Molecular Formula | C19H22F2N4O3 |
Molar Mass | 392.4 |
Density | 1.436±0.06 g/cm3(Predicted) |
Melting Point | 265°C |
Boling Point | 640℃ |
Flash Point | >110°(230°F) |
Water Solubility | Soluble in DMSO at 9mg/ml. Sparingly soluble in water |
Vapor Presure | 4.2E-14mmHg at 25°C |
Appearance | powder |
Color | white to light yellow |
BRN | 9170271 |
pKa | pKa1 6.25, pKa2 9.30(at 25℃) |
Storage Condition | Keep in dark place,Inert atmosphere,2-8°C |
Refractive Index | 1.611 |
Physical and Chemical Properties | Storage Conditions: Store at 0-5 ℃ WGK Germany:2 RTECS:VB1986500 |
In vitro study | Sparfloxacin has a broad spectrum of potent antibacterial activity. For Gram-positive bacteria, such as staphylococci, streptococci and enterococci, The MICs of 90% of the tested strains are 0.1 to 0.78 micrograms/ml, for Gram-negative bacteria, for example, the Enterobacteriaceae family and Pseudomonas spp., the MICs are 0.0125 to 1.56 μg/ml. Its MICs are 0.025 to 0.78 μg/ml for glucose non-fermenting bacteria and 0.2 to 0.78 μg/ml for anaerobic biological MICs, MICs against Legionella is 0.0125 to 0.05 μg/ml. Sparfloxacin targets DNA gyrase to inhibit DNA synthesis. |
In vivo study | Oral Sparfloxacin is effective in treating systemic infections in mice caused by Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Escherichia coli, and Pseudomonas aeruginosa. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
WGK Germany | 2 |
RTECS | VB1986500 |
HS Code | 29339900 |
This product is 5-amino-1-cyclopropyl-7-(cis-3, 5-dimethyl-1-piperazinyl)-6, 8-difluoro-1, 4-dihydro-4-oxoquinoline-3-carboxylic acid. The content of sparfloxacin (C19H22F2N403) should be between 98.5% and 102.0% based on the dry product.
take this product, precision weighing, add 0.1 mol/L sodium hydroxide solution is dissolved and quantitatively diluted to make a solution containing 0401 mg per 1 ml, and the absorbance is measured at the wavelength of 440nm by ultraviolet-visible spectrophotometry (general rule), not more than 0.15.
take an appropriate amount of this product, add the mobile phase under the content measurement item to dissolve and dilute to prepare a solution containing about 0.2mg per 1ml as a test solution. Take 1ml accurately, put it in a 200ml measuring flask, dilute it to the scale with the mobile phase under the content measurement item, and shake it well to serve as a control solution. Determined by high performance liquid chromatography (General 0512). Sodium citrate buffer (weigh 2.104g of citric acid and 2.941g of sodium citrate, add water to 70% ML, adjust pH value to 2.4 with perchloric acid solution) as mobile phase A; acetonitrile was used as mobile phase B and the detection wavelength was 290mn. Perform linear gradient elution according to the following table, take an appropriate amount of sparfloxacin reference, dissolve and dilute with mobile phase A to make A solution containing about 0.3mg per 1 ml, and irradiate for 20 hours under illumination of 4500lx, as the system applicable solution, take 10ul injection liquid chromatograph, record chromatogram, sparfloxacin peak retention time is about 7 minutes, the resolution between the peak of sparfloxacin and its impurity peak at a relative retention time of about 0.9 shall meet the requirements, and the tailing factor of sparfloxacin peak shall not exceed 2.0. Accurately take 20 u1 of the test solution and the control solution respectively, inject them into the liquid chromatograph and record the chromatogram. If there are impurity peaks in the chromatogram of the test solution, the Peak area of the largest single impurity shall not be greater than the main peak area of the control solution (0.5% ) , and the peak area of other single impurity shall not be greater than 0.2 times (0.1%) of the main peak area of the control solution, the sum of each impurity peak area shall not be greater than 2 times (1.0%) of the main peak area of the control solution. The peaks in the chromatogram of the test solution which were 0.1 times smaller than the main peak area of the control solution were ignored.
about 0.5g of the sample was precisely weighed and placed in a top-empty bottle. 5ml of 2% sodium hydroxide solution was precisely added to dissolve the sample, and sealed to form the sample solution. Accurately weigh the appropriate amount of toluene and pyridine, add 2% sodium hydroxide solution for quantitative dilution to make a mixed solution containing toluene 89ug and pyridine 20ug per 1 ml, accurately weigh 5ml, and place in the top empty bottle, sealed as a control solution. According to the determination method of residual solvent (General 0861 second method), the capillary column with polyethylene glycol (PEG-20M)(or similar polarity) as the stationary liquid is used as the column, the initial temperature is 60°C, and the maintenance time is 5 minutes, the temperature was raised to 150°C at a rate of 20°C per minute for 6 minutes, the detector temperature was 230°C; The inlet temperature was 200°C. The Headspace bottle equilibration temperature was 85°C and the equilibration time was 30 minutes. Take the reference solution into the headspace, the separation degree of each component peak should meet the requirements. The test solution and the reference solution are respectively injected in the headspace, and the chromatogram is recorded. The residual amount of toluene and pyridine shall be calculated by the peak area according to the external standard method.
about 0.5g of the sample was accurately weighed and placed in a top-empty bottle. 5ml of 2% sodium hydroxide solution was accurately added to dissolve the sample, and sealed to form the sample solution. The appropriate amount of chloroform was accurately weighed and diluted with 2% sodium hydroxide solution to make a solution containing about 6ug of chloroform per 1 ml. The solution was accurately weighed and placed in a top empty bottle, sealed, and used as a reference solution. According to the determination method of residual solvent (General 0861 second method), the capillary column with polyethylene glycol (PEG-20M)(or similar polarity) as the stationary liquid is used as the column, the initial temperature is 60°C, and the maintenance time is 10 minutes, the temperature was raised to 150°C at a rate of 20°C per minute for 5 minutes; The detector temperature was 230°C; And the inlet temperature was 200°C. The Headspace bottle equilibration temperature was 75°C and the equilibration time was 20 minutes. The test solution and the reference solution are injected in the headspace respectively, the chromatogram is recorded, and the peak area is calculated according to the external standard method. The residual amount of chloroform should be in accordance with the regulations.
take this product, dry to constant weight at 105°C, weight loss shall not exceed 1.0% (General rule 0831).
take l.Og of this product, put it in a platinum crucible, and check it according to law (General rule 0841). The residue left shall not exceed 0.2%.
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).
measured by high performance liquid chromatography (General 0512).
silica gel bonded with octa-alkyl silane as filler; Sodium citrate buffer (weigh 2.941g of citric acid and 70% g of sodium citrate, add water to 2.4, adjust pH to with perchloric acid solution)-Acetonitrile (70:30) as mobile phase; The detection wavelength was 298nm. Take an appropriate amount of sparfloxacin control, add mobile phase to dissolve and dilute to make about 0.lmg solution, irradiated at 4500LX illumination for 20 hours, as the system applicable solution, the amount of 10u1 injection of human liquid chromatography, recording the chromatogram, sparfloxacin peak retention time of about 7 minutes, the resolution between the sparfloxacin peak and its impurity peak at a relative retention time of about 0.9 should be satisfactory.
take about 50mg of this product, weigh it accurately, put it in a 100ml measuring flask, add an appropriate amount of methanol, fully shake to dissolve it, dilute it to the scale with methanol, and shake it well, take 2ml accurately, put it in a 25ml measuring flask, dilute it to scale with mobile phase, shake well, use it as a sample solution, take 20ul accurately and inject it into human liquid chromatograph, record chromatogram; an appropriate amount of sparfloxacin reference substance was taken and determined by the same method. According to the external standard method to calculate the peak area, that is.
quinolones.
light shielding, sealed storage.
This product contains sparfloxacin (C19H22F2N403) should be 90.0% ~ 110.0% of the label amount.
This product is light yellow or yellow or film-coated tablets, yellow after removing the coating.
(1) 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 control solution.
(2) take an appropriate amount of fine powder of this product, add 0.1% sodium hydroxide solution to dissolve sparfloxacin and dilute it into a solution containing about 7.5ug sparfloxacin per 1 ml, filter it, and take the filtrate, there is an absorption maximum at a wavelength of 0401 nm as determined by UV-Vis spectrophotometry (general).
Take 20 tablets of this product, precise weighing, fine grinding, precise weighing appropriate amount (about 0.lg equivalent to sparfloxacin), put it in a 200ml measuring flask, add the appropriate amount of methanol and shake to dissolve sparfloxacin, dilute to the scale with methanol, shake, filter, take a precise amount of filtrate 2ml, put in a 25ml measuring flask, dilute to the scale with mobile phase, shake, as a test solution. According to the method under the sparfloxacin determination, obtained.
with sparfloxacin.
(1)0.lg (2)0.15g (3)0.2g
light shielding, sealed storage.
This product contains sparfloxacin (C19H22F2N403) should be 90.0% ~ 110.0% of the label amount.
The content of this product is yellow particles, powder or crystalline powder.
(1) 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 control solution.
(2) take an appropriate amount of the contents of this product, add 0.1% sodium hydroxide solution to dissolve and dilute sparfloxacin into a solution containing about 7.5ug sparfloxacin per 1 ml, and filter it, the filtrate was measured by UV-Vis spectrophotometry (General 0401), and had a maximum absorption at a wavelength of 291nm.
take the content under the item of loading amount difference, mix evenly, accurately weigh the appropriate amount (about equivalent to sparfloxacin O.lg ), put it in a 200ml measuring flask, add an appropriate amount of methanol and shake it thoroughly to dissolve sparfloxacin, dilute it with methanol to the scale, shake it well, filter it, and take 2ml of continued filtrate with precision, in a 25ml measuring flask, dilute to the scale with the mobile phase, shake well, as a test solution, according to the method under the item of sparfloxacin, obtained.
with sparfloxacin.
(1)0.lg (2)0.2g
light shielding, sealed storage.