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05:08
Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
Published on: September 20, 2017
Salt formation to improve drug solubility.
1Science, Technology and Outsourcing Section, Novartis Pharmaceuticals Corporation, One Health Plaza, East Hanover, NJ 07936, USA. abu.serajuddin@novartis.com
Advanced Drug Delivery Reviews
|July 10, 2007
Summary
Drug salt formation enhances solubility and dissolution. Understanding physicochemical principles like pH, pKa, and intrinsic solubility (S0) is crucial for selecting optimal drug salt forms and ensuring effective solid dosage form development.
Area of Science:
- Pharmaceutical Chemistry
- Physical Chemistry
- Drug Development
Background:
- Salt formation is a primary strategy to improve drug solubility and dissolution rates.
- Physicochemical principles governing drug solubility are essential for pharmaceutical formulation.
Purpose of the Study:
- To present the physicochemical principles of drug salt solubility.
- To discuss the influence of pH-solubility profiles on salt formation and dissolution.
- To elaborate on factors affecting salt screening and selection for optimal drug development.
Main Methods:
- Discussion of physicochemical principles of salt solubility.
- Analysis of pH-solubility profiles for acidic and basic drugs.
- Consideration of non-ideality in salt solubility due to self-association.
Main Results:
- Key factors influencing salt formation and dissociation include intrinsic solubility (S0), pH, pKa, solubility product (Ksp), and pH of maximum solubility (pHmax).
- Interrelationships of these factors guide salt screening and selection.
- Factors affecting salt dissolution in various conditions, including reactive media and excess common ions, are detailed.
Conclusions:
- Optimal salt form selection relies on understanding the interplay of physicochemical properties.
- Knowledge of these principles aids in the development of effective solid dosage forms.
- Salt formation remains a critical method for enhancing drug solubility and dissolution characteristics.
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