Human biliary amount prediction using simple, bile flow-rate corrected and uridine diphosphate glucuronosyltransferase activity corrected allometric methods

Author:

Giri Poonam1,Patel Harilal1,Srinivas Nuggehally R1

Affiliation:

1. Department of Drug Metabolism & Pharmacokinetics, Zydus Research Centre, NH-8A, Tal-Sanand, Moraiya, Ahmedabad 382 210, Gujarat, India

Abstract

Aim: Retrospective scaling of human biliary amounts has been performed using allometry. Methods: Human biliary excretory data for 14 drugs were predicted using simple, bile flow-rate corrected and uridine diphosphate glucuronosyltransferase (UDPGT) activity corrected allometry methods. Allometry was performed using Y = aXb relationship with correction factors. Statistical tests consisting of fold difference (predicted/observed) and root-mean-square error (RMSE) computation were carried out. Results: UDPGT activity corrected allometry predicted higher biliary amounts in humans as compared with other methods. The RMSE values were 38, 32 and 81 for simple, bile flow-rate corrected and UDPGT activity corrected allometry, respectively. Conclusion: Although data showed the usefulness of the approaches for human biliary predictions in the decision process for nominating drug candidate(s) based on % RMSE and fold differences, for some drugs prediction appeared not satisfactory using any of the methods.

Publisher

Future Science Ltd

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