Pharmaceutical development of a parenteral formulation of conivaptan hydrochloride.

Unlabelled: Conivaptan hydrochloride injection (Vaprisol®) was developed for the treatment of hyponatremia. Because the drug is very slightly soluble in water, pH control and cosolvency techniques were used to achieve the optimum concentration required for clinical trial material. Stability studies on retained samples of the clinical trial material for early-phase trials showed white visible particulates mainly in the headspace of the glass ampoule long after completion of the trials.

Effects of ursodeoxycholic acid on the pharmacokinetics and pharmacodynamics of intravenous and oral midazolam in healthy volunteers.

Animal and in vitro studies suggest that ursodeoxycholic acid (UDCA) can induce cytochrome P450 3A (CYP3A) expression and enhance its activities. On the other hand, Becquemont et al. demonstrated that UDCA had no influence on intestinal CYP3A activities.