Because of the use of combinatorial chemistry there are new pharmaceutical active ingredients (APIs) that that cannot be used in commercial pharmaceutical products due to their low solubility in aqueous medium. Two of the most promising strategies to solve these problems are: 1) conversion of the APIs from crystalline to amorphous state and 2) the preparation of formulations in solid dispersions. In the first strategy, the enhanced solubility of the amorphous state is due that no additional energy is required to break the crystalline network during the dissolution process. In the case of dispersions, a decreased in the particle size of the API and an increment of porosity of the final product favors the solubility process. By synergizing these two strategies and forming a solid dispersion where both the excipient and the API are in amorphous state, the solubility process of poorly soluble drugs can be maximized. In our research group, we have developed a new method to prepare formulations in the form of solid vitreous dispersions, called two-phase amorphous-amorphous solid drug dispersion (AASD). The AASD consists of a sugar-based excipient that is an amorphous matrix for the API, which is dispersed in the form of micro and nano-clusters in an amorphous state. In the present work this methodology was applied to produce a new amorphous drug formulation in the form of solid nano-dispersion that has the potential to be used for the treatment of hypercholesterolemia. X-ray powder diffraction technique was used to carry out structural characterization to demonstrate the amorphous state of the dispersions, where the AASD-formulation showed stability in the amorphous state. The particle size of the API in the AASD was characterized through DLS, having an average size of particle of the API of 375nm. We are currently working in the evaluation of the solubility enhancement of the new formulation, which has already presented an increase compared to the crystalline commercial API.

Preparation and characterization of new solid micro and nanodispersions of amorphous drugs

256th National Meeting (2018)

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