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Solubility

Solubility

Solution, Solubility, and Solubility Equilibrium
A solution is a homogeneous mixture composed of a solvent, the major component, and a solute, the minor component. The physical state of a solution—solid, liquid, or gas—is typically the same as that of the solvent. Solute concentrations are often described with qualitative terms such as dilute (of relatively low concentration) and concentrated (of relatively high concentration).
In a solution, the solute particles (molecules, atoms, and/or ions)...

Factors Affecting Solubility

Factors Affecting Solubility

Compared with pure water, the solubility of an ionic compound is less in aqueous solutions containing a common ion (one also produced by dissolution of the ionic compound). This is an example of a phenomenon known as the common ion effect, which is a consequence of the law of mass action that may be explained using Le Chȃtelier’s principle. Consider the dissolution of silver iodide:

Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH

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 in drug...

Solubility of Ionic Compounds

Solubility of Ionic Compounds

Solubility is the measure of the maximum amount of solute that can be dissolved in a given quantity of solvent at a given temperature and pressure. Solubility is usually measured in molarity (M) or moles per liter (mol/L). A compound is termed soluble if it dissolves in water.

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...

Bioavailability Enhancement: Drug Solubility Enhancement

Bioavailability Enhancement: Drug Solubility Enhancement

Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...

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In vitro Digestion of Emulsions in a Single Droplet via Multi Subphase Exchange of Simulated Gastrointestinal Fluids

In vitro Digestion of Emulsions in a Single Droplet via Multi Subphase Exchange of Simulated Gastrointestinal Fluids

Published on: November 18, 2022

What is modulating solubility in simulated intestinal fluids?

Giorgio Ottaviani¹, Daniel J Gosling, Celine Patissier

¹Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, Basel, Switzerland. giorgio.ottaviani@novartis.com

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences

|July 27, 2010

Summary

This summary is machine-generated.

Understanding compound solubility in simulated intestinal fluid (FaSSIF-V2) reveals key roles for ionization and lipophilicity. These factors, along with crystal packing, uniquely influence solubility compared to aqueous buffers, aiding formulation development.

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Area of Science:

Pharmaceutical Sciences
Physical Chemistry
Drug Delivery

Background:

Understanding drug solubility in gastrointestinal fluids is crucial for oral bioavailability.
Simulated intestinal fluid (FaSSIF-V2) mimics in vivo conditions, offering a relevant medium for solubility studies.
Factors like ionization, lipophilicity, and crystal packing are known to influence compound solubility.

Purpose of the Study:

To identify the key parameters governing the selective modulation of compound solubility in simulated intestinal fluids.
To compare solubility behavior in FaSSIF-V2 with aqueous buffers to understand medium-specific effects.
To provide insights for medicinal chemists and formulation scientists in drug development.

Main Methods:

Solubility assessment of 25 diverse reference compounds.
Measurement in simulated intestinal fluid (FaSSIF-V2).
Comparison with solubility in aqueous phosphate and maleate buffers.

Main Results:

Electrostatic interactions significantly influence the solubility of ionizable compounds (acids and bases) in FaSSIF-V2.
Ionized acids showed no solubility increase in FaSSIF-V2, potentially due to electrostatic repulsion.
Lipophilicity is critical for charged bases (logP>4 or logD(6.5)>1.9) and enhances solubility more than crystal packing for some compounds.
FaSSIF-V2 components improved solubility of basic compounds more than those limited by crystal packing.

Conclusions:

Ionization, lipophilicity, and crystal packing play distinct and important roles in controlling compound solubility in FaSSIF-V2.
Solubility behavior in FaSSIF-V2 differs significantly from aqueous buffers due to specific interactions.
This study offers valuable guidance for optimizing drug solubility and formulation strategies.