RESULTS: The main pharmacokinetic parameters after oral administration of domestic and imported loxoprofen sodium tablet(60mg) were: t1/2ke 93. 9 ± 19.8min, 92.4± 16.3min; AUC0-t 596.97 ± 104.l2μg. min.
Calibration curves were linear within 0.2~12.0 μg·ml -1(r=0.9998) and the minimum detection concentration was 0.2 μg·ml -1.The main pharmacokinetic parameters after oral administration of dome stic and imported loxoprofen sodium tablet (60 mg)were:t 1/2 were 1.3 9±0.15 h and 1.41±0.15 h;
After 4 weeks of treatment, 92.42% of the AS patients responded to loxoprofen sodium. Significant improvements were noticed in all 3 primary outcome measurements( P <0.05).
METHODSAll 80 patients from the HuBei Provincial TCM Hospital conforming to the diagnostic standard, were randomly divided into two groups: therapeutic group of TongBi 2 (GroupA, n=40) and comparative group of Loxoprofen Sodium Tablets(GroupB, n=40), with MTX for both groups as basic treatment.
In contrast, the combination of enoxacin at 100 mg/kg and either ketoprofen at 125 mg/kg or pranoprofen at 500 mg/kg induced clonic convulsions, while that of enoxacin at 400 mg/kg and loxoprofen sodium at 600 mg/kg induced no convulsion.
The oral administration of ketoprofen, pranoprofen or loxoprofen sodium induced no convulsion up to 1000 mg/kg, 500 mg/kg and 600 mg/kg, respectively, and that of enoxacin induced no convulsion at more than 5000 mg/kg.
Convulsions induced by the combination of enoxacin, a new antimicrobial, and nonsteroidal anti-inflammatory drugs including nimesulide, ketoprofen, pranoprofen and loxoprofen sodium, were investigated in mice.
A facile method for preparation of loxoprofen sodium is disclosed.Ethyl 2 ( p bromomethyl phenyl) propionate,prepared from toluene via acylation,ketalization,rearrangement,hydrolysis,bromination and esterification,was subjected to phase transfer ca talyzed alkylation with ethyl 2 oxocyclopentanecarboxylate,followed by hydrolysis with decarboxylation and salt formation in one pot procedure to afford loxoprofen sodium in about 35% overall yield.
In the presence of sodium t- butoxide and DMSO,ethyl 2 - oxocyclopentanecarboxylate was subjected to C- alkylation with 2 - ( 4- bromomethylphenyl) propanoic acid with high regioselectivity to give 2 - [4 - ( 1 - ethoxycarbonyl- 2 - oxo- 1 - cyclopentanylmethyl) phenyl]propanoic acid ( 4) which was followed by hydrolysis,decarboxylation and saltformation to afford loxoprofen sodium in about72 % overall yield.The effects of reaction temperature and different solvents on yield of4 were a...
Objective:For improving and shortening synthetic process and raising yield.Methods:2-(p-bromomrthyl phenyl)propionic acid is prepared from toluene,and alkylated with 2-oxocyclopentane carboxylate in medium of ethanol,DMF,and sodium hydroxide,and loxoprofen sodium is obtained following the product of the former reaction is hydrolyzed and decarboxylated.Results:The product thus obtained is identified with IR and JH1,D,Z-NMR.Conclusion:A shorter new process for synthesis of loxoprofen...