Dr Gabriela Ruphuy Chan, University of Chemistry and Technology Prague; Prof. František Stěpánek, University of Chemistry and Technology Prague City*: Prague
University of Chemistry and Technology Prague
Poor solubility of drugs and their associated low dissolution rate in the aqueous gastrointestinal fluids is one of the most frequent causes of low bioavailability, mainly in the case of oral dosage forms, which is the most commonly employed and convenient route of administration. Given that about 90% of drugs in the discovery pipeline and over 40% with market approval are insoluble or poorly soluble in water, the pharmaceutical industry is focusing efforts in the development of strategies to improve the solubility of drugs in water.
The invention relates to the formulation of composites comprised of yeast-derived β-glucan particles (GPs) and water-insoluble or poorly water-soluble drugs. The composites can exhibit different crystallinity degrees depending on the formulation and, consequently, dissolution kinetics can be controlled. Yeast-derived β-glucan particles are used as carriers for the encapsulation and amorphization of insoluble or poorly-water soluble drugs; amorphous formulations exhibiting faster dissolution rates, and consequently, enhanced drug bioavailability. The invention also relates to the method of preparation of the composites by spray drying, and the use thereof.
The presented technology is targeted at pharmaceutical companies wanting to develop new drug forms with controlled dissolution kinetics and/or improved flowability and dispersibility properties. The invention is also targeted at food companies wanting to incorporate insoluble active ingredients into food products, e.g. vitamins or natural colorants such as curcumin.
The encapsulation method has been fully developed. The produced composites were characterized in terms of crystallinity, dissolution kinetics, flowability, and dispersibility. Pharmacokinetic studies are planned.
will be applied for soon