Solubilizing properties of new surface-active agents, products of catalytic oxyethylation of cholic acid

Acta Pol Pharm. 2013 Nov-Dec;70(6):1065-77.

Abstract

Solubilizing properties of aqueous solutions of a series of surface-active agents, products of oxyethylation of cholic acid, were examined in the present study. The content of oxyethylated segments determined by means of the 1H NMR method enabled the verification of the molecular mass of surfactants along with the calculation of the structural hydrophilic-lipophilic balance (HLB), the solubility parameter delta1/2, and the required solubility level of balance HLB(R). Viscosimetric measurements enabled the calculation of the limiting viscosity number, the content-average molecular mass, the effective volume, the hydrodynamic radius of the surfactant micelle and their equilibrium adducts with rutin, diclofenac and loratadine (BCS Class II and III). By means of the spectrophotometric method (UV) the amount of the solubilized diclofenac, loratadine and rutin (rutoside) was determined in the equilibrium system (saturated solution) in the environment of aqueous solutions of cholic acid derivatives of n(TE) = 20-70. The obtained results serve as a basis for determining the solubilization mechanism of lipophilic therapeutic products and indirectly for estimating the influence of the above process on pharmaceutical as well as biological availability of a micellar adduct from model drug forms (Lindbladt lithogenolitic index).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Chemistry, Pharmaceutical
  • Cholic Acids / chemistry*
  • Diclofenac / chemistry
  • Hydrophobic and Hydrophilic Interactions
  • Loratadine / chemistry
  • Magnetic Resonance Spectroscopy
  • Micelles
  • Oxidation-Reduction
  • Particle Size
  • Rutin / chemistry
  • Solubility
  • Spectrophotometry, Ultraviolet
  • Surface-Active Agents / chemistry*
  • Technology, Pharmaceutical / methods
  • Viscosity

Substances

  • Cholic Acids
  • Micelles
  • Surface-Active Agents
  • Diclofenac
  • Rutin
  • Loratadine