Mejoramiento de la Solubilidad Acuosa de la fracción alcaloidea de Banisteriopsis Caapi (ayahuasca), mediante el desarrollo de dispersiones sólidas in vitro, utilizando tres tipos de polímeros Hidrofílicos

Abstract

The aqueous solubility characteristics of the alkaloid fraction of Banisteriopsis caapi (Ayahuasca) were improved by obtaining an optimized system of solid dispersions in vitro, using different types of hydrophilic polymers, in order to improve its bioavailability characteristics; research developed in the laboratory of Natural Products Phytochemistry, School of Biochemistry and Pharmacy of the Polytechnic School of Chimborazo. At laboratory scale the alkaloid fraction of Banisteriopsis caapi (Ayahuasca) was obtained the beta-carbolinic alkaloid harmine, being identified and isolated from the plant Banisteriopsis caapi, against the reference standard Harmine 98% purity (BATCH CPC20140312). Its biopharmaceutical characteristics were determined by means of aqueous solubility, permeability, solid state properties and dissolution tests, resulting in low solubility and high permeability, which allowed placing the TA expressed as harmine within the Biopharmaceutical Class II classification. Fifteen solid dispersions of the alkaloid fraction of Banisteriopsis caapi plus the hydrophilic polymers were developed and when evaluating their biopharmaceutical characteristics in vitro, a DS with a higher solubility than that of the pure active principle and the other DSs was obtained. Through the application of solid dispersions, a decrease in particle size was obtained, going from crystals to amorphous crystals with greater wettability, characteristics that allowed improving its solubility and dissolution profile and therefore improving its bioavailability. The application of solid dispersions in pharmaceutical technology shows an efficient result. Therefore, it is recommended to apply it to improve other active principles with poorly soluble characteristics, as well as to evaluate the pharmacological activity of the alkaloid fraction of Banisteriopsis caapi (Ayahuasca) and the best DS since it possesses pharmacological properties that could help to minimize neurodegenerative disorders.