6,8-Difluoro-1-(2-Fluoroethyl)-1,4-Dihydro-7-(4-Methyl-1-Piperazinyl)-4-Oxo-3-Quinolinecarboxylic Acid
Fleroxacin
CAS: 79660-72-3
Molecular Formula: C17H18F3N3O3
6,8-Difluoro-1-(2-Fluoroethyl)-1,4-Dihydro-7-(4-Methyl-1-Piperazinyl)-4-Oxo-3-Quinolinecarboxylic Acid - Names and Identifiers
6,8-Difluoro-1-(2-Fluoroethyl)-1,4-Dihydro-7-(4-Methyl-1-Piperazinyl)-4-Oxo-3-Quinolinecarboxylic Acid - Physico-chemical Properties
| Molecular Formula | C17H18F3N3O3 |
| Molar Mass | 369.34 |
| Density | 1.409±0.06 g/cm3(Predicted) |
| Melting Point | 264-266°C |
| Boling Point | 535.3±50.0 °C(Predicted) |
| Flash Point | 277.6°C |
| Solubility | 0.1 M NaOH: 10 mg/mL |
| Vapor Presure | 2.73E-12mmHg at 25°C |
| Appearance | Solid(white to off-white) |
| Color | white to off-white |
| Merck | 14,4099 |
| pKa | -0.54±0.20(Predicted) |
| Storage Condition | Sealed in dry,Room Temperature |
| Refractive Index | 1.568 |
| MDL | MFCD00864880 |
| Physical and Chemical Properties | Acute toxic LD50 mice, rats, dogs (mg/kg):>4000,>4000,>1000 oral. Acute toxic LD50 mice (mg/kg):217~237 intravenous injection. Fleroxacin hydrochloride (Fleroxacin Hydrochloride):Cl7H18F3N3O3?HCl. Crystallized in water with melting point 269~271 ℃ (decomposition). |
| Use | Broad-spectrum antibacterial agents |
| In vivo study | Fleroxacin (Ro 23-6240) is a new trifluorinated quinolone exhibiting high activity against a broad spectrum of gram-negative and gram-positive bacteria. Fleroxacin is characterized pharmacokinetically by a long elimination half-life (9 to 10 h) and high concentrations in plasma (e.g., maximum concentration of 2.3 micrograms/ml after an oral dose of 200 mg). Fleroxacin (Ro 23-6240) is effective against Haemophilus ducreyi in vitro. Fleroxacin (Ro 23-6240), 200 or 400 mg as a single oral dose, is efficacious therapy for microbiologically proven chancroid in patients who do not have concurrent HIV-1 infection. Among HIV-1-infected men, a single dose of 200 or 400 mg of fleroxacin is inadequate therapy for chancroid. |
6,8-Difluoro-1-(2-Fluoroethyl)-1,4-Dihydro-7-(4-Methyl-1-Piperazinyl)-4-Oxo-3-Quinolinecarboxylic Acid - Risk and Safety
| WGK Germany | 2 |
| RTECS | VB1999050 |
| HS Code | 29335990 |
6,8-Difluoro-1-(2-Fluoroethyl)-1,4-Dihydro-7-(4-Methyl-1-Piperazinyl)-4-Oxo-3-Quinolinecarboxylic Acid - Reference
| Reference Show more | 1. [IF=7.514] Bolong Fang et al."Glucose oxidase-induced colorimetric immunoassay for qualitative detection of danofloxacin based on iron (Ⅱ) chelation reaction with phenanthroline."Food Chem. 2020 Oct;328:127099 2. [IF=2.863] Yu Zhang et al."Antibiotic residues in cattle and sheep meat and human exposure assessment in southern Xinjiang, China."Food Sci Nutr. 2021 Nov;9(11):6152-6161 |
6,8-Difluoro-1-(2-Fluoroethyl)-1,4-Dihydro-7-(4-Methyl-1-Piperazinyl)-4-Oxo-3-Quinolinecarboxylic Acid - Standard
Authoritative Data Verified Data
This product is 6, 8-difluoro-1-(2-fluoroethyl)-1, 4-dihydro-7 '-4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid. The content of fleroxacin (C17H18F3N303) should be 98.5% to 102.0% based on the dry product.
Last Update：2024-01-02 23:10:35
6,8-Difluoro-1-(2-Fluoroethyl)-1,4-Dihydro-7-(4-Methyl-1-Piperazinyl)-4-Oxo-3-Quinolinecarboxylic Acid - Trait
Authoritative Data Verified Data
- This product is white to yellowish crystalline powder; Odorless.
- This product is slightly soluble in dichloromethane, very slightly soluble in methanol, very slightly soluble or almost insoluble in water, almost insoluble in ethyl acetate; Soluble in glacial acetic acid, slightly soluble in sodium hydroxide solution.
Last Update：2022-01-01 13:40:41
6,8-Difluoro-1-(2-Fluoroethyl)-1,4-Dihydro-7-(4-Methyl-1-Piperazinyl)-4-Oxo-3-Quinolinecarboxylic Acid - Differential diagnosis
Authoritative Data Verified Data
- take an appropriate amount of this product and fleroxacin reference substance, and add methylene chloride-methanol (4:1) respectively to make a solution containing 1 mg per 1 ml as the test solution and the reference solution; an appropriate amount of fleroxacin control and ofloxacin control was separately taken, and dichloromethane-methanol (4:1) was added to prepare a mixed solution containing about 1 mg fleroxacin and 1 mg ofloxacin per 1 ml as a system-applicable solution. According to the thin layer chromatography (General 0502) test, draw 2ul of each of the above three solutions, respectively, on the same silica gel GF 254 thin layer plate, with ethyl acetate-methanol-concentrated ammonia solution (5:6:2) for the purpose of developing the solvent, expanding, taking out, drying, and placing the UV lamp (254nm) for viewing, the system applicable solution should show two clearly separated spots, the position and fluorescence of the main spot displayed by the test solution should be the same as the position and fluorescence of the main spot of the control solution.
- 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 799).
- two items (1) and (2) above can be selected as one item.
Last Update：2022-01-01 13:40:41
6,8-Difluoro-1-(2-Fluoroethyl)-1,4-Dihydro-7-(4-Methyl-1-Piperazinyl)-4-Oxo-3-Quinolinecarboxylic Acid - Exam
Authoritative Data Verified Data
clarity and color of solution
take 5 parts of this product, each 0.5g, respectively, after adding 10ml of sodium hydroxide solution to dissolve, the solution should be clear and colorless; If it is turbid, with No. 2 Turbidity standard solution (General rule 0902 first method) comparison, shall not be more concentrated; If color, with yellow or yellow-green No. 5 standard colorimetric liquid (General Principles 0901 first method), shall not be deeper. (For injection)
Related substances
take an appropriate amount of this product, add the mobile phase to dissolve and dilute to make a solution containing about 0.2mg per 1 ml as a test solution; Take an appropriate amount for precision measurement, A solution containing about 0.4ug per 1 ml was prepared as a control solution by quantitative dilution with mobile phase. The appropriate amount of the control solution was accurately taken, and diluted with the mobile phase to prepare a solution containing about 0.08 mesh per 1 ml as a sensitivity solution. According to the chromatographic conditions under the content determination, the sensitivity solution 20u1 is injected into the human liquid chromatograph, and the signal-to-noise ratio of the peak height of the main component chromatogram should be greater than 10. 20 u1 of the test solution and the control solution were respectively injected into the liquid chromatograph, and the chromatogram was recorded to 2 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 (0.2%), the sum of each impurity peak area shall not be greater than 5 times (1.0%) of the main peak area of the control solution, and the peaks in the chromatogram of the test solution which are smaller than the main peak area of the sensitive solution are ignored.
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, put it in platinum crucible, and check it according to law (General rule 0841). The remaining residue shall not exceed 0.2% (for oral use) or 0.1% (for injection).
Heavy metals
The residue left under the item of taking the ignition residue shall not contain more than 20 parts per million of heavy metals (for oral use) and shall be inspected by law (General Principles 0821 second law). Or 10 parts per million (for injection).
bacterial endotoxin
take this product, check according to law (General rule 1143), the amount of endotoxin in fleroxacin per 1 mg should be less than 0.125EU. (For injection)
Last Update：2022-01-01 13:40:43
6,8-Difluoro-1-(2-Fluoroethyl)-1,4-Dihydro-7-(4-Methyl-1-Piperazinyl)-4-Oxo-3-Quinolinecarboxylic Acid - 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 as filler (4.6mm X 25O mm,5um or equivalent chromatography column); Triethylamine phosphoric acid solution (take 5ml of triethylamine and 7ml of phosphoric acid, add water to 1000ml)-Acetonitrile (87:13) as mobile phase; Detection wavelength was 286NM, column temperature was 30°C. Take about 10mg of fleroxacin reference substance, add 1 ml of sodium hydroxide solution to dissolve, put 60 ° C. Water bath to heat for 60 minutes, let it cool, and dilute with mobile phase to make a solution containing about 0.4mg fleroxacin per 1 ml; take an appropriate amount of pefloxacin reference, add mobile phase to dissolve and dilute to make a solution containing about 2.5ug per lml, mix the above two solutions in equal volume, and use 20u1 to inject human liquid chromatograph as the applicable solution for the system, record chromatogram, impurity I Peak (relative retention time is about 0.96) and fleroxacin peak between the separation degree should be greater than 1.0, impurity II peak (alkali degradation peak, relative retention time is about 0.92) the degree of separation from impurity I Peak, fleroxacin peak and pefloxacin peak should meet the requirements.
assay
take the appropriate amount of this product, precision weighing, plus mobile phase dissolution and quantitative dilution made from each lml containing about O.O8mg solution, as a test solution, the precise amount of 20u1 was injected into the liquid chromatograph, and the chromatogram was recorded, the mobile phase is added to dissolve and dilute to prepare a solution containing about 0.08mg per 1 ml, which is determined by the same method and calculated by peak area according to external standard method.
Last Update：2022-01-01 13:40:43
6,8-Difluoro-1-(2-Fluoroethyl)-1,4-Dihydro-7-(4-Methyl-1-Piperazinyl)-4-Oxo-3-Quinolinecarboxylic Acid - Category
Authoritative Data Verified Data
quinolones.
Last Update：2022-01-01 13:40:44
6,8-Difluoro-1-(2-Fluoroethyl)-1,4-Dihydro-7-(4-Methyl-1-Piperazinyl)-4-Oxo-3-Quinolinecarboxylic Acid - Storage
Authoritative Data Verified Data
light-shielded, sealed, and stored in a dry place.
Last Update：2022-01-01 13:40:44
6,8-Difluoro-1-(2-Fluoroethyl)-1,4-Dihydro-7-(4-Methyl-1-Piperazinyl)-4-Oxo-3-Quinolinecarboxylic Acid - Fleroxacin tablets
Authoritative Data Verified Data
This product contains fleroxacin (C17H18F3N303) should be labeled the amount of 90.0% to 110.0%.
trait
This product is a white to yellowish tablet or film-coated tablet, white to yellowish after removing the coating.
identification
- take an appropriate amount of the fine powder of this product, add dichloromethane-methanol (4:1) to dissolve fleroxacin and dilute it to prepare a solution containing 1 mg per 1 ml, shake, filter, the filtrate was used as a test solution, and the same results were obtained according to the identification (1) Test under the item of fleroxacin.
- 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.
- take an appropriate amount of fine powder of this product and add O.lmol/L hydrochloric acid solution to dissolve and dilute fleroxacin into a solution containing 6ug fleroxacin per lml, filtered, and then the filtrate was measured by UV-Vis spectrophotometry (General 0401), there is maximum absorption at wavelengths of 286NM and 320nm.
examination
- dissolution dissolution of this product, according to the dissolution and release determination method (General rule 0931 The first method), hydrochloric acid solution (9-1000)900ml as the dissolution medium, the rotation speed is 75 rpm, operate in accordance with the law, after 30 minutes, take 10ml of solution, filter, take the appropriate amount of filtrate, dilute quantitatively with hydrochloric acid solution (9-1000) to make a solution containing about 4ug of fleroxacin per lml, measure absorbance at 286nm wavelength according to UV-visible spectrophotometry (General rule 0401); Take appropriate amount of fleroxacin reference, add hydrochloric acid solution (9-1000) the solution containing 4ug per 1 ml was prepared by dissolution and quantitative dilution, and the dissolution amount of each tablet was calculated by the same method. 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
Take 10 tablets of fleroxacin, grind them, weigh them accurately, put them in a 0.16 measuring flask, add mobile phase to dissolve fleroxacin and dilute them to the scale, shake well, filter, Take 5ml of the filtrate accurately, put it in a 100ml measuring flask, dilute it with mobile phase to the scale, shake well, use it as a test solution, and measure it according to the method under fleroxacin, that's right.
category
Same as fleroxacin.
specification
O.lg
storage
light-shielded, sealed, and stored in a dry place.
Last Update：2022-01-01 13:40:45
6,8-Difluoro-1-(2-Fluoroethyl)-1,4-Dihydro-7-(4-Methyl-1-Piperazinyl)-4-Oxo-3-Quinolinecarboxylic Acid - Fleroxacin capsules
Authoritative Data Verified Data
This product contains fleroxacin (C17H18F3N303) should be labeled the amount of 90.0% to 110.0%.
trait
The contents of this product are white to yellowish particles or powder.
identification
- take an appropriate amount of the contents of this product, add methylene chloride-methanol (4:1) to dissolve fleroxacin and dilute it to prepare a solution containing 1 mg per 1 ml, shake, filter, the filtrate was used as a test solution, and the same results were obtained according to the identification (1) Test under the item of fleroxacin.
- 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.
- take an appropriate amount of the contents of this product and add 0.lmol/L hydrochloric acid solution to dissolve and dilute fleroxacin into a solution containing 6ug fleroxacin per lml, filtered, and then the filtrate was measured by UV-Vis spectrophotometry (General 0401), there is maximum absorption at wavelengths of 286NM and 320nm.
examination
- dissolution dissolution of this product, according to the dissolution and release determination method (General rule 0931 The first method), hydrochloric acid solution (9-1000)900ml as the dissolution medium, the rotation speed is 75 rpm, operate in accordance with the law, after 30 minutes, take 10ml of solution, filter, take the appropriate amount of filtrate, dilute quantitatively with hydrochloric acid solution (9-1000) to make a solution containing about 4ug of fleroxacin per lml, measure absorbance at 286nm wavelength according to UV-visible spectrophotometry (General rule 0401); Take appropriate amount of fleroxacin reference, add hydrochloric acid solution (9-1000) the solution containing 4% per 1 ml was prepared by dissolution and quantitative dilution, and the dissolution amount of each particle was calculated by the same method. The limit is 80% of the labeled amount and shall be in accordance with the provisions.
- others should comply with the relevant provisions under the capsule (General 0103).
Content determination
take the contents under the difference of loading amount, mix evenly, weigh an appropriate amount (about 0.16g equivalent to fleroxacin) accurately, and put it in a 100ml measuring flask, add mobile phase to dissolve fleroxacin and dilute to the scale, shake well, filter, Take 5ml of continuous filtrate accurately, put it in a 100ml measuring flask, dilute to the scale with mobile phase, shake well, as a test solution, fleroxacin was measured according to the method described above.
category
Same as fleroxacin.
specification
O.lg
storage
light-shielded, sealed, and stored in a dry place.
Last Update：2022-01-01 13:40:46
Supplier List
Multiple SpecificationsSpot supply
Product Name: Fleroxacin Visit Supplier Webpage Request for quotationCAS: 79660-72-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Multiple SpecificationsSpot supply
Product Name: Fleroxacin Visit Supplier Webpage Request for quotationCAS: 79660-72-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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