Highly sensitive glycosylamine labelling of O-glycans using non-reductive β-elimination.

When developing biopharmaceuticals, glycans are the most important posttranslational protein modifications that must be addressed because they affect the between-protein interactions that maintain homeostasis. The glycan profile may be defined as a critical quality attribute of a biopharmaceutical. Comprehensive analysis of protein glycosylation must overcome challenges such as the release, labelling, separation and detection of O-glycans.

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.

Excipient hydrolysis and ester formation increase pH in a parenteral solution over aging.

Recently, the number of drug substances that are poorly water-soluble has increased dramatically. This makes improving solubility one of the most critical tasks in pharmaceutical development today. In this study, the physicochemical stability of an injectable solution of conivaptan hydrochloride salt was investigated.