Determination of ADME and Bioavailability Following Intravenous, Oral, and Dermal Routes of Exposure

Abstract

Humans are exposed to chemicals either voluntarily or involuntarily through several routes. Therapeutic drugs are introduced into the human system via a number of routes including, but not limited to, oral, inhalation, intravenous (i.v.), topical, and subcutaneous. For occupational and environmental chemicals, the major routes of human exposure are inhalation, dermal, and oral. To determine the extent of exposure to chemicals, the concentration of the active molecules is measured in a biological medium. Determination of absolute and/or relative bioavailability of occupational and environmental chemical exposure through different routes is critical in understanding the risk to the general population of a low-level exposure to these chemicals. This unit describes typical protocol designs to generate data for the calculation of absorption, distribution, metabolism, and elimination (ADME) and absolute and relative bioavailability of chemicals when exposed through i.v., oral, and dermal routes.

The Modulatory Properties of Astragalus membranaceus Treatment on Triple-Negative Breast Cancer: An Integrated Pharmacological Method

“…In this process, three ADME-related models, including oral bioavailability (OB), Caco-2 permeability, and drug likeness (DL), were employed to identify the bioactive compounds with favorable pharmacokinetic properties. As one of the most vital pharmacokinetic parameters of orally administered drugs, OB plays a key role in the efficiencies of bioactive compounds in systemic circulation (Saghir, 2009; Tian et al, 2011; Xu et al, 2012). The Caco-2 cell model was used as a standard in vitro screening tool for predicting intestinal drug absorption and drug transport mechanisms.…”

A Biomedical Investigation of the Hepatoprotective Effect of Radix salviae miltiorrhizae and Network Pharmacology-Based Prediction of the Active Compounds and Molecular Targets

“…The ADME system used in this study including PreOB (predict oral bioavailability) and PreCaco-2 (predict Caco-2 permeability). Oral bioavailability (OB) is one of the most vital pharmacokinetic properties of orally administered drugs as it plays an important role for the efficiency of the drug delivery to the systemic circulation [54,55]. Here, a reliable in silico screening model OBioavail 1.1 was employed in OB value calculation of the constituents in Danshen.…”

A Network-Based Pharmacology Study of the Herb-Induced Liver Injury Potential of Traditional Hepatoprotective Chinese Herbal Medicines

“…The ADME system used in this study including predict oral bioavailability (PreOB) and predict Caco-2 permeability (PreCaco-2). Oral bioavailability (OB) is one of the most vital pharmacokinetic properties of orally administered drugs as it plays an important role for the efficiency of the drug delivery to the systemic circulation [ 40 , 41 ] Here, a reliable in silico screening model (OBioavail 1.1) was employed in OB value calculation of the constituents in XCHT and Heshouwu . This model was constructed based on 805 structurally diverse drugs and drug-like molecules.…”