Pharmaceutical Research

, Volume 11, Issue 10, pp 1385–1390

Formulation and Intestinal Absorption Enhancement Evaluation of Water-in-Oil Microemulsions Incorporating Medium-Chain Glycerides

Authors

  • Panayiotis P. Constantinides
    • Department of Drug Delivery, Pharmaceutical TechnologiesSmithKline Beecham Pharmaceuticals
  • Jean-Paul Scalart
    • School of PharmacyUniversity of Rennes
  • Cindy Lancaster
    • Department of Drug Delivery, Pharmaceutical TechnologiesSmithKline Beecham Pharmaceuticals
  • Joseph Marcello
    • Department of Drug Delivery, Pharmaceutical TechnologiesSmithKline Beecham Pharmaceuticals
  • Gary Marks
    • Department of Drug Delivery, Pharmaceutical TechnologiesSmithKline Beecham Pharmaceuticals
  • Harma Ellens
    • Department of Drug Delivery, Pharmaceutical TechnologiesSmithKline Beecham Pharmaceuticals
  • Philip L. Smith
    • Department of Drug Delivery, Pharmaceutical TechnologiesSmithKline Beecham Pharmaceuticals
Article

DOI: 10.1023/A:1018927402875

Cite this article as:
Constantinides, P.P., Scalart, J., Lancaster, C. et al. Pharm Res (1994) 11: 1385. doi:10.1023/A:1018927402875

Abstract

We developed self-emulsifying water-in-oil (w/o) microemulsions incorporating medium-chain glycerides and measured their conductance, viscosity, refractive index and particle size. Formulation of Calcein (a water-soluble marker molecule, MW = 623), or SK&F 106760 (a water-soluble RGD peptide, MW = 634) in a w/o microemulsion having a composition of Captex 355/Capmul MCM/Tween 80/Aqueous (65/22/10/3, % w/w), resulted in significant bioavailabil-ity enhancement in rats relative to their aqueous formulations. Upon intraduodenal administration the bioavailability was enhanced from 2% for Calcein in isotonic Tris, pH 7.4 to 45% in the microemulsion and from 0.5% for SK&F 106760 in physiological saline to 27% in the microemulsion formulation. The microemulsion did not induce gross changes in GI mucosa at a dosing volume of 3.3 ml/kg. These results suggest that water-in-oil microemulsion systems may be utilized for enhancement of intestinal drug absorption.

water-in-oil microemulsionsmedium-chain glyceridesenhancerintestinal absorptionfibrinogen receptor antagonist

Copyright information

© Plenum Publishing Corporation 1994