Tosufloxacin (tosylate)
(Synonyms: 甲苯磺酸妥舒沙星) 目录号 : GC45065
A fluoroquinolone antibiotic
Cas No.:115964-29-9
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
Tosufloxacin is a fluoroquinolone antibiotic. It has activity against diverse aerobic and anaerobic bacteria in vitro. Tosufloxacin is also effective against bacterial persisters, showing significant activity against S. aureus and uropathogenic E. coli persisters. As with many other quinolones, tosufloxacin use can be associated with significant side effects.
| Cas No. | 115964-29-9 | SDF | |
| 别名 | 甲苯磺酸妥舒沙星 | ||
| Canonical SMILES | O=C1C2=C(N=C(N3CCC(N)C3)C(F)=C2)N(C4=CC=C(F)C=C4F)C=C1C(O)=O.CC5=CC=C(S(O)(=O)=O)C=C5 | ||
| 分子式 | C19H15F3N4O3•C7H8O3S | 分子量 | 576.5 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml,Ethanol: slightly soluble | 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 | 1.7346 mL | 8.673 mL | 17.3461 mL |
| 5 mM | 0.3469 mL | 1.7346 mL | 3.4692 mL |
| 10 mM | 0.1735 mL | 0.8673 mL | 1.7346 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。
Simultaneous Determination of 15 Sulfonate Ester Impurities in Phentolamine Mesylate, Amlodipine Besylate, and Tosufloxacin tosylate by LC-APCI-MS/MS
J Anal Methods Chem 2019 Oct 7;2019:4059765.PMID:31687249DOI:10.1155/2019/4059765.
Sulfonate esters have been recognized as potential genotoxic impurities (PGIs) in pharmaceuticals. An LC-MS/MS method was developed and validated for the simultaneous determination of 15 sulfonate esters, including methyl, ethyl, propyl, isopropyl, and n-butyl esters of methanesulfonate, benzenesulfonate, and p-toluenesulfonate in drug products. The method utilized atmospheric pressure chemical ionization (APCI) in multiple reaction monitoring (MRM) mode for the quantitation of impurities. The method employed an ODS column as the stationary phase and water-acetonitrile as the solvents for gradient elution without derivatization steps. The method was specific, linear, accurate, precise, and robust. Recoveries of the sulfonic esters from three drug matrices were observed in the range of 91.6∼109.0% with an RSD of not greater than 17.9% at the concentration of the LOQ and in the range of 90.4%∼105.2% with an RSD of not greater than 7.1% at the concentration of 50 ng/mL for the methanesulfonates and 10 ng/mL for the benzenesulfonates and p-toluenesulfonates. The LOD was not greater than 15 ng/mL, 2 ng/mL, and 1 ng/mL for the methanesulfonate, benzenesulfonate, and p-toluenesulfonate esters, respectively. This method was sufficiently sensitive to detect the 15 PGIs in the phentolamine mesylate tablet, amlodipine besylate tablet, and Tosufloxacin tosylate tablet. This analytical method is a direct, specific, rapid, and accurate quality control tool for the determination of the 15 sulfonate esters that are most likely to exist in drug products.
[Mn2+-cTMAB-sensitized fluorescent microscopic determination of Tosufloxacin tosylate based on a self-ordered ring]
Guang Pu Xue Yu Guang Pu Fen Xi 2014 Feb;34(2):445-9.PMID:24822418doi
With the development of antimicrobial drugs, drug residue in animal products has a serious potential hazards for the environment and public health, it is urgent to set up drug residue detection method with low detection limit and good selectivity. In our paper, with poly (vinyl alcohol)-124 (PVA-124) and NH3-NH4Cl (pH 10.50) as the medium, Mn2+ and cetyltrimethyl ammonium bromide (CTMAB) as sensitizer, Tosufloxacin tosylate (TSFX) formed a self-ordered ring (SOR) on a hydrophobic glass slide support. When the droplet volume is 0.20 microL, the TSFX can be detected in the range of 4.05 x 10(-14) approximately 4.28 x 10(-13) mol x ring(-1) (2.02 x 10(-7) approximately 2.14 x 10(-6) mol x L(-1)), and the limit of detection (LOD) can reach 4.1 x 10(-15) mol x ring(-1) (2.0 x 10(-8) mol x L(-1)). The established method had been applied satisfactorily to determine the content of TSFX in tablet, which close to the marked value of 0.15 g x piece(-1)) found value: 0.144 g x piece(-1)) and the results of TSFX concentrations in rabbit serum at different time after dosing with the recoveries of 90.0% - 105.0% and RSDs 1.9% - 3.3% were satisfactory. Xilinguole of Inner Mongolia is the national important livestock products ground, whose lamb is the main suppling source for Beijing-Tianjin-Tangshan region. It is very urgent to detect residue of antibacterial drug in its sheep tissue samples (meat, liver, kidney). In this paper, when acetonitrile was used as extraction agent in pretreatment of sheep tissue samples in six rangelands including Sonid Right Banner, Xiwuzhumuqin Banner, Xilinhot City, Duolun County, The white Flag Town and The Blue Flag Town, the extract can be directly determined with SOR technology without filtering process, the sample standard addition recovery of sheep tissues were 92.0%-101.0% and RSDs were less than 2.7%. The results indicated that the SOR technique can be successfully applied to pharmaceuticals and biological samples, which broaden the applied range of SOR technique. The assay would provide reliable experimental data and theoretical basis for the relevant departments.
Synthesis and biological properties of A-71497: a prodrug of Tosufloxacin
Drugs Exp Clin Res 1990;16(9):435-43.PMID:2100244doi
Tosufloxacin (5, A-61827 tosylate or T-3262) is currently under product development by both Abbott Laboratories and Toyama Chemical Co. Its registration as antibacterial agent has been approved in Japan. It has been found to be extremely effective in treating several bacterial infections. However, due to its inherent low water solubility, the development of an intravenous formulation will be extremely difficult and may preclude its parenteral use. In search of a more water-soluble analog of Tosufloxacin for parenteral use, the 3-formyl derivative of tosulfoxacin, A-71497 (13), was synthesized for evaluation. It was found to produce high plasma levels of Tosufloxacin upon both oral and subcutaneous administration to mice. High plasma levels of Tosufloxacin were also obtained when 13 was administered both orally and intravenously to dogs. It possesses increased water solubility and makes the development of intravenous formulation possible. The chemical synthesis as well as biological properties of A-71497 (13) are described.
In-vitro activities of temafloxacin, Tosufloxacin (A-61827) and five other fluoroquinolone agents
J Antimicrob Chemother 1989 Apr;23(4):527-35.PMID:2745259DOI:10.1093/jac/23.4.527.
Tosufloxacin (A-61827) is the tosylate salt of A-60969 (T-3262). Temafloxacin (A-62254) is the hydrochloride salt of A-63004. Both compounds were tested against 945 aerobic bacterial isolates and their in-vitro activities were compared to those of five other fluoroquinolones. Ciprofloxacin and Tosufloxacin were similar in their activity against the Enterobacteriaceae and Pseudomonas species. Temafloxacin and ofloxacin were similar in their activity against the Gram-negative bacilli. Strains that were susceptible to ciprofloxacin were also susceptible to ofloxacin, temafloxacin and Tosufloxacin. Against nalidixic acid-resistant enteric bacilli, the potency of all seven fluoroquinolones was compromised. Enoxacin and fleroxacin were the least active drugs against Gram-positive species. Tosufloxacin was particularly active against the Gram-positive species; ciprofloxacin, difloxacin and temafloxacin were less active.
Effect of xanthan gum-based food thickeners on the dissolution profile of fluoroquinolones oral formulations
J Pharm Health Care Sci 2020 Nov 30;6(1):25.PMID:33292643DOI:10.1186/s40780-020-00181-9.
Background: Xanthan gum-based food thickeners (XG-FTs) are often ingested by patients with dysphagia to prevent aspiration during drug treatment. Reportedly, XG-FTs affect tablet disintegration, drug dissolution rates, and reduce the efficacy of postprandial antihyperglycemic agents. The absorption rate and quantity of fluoroquinolone antimicrobial agents correlate with drug efficacy, raising concern about the impact of XG-FTs. Previously, we reported that film-coated tablets were less susceptible to the effects of XG-FT than conventional and orally disintegrating tablets. Here, we compare the effect of XG-FTs on dissolution profiles of three oral fluoroquinolone-based film-coated tablets by evaluating the dissolution of crushed products, fine granules, and film-coated fine granules. Methods: We examined formulations of Tosufloxacin tosylate monohydrate (TFLX), levofloxacin hemihydrate (LVFX), and ciprofloxacin hydrochloride hydrate (CPFX). The formulations were immersed in 20 mL of 1.5% (w/v) XG-FT aqueous solution for 2.5 min followed by a dissolution test using the paddle method according to the Japanese Pharmacopoeia (dissolution test solution pH 1.2; volume 900 mL; temperature 37 ± 0.5 °C). The dissolution profile was evaluated according to the dissolution quantity indicated in product specifications and guidelines for bioequivalence testing of generic drugs. The 15-min mean dissolution rate was determined for a formulation immersed in 1.5% (w/v) XG-FT aqueous solution and compared with that for a non-immersed formulation (control). Fluoroquinolone film-coated tablets were mixed with starch-based FTs, guar gum-based FTs, or XG-FTs to observe their appearances. Results: The dissolution profile of LVFX film-coated tablets was not affected by XG-FTs, but the dissolution of TFLX and CPFX was delayed. For crushed film-coated tablets, the 15-min mean dissolution rate was significantly delayed for all three fluoroquinolones when compared with that of uncrushed products. The dissolution profile of TFLX film-coated fine granules was unchanged by XG-FTs. CPFX film-coated tablets and crushed products produced a gel-like precipitate when mixed with XG-FTs and failed to meet product-dissolution specifications. A gel-like precipitate was also observed with guar gum-based FTs. Conclusion: The effect of XG-FTs on the dissolution profile of film-coated fluoroquinolone formulations varied depending on the formulation. The CPFX formulation formed a gel-like precipitate when immersed in XG-FTs resulting in a significantly delayed dissolution.