Development of soft dosage forms of pyrimidine derivatives based on carbopols

Abstract

In the process of improving the technology for obtaining and expanding the range of dosage forms of known pharmaceutical substances, an important aspect is to reduce side effects and ensure ease of use. At the same time, medicines should provide the most important properties of pharmaceutical substances, namely, their most rapid and complete release from the base of the dosage form and penetration into the target organ, which should serve as factors in justifying formulations and technologies of effective and safe medicines [3, 4]. Due to the lesser manifestation of side effects and ease of use, soft dosage forms (gels, ointments) are among the most demanded dosage forms on the modern pharmaceutical market. The trend towards replacing hydrophobic bases in soft dosage forms with hydrophilic ones has been traced in pharmacy for quite a long time, since gels provide higher efficiency in application due to better penetration of pharmaceutical substances through the skin barrier relative to hydrophobic ointments. The presence of a polymer-gelling agent in gels determines not only the rheological properties of medicines, but also allows a highly dispersed solid phase of a pharmaceutical substance to be included in the network structure of a polymer and to maintain the dispersion of a pharmaceutical substance poorly soluble in water during storage. Methyluracil, also known as dioxomethyltetrahydropyrimidine, is a derivative of pyrimidine, a structural element of nucleic acids and is used in the treatment of diseases of various etiologies, mainly to improve the course of regeneration in damaged tissues. A significant disadvantage of methyluracil is its low solubility in water, which significantly affects the degree of release of the pharmaceutical substance from the base of the drug [1]. Due to the lack of methyluracil gels on the pharmaceutical market, their development using acrylic acid derivatives in order to improve the biopharmaceutical properties of a pharmaceutical substance is an important problem in pharmacy.