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Flomoxef sodium Sale

(Synonyms: 氟氧头孢钠) 目录号 : GC36054

Flomoxef sodium 是一种奥沙环类抗生素,对多种革兰氏阳性菌均具有良好的抗菌活性。

Flomoxef sodium Chemical Structure

Cas No.:92823-03-5

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产品描述

Flomoxef sodium is a oxacephem group antibiotic, with excellent activity against various Gram-positive bacteria[1][2].

[1]. Yazawa K, et al. In-vitro activity of flomoxef, a new oxacephem group antibiotic, against Nocardia in comparison with other cephalosporins. J Antimicrob Chemother. 1989 Dec;24(6):921-5. [2]. Simon C, et al. In vitro activity of flomoxef in comparison to other cephalosporins. Infection. 1988 Mar-Apr;16(2):131-4.

Chemical Properties

Cas No. 92823-03-5 SDF
别名 氟氧头孢钠
Canonical SMILES O=C(C(N12)=C(CSC3=NN=NN3CCO)CO[C@]2([H])[C@](OC)(NC(CSC(F)F)=O)C1=O)O[Na]
分子式 C15H17F2N6NaO7S2 分子量 518.45
溶解度 DMSO : ≥ 250 mg/mL (482.21 mM); H2O : 250 mg/mL (482.21 mM; Need ultrasonic) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 1.9288 mL 9.6441 mL 19.2883 mL
5 mM 0.3858 mL 1.9288 mL 3.8577 mL
10 mM 0.1929 mL 0.9644 mL 1.9288 mL
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Research Update

Intravitreal Flomoxef sodium in rabbits

Ophthalmic Res 1993;25(2):128-36.PMID:8321517DOI:10.1159/000267275.

We studied the intraocular concentration of Flomoxef sodium in nonvitrectomized and vitrectomized eyes of albino rabbits after intravenous administration of 100 mg/kg Flomoxef sodium. The concentration of Flomoxef sodium in the vitreous body was undetectable (< 0.1 micrograms/ml) in nonvitrectomized eyes. Retinal toxicity of Flomoxef sodium was investigated with ophthalmoscopy, electroretinography (ERG) and light microscopy after intravitreal injection of 200, 500, 1,000 and 2,000 micrograms Flomoxef sodium in albino and pigmented rabbits. No ERG changes were induced with 200 micrograms. Other higher doses caused transient ERG changes. After the 200-micrograms injection, the intravitreal concentration decreased exponentially, the half-life being 4.4 h. The antibacterial activity, broad coverage and low intravitreal toxicity of Flomoxef sodium suggest that this compound may be used to treat bacterial endophthalmitis.

Flomoxef sodium and levofloxacin concentrations in aqueous humor

Ocul Immunol Inflamm 2005 Apr-Jun;13(2-3):229-34.PMID:16019684DOI:10.1080/09273940590928607.

Aims: We intravenously administered Flomoxef sodium (FMOX) 120 minutes before cataract surgery, topically administered levofloxacin (LVFX) into the eyes four times at 30-minute intervals before surgery, and measured the aqueous humor concentrations of these agents to investigate their penetration into the aqueous humor and their efficacy in the prevention of postoperative endophthalmitis. Methods: Sixty-eight patients who underwent cataract surgery at the Department of Ophthalmology, Yokohama City University School of Medicine, or its affiliate, Kanazawa Hospital, Yokohama, were enrolled in this study. They received one or both of the following: 1.0 g FMOX via a 20-minute intravenous drip and LVFX ophthalmic solution applied four times at 30-minute intervals, both beginning two hours before the operation. Aqueous humor was aspirated from the anterior chamber and assayed for FMOX and LVFX concentrations using high-performance liquid chromatography (HPLC). Results: The mean intraoperative FMOX and LVFX concentrations in the patients' aqueous humor were 1.21 +/- 0.63 microg/ml and 0.69 +/- 0.47 microg/ml, respectively. These concentrations sufficiently exceeded the MIC90 values against Staphylococcus epidermidis, S. aureus, and Propionibacterium acnes. Conclusions: The FMOX and LVFX concentrations in the aqueous humor sampling were adequate to kill bacteria in vitro. These drugs may have efficacy in the prevention of postoperative endophthalmitis in patients undergoing cataract surgery.

Separation and characterization of unknown impurities and isomers in Flomoxef sodium by LC-IT-TOF MS and study of their negative-ion fragmentation regularities

J Pharm Biomed Anal 2017 Jun 5;140:81-90.PMID:28343077DOI:10.1016/j.jpba.2017.03.032.

Thirteen unknown impurities in Flomoxef sodium were separated and characterized by liquid chromatography coupled with high resolution ion trap/time-of-flight mass spectrometry (LC-IT-TOF MS)with positive and negative modes of electrospray ionization method for further improvement of official monographs in pharmacopoeias. The fragmentation patterns of impurities in flomoxef in the negative ion mode were studied in detail, and new negative-ion fragmentation regularities were discovered. Chromatographic separation was performed on a Kromasil C18 column (250mm×4.6mm, 5μm). The mobile phase consisted of (A) ammonium formate aqueous solution (10mM)-methanol (84:16, v/v) and (B) ammonium formate aqueous solution (10mM)-methanol (47:53, v/v). In order to determine the m/z values of the molecular ions and formulas of all detected impurities, full scan LC-MS in both positive and negative ion modes was firstly executed to obtain the m/z value of the molecules. Then LC-MS2 and LC-MS3 were carried out on target compounds to obtain as much structural information as possible. Complete fragmentation patterns of impurities were studied and used to obtain information about the structures of these impurities. Structures of thirteen unknown degradation products in Flomoxef sodium were deduced based on the high resolution MSn data with both positive and negative modes. The forming mechanisms of degradation products in Flomoxef sodium were also studied.

Effects of added antibiotics on the basic properties of anti-washout-type fast-setting calcium phosphate cement

J Biomed Mater Res 1998 Feb;39(2):308-16.PMID:9457562DOI:10.1002/(sici)1097-4636(199802)39:2<308::aid-jbm19>3.0.co;2-8.

The effect of added antibiotics on the basic properties of anti-washout-type fast-setting calcium phosphate cement (aw-FSCPC) was investigated in a preliminary evaluation of aw-FSCPC containing drugs. Flomoxef sodium was employed as the antibiotic and was incorporated into the powder-phase aw-FSCPC at up to 10%. The setting time, consistency, wet diametral tensile strength (DTS) value, and porosity were measured for aw-FSCPC containing various amounts of Flomoxef sodium. X-ray diffraction (XRD) analysis was also conducted for the identification of products. To evaluate the drug-release profile, set aw-FSCPC was immersed in saline and the released Flomoxef sodium was determined at regular intervals. The spread area of the cement paste as an index of consistency of the cement increased progressively with the addition of Flomoxef sodium, and it doubled when the aw-FSCPC contained 8% Flomoxef sodium. In contrast, the wet DTS value decreased with increase in Flomoxef sodium content. Bulk density measurement and scanning electron microscopic observation revealed that the set mass was more porous with the amount of Flomoxef sodium contained in the aw-FSCPC. The XRD analysis revealed that formation of hydroxyapatite (HAP) from aw-FSCPC was reduced even after 24 h, when the aw-FSCPC contained Flomoxef sodium at > or = 6%. Therefore, the decrease of wet DTS value was thought to be partly the result of the increased porosity and inhibition of HAP formation in aw-FSCPC containing large amounts of Flomoxef sodium. The Flomoxef sodium release from aw-FSCPC showed the typical profile observed in a skeleton-type drug delivery system (DDS). The rate of drug release from aw-FSCPC can be controlled by changing the concentration of sodium alginate. Although Flomoxef sodium addition has certain disadvantageous effects on the basic properties of aw-FSCPC, we conclude that aw-FSCPC is a good candidate for potential use as a DDS carrier that may be useful in surgical operations.

Effect of granulocyte-colony stimulating factor on empiric therapy with Flomoxef sodium and tobramycin in febrile neutropenic patients with hematological malignancies. Kan-etsu Hematological Disease and Infection Study Group

Int J Hematol 1999 Feb;69(2):81-8.PMID:10071455doi

The clinical effects of concomitant use of granulocyte-colony stimulating factor (G-CSF) on empiric antibiotic therapy in febrile neutropenic patients were evaluated in a randomized fashion. Two hundred and fourteen neutropenic febrile episodes (neutrophil counts < 1.0 x 10(9)/l) were treated with Flomoxef sodium and tobramycin with or without G-CSF. The resolution of fever at day 4 (excellent response) or at day 7 (good response) was deemed effective. Among 157 evaluable episodes, the observed excellent responses were 31 (38.8%) and the good responses were 20 (25.0%) in the G-CSF group; those in the control group were 26 (33.8%) and 25 (32.5%), respectively. The overall efficacy rate was 63.8% (51/80) in the G-CSF group and 66.2% (51/77) in the control group (not significant). The initial neutrophil count was 0.186 +/- 0.249 x 10(9)/l in the G-CSF group and 0.235 +/- 0.290 x 10(9)/l in the control group, and rose to 2.889 +/- 4.198 x 10(9)/l and 0.522 +/- 0.844 x 10(9)/l, respectively, at day 7. These results indicate that G-CSF does not affect the rate of response to empiric antibiotic therapy in febrile neutropenic patients, although a significant effect of G-CSF was observed on neutrophil recovery.