The use of saliva instead of plasma as a surrogate in drug bioava | 6228
Journal of Developing Drugs

Journal of Developing Drugs
Open Access

ISSN: 2329-6631

+44 7868 792050

The use of saliva instead of plasma as a surrogate in drug bioavailability and bioequivalence studies in humans

Joint International Conference and Expo on Industrial Pharmacy & 5th Global Pharmacovigilance Summit

April 28-29, 2016 Dubai, UAE

Nasir M Idkaidek

Petra University, Jordan

Posters & Accepted Abstracts: J Develop Drugs

Abstract :

Introduction: Salivary excretion of some drugs has been reported previously as a good indicator for drug bioavailability, therapeutic drug monitoring, pharmacokinetics and drug abuse because saliva sampling offers simple, non-invasive and cheap method as compared with plasma sampling with no contamination risk. The rules of drug protein binding and membrane permeability on salivary excretion were previously investigated for several drugs, where a salivary excretion classification system (SECS) was proposed. Aim: The research purpose is to study and compare the pharmacokinetics of selected drugs in plasma and saliva matrixes in healthy human volunteers, and to suggest using non-invasive saliva sampling instead of plasma as a surrogate in bioavailability and bioequivalence (BA/BE) studies. Materials & Methods: Four different pilot BA/BE studies were done in 12-18 healthy humans. Saliva and plasma samples were collected for 3-5 half life values of metformin, tolterodine, rosuvastatin, and paracetamol after oral dosing. Saliva and plasma samples were assayed using LC-MSMS, then pharmacokinetic parameters were calculated by non-compartmental analysis using Kinetica program. Effective intestinal permeability (Peff) values were also optimized to predict the actual average plasma profile of each drug by Nelder-Mead algorithm of the Parameter Estimation module using SimCYP program. Results & Discussion: All studied drugs showed salivary excretion with strong correlation coefficients between saliva and plasma concentrations. The optimized Peff ranged 1.44��?68.3 x 10-4 cm/sec for the drugs under investigation. Saliva/plasma concentrations ratios ranged 0.17��?1.5. Inter and intra individual variability of primary pharmacokinetic parameters in saliva matrix were either close to or higher than plasma matrix. This requires larger sample size in saliva studies for some drugs. Our results suggested that there is a potential in BA/BE studies for saliva to be considered as a surrogate for plasma concentration, which goes along with drug regulations. The use of saliva instead of plasma in such studies makes them non-invasive, easy and with a lower clinical burden.

Biography :