Using of Hansen solubility parameters as a prescreening method in the development of dosage form formulations

T. Ye Kolisnyk, O. A. Ruban, V. V. Mohylyuk

Research output: Contribution to journalArticlepeer-review

Abstract

Introduction. Hansen solubility parameters (δd, δp, δh) allow predicting the likeliness for solubility of pharmaceutical ingredients in each other, and, therefore, scientifically narrowing the range of objects and the total scope of experimental research. One of the ways for determining δd, δp, δh is the calculation method of group contributions: all three parameters are calculated based on the contributions to the corresponding intermolecular interactions of the structural groups composing the molecule. The closer the solubility parameters are for two substances, the more likely they are soluble in each other. The purpose of the study is the comparison of the predicted solubility of medicinal substances according to the calculated Hansen solubility parameters with previously published experimental data to illustrate the possibilities of using the method as prescreening in the formulation development of dosage forms. Materials and methods. Hansen solubility parameters were determined by the group contribution method according to Van Krevelen and Hoftizer using the molar volumes of the corresponding structural groups according to Fedors for the following active pharmaceutical ingredients (APIs) and excipients: nimesulide, meloxicam, and glycerol, ethylene glycol, propylene glycol, polyethylene oxide (PEO) 400. The results of the study. According to the calculations, the best solvent for both nimesulide and meloxicam is PEO 400. Using the criterion of Δδ ≤ 5 MPa0.5, nimesulide is likely soluble in PEO 400 only, while meloxicam is likely insoluble in either solvent. For each of the listed APIs, the Δδ ranking coincides with the experimental range of solubility in the same solvents. Was noticed, that among of the selected excipients based on the calculated data, PEO 400 is the closest to both APIs in terms of its molecular contribution to the energy of hydrogen bonds. Conclusions. Hansen solubility parameters determined by the calculation method of group contributions according to Van Krevelen and Hoftizer, allow to do the scientifically based selection of promising excipients at the stage of planning research on the formulation development of various dosage forms.

Original languageEnglish
Pages (from-to)128-133
JournalUkrains'kij Zurnal Vijskovoi Medicini
Volume3
Issue number4
DOIs
Publication statusPublished - 30 Dec 2022
Externally publishedYes

Keywords*

  • Hansen solubility parameters
  • meloxicam
  • method of group contributions
  • nimesulide
  • solubility

Field of Science*

  • 3.1 Basic medicine

Publication Type*

  • 1.1. Scientific article indexed in Web of Science and/or Scopus database

Fingerprint

Dive into the research topics of 'Using of Hansen solubility parameters as a prescreening method in the development of dosage form formulations'. Together they form a unique fingerprint.

Cite this