173531-58-3
Naphthoquine Phosphate
CAS: 173531-58-3
Molecular Formula: C24H31ClN3O5P
173531-58-3 - Names and Identifiers
173531-58-3 - Physico-chemical Properties
| Molecular Formula | C24H31ClN3O5P |
| Molar Mass | 507.95 |
| Solubility | 10 mM in DMSO |
| Storage Condition | under inert gas (nitrogen or Argon) at 2-8°C |
| In vivo study | The monkeys (Treated with Plasmodium knowlesi ) are treated i.g. once daily for 3 days with 6 or 10 mg/kg of Naphthoquine phosphate respectively. At 24 h after Naphthoquine phosphate administration, the parasite reduction rate is higher than 90%. |
173531-58-3 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.65 ml | 8.252 ml | 16.503 ml |
| 5 mM | 0.33 ml | 1.65 ml | 3.301 ml |
| 10 mM | 0.165 ml | 0.825 ml | 1.65 ml |
| 5 mM | 0.033 ml | 0.165 ml | 0.33 ml |
Last Update：2024-01-02 23:10:35
173531-58-3 - Compound naphthoquine phosphate tablets
Authoritative Data Verified Data
This product contains naphthoquine phosphate (C24H28N3OCl • 2H3PO4 • 2H2O) and artemisinin (C15H2205) should be 90.0% ~ 110.0% of the label amount.
prescription
naphthoquine phosphate (equivalent to naphthoquine) 78.3g(50g ) 156.6g( 100g)
Artemisinin 125g 250g
Appropriate amount of excipients
Made of 1000 tablets 1000 tablets
trait
This product is a light yellow tablet or film-coated tablet, which shows a light yellow color after removing the coating.
identification
- take an appropriate amount of the fine powder of this product (about 30mg of artemisinin), add 10ml of anhydrous ethanol, shake to dissolve artemisinin, filter, and take several drops of the filtrate on the white porcelain plate, add 1 drop of 1% vanillin sulfuric acid solution, which shows pink color.
- take the test solution under the item of naphthoquine phosphate for content determination and measure it by UV-Vis spectrophotometry (General rule 0401), there is a maximum absorption at the wavelength of 341Nm and 221nm.
- take an appropriate amount of fine powder of this product (about 50mg of naphthoquine), add 10ml of water, heat to dissolve naphthoquine phosphate, filter, take 5ml of filtrate, add several drops of ammonia test solution, filter, the reaction of (2) and (3) was identified by neutralization with sulfuric acid, and the solution showed phosphate (general document 0301).
examination
- Related substances I take an appropriate amount of fine powder of this product (about 50mg equivalent to naphthoquine), add 70% methylated solution, fully shake, filter, the filtrate was taken as a test solution; 1ml was accurately measured, placed in a 70% measuring flask, diluted to a scale with methanol solution, and shaken to obtain a control solution. According to the thin layer chromatography (General 0502) test, absorb the above two solutions of 40 u1, respectively, on the same silica gel HF254 thin layer plate, with petroleum ether-ethyl acetate-diethylamine (20:6:1) for the development of the solvent, expand, take out, dry, set the UV lamp (254nm) under the inspection, the test solution such as impurity spots, compared with the main spot of the control solution, not deeper, and impurity spots should not be more than 2.
- Related substances II: take an appropriate amount of fine powder of this product (about 150mg of artemisinin), add 10ml of acetone, fully shake, filter, and take the continued filtrate as the test solution; take 0.5ml accurately, put it in a 100ml measuring flask, dilute it to the scale with acetone, shake it, and use it as the control solution (1 ) ; Take 5ml of the control solution (l) accurately, put it in a 10ml measuring flask and use it. Ketone diluted to the scale, shake, as a control solution (2 ); Take the appropriate amount of artemisinin and dihydroartemisinin, and acetone dissolved and diluted to make every 1 ml containing artemisinin lOmg and dihydroartemisinin 0. A mixed solution of 1 mg is used as a system-applicable solution. According to the thin layer chromatography (General 0502) test, absorb 10 u1 of each of the above four solutions and put them on the same silica gel G thin layer plate respectively, 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% fermentative solution containing 2% vanillin, and heat at 85°C for 10~20 minutes until the spots are clear. The applicable solutions of the system 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%).
- dissolution naphthoquine phosphate this product was taken according to the dissolution and release determination method (General rule 0931 method 1), using water as dissolution medium, rotating speed of 100 rpm, operate according to law, after 30 minutes, take 5ml of solution, filter, take 2ml (prescription I) or lml (prescription II) of the filtrate, put it in a 10ml measuring flask, dilute it with water to the scale, shake well and measure the absorbance at the wavelength of 341mn by UV-Vis spectrophotometry (General 0401). Calculate the dissolution of each tablet according to the absorption coefficient of C24H28N3OCl • 2H3P04 • 2H20 of 295, the limit is 70% of the labeled amount and shall be in accordance with the provisions.
- artemisinin take this product, according to the dissolution and release determination method (General rule 0931 The second method), with 0.5% of sodium dodecylcorylester solution as the dissolution medium, speed is 100 rpm, after 45 minutes, take 10ml of the solution, filter it, take 5ml of the filtrate accurately, put it in a 50ml measuring flask, add 5ml of anhydrous fermentation broth and 20ml of 0.2% sodium hydroxide solution, shake it well, heat in a water bath at 50°C for 30 minutes, take it out, cool it in running water, let it cool, and use it as a test solution. Take another artemisinin reference product about 10 mg, weigh it accurately, and put it in a 50ml measuring flask, add anhydrous ethanol to dissolve and dilute to the scale, shake well, take 5ml accurately, put it in a 50ml measuring flask, and operate in the same method from "add absolute ethanol 5ml", as a reference solution. According to the high performance liquid chromatography (General 0512) test, the octanosilane bonded silica gel was used as the filler; The methanol-phosphate buffer solution (pH 5.8 ) (50:50) was used as the mobile phase; the detection wavelength was 260mn, and the number of theoretical plates was not less than 2000 according to the artemisinin peak. Take the above two kinds of solution, dilute to the scale with 0.08mol/L acetic acid solution respectively before injection, shake well, immediately take 20ul accurately and inject into liquid chromatograph respectively, record chromatogram, according to the external standard method, the dissolution amount of each tablet is calculated by the peak area of artemisinin, and the limit is 70% of the labeled amount.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
Content determination
-
Take 20 tablets of caicoquine phosphate, precise weighing, fine grinding, precise weighing appropriate amount (equivalent to 20mg of naphthoquine phosphate), put it in a 100ml measuring flask, and add O.Olmol/L phosphoric acid solution, shaking to dissolve naphthoquine phosphate, with O. Dilute the Olmol/L phosphoric acid solution to the scale, shake well, filter, Take 5ml of the filtrate accurately, put it in a 50ml measuring flask, dilute it to the scale with water, shake well, and use it as a test solution, the absorbance was measured at a wavelength of 0401 NM according to UV-Vis spectrophotometry (General 295), and the absorption coefficient of C24H28N3OCl · 2H3P04 · 2H20 was calculated.
- crude Artemisia acid was determined by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica gel as filler; Acetonitrile-water (55:45) as mobile phase; The detection wavelength was 210mn. The number of theoretical plates shall not be less than 2000 according to artemisinin peak.
- determine the content of naphthoquine phosphate, accurately weigh the appropriate amount (about 50mg equivalent to artemisinin), put it in a 25ml measuring flask, add the appropriate amount of acetonitrile, shake to dissolve artemisinin, dilute with acetonitrile to scale, shake, filter, take the filtrate accurately and inject 20u1 into the liquid chromatograph, record the chromatogram; Take an appropriate amount of artemisinin reference product, weigh it accurately, acetonitrile was added for dissolution and quantitative dilution to make about 2 per 1 ml. 0mg solution, the same method. According to the external standard method to calculate the peak area, that is.
category
antimalarial drugs.
storage
sealed and stored in a dry place.
Last Update：2022-01-01 14:18:35
173531-58-3 - Reference Information
| biological activity | Naphthoquine phosphate is an effective antimalarial agent with oral activity. Naphthoquine phosphate has a complete killing function against the schizonts of a variety of plasmodium, including the resistance of Plasmodium falciparum to chloroquine. |
Last Update：2024-04-09 20:45:29
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CAS: 173531-58-3
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
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Product Name: Naphthoquine (phosphate) Visit Supplier Webpage Request for quotation
CAS: 173531-58-3
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Mobile: 18021002903
QQ: 3008007409
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CAS: 173531-58-3
Tel: 18301782025
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