| abstract |
Tolvaptan solid dispersions and methods of making the same are disclosed. The solid dispersion comprises tolvaptan and cross-linked polyvinylpyrrolidone in a weight ratio of 1: 0.05-20, preferably 1: 0.1-10, more preferably 2: 1. Solid dispersions may also include water-soluble polymers such as polyvinylpyrrolidone, hydroxypropylcellulose, hydroxyethylcellulose or methylcellulose. The weight ratio of tolvaptan: crosslinked polyvinylpyrrolidone: water soluble polymer is preferably 2: 1: 0.1. Solid dispersions show good thermodynamic stability and solubility. Its pharmaceutical compositions have improved release rates and bioavailability. |