Predictive Potential of Acido-Basic Properties, Solubility and Food on Bioequivalence Study Outcome: Analysis of 128

Dejan Krajcar1,2, Rebeka Jereb3, Igor Legen3

  • 1Lek Pharmaceuticals d.d., A Sandoz Company, Verovskova 57, 1526, Ljubljana, Slovenia. dejan.krajcar@sandoz.com.

Drugs in R&D
|June 10, 2023
PubMed
Abstract

Related Concept Videos

Bioequivalence: Overview01:16

Bioequivalence: Overview

Pharmaceutical equivalents, by definition, are drug products with the same active ingredient in the same quantities, encapsulated in identical dosage forms, and intended for the same administration routes. These pharmaceutical equivalents are deemed bioequivalent if the bioavailability of the active entity in the drug preparations is similar. Moreover, pharmaceutical equivalents demonstrating bioequivalence are also regarded as therapeutically equivalent. This means that when used as directed,...
1.1K
Titration of a Weak Acid with a Weak Base01:08

Titration of a Weak Acid with a Weak Base

Weak acids and bases do not undergo dissociation completely, and titrations between these two are rarely studied. When such studies are performed, say, for the titration of a weak acid with a weak base, the titration curve plots the change in pH as a function of the volume of base added. Take the titration of acetic acid with ammonia, for instance. During the titration, these two species form ammonium acetate and water, but the pH change is slow and gradual.
As a result, there is no simple...
3.0K
Solution Composition During Acid/Base Titrations01:17

Solution Composition During Acid/Base Titrations

The titration of a weak acid with a strong base results in the formation of water and the conjugate base of the acid. For instance, titrating acetic acid with sodium hydroxide leads to the formation of water and sodium acetate. A solution of acetic acid and sodium acetate constitutes a buffer whose relative concentration at different stages of the titration is indicated by the α values, which represent percentages of the weak acid and its conjugate base.
The α0 and α1 values...
614
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH01:21

Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH

Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
1.6K
Factors Influencing Drug Absorption: Physicochemical Parameters01:22

Factors Influencing Drug Absorption: Physicochemical Parameters

The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
330
Titration in Nonaqueous Solvents01:16

Titration in Nonaqueous Solvents

Most acid-base titrations are performed in an aqueous medium. In aqueous titrations, water competes with weaker acids or bases for proton donation or acceptance, leading to ambiguous endpoints in the titration curve. Water also affects the partial ionization of weak acids or bases. For example, water accepts a proton from acetic acid to form hydronium and acetate ions. The hydronium ion formed is a stronger acid than acetic acid, and the acetate ion is a stronger base than water. As a result,...
883