Аssessment of deconvolution method ability to estimate metoclopramide (mcp) systemic availability after p.o. administration to healthy volunteers

Аssessment of deconvolution method ability to estimate metoclopramide (mcp) systemic availability after p.o. administration to healthy volunteers

Oral presentation

Anton Filipov, Кristina Bozhinova, Hristo Petkov, Tsveta Sarafska, Ivanka Atanasova, Dimiter Terziivanov
Faculty of Chemistry and Pharmacy, Sofia University Saint Kliment Ohrisdki

Deconvolution is a model-independent method for determining absorption rate. The Deconvolution method requires no assumptions regarding the number of compartments in the model or the kinetics of absorption. Linear distribution and elimination are assumed. Deconvolution requires data obtained after both p.o. and i.v. administration in the same subject and assumes no differences in the pharmacokinetics of drug distribution and elimination from one study to the other. Drug concentrations must be measured at the same times following both p.o. and i.v. administration during the time that drug is absorbed after p.o. administration. Aim: To compare the values of MCP systemic availability, Fabs, after p.o. administration, as estimated by the classical pharmacokinetic (PK) method, with those calculated by the Deconvolution method. Discussion and conclusions: MCP absolute bioavailability, Fabs, after p.o. input was evaluated by means of the classical comparison of area under the curves (AUCs) ratios after p.o. and i.v. drug administration. Deconvolution method offers opportunity to calculate MCP amount reaching systemic circulation and its ratio regarding the oral dose. Comparing Fabs with the amount reaching systemic circulation (ARSC/DP.O.) ratio revealed NO statistically significant difference and suggests the ability of the Deconvolution method to be used instead of classical AUC method for assessing drug absolute bioavailability. The estimates of Fabs and ARSC/DP.O. ratio are in a very good agreement with the reported results with regard to its systemic availability after oral administration of 10mg.
Keywords: Deconvolution method, metoclopramide, bioavailability