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Preparation and Pharmacological Evaluation of Novel Orally Active Ester Prodrugs of Ketoprofen with Non‐Ulcerogenic Property
Author(s) -
Dhakane Valmik D.,
Thakare Vishnu N.,
Dongare Sakharam B.,
Bhale Pravin S.,
Mule Yoginath B.,
Bandgar Babasaheb P.,
Chavan Hemant V.
Publication year - 2016
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12719
Subject(s) - ketoprofen , prodrug , pharmacology , bioavailability , pharmacokinetics , chemistry , drug , plasma concentration , medicine
This study investigates anti‐inflammatory activity with improved pharmacokinetic and non‐ulcerogenic properties of various novel synthesized prodrugs of ketoprofen in experimental animals. Prodrugs 3a , 3f and 3k were found to possess significant anti‐inflammatory activity with almost non‐ulcerogenic potential than standard drug ketoprofen ( 1) in both normal and inflammation‐induced rats. The experimental findings elicited higher AUC and plasma concentration at 1 and 2 h indicating improved oral bioavailability as compared to parent drug ketoprofen. These prodrugs are found to have no gastric ulceration with retained anti‐inflammatory activity. Therefore, present experimental findings demonstrated significant improvement of various pharmacokinetic properties with non‐ulcerogenic potential of ester prodrugs of ketoprofen.