Study of in-vitro biotransformation of prodrugs of Ester and Amide linkages of Ibuprofen, Diclofenac Sodium and Paracetamol in acidic and alkaline medium

  • Posted on: 31 July 2017
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PharmaTutor (August - 2017)

 

ISSN: 2347 - 7881
(Volume 5, Issue 8)

 

Received On: 23/05/2017; Accepted On: 23/05/2017; Published On: 01/08/2017

 

AUTHORS:
Dhrubo Jyoti Sen
Department of Pharmaceutical Chemistry,
Shri Sarvajanik Pharmacy College,
Mehsana, Gujarat, India
dhrubosen69@yahoo.com

 

 

ABSTRACT:
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 for hydrolysis in both acidic pH (gastric pH) and basic pH (intestinal pH) to produce parent drug ibuprofen, diclofenac and paracetamol by biotransformation in in-vivo; so it will be implemented as a Prodrug which can show prolong action on pain and fever after getting release into free parent drug by biotransformation. The HPLC (High Performance Liquid Chromatography) study reports the retention time (Rt) and release kinetics of three Prodrugs by taking HPLC degradation datas of three samples of Prodrugs and individual HPLC datas 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.  Keywords: Prodrug-A/Prodrug-B/Prodrug-C, Ibuprofen, Paracetamol, Diclofenac sodium, Molecular weight, logP, UV λmax, IR, Mobile phase, TLC-Rf value, HPLC-Rt value, LOD, LOC.

 

 

How to cite this article: Sen DJ; Study of in-vitro biotransformation of prodrugs of Ester and Amide linkages of Ibuprofen, Diclofenac Sodium and Paracetamol in acidic and alkaline medium; PharmaTutor; 2017; 5(8); 49-65

 

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