Title :
Research on esterified prodrugs of naproxen
Author :
Yang, Houci ; Yang, Gen-sheng
Author_Institution :
Coll. of Pharm. Sci., Zhejiang Univ. of Technol., Hangzhou, China
Abstract :
Naproxen was a popular non-steroidal anti-inflammatory drug (NSAID), which might cause side effects. The subject hoped to reduce the side-effect of naproxen by the synthesis of its prodrugs and keep its therapeutic effect as an anti-inflammatory drug. Fifteen prodrugs of naproxen had been synthesized with the use of DCC as a dehydrater and DMAP as a catalyzer. The chemical stability of prodrugs had been investigated with acid-base titration. The anti-inflammatory effect of the prodrugs had been determined by the curing of engorgement in the ears of Mus musculus albus. The action of prodrugs in vivo was studied with HPLC. The paper also reported the preparation of the emulsion of prodrugs to help increase their bioavailability. The result indicated that naproxen-esterifled prodrugs were stable against chemical hydrolysis, could remain or even enhance their effects and reduce by-effect.
Keywords :
biochemistry; chromatography; drugs; ear; emulsions; DCC; DMAP; HPLC; Mus musculus albus; acid-base titration; catalyzer; chemical hydrolysis; chemical stability; curing; dehydrater; ears; emulsion; in-vivo prodrugs; naproxen-esterifled prodrugs; nonsteroidal antiinflammatory drug; therapeutic effect; Blood; Chemicals; Drugs; Ear; Equations; Gastrointestinal tract; Mice; chemical stability; emulsion; naproxen; pharmacodynamics; pharmacokinetics; prodrug;
Conference_Titel :
Remote Sensing, Environment and Transportation Engineering (RSETE), 2011 International Conference on
Conference_Location :
Nanjing
Print_ISBN :
978-1-4244-9172-8
DOI :
10.1109/RSETE.2011.5966179