Solubilization of bromhexine hydrochloride in aqueous lecithin dispersions. Physicochemical characterization of interactions between drug and carrier

Pharmazie. 2001 Sep;56(9):734-7.

Abstract

In aqueous systems bromhexine hydrochloride (Br-HCl) has a poor solubility (4.54 mg/g) and displays no amphiphilic character e.g. self association. Therefore the drug is molecularly dispersed in water until the solubility product of Br-HCl is exceeded. Solubilization of Br-HCl is linearly increased on addition of lecithin; calculations show that 10 mg Phospholipon 90G (P 90G) enable solubilization of additional 1.25 mg Br-HCl after the solubility product of Br-HCl has been exceeded. This means that four to five phospholipid molecules are needed for the solubilization of one drug molecule. Ternary systems with P 90G concentrations up to 20% have a lamellar microstructure. The systems are multilamellar vesicle dispersions as polarisation microscopy, transmission electron microscopy and small-angle X-ray diffractometry suggest. Furthermore, Br-HCl solubilization leads to a significant reduction of the interlamellar distance d and increases the elastic properties of the systems. 31P NMR data provide evidence that Br-HCl is solubilized within the lipophilic part of the phospholipid bilayer.

MeSH terms

  • Bromhexine / chemistry*
  • Chemical Phenomena
  • Chemistry, Physical
  • Chromatography, High Pressure Liquid
  • Colloids
  • Drug Carriers
  • Emulsions
  • Expectorants / chemistry*
  • Magnetic Resonance Spectroscopy
  • Microscopy, Electron, Scanning Transmission
  • Microscopy, Polarization
  • Particle Size
  • Phosphatidylcholines / chemistry*
  • Photons
  • Rheology
  • Surface Tension
  • Water
  • X-Ray Diffraction

Substances

  • Colloids
  • Drug Carriers
  • Emulsions
  • Expectorants
  • Phosphatidylcholines
  • phospholipon 90G
  • Water
  • Bromhexine