Examples of the application of cyclodextrin in formulation of oral drug preparations

Abstract

Fendiline hydrochloride [N-/1-phenylethyl/-3, 3-diphenylpropylamine. HCl] is a sparingly soluble and hardly absorbable coronary vasodilator. The fendiline base forms complex with β-cyclodextrin in a molar ratio of 1∶2. The enhanced solubility and dissolution rate of the complex resulted in a better bioavailability of the drug, which is represented by the elevated blood levels in rats. The β-cyclodextrin complex of PGI₂Me /3% active ingredient content/ was prepared. The freeze-dried powder can be stored at 0°C for 1.5 years, while the pure substance only for 4 months. The biological effectiveness of the complex agrees well with that of the active ingredient. After oral administration the cytoprotective effect of the free and complexed drug on indomethacin induced ulcers in rats was similar in their order of magnitude, however the prolonged effect of the complex was detected in this case too.