Rheological and solid-state NMR assessments of copovidone/clotrimazole model solid dispersions.

This study aims to assess several model solid dispersions by using dynamic oscillatory rheology, solid-state NMR and other solid phase characterization techniques, and correlate their viscoelastic responses with processing methods and microstructures. A model active pharmaceutical ingredient (API), clotrimazole, was compounded with copovidone to form solid dispersions via various techniques with different mixing capabilities. Physicochemical characterizations of the resulting solid dispersions demonstrated that simple physical mixing led to a poorly mixed blend manifested by existence of large API crystalline content and heterogeneous distribution.

Effect of added alkalizer and surfactant on dissolution and absorption of the potassium salt of a weakly basic poorly water-soluble drug.

Telcagepant potassium salt (MK-0974) is an oral calcitonin gene-related peptide receptor inhibitor investigated for the treatment of acute migraine. Under gastric pH conditions, the salt rapidly gels, then converts to an insoluble neutral form that creates an impervious shell on the tablet surface, resulting in a slow and variable release dissolution rate and poor bioavailability. Early attempts to develop a solid dosage form, including solid dispersion and nanosuspension formulations, resulted in low exposures in preclinical studies.