Preformulative and formulative studies on inclusion complexes between cyclodextrins and ursodeoxycholic acid

Three different methods (evaporation, spray-drying and lyophilisation) were used to prepare the complex between ursodeoxycholic acid and cyclodextrin (beta CD or HP beta CD). A small fraction of free drug not included into the cyclodextrin cavity along with the complex was noticed only for the complexes prepared using the evaporation method. Preformulative parameters of at least three batches of each complex were evaluated in view of the industrial preparation method selected. All the methods guarantee good reproducibility, but the surface area and the density of the complex powders were chiefly affected. Given the low-density value, the spray-dried and lyophilised complexes need to be transformed into granules before tablet preparation. The formulative parameters of the tablets were also evaluated. The disintegration test of both uncoated and coated tablets prepared with the granules obtained form the different beta CD complexes was not satisfactory. In spite of the long disintegration time, the ursodeoxycholic acid dissolution rate from the tablets was similar to that observed in the case of the inclusion complex powders.

Three different methods (evaporation, spray-drying and lyophilisation) were used to prepare the complex between ursodeoxycholic acid and cyclodextrin (βCD or HPβCD). A small fraction of free drug not included into the cyclodextrin cavity along with the complex was noticed only for the complexes prepared using the evaporation method. Preformulative parameters of at least three batches of each complex were evaluated in view of the industrial preparation method selected. All the methods guarantee good reproducibility, but the surface area and the density of the complex powders were chiefly affected. Given the low-density value, the spray-dried and lyophilised complexes need to be transformed into granules before tablet preparation. The formulative parameters of the tablets were also evaluated. The disintegration test of both uncoated and coated tablets prepared with the granules obtained from the different βCD complexes was not satisfactory. In spite of the long disintegration time, the ursodeoxycholic acid dissolution rate from the tablets was similar to that observed in the case of the inclusion complex powders