Consequence of Solubility Alteration by Salt Effect on Dissolution Enhancement and Biological Response of a Solid Dispersion of an Experimental Antianginal Drug

Abstract

Improvement of dissolution rate of a poorly water-soluble experimental anti-anginal drug has been obtained by solid dispersion preparation. Its solubility decreased with rising chloride ion concentration and biological responses in dogs varied with the gastrointestinal administration site. A correlation seemed to exist between the apparent solubility and the heart rate activity.

Oral Absorption, Intestinal Metabolism and Human Oral Bioavailability

“…In fact, the rank order of dissolution rates of theophylline was closely correlated with the clinical blood exposure. This report led many additional studies that demonstrated the influence of the salt form on drug dissolution and the benefit of changing nonionized drug to salts (Nelson 1957;Nelson 1958;Berge et al 1977;Nang et al 1977;Chowhan 1978;Chen et al 2002;Hendriksen et al 2003;Huang and Tong 2004;Strickley 2004;Li et al 2005) …”