Optimization and validation of a high performance liquid chromatography method for rapid determination of sinafloxacin, a novel fluoroquinolone in rat plasma using a fused-core C18-silica column

Q3 · MEDICINE

Article

Author: Feng, Bo ; Zhang, Xiurong ; Xie, Rui ; Fan, Guorong ; Wang, Shuowen ; Wei, Hua ; Wu, Yutian ; Wen, Jun ; Cui, Lijun

A novel, simple and rapid high performance liquid chromatographic method has been developed and validated for the determination of sinafloxacin, a new fluoroquinolone, in rat plasma using 96-well protein precipitation, fused-core C(18)-silica column (4.6mmx50mm, 2.7microm) packed with a new solid support, which is made of 2.7microm particles that consist of a 1.7microm solid core covered with a 0.5microm thick shell of porous silica.The chromatographic separation was achieved with a mobile phase of 20:80 (v/v) of acetonitrile and phosphate buffer (pH=3.0) at a flow rate of 1mlmin(-1). Fluorescence detection was employed with lambda(ex) 295nm and lambda(em) 505nm. Lomefloxacin was used as internal standard (IS). The total analysis time was as short as 3min. The method was sensitive with a limit of detection (LOD) of 2ngml(-1), with good linearity (R(2)=0.9996) over the linear range of 5-500ngml(-1). The intra-day and inter-day precision was less than 5.8% and accuracy ranged from 100.3% to 103.5% for quality control (QC) samples at three concentrations of 10, 50 and 400ngml(-1).The fused-core C(18)-silica column method offered high sample throughput, low injection volume and low consumption of organic solvents. The method was successfully employed in the pharmacokinetic study of sinafloxacin formulation product after tail vein injection to healthy rats.

01 Dec 2009·Veterinary Research CommunicationsQ3 · AGRICULTURAL & FORESTRY SCIENCE

Preparation and evaluation of danofloxacin mesylate microspheres and its pharmacokinetics in pigs

Q3 · AGRICULTURAL & FORESTRY SCIENCE

Article

Author: Cuilan Chen ; Haigang Wu ; Diyun Ai ; Jiyue Cao ; Chunmei Wang ; Jing Li ; Hongchun Shen ; Heng Lin ; Weixue Yi ; Yuanhua Qi

Danofloxacin mesylate gelatin microspheres (DFM-GMS) were prepared by an emulsion chemical crosslinking technique. Distribution of particle size, morphologic characteristics, drug content, and drug stability were evaluated. In-vitro study showed that the release of danofloxacin mesylate (DFM) from microspheres was much slower than from the raw material (DFM) in the release medium. Pharmacokinetic characteristics were evaluated following intramuscular injection of DFM-GMS or DFM in pigs at dosage of 2.5 mg/kg body weight. Elimination half-life (t(1/2β)) of the drug was 24.32 h for DFM-GMS, and 6.61 h for DFM (P < 0.01). Overall, DFM-GMS could be applied as a long-acting and lung targeting dosage form of DFM for clinical application.

01 Nov 2009·Analytical SciencesQ4 · CHEMISTRY

Spectroscopic Studies on the Binding of a New Quinolone Antibacterial Agent: Sinafloxacin to DNA

Q4 · CHEMISTRY

Article

Author: Yutian Wu ; Guocai Lu ; Guorong Fan ; Yan Fei

The binding of sinafloxacin to DNA has been studied by fluorescence spectroscopy and UV-vis absorption spectroscopy. The variations in the spectroscopic characteristics of sinafloxacin upon addition of DNA were observed. Salt concentration effect, KI quenching, fluorescence polarization, DNA denaturation experiments, melting temperature (T(m)) curves and viscosity measurements were studied to investigate the binding mechanism. It was proved that the fluorescence quenching of sinafloxacin is a result of the formation of sinafloxacin-DNA complex. Quenching constants were determined using the Stern-Volmer equation. From the experiment evidence, the major binding mode of sinafloxacin with DNA was evaluated to be the groove binding.

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Indication	Highest Phase	Country/Location	Organization	Date
Bacterial Infections	Phase 1	CN	Jiangsu Hansoh Pharmaceutical Co. Ltd.	-
Bacterial Infections	Phase 1	CN	Shanghai Xinchuang Medical Technology Co., Ltd.	-

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