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Preparation and Pharmacological Evaluation of Novel Orally Active Ester Prodrugs of Ketoprofen with Non-Ulcerogenic Property.
Dhakane, Valmik D; Thakare, Vishnu N; Dongare, Sakharam B; Bhale, Pravin S; Mule, Yoginath B; Bandgar, Babasaheb P; Chavan, Hemant V.
Afiliación
  • Dhakane VD; Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Solapur University, Solapur, Maharashtra, 413 255, India.
  • Thakare VN; Department of Pharmacology, Sinhgad Institute of Pharmaceutical Sciences, Kusgaon (Bk), Lonavala, Maharashtra, 410 401, India.
  • Dongare SB; Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Solapur University, Solapur, Maharashtra, 413 255, India.
  • Bhale PS; Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Solapur University, Solapur, Maharashtra, 413 255, India.
  • Mule YB; Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Solapur University, Solapur, Maharashtra, 413 255, India.
  • Bandgar BP; Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Solapur University, Solapur, Maharashtra, 413 255, India.
  • Chavan HV; Department of Chemistry, A.S.P. College Devrukh, Dist.-Ratnagiri, Maharashtra, 415 804, India.
Chem Biol Drug Des ; 87(6): 878-84, 2016 Jun.
Article en En | MEDLINE | ID: mdl-26715009
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Profármacos / Cetoprofeno Límite: Animals Idioma: En Revista: Chem Biol Drug Des Asunto de la revista: BIOQUIMICA / FARMACIA / FARMACOLOGIA Año: 2016 Tipo del documento: Article País de afiliación: India Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Profármacos / Cetoprofeno Límite: Animals Idioma: En Revista: Chem Biol Drug Des Asunto de la revista: BIOQUIMICA / FARMACIA / FARMACOLOGIA Año: 2016 Tipo del documento: Article País de afiliación: India Pais de publicación: Reino Unido