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Preparation and Pharmacological Evaluation of Novel Orally Active Ester Prodrugs of Ketoprofen with Non‐Ulcerogenic Property |
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| Authors: | Valmik D. Dhakane Vishnu N. Thakare Sakharam B. Dongare Pravin S. Bhale Yoginath B. Mule Babasaheb P. Bandgar Hemant V. Chavan |
| Affiliation: | 1. Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Solapur University, Solapur, Maharashtra, India;2. Department of Pharmacology, Sinhgad Institute of Pharmaceutical Sciences, Kusgaon (Bk), Lonavala, Maharashtra, India;3. Department of Chemistry, A.S.P. College Devrukh, Dist.‐Ratnagiri, Maharashtra, India |
| 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. |
| Keywords: | anti‐inflammatory activity ketoprofen non‐ulcerogenic pharmacokinetic profile prodrug |