Flucloxacillin sodium
(Synonyms: 氟氯西林钠) 目录号 : GC33709
A β-lactam antibiotic
Cas No.:1847-24-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Animal experiment: |
Rats: On the day of the experiment the animal is given an intravenous bolus injection of 200 mg/kg as pure free acid sodium flucloxacillin (dose volume: 1 mL sterile water per kg) and then return to the metabolism cage. Urine is collected directly into individual CO2 cooled containers for a period of 24 h before dosing and then at frequent intervals after dosing[3]. |
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References: [1]. Paton DM, et al. Bioavailability and half-life of two preparations of flucloxacillin. N Z Med J. 1982 Nov 10;95(719):766-8. |
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Flucloxacillin is a β-lactam antibiotic.1 It is active against clinical isolates of S. aureus (MICs = 0.12-0.25 mg/L). Flucloxacillin (42.3 mg/kg every six hours) decreases vegetation titers in a rat model of aortic valve endocarditis induced by S. aureus. Formulations containing flucloxacillin have been used in the treatment of bacterial infections.
1.Entenza, J.M., Vouillamoz, J., Glauser, M.P., et al.Levofloxacin versus ciprofloxacin, flucloxacillin, or vancomycin for treatment of experimental endocarditis due to methicillin-susceptible or -resistant Staphylococcus aureusAntimicrob. Agents Chemother.41(8)1662-1667(1997)
| Cas No. | 1847-24-1 | SDF | |
| 别名 | 氟氯西林钠 | ||
| Canonical SMILES | [O-]C([C@@H]1N(C2=O)[C@]([C@@H]2NC(C(C(C(C(F)=CC=C3)=C3Cl)=NO4)=C4C)=O)([H])SC1(C)C)=O.[Na+] | ||
| 分子式 | C19H16ClFN3NaO5S | 分子量 | 475.85 |
| 溶解度 | Water : ≥ 100 mg/mL (210.15 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1015 mL | 10.5075 mL | 21.015 mL |
| 5 mM | 0.4203 mL | 2.1015 mL | 4.203 mL |
| 10 mM | 0.2102 mL | 1.0508 mL | 2.1015 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Polymorphism of Flucloxacillin sodium
Pharmazie 2011 Dec;66(12):933-5.PMID:22312697doi
The polymorphism of Flucloxacillin sodium has not been discussed sufficiently so far. Flucloxacillin sodium which was crystallized with different solvents, was found to exist in amorphism and three crystal forms (I, II, III). This results were confirmed by infra-red (IR) spectra, thermogravimetry (TG), X-ray diffraction analysis (XRD) and equilibrium solubility. It is noticed that form III has very good solubility in phosphate buffer solution, with an average solubility of 0.86 g (20-40 degrees C). However, more efforts are needed to carry out and decide whether this form can be used for industrial production.
Intravenous antimicrobial administration through peripheral venous catheters - establishing risk profiles from an analysis of 5252 devices
Int J Antimicrob Agents 2022 Apr;59(4):106552.PMID:35183678DOI:10.1016/j.ijantimicag.2022.106552.
Introduction: Peripheral venous catheters (PVCs) are used to administer antimicrobials, but many fail prior to completion of therapy. While some antimicrobials are known to increase the PVC failure rate, risk profiles for many are unclear. Objective: To synthesize data from prospective PVC studies conducted between 2013 and 2019 to determine associations between common antimicrobials and PVC failure. Methods: A secondary analysis was undertaken of seven randomized controlled trials and two prospective cohort studies from three quaternary hospitals (two adult and one paediatric) in Australia between 2013 and 2019. The primary outcome was PVC failure due to vessel injury (occlusion, infiltration or extravasation) or irritation (pain or phlebitis). Associations between antimicrobial use and PVC failure were explored using multi-variable Cox regression. Results: In total, 5252 PVCs (4478 patients) were analysed; vessel injury and irritations occurred in 19% and 11% of all PVCs, respectively. Vessel injury was significantly associated with cefepime hydrochloride [hazard ratio (HR) 2.50; 95% confidence interval (CI) 1.44-4.34], ceftazidime pentahydrate (HR 1.91, 95% CI 1.11-3.31), Flucloxacillin sodium (HR 1.84, 95% CI 1.45-2.33), lincomycin hydrochloride (HR 1.67, 95% CI 1.10-2.52) and vancomycin hydrochloride (HR 1.73, 95% CI 1.25-2.40). Irritation was significantly associated with Flucloxacillin sodium (HR 2.58, 95% CI 1.96-3.40). Conclusions: This study identified several antimicrobials associated with increased PVC failure, including some that were already known to be associated and some that had not been identified previously. Research is needed urgently to determine superior modes of delivery (e.g. dilution, infusion time, device type) that may prevent PVC failure.
Pharmacokinetics and bioavailability of flucloxacillin in elderly hospitalized patients
J Clin Pharmacol 1995 Jan;35(1):31-6.PMID:7751411DOI:10.1002/j.1552-4604.1995.tb04742.x.
The pharmacokinetics and oral bioavailability of flucloxacillin were studied in five female and two male patients (age 68-87 yr) who had been hospitalized for orthopedic surgeries. A single dose of intravenous or oral Flucloxacillin sodium (500 mg) was administered in random order on different occasions separated by at least 2 days. Blood and urine samples were taken up to 24 hours after drug administration and levels of flucloxacillin and 5-hydroxymethylflucloxacillin (5-HMF), a major metabolite, were measured by high-performance liquid chromatography. Flucloxacillin elimination, but not oral absorption, was reduced in the elderly, compared with data from young healthy subjects reported elsewhere. Total clearance, renal clearance, and volume of distribution were 0.083 +/- 0.013 L/kg/hr, 0.038 +/- 0.01 L/kg/hr, and 0.184 +/- 0.034 L/kg, respectively. Regression of flucloxacillin renal clearance (Clr) on estimated creatine clearance (CLcr) gave the relationship: Clr = 0.755 (CLcr) + 10.6 (r = 0.91; P = 0.004). Terminal half-lives for flucloxacillin and 5-HMF were 2.21 +/- 0.51 hr and 3.0 +/- 0.75 hr, respectively after intravenous administration. Flucloxacillin was absorbed rapidly after oral administration with a mean absorption time of 0.95 +/- 0.34 hr, and time to reach peak concentration of 1.20 +/- 0.29 hr. The absolute bioavailability of flucloxacillin from capsules was 54.4 +/- 18.8%.
Assessment of the stability of citrate-buffered flucloxacillin for injection when stored in two commercially available ambulatory elastomeric devices: INfusor LV (Baxter) and Accufuser (Woo Young Medical): a study compliant with the NHS Yellow Cover Document (YCD) requirements
Eur J Hosp Pharm 2020 Mar;27(2):90-94.PMID:32153771DOI:10.1136/ejhpharm-2018-001515.
Objectives: To investigate the effect of pH and buffers on the degradation rate of flucloxacillin and to determine if flucloxacillin can be stabilised using a buffered diluent for up to 14 days when stored at 2°C-8°C including a 24-hour infusion period at 32°C in two elastomeric devices (Accufuser and INfusor LV) filled to 240 mL. Testing as per the NHS Pharmaceutical Quality Assurance Committee Yellow Cover Document (YCD) requirements. Methods: A validated stability indicating high-performance liquid chromatography method was used for assessing the stability of flucloxacillin diluted in 0.3% w/v citrate-buffered saline pH 7.0 when stored at 2°C-8°C in two ambulatory devices (Accufuser and INfusor LV). Flucloxacillin at 10 and 50 mg/mL diluted in 0.3% w/v citrate-buffered saline pH 7.0 to a final volume of 240 mL and stored at 2°C-8°C, including 24 hours at 32°C, was tested from two batches in replicate (n=3) at five time points for up to 14 days according to the requirements of the YCD. Results: Greater than 95% of the zero-time concentration of flucloxacillin at 10 and 50 mg/mL remained when stored at 2°C-8°C after 14 days including 24 hours at 32°C in both Accufuser and INfusor LV devices. Conclusions: Flucloxacillin sodium stability was improved, and complied with UK national standards, by using a diluent of 0.3% w/v citrate-buffered saline pH 7 in both Accufuser and INfusor LV ambulatory devices when filled to 240 mL. The data support assigning a shelf-life of up to 14 days (13 days stored at 2°C-8°C and 24 hours at 32°C). Flucloxacillin may now be used appropriately as a continuous 24-hour infusion in outpatient parenteral antimicrobial therapy services, providing further opportunity to avoid or shorten patient hospital stays, as well as support ideal antimicrobial stewardship principles.
Bioavailability and half-life of two preparations of flucloxacillin
N Z Med J 1982 Nov 10;95(719):766-8.PMID:6959033doi
The comparative bioavailability of two formulations of 250 mg Flucloxacillin sodium capsules in eight fasted healthy volunteers was examined. There were no significant differences in the peak serum concentrations, time to peak concentration or area under the curves with the two formulations indicating that the two batches studied did not differ in bioavailability. The serum elimination half-life of flucloxacillin was 1.31-1.39 hours, and six hours after administration of a single 250 mg dose the serum concentration of flucloxacillin was 0.46 micrograms/ml.