Ionic Strength Dependency Analysis

Ionic Strength Dependency Analysis evaluates how the solubility and stability of a drug substance are influenced by the concentration of ions (e.g., salts, buffers) in a solution. This test is critical for optimizing formulations intended for physiological fluids (e.g., blood, gastrointestinal fluids) and ensuring compliance with USP <1151> and ICH Q6A guidelines.
Ionic strength quantifies the total concentration of ions in a solution and is calculated as:

Ionic strength calculation formula. (STEMart Original)

Ionic Strength Dependency Analysis measures how changes in Ionic Strength (via added salts, buffers, or counterions) affect:

  • Drug solubility: Salts can increase (salting-in) or decrease (salting-out) solubility.
  • Colloidal stability: Ionic strength impacts zeta potential and aggregation in nanosuspensions.
  • Protein conformation: High II may destabilize biologics via charge shielding or Hofmeister effects.

Illustration of effect of ionic strength on the solubility of a specific protein in NaCl solution. (STEMart Original)

Fig.1 Effect of ionic strength on the solubility of a specific protein in NaCl solution. (STEMart Original)

Key Test Parameters

  • Solubility vs. Ionic Strength: Measure solubility in NaCl, KCl, or buffer solutions across different ionic strengths.
  • Critical Coagulation Concentration (CCC): Determine the ionic strength at which colloids aggregate (via DLS or turbidity).
  • pH-Ionic Strength Interplay: Assess combined effects of pH and ionic strength on ionization and solubility.
  • Excipient Compatibility: Test common buffers for salting-out risks.

Measurement Technologies

Shake-Flask Method (USP <1176>)

  • Principle: Saturate drug in solutions of varying ionic strength, filter, and quantify dissolved API.
  • Results: Solubility vs. ionic strength curves.
    • High accuracy for thermodynamic solubility.
    • Compatible with HPLC/UV-Vis quantification.

Potentiometric Titration

  • Principle: Use ion-selective electrodes to measure activity coefficients and calculate II effects.
  • Results: Activity vs. ionic strength profiles.
    • Direct measurement of ion-drug interactions.
    • Automated systems (e.g., Sirius T3) enable high-throughput screening.

Dynamic Light Scattering (DLS)

  • Principle: Monitor particle size changes as ionic strength increases to detect aggregation.
  • Results: Hydrodynamic diameter and CCC values.
    • Real-time tracking of colloidal instability.

Zeta Potential Analysis

  • Principle: Measure surface charge (zeta potential) to predict electrostatic stabilization.
  • Results: Zeta potential vs. ionic strengths plots.
    • Identifies critical II thresholds for colloidal systems.

Partner With Us

  • Holistic Expertise: From ionic strength screening to formulation mitigation.
  • Advanced Tools: Sirius T3, Malvern Zetasizer, and HPLC-MS for ion-drug interaction studies.
  • Regulatory Alignment: Protocols pre-validated for FDA/EMA submissions.

For more information on our Ionic Strength Dependency Analysis service or to discuss your specific requirements, please contact us today.

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