Dissolution Rate of Cholesterol in Monooctanoin

Authors

  • Joseph B. Bogardus

    Corresponding author
    1. College of Pharmacy, University of Kentucky, Lexington, Kentucky 40536–0053
    • Joseph B. Bogardus, Ph.D., Associate Director, Pharmaceutical Product Development, Bristol-Myers Co., P. O. Box 4755, Syracuse, New York 13221–4755.
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Abstract

Monooctanoin is used clinically for dissolution of common bile duct cholesterol gallstones. A number of factors influencing the dissolution rate of cholesterol monohydrate in this solvent were investigated. Water increased cholesterol dissolution rate in a manner inconsistent with previous solubility measurements. Dissolution rate increased approximately 50% in the presence of 10 to 15% water in monooctanoin. Further studies on viscosity, the effect of polymers and temperature showed that the solvent viscosity had a dominating influence on dissolution rate. This was thought to be caused by the interaction of cholesterol with the solvent in the dissolving surface layer which caused a decrease in the diffusion coefficient (and dissolution rate) of cholesterol. Reducing viscosity and increasing temperature were identified as possible approaches for increasing cholesterol gallstone dissolution rate in monooctanoin.

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