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Full-Text Articles in Pharmaceutics and Drug Design
Inhibition Of Oxidative And Conjugative Metabolism Of Buprenorphine Using Generally Recognized As Safe (Gras) Compounds Or Components Of Dietary Supplements, Neha V. Maharao
Theses and Dissertations
This dissertation aimed at developing an inhibitor strategy to improve the oral bioavailability (Foral) and systemic exposure (AUC∞) of buprenorphine (BUP) as well as reduce the variability associated with them. Twenty-seven generally recognized as safe (GRAS) compounds or dietary substances were evaluated for their potential to inhibit the oxidative and conjugative metabolism of BUP, using pooled human intestinal and liver microsomes. In both the organs, oxidation appeared to be the major metabolic pathway with a 6 fold (intestine) and 4 fold (liver) higher intrinsic clearance than glucuronidation. Buprenorphine was predicted to show low and variable F …