A Study of Absorption and Selected Molecular Physicochemical Properties of Some Antipsychotic Drugs

Abstract

Antipsychotic drugs are commonly prescribed for different mental disorders and can be classified into two main groups: the first which contain originally developed antipsychotics of the first generation or typical antipsychotics and the other group with newly developed antipsychotics or atypical antipsychotics of the second generation. In this study, eleven antipsychotic drugs (chlorpromazine, flupentixol, haloperidol, zuclopenthixol, aripiprazole, clozapine, olanzapine, quetiapine, risperidone, sertindole, ziprasidone) were investigated to evaluate significance of their molecular physicochemical properties (lipophilicity, aqueous solubility, polar surface area, molecular weight, volume value and acidity) for their bioavailability. Relationships between literature available intestinal absorption data of antipsychotic drugs and their lipophilicity descriptor with one additional molecular descriptor, investigated using multiple linear regression analysis provided high correlations for molecular descriptors, Mw, Vol, pKa, as additional independent variables. Values of correlation coefficients (R2) were ranged from 0.951 (for Vol) above 0.944 (for Mw) to 0.923 (for pKa).