| abstract |
A solid dispersion of tolvaptan and its method of preparation are described. 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. The solid dispersion may also comprise a water soluble polymer, such as polyvinylpyrrolidone, hydroxypropyl cellulose, hydroxyethyl cellulose or methyl cellulose. The weight ratio of tolvaptan: cross-linked polyvinylpyrrolidone: water soluble polymers is preferably 2: 1: 0.1. The solid dispersion exhibits good thermodynamic stability and solubility. The pharmaceutical compositions thereof have a better release rate and bioavailability. |