Dec 24, 2005

Biorelevant dissolution media: aggregation of amphiphiles and solubility of estradiol

Journal of Pharmaceutical Sciences
David Ilardia-AranaAnette Müllertz

Abstract

Biorelevant dissolution media containing bile salt and lecithin at concentrations appropriate for fed and fasted state are useful when testing oral solid formulations of poorly water-soluble drugs. Dilution of amphiphile solutions affects the aggregation state of the amphiphiles because bile salt is partitioned between the aqueous phase and the aggregates. The aim of the investigation was to study the effect of dilution on the size distribution of aggregates and its effect on the solubilization capacity. Clear buffered solutions of four intestinal amphiphiles (sodium glycocholate, lecithin, monoolein, and oleic acid) and a combination of these were prepared at high bile salt concentration. Micelles in the glycocholate solutions decreased in size when diluted. The addition of insoluble amphiphiles led to bigger micelles with no clear correlation between size of the micelles and amphiphile concentration. Dilution of the two- and four component media caused enlargement of the mixed micelles and formation of vesicles. The solubility of estradiol in the buffer solution was increased with addition of the amphiphiles. A good correlation (R(2) = 0.987) was found between estradiol solubility and mass concentration of the amphiphiles. Th...Continue Reading

  • References6
  • Citations20
  • References6
  • Citations20

Citations

Mentioned in this Paper

Monoolein
Buffers
Bile Acid Measurement
Structure-Activity Relationship
Aggregation
Estradiol, (16 alpha,17 beta)-Isomer
Lecithinum, lecithin, Homeopathic preparation
Estradiol Measurement
Vesicle
Ampholytes

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