A penem antibiotic faropenem sodium was synthesized by condensation of(3R,4R)-4-acetoxy- 3-[(1R)-(tert-butyldimethylsilyoxy)ethyl]-2-azetidinone and(R)-tetrahydrofuran-2-thiolcarboxylic acid,followed by acylation,Wittig reaction,deprotection and hydrolysis with an overall yield of about 37%.
RESULTS The plasma concentration-time curves of Faropenem are fitted to an one-compartment model after an oral Faropenem sodium tablet in single dose(200, 400, 600 mg). The main pharmacokinetic parameters were as follows:t_ max (0.85±0.29),(0.73±0.34) and (0.88±0.29)h;
METHODS 30 Healthy volunteers (15 male, 15 female) were divided into three groups randomly,and were given a single oral dose (200, 400, 600 mg) of Faropenem sodium tablet. Blood samples were collected from elbow vein at certain sampling times.
Methods: The residual solvents in Faropenem sodium were determined by GC with HP-5 capillary column (30 m×0.53 mm, 1.5 μm) , FID detector and using nitrogen as carrier gas. The injector temperature was 200 ℃ and the detector temperature was 250 ℃.
Objective: To establish a method for detection of the residual solvents in Faropenem sodium. Methods: The residual solvents in Faropenem sodium were determined by GC with HP-5 capillary column (30 m×0.53 mm, 1.5 μm) , FID detector and using nitrogen as carrier gas. The injector temperature was 200 ℃ and the detector temperature was 250 ℃. The column temperature was raised by program, the initial temperature was 35 ℃, maintained for 5 min, raised to 120 ℃ with a rate of 10 ℃/min, main...
OBJECTIVE To develop a HPLC method for determination of related substances of faropenem sodium METHODS Faropenem sodium and its related substances were separated by using a mobile phase consisted of acetonitrile 0 02 mol·L -1 triethylamine ( 14∶86 ,pH 2 5) at a flow rate of 1 0 mL·min -1 on an Aglient Zorbax Zclipse XDB C 18 column and detected at 247 nm RESULTS The resolution and sensitivity of related substances were acceptable The detection lim...
Objective To investigate the thermal kinetic characteristics of faropenem sodium at 60℃ and determine the main thermal degradation impurity. Methods An HPLC method was carried out to (detect) the quantity of faropenem at 60℃ in different period of times. The data was fitting in with appropriate dynamic equations to calculate the half-life. The main thermal degradation impurity was isolated by preparation HPLC and identified by MS, ()~1H-NMR, ()~(13)C-NMR, IR and UV. Results The chemical ki...