The Rule of Unity for Human Intestinal Absorption 2: Application to Pharmaceutical Drugs that are Marketed as Salts

Title:The Rule of Unity for Human Intestinal Absorption 2: Application to Pharmaceutical Drugs that are Marketed as Salts

Volume: 12 Issue: 2

Author(s): Raj B. Patel, Brittany Admire and Samuel H. Yalkowsky

Affiliation:

Keywords: Absorption, oral dose, prediction, permeability, salts, solubility.

Abstract: The efficiency of the human intestinal absorption (HIA) of the 59 drugs which are marketed as salts is predicted using the rule of unity. Intrinsic aqueous solubilities and partition coefficients along with the drug dose are used to calculate modified absorption potential (MAP) values. These values are shown to be related to the fraction of the dose that is absorbed upon oral administration in humans (FA). It is shown that the MAP value can distinguish between drugs that are poorly absorbed (FA <0.5) and those that are well absorbed (FA ≥ 0.5). Inspection of the data as well as a receiver operative characteristic (ROC) plot shows that a single critical MAP value can be used for predicting efficient human absorption of drugs. This forms the basis of a simple rule of unity based solely on in vitro data for predicting whether or not a drug will be well absorbed at a given dose.

Cite this article as:

B. Patel Raj, Admire Brittany and H. Yalkowsky Samuel, The Rule of Unity for Human Intestinal Absorption 2: Application to Pharmaceutical Drugs that are Marketed as Salts, Current Drug Delivery 2015; 12 (2) . https://dx.doi.org/10.2174/1567201811666141022100320