fine powder of this product (about equivalent to piperaquine lOOmg) and add 0.lmol/L hydrochloric acid solution 15ml, shake to dissolve, filtered, filtrate in separatory funnel, add lmol/L sodium hydroxide solution 2ml, make white precipitate, add dichloromethane 15ml, shaking extraction, static stratification, take the dichloromethane layer washed with water 2 times, each time 15ml, take the dichloromethane layer, through anhydrous sodium sulfate filtration, filtrate 60 deg C water bath to dry, dry at 80°C for 30 minutes and measure by infrared spectrophotometry (General 0402). The infrared absorption spectrum of this product should be consistent with the control spectrum (Spectrum set 274 Figure).
- two items (1) and (2) above can be selected as one item.
examination
- Take appropriate amount of fine powder (about equivalent to artemisinin lOOmg) under the content determination item of related substances, add appropriate amount of acetone to dissolve, filter, volatilize the residue to acetone, add 80% acetonitrile to dissolve and dilute to 10ml, shake, as a test solution; Precision take 1 ml, put in a ml measuring flask, diluted with 80% acetonitrile to scale, shake, as a control solution. An appropriate amount of 7-chloro-4-hydroxyquinoline (impurity II) control was taken, dissolved and diluted with 80% acetonitrile to prepare a solution containing about 1 ml as the impurity II positioning solution. According to the chromatographic conditions of artemisinin under the content determination item, 20ul of each of the above solutions were accurately measured and injected into human liquid chromatography respectively. The chromatogram was recorded to 1.5 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, except the impurity II peak, Artemisia annua (impurity I, relative retention time is about 0.8) the peak area multiplied by the correction factor of 0.027 shall not be greater than 0.2 times (0.2%) of the main peak area of the control solution, and the peak area of other individual impurities shall not be greater than 3 times (3.0%) of the main peak area of the control solution, the sum of each impurity peak area shall not be greater than 5 times (5.0%) of the main peak area of the control solution. The chromatogram of the test solution is 0.05 times smaller than the main peak area of the control solution.
- the related substances were protected from light. Take the appropriate amount of fine powder under the content determination item, add the mobile phase to dissolve and dilute to make a solution containing about 1 mg of piperaquine per 1ml, filter, and take the continued filtrate as the test solution; Take 1ml for precision measurement, set in a 100ml measuring flask, dilute to the scale with the mobile phase, and shake to serve as a control solution. In addition to the detection wavelength of 216nm, according to the chromatographic conditions of piperaquine under the content determination item, 20 u1 of the test solution and the control solution were accurately measured, and human liquid chromatography was injected respectively, the chromatogram was recorded to 3 times of the retention time of the main component 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 the area of the main peak of the control solution (1.0%), and the sum of each impurity peak area shall not be greater than 2.5 times (2.5%) of the area of the main peak of the control solution..
- dissolution artemisinin take this product, according to the dissolution and release determination method (General 0931 second method), with 0.5% sodium dodecyl sulfate phosphate buffer (sodium dihydrogen phosphate 6.9g, sodium hydroxide 0.9g, sodium Dodecyl Sulfate 5G, add water 800ml, ultrasonic for 30 minutes, adjust pH to 6.8 with 2mol/L sodium hydroxide solution, dilute to 1000ml)1000ml with water as dissolution medium, rotate at 75 rpm, operate according to law, after 45 minutes, the solution was filtered, and the filtrate was taken as the test solution, add anhydrous ethanol to dissolve and quantitatively dilute to prepare a solution containing about 1.25mg per 1 ml, shake well, take 5ml accurately, put it in a 100ml measuring flask, dilute to the scale with dissolution medium, shake well, as a control solution. The dissolution amount of each tablet was calculated as measured by the method under the content measurement item. The limit is 70% of the labeled amount and shall be in accordance with the provisions.
- take piperaquine and take 0931 mol/L hydrochloric acid solution as dissolution medium at 50 RPM according to the dissolution and release determination method (General rule 0.05 second method), operate according to law, after 30 minutes, take 10ml of the solution, filter, take 2ml of precision, put it in a 100ml measuring flask, dilute to the scale with dissolution medium, shake well, as a test solution; another appropriate amount of piperaquine reference substance was added to precisely weigh the solution, dissolved with dissolution medium and quantitatively diluted to prepare a solution containing 0.75mg per lml. Shake well, precisely weigh 1 ml and place it in a 100ml measuring flask, dilute to the scale with the dissolution medium, shake, as a control solution. The elution amount of each tablet was calculated by measuring the absorbance at a wavelength of 0401 NM according to ultraviolet-visible spectrophotometry (general rule). The limit is 80% 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
- halogen was measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica gel as filler (4.6 mmX150mm,5um ); Acetonitrile-water (50:50) as mobile phase; The detection wavelength was 210mn; the degree of separation between the artemisinin peak (retention time of about 10 minutes) and the impurity I Peak (relative retention time of about 0.8) should be greater than 4.0.
- determination of 20 tablets of this product, precision weighing, fine grinding, precision weighing appropriate amount (about equivalent to artemisinin lOOmg), 100ml measuring flask, add appropriate amount of acetonitrile, ultrasonic dissolution, cool, dilute to scale with acetonitrile, shake, filter, take the filtrate as a test solution, take 20ul of precision, inject into the liquid chromatograph, record the chromatogram; Take an appropriate amount of artemisinin reference, precision weighing, plus acetonitrile dissolved and quantitative dilution to prepare about 1 mg per 1 mL solution, the same method for determination. According to the external standard method to calculate the peak area, that is.
- Piperaquine was measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica gel as filler; Acetonitrile-0.1% trichloroacetic acid solution-triethylamine (18:82:0.2, phosphoric acid to adjust pH to 2.5) mobile phase; The detection wavelength was 347MN; The resolution between piperaquine peak and adjacent chromatographic peaks should be greater than 2.0.
- determination method: take an appropriate amount of the above-mentioned fine powder (about 250mg equivalent to piperaquine), weigh it accurately, place it in a 250ml measuring flask, add an appropriate amount of mobile phase, dissolve it with ultrasound, and let it cool, dilute to the scale with mobile phase, shake, filter, Take 5ml of filtrate accurately, put it in 50ml measuring flask, dilute to the scale with mobile phase, shake well, as a test solution, take 20 u1 accurately, inject human liquid chromatograph, record chromatogram; Take appropriate amount of piperaquine reference substance, accurately weigh, add mobile phase to dissolve and quantitatively dilute to make about 0 in 1 ml. lmg solution, the same method for determination. According to the external standard method to calculate the peak area, that is.
category
antimalarial drugs.
storage
shade, seal, and store in a cool and dry place.
Last Update：2022-01-01 13:32:45
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