title: Preparation and Pharmacological Evaluation of Novel Orally Active Ester Prodrugs of Ketoprofen with Non-Ulcerogenic Property.
abstract: 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.
authors.affiliation: Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Solapur University, Solapur, Maharashtra, 413 255, India.
authors.forename: Valmik D
authors.initials: VD
authors.lastname: Dhakane
authors.affiliation: Department of Pharmacology, Sinhgad Institute of Pharmaceutical Sciences, Kusgaon (Bk), Lonavala, Maharashtra, 410 401, India.
authors.forename: Vishnu N
authors.initials: VN
authors.lastname: Thakare
authors.affiliation: Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Solapur University, Solapur, Maharashtra, 413 255, India.
authors.forename: Sakharam B
authors.initials: SB
authors.lastname: Dongare
authors.affiliation: Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Solapur University, Solapur, Maharashtra, 413 255, India.
authors.forename: Pravin S
authors.initials: PS
authors.lastname: Bhale
authors.affiliation: Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Solapur University, Solapur, Maharashtra, 413 255, India.
authors.forename: Yoginath B
authors.initials: YB
authors.lastname: Mule
authors.affiliation: Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Solapur University, Solapur, Maharashtra, 413 255, India.
authors.forename: Babasaheb P
authors.initials: BP
authors.lastname: Bandgar
authors.affiliation: Department of Chemistry, A.S.P. College Devrukh, Dist.-Ratnagiri, Maharashtra, 415 804, India.
authors.forename: Hemant V
authors.initials: HV
authors.lastname: Chavan
mesh_terms: D000284:Administration, Oral; D000818:Animals; D004353:Drug Evaluation, Preclinical; D007660:Ketoprofen / Q000009:adverse effects / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D051379:Mice; D011355:Prodrugs / Q000009:adverse effects / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D051381:Rats; D016205:Sigmodontinae; D013276:Stomach Ulcer / Q000097:blood / Q000139:chemically induced
chemical_list: D011355:Prodrugs; D007660:Ketoprofen
keywords: anti-inflammatory activity; ketoprofen; non-ulcerogenic; pharmacokinetic profile; prodrug