Thu, 23 Nov 2017

Quantitative Structure-Pharmacokinetic Relationship (QSPkR) Analysis of the Serum Protein Binding Values for Antidiabetic Agents In Humans

Sethi Reeta1, Paul Yash2

1.Shri Jagdish Prasad Jhabarmal Tibrewala University, Jhunjhunu (Rajasthan)

2.Lord Shiva College of Pharmacy, Sirsa (Haryana)


ABSTRACT

An estimate of Serum protein binding (%SPB) is of paramount importance in assessing the efficacy of drugs used to treat diabetes in patients.  This study was conducted to develop Quantitative Structure Pharmacokinetic Relationship (QSPkR) for the prediction of %SPB in human for congeneric series of 23 antidiabetic drugs, using computer assisted Hansch approach.  The QSPkR correlations were duly analyzed using a battery of apt statistical  procedures and validated using leave-one-out (LOO) approach. Analysis of several hundreds of QSPkR correlations developed in this study revealed high degree of cross- validated coefficients (Q2) using LOO method (p<0.001). The overall predictability was found to be high serum protein binding (%SPB) ( R2=0.8709, F=19.20, S2=93.89, Q2=0.6685, p<0.001). Serum protein binding (%SPB) in  the present QSPkR investigations was found to depend upon electrostatic  and constitutional parameters. Its positive dependence on such descriptors indicates that hydrogen bonding and vander Waals’ interactions play a stellar role in governing protein binding.

Keywords: Quantitative structure pharmacokinetic relationships (QSPkR), Serum protein binding, In Silico ADME, antidiabetic drugs


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