2-oxo-1-imidazolidinyl)carbonyl)amino)phenylacetyl)amino)-,monosodiumsalt,(
azlocillin sodium
CAS: 37091-65-9
Molecular Formula: C20H22N5NaO6S
2-oxo-1-imidazolidinyl)carbonyl)amino)phenylacetyl)amino)-,monosodiumsalt,( - Names and Identifiers
2-oxo-1-imidazolidinyl)carbonyl)amino)phenylacetyl)amino)-,monosodiumsalt,( - Physico-chemical Properties
| Molecular Formula | C20H22N5NaO6S |
| Molar Mass | 483.47 |
| Melting Point | >199oC (dec.) |
| Flash Point | >110°(230°F) |
| Water Solubility | Freely soluble in water |
| Solubility | DMSO 97 mg/mL;Water 97 mg/mL;Ethanol 3 mg/mL |
| Appearance | White solid |
| Color | White to Off-White |
| Storage Condition | Inert atmosphere,2-8°C |
| Stability | Hygroscopic |
| MDL | MFCD07793330 |
| Use | It is a semi-synthetic broad-spectrum antimycin, and has antibacterial activity against Pseudomonas aeruginosa, anaerobic bacteria, Escherichia coli, etc. |
| In vitro study | More than 75% of Pseudomonas aeruginosa strains were inhibited by Azlocillin (12.5 μg/mL). Azlocillin (12.5 μg/mL) showed antibacterial activity against indole-negative and positive Proteobacteria with inhibition rates of 98% and 71%, respectively. Azlocillin is more active than mezlocillin,ticarcillin, and arbenicillin in Pseudomonas aeruginosa strains and has the same activity as BLP-1654. The acyl side chain of Azlocillin has a ureido-(urea) structure, hence the name "penicillin" or, more precisely, "acylurea penicillin". In vitro studies on Pseudomonas aeruginosa showed that the activity of piperacillin was 2 times that of azlocillin, 4 times that of mezlocillin and ticarcillin, and 8 times that of carbicillin. In morphological studies, Azlocillin produces elongated Bacterial morphologies that delay, and even do not lyse, the cells. The MICs of Azlocillin against Pseudomonas aeruginosa was 12.5 μg/mL. Azlocillin (3.125 μg/mL) caused a decrease in the growth rate of P. Aeruginosa, but no bactericidal phase. Gradually increase the concentration of Azlocillin drug, reduce the initial log phase. Low concentrations of tobramycin (0.5 μg/ml) combined with high or low concentrations of Azlocillin were more effective against P. Aeruginosa than a single component. Under the inhibition of AmpC enzyme, the strain was Diluted 1-2 times, which was more resistant to azlocillin and increased its efflux or impermeability. These second-generation β-lactamases were susceptible to ceftazidime at 4 mg/L and most resistant to Azlocillin (MIC ≥ 128 mg/L in 10/14 cases). |
| In vivo study | In the empirical treatment of febrile neutropenic patients, Azlocillin/netilmicin treatment had an infection suppression rate of 42% (28/67) with 15% adverse events. |
2-oxo-1-imidazolidinyl)carbonyl)amino)phenylacetyl)amino)-,monosodiumsalt,( - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 42/43 - May cause sensitization by inhalation and skin contact. |
| Safety Description | 36 - Wear suitable protective clothing. |
| WGK Germany | 3 |
| RTECS | XH9250000 |
2-oxo-1-imidazolidinyl)carbonyl)amino)phenylacetyl)amino)-,monosodiumsalt,( - Standard
Authoritative Data Verified Data
This product is (2S, 5R,6R)-3, 3-dimethyl-6-[(R)-2-(2-oxo-1-imidazolidinylformylamino) 2-phenylacetamido]-7-oxo-4-thia-1-azabicyclo [3.2.0] heptane-2-carboxylate sodium salt. The content of C20H23N5O6S shall not be less than 90.0% calculated as anhydrous.
Last Update：2024-01-02 23:10:35
2-oxo-1-imidazolidinyl)carbonyl)amino)phenylacetyl)amino)-,monosodiumsalt,( - Trait
Authoritative Data Verified Data
- This product is white or off-white powder or loose mass; Odorless; With hygroscopicity.
- This product is soluble in water, slightly soluble in ethanol, insoluble in ethyl acetate or acetone.
specific rotation
take this product, precision weighing, add water to dissolve and quantitatively dilute to a solution containing about 10mg in μl ML, and determine according to law (General rule 0621). The specific rotation is 170 ° to 200 °.
Last Update：2022-01-01 12:00:40
2-oxo-1-imidazolidinyl)carbonyl)amino)phenylacetyl)amino)-,monosodiumsalt,( - Introduction
Azlocillin is a semi-synthetic penicillin and a potent 1-lactam antibiotic. It is usually used to resist Pseudomonas aeruginosa and develop new antibiotics. Azlocillin inhibits the synthesis of penicillin-binding protein (PBP)-dependent bacterial cell walls.
Last Update：2022-10-16 17:24:56
2-oxo-1-imidazolidinyl)carbonyl)amino)phenylacetyl)amino)-,monosodiumsalt,( - Differential diagnosis
Authoritative Data Verified Data
- 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 773).
- This product shows the reaction of sodium salt identification (1) (General rule 0301).
Last Update：2022-01-01 12:00:40
2-oxo-1-imidazolidinyl)carbonyl)amino)phenylacetyl)amino)-,monosodiumsalt,( - Exam
Authoritative Data Verified Data
pH
take this product, add water to make a solution containing O.lg per lml, and determine it according to law (General 0631). The pH value should be 6.0~8.0.
clarity and color of solution
take 5 parts of this product, each 0.56g, respectively, and add 5ml of water to dissolve immediately after observation, the solution should be clear and colorless; If it is turbid, with No. 1 turbidity standard solution (General rule 0902 first method) comparison, shall not be more concentrated; If the color, and yellow or yellow-green No. 3 Standard Colorimetric liquid (General Principles 0901 first method), shall not be deeper.
Related substances
take an appropriate amount of this product, add the mobile phase to dissolve and dilute to make a solution containing about 0.5mg of Azlocillin per 1 ml, as a test solution; Take an appropriate amount of precision, A solution containing about 10ug of Azlocillin per 1 ml was prepared as a control solution by quantitative dilution with mobile phase. According to the chromatographic conditions under the content determination item, 20 u1 of each of the test solution and the control solution are accurately measured and injected into the human liquid chromatograph respectively, and the chromatogram is 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 0.75 times (1.5%) of the area of the main peak of the control solution, the sum of each impurity peak area shall not be greater than 1.5 times (3.0%) of the main peak area of the control solution.
Azlocillin polymer
measured by size exclusion chromatography (General 0514).
chromatographic conditions and system suitability test
with dextran gel G-10(40 ~ 120um) as the filler, the inner diameter of the glass column is 1.0~1.4, the length of the column is 30 ~ 40cm, mobile phase A was 7.0 mol/L phosphate buffer (pH 0.05) [0.05mol/L disodium hydrogen phosphate solution -0.05mol/L sodium dihydrogen phosphate solution (61:39)]; Mobile phase B was water, the flow rate was 1.5ml per minute, the detection wavelength was 254nm, 0.2~2000 u1 of 100 mg/ml Blue dextran 200 solution was measured, and human liquid chromatography was injected, and the determination was carried out with mobile phases A and B respectively, the chromatogram was recorded. The number of theoretical plates is not less than 2000 calculated by the Blue dextran 400 peak, and the tailing factor should be less than 2.0. The ratio of the retention times of the Blue dextran 2000 peak in the two mobile phase systems should be between 0.93 and 1.07, the ratio of the retention time of the main peak of the control solution to the polymer peak in the test solution and the Blue dextran 2000 peak in the corresponding chromatographic system should be between 0.93 and 1.07, weighing about 0.4g of Azlocillin sodium, in a 10ml child bottle, dissolve and dilute to the mark with 0.04mg/ml of a 2000 solution of Blue dextran, and shake. Take 100~200u1 and inject it into human liquid chromatograph, measure with mobile phase A, and record chromatogram. The ratio of the peak height of the polymer to the valley height between the monomer and the polymer should be greater than 2.0. In addition, the mobile phase B is used as the mobile phase, and the relative standard deviation of the peak area should not be more than 100 when the control solution is 200-5.0% u1 for 5 consecutive injections.
preparation of control solution
take an appropriate amount of Azlocillin reference substance, weigh it precisely, add an appropriate amount of 0.5% sodium bicarbonate solution (about 1 ml of 0.5% sodium bicarbonate solution per 6.25mg) to dissolve it, A solution containing about 50ug per 1 ml was prepared by quantitative dilution with water.
assay
take about 0.3g of this product, weigh it accurately, put it in a 10ml measuring flask, add water to dissolve and dilute it to the scale, shake it well. Immediately, 100~200u1 was accurately weighed and injected into human liquid chromatograph, and the mobile phase A was used as the mobile phase for measurement, and the chromatogram was recorded. In addition, 100 ~ 200ul of the control solution was injected into the human liquid chromatograph, the mobile phase B was used as the mobile phase, and the same method was used for determination, and the chromatogram was recorded. According to the external standard method with Azlocillin peak area calculation, the amount of Azlocillin polymer should not exceed 0.3%.
residual solvent
take about 0.5g of the sample, precision weigh it, place it in the top empty bottle, precision add the internal standard solution (take an appropriate amount of methyl ethyl ketone, dilute with water to make a solution containing about 250% per 1 ml) 5ml to dissolve, seal, as a test solution; Precision weighing methylene chloride, acetone, ethyl acetate, ethanol and isopropanol in appropriate amounts, prepare mixed solution containing dichloromethane 60ug, acetone, ethyl acetate, ethanol and isopropyl alcohol 0.5mg for each lml by quantitative dilution with internal standard solution, take 5ml for precise measurement, place in the top empty bottle, Seal, as a control solution. Determined according to the residual solvent assay (General 0861 second method). A capillary column with 100% dimethylpolysiloxane (or similar polarity) as a stationary liquid is used as a chromatographic column, the initial temperature is 30°C, and the temperature is maintained for 7 minutes, and then the temperature is raised to 180°C at a rate of 50°C per minute for 5 minutes. The inlet temperature was 200°C, the detector temperature was 250°C, the headspace bottle equilibrium temperature was 85°C, and the equilibrium time was 30 minutes. The reference solution is injected in the headspace, and the peaks are obtained in the order of ethanol, acetone, isopropanol, dichloromethane, butanone (internal standard) and ethyl acetate. The degree of separation between peaks of each component shall meet the requirements. The test solution and the reference solution were respectively injected in headspace, Record the chromatogram and calculate the ratio of peak area according to the internal standard method. The residual amount of ethanol, acetone, isopropanol, dichloromethane and ethyl acetate shall meet the requirements.
moisture
take this product, according to the determination of moisture (General 0832 first method 1), the water content shall not exceed 2.0%.
visible foreign body
take 5 parts of this product, each 3.0g, plus particle inspection water dissolution, inspection according to law (General 0904), should comply with the provisions. (For aseptic dispensing)
insoluble particles
Take 3 parts of this product, Add particle inspection water to dissolve and dilute to make a solution containing 30mg per lml, check according to law (General rule 0903), in each lg sample, particles containing 10um and more than 10um shall not exceed 6000 particles, and particles containing 25um and more than 25um shall not exceed 600 particles. (For aseptic dispensing)
bacterial endotoxin
take this product, check according to law (General rule 1143), each lmg of Azlocillin containing endotoxin should be less than 0.070EU. (For injection)
sterile
take this product, dissolve and dilute with appropriate solvent, after membrane filtration treatment, inspection according to law (General rule 1101), should comply with the provisions. (For aseptic dispensing)
Last Update：2022-01-01 13:31:31
2-oxo-1-imidazolidinyl)carbonyl)amino)phenylacetyl)amino)-,monosodiumsalt,( - 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; Phosphate buffer solution (anhydrous dipotassium hydrogen phosphate 4.09g and potassium dihydrogen phosphate 0.58g, dissolved in water and diluted to 1000ml)-acetonitrile (85:15) as the mobile phase; the detection wavelength was 2 l0mn. Weigh the appropriate amount of ampicillin and Azlocillin respectively, add the mobile phase to dissolve and dilute to make a mixed solution containing about 6Hg ampicillin and 0.25mg Azlocillin per 1 ml. Inject 20u1 into liquid chromatograph and record the chromatogram. The separation degree between ampicillin peak and Azlocillin peak should be greater than 10. The degree of separation between Azlocillin peak and adjacent impurity peak should meet the requirements.
assay
take an appropriate amount of this product, precision weighing, and add mobile phase to dissolve and quantitatively dilute to a solution containing 0.25mg of Azlocillin per lml as the test solution, and inject 20u1 into the liquid chromatograph with precision, record the chromatogram; Take an appropriate amount of Azlocillin reference substance, and determine by the same method. Calculate the content of C20H23N5O6S in the sample by the peak area according to the external standard method.
Last Update：2022-01-01 13:31:32
2-oxo-1-imidazolidinyl)carbonyl)amino)phenylacetyl)amino)-,monosodiumsalt,( - Category
Authoritative Data Verified Data
B-lactam antibiotics, penicillins.
Last Update：2022-01-01 13:31:32
2-oxo-1-imidazolidinyl)carbonyl)amino)phenylacetyl)amino)-,monosodiumsalt,( - Storage
Authoritative Data Verified Data
sealed and stored in a dry place.
Last Update：2022-01-01 13:31:32
2-oxo-1-imidazolidinyl)carbonyl)amino)phenylacetyl)amino)-,monosodiumsalt,( - Azlocillin Sodium for Injection
Authoritative Data Verified Data
This product is a sterile powder or sterile lyophilized product of Azlocillin sodium. The content of Azlocillin (C20H23N5O6S) shall not be less than 90.0% calculated as anhydrous; The content of Azlocillin (C20H23N5O6S) shall be 95.0% to 105.0% of the label amount calculated as average loading.
trait
This product is white or off-white powder or loose lumps.
identification
The same results were obtained according to the identification tests (1) and (3) under Azlocillin sodium.
examination
- the clarity and color of the solution are 5 bottles of this product, and the water is added according to the labeled amount to make each lml containing 0.lg solution, the solution should be clear and colorless; If it is turbid, it should not be more concentrated than the 1# turbidity standard solution (General 0902 first method); If it is colored, no deeper color shall be compared with the yellow or yellow-green standard colorimetric solution No. 3 (General rule 0901 method 1).
- insoluble particles take this product, add particles to the labeled amount, dissolve it in water and dilute it to prepare a solution containing 30mg per lml, and check it according to law (General rule 0903). The labeled amount is l. The conversion of Og below is: Per l. No more than 6000 particles with lOum and more than 10um and no more than 600 particles with 25um and more than 25um in the Og sample; The labeled amount is 1.Og or more (including 1.0g): each sample container containing 10um and 10um or more particles shall not exceed 6000, containing 25um and 25um or more particles shall not exceed 600.
- the pH, related substances, Azlocillin polymer, moisture, bacterial endotoxin and sterility should be checked according to the method under Azlocillin sodium.
- others should comply with the relevant provisions under injection (General 0102).
Content determination
The contents under the item of loading amount difference were obtained by measuring according to the method under the item of Azlocillin sodium.
category
with Azlocillin sodium.
specification
calculated as C20H23N506S (l)0.5g (2)1.0g(3)1.5g (4)2.0g (5) 3.og
storage
sealed and stored in a dry place.
Last Update：2022-01-01 13:31:33
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Spot supply
Product Name: Azlocillin sodium Visit Supplier Webpage Request for quotationCAS: 37091-65-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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