The invention relates to a method of preparation of a soluble formulation of water-insoluble pentacyclic and tetracyclic terpenoids wherein the water-insoluble terpenoid having a free carboxylic, hydroxy or amino functional group is derivatized. The object of this invention is further a soluble formulation containing an inclusion complex of the derivatized terpenoid with cyclodextrin and optionally water and pharmaceutically acceptable auxiliary substances.