Study of in-vitro biotransformation of prodrugs of Ester and Amide linkages of Ibuprofen, Diclofenac Sodium and Paracetamol in acidic and alkaline medium
نویسنده
چکیده
Our goal is to perform in-vitro biotransformation of Prodrugs of ibuprofen+paracetamol, diclofenac sodium+paracetamol and ibuprofen+diclofenac sodium by acidic and alkaline hydrolysis of both ester (–COO–) and amide (–CONH–) linkages into free drugs and chromatographically separation of their Rt in HPLC. Since both ester (–COO–) and amide (–CONH–) linkages are susceptible to hydrolysis in both acidic pH (gastric pH) and basic pH (intestinal pH) to produce parent drug ibuprofen, diclofenac and paracetamol by biotransformation in invivo; so it will be implemented as a Prodrug which can show prolong action on pain and fever after getting released into free parent drug by biotransformation. The HPLC (High-Performance Liquid Chromatography) study reports the retention time (Rt) and releases kinetics of three Prodrugs by taking HPLC degradation data of three samples of Prodrugs and individual HPLC data of parent drugs separately to compare the Rt value of release of three drugs from Prodrugs in both acidic and alkaline pH. Prodrug–A (logP=4.56) releases Ibuprofen & Paracetamol, Prodrug–B (logP=4.90) releases Diclofenac & Paracetamol and Prodrug–C (logP=6.13) releases Ibuprofen & Diclofenac. This is a comparison study of drug release in in-vitro gastric as well as intestinal pH focusing on in-vivo biotransformation.
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