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  • Improvement of physicochemical properties of N-4472. Part II: characterization of N-4472 microemulsion and the enhanced oral absorption.

Improvement of physicochemical properties of N-4472. Part II: characterization of N-4472 microemulsion and the enhanced oral absorption.

International journal of pharmaceutics (2002-09-25)
K Itoh, S Matsui, Y Tozuka, T Oguchi, K Yamamoto
ZUSAMMENFASSUNG

The optimized formulation of N-4472, N-[2-(3,5-di-tert-butyl-4-hydroxyphenethyl)-4,6-difluorophenyl]-N'-[4-(N-benzylpiperidyl)] urea, which was a poorly water-soluble drug, was developed by utilizing the complexation between N-4472 and L-ascorbic acid (VC). It was found that the formulation with Gelucire((R)) 44/14, HCO-60((R)) and sodium dodecyl sulfate provided a self-microemulsifying system consisting of fine droplets in approximately 18 nm size with a narrow distribution. 1H-NMR spectroscopic study indicated that the N-4472/VC complex was molecularly incorporated into surfactant molecular assembly in the microemulsion droplets. It was found that the N-4472 microemulsion was stable at the pH range from 2.0 to 7.0, suggesting the stability in the gastrointestinal tract. When the microemulsion containing N-4472/VC complex was orally administrated in rats, high AUC value of N-4472 (2 to 4-fold) was observed in comparison with the aqueous solution containing N-4472/VC complex.

MATERIALIEN
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Marke
Produktbeschreibung

Sigma-Aldrich
Rizinusöl, hydriert, ethoxyliert
Sigma-Aldrich
Rizinusöl, ethoxyliert, pH range 6.0-8.0
Sigma-Aldrich
Rizinusöl, ethoxyliert