Dissolution in a Neutral Aqueous Media of a New Strongly Low Water Solubility Active Pharmaceutical Ingredient
摘要
Water poorly soluble drugs often need higher dose in order to reach therapeutic concentrations in plasma after oral administration. Drug therapeutic effectiveness depends on the ability of the administration form to deliver the drug to its site of action at a rate and quantity sufficient to obtain the desired pharmacological response. Factors associated to the formulation may modify the dissolved amount and the dissolution rate, and, therefore, its bioavailability. Knowledge of the basic characteristics, both biopharmaceutical and physical-chemical, influences the choice and development of the final pharmaceutical form, including the excipients to be used. The main objective of the present work is the development of a formulation for dissolving in an aqueous media an API with strongly low water solubility. The study was performed for seven formulations choices at API concentrations of 1, 10 and 50 mg L−1. The mixtures choices g and h, formed by two surfactants, a polymer and a co-solvent, showed an excellent capacity to completely dissolve the API at concentration of 1 mg L−1. In addition, the API saturation concentration was determined. Likewise, it was observed the low stability of the API in dissolution.