Biorelevant dissolution testing of St John's wort products.

Abstract

In contrast to chemically defined drugs, most herbal medicinal products (HMPs) are poorly characterized in terms of their pharmaceutical properties. In many cases it is assumed that the plant extract as a whole is the active moiety, since it is often difficult to identify the individual components responsible for the pharmacological activity and even more difficult to assess synergies among the various components. However, where the active components have been identified, it should be possible to compare products with respect not only to content uniformity but also to their biopharmaceutical properties. The aim of this study was to investigate and compare the dissolution characteristics of several St John's wort products under biorelevant conditions. Components of St John's wort known, or suspected, to play a role in its antidepressant activity include phloroglucines, naphthodianthrones and the flavonoids. Since these groups have a broad spectrum of polarity and solubility, dissolution was studied for representative compounds from each group. Although the labelling indicates that several of the products studied should be pharmaceutically equivalent, dissolution under biorelevant conditions revealed that they have quite different release profiles and cannot be considered switchable. It was concluded that biorelevant dissolution testing can be a powerful tool for comparing HMPs as well as synthetically produced drug products.