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Спутники
РН
SpaceX
Роскосмос
NASA
СпутникиРНSpaceXРоскосмосNASABackground. The poor solubility of active pharmaceutical ingredients in aqueous media poses a serious challenge to drug development due to their low absolute oral bioavailability.Objective − development of a self-emulsifying drug delivery system (SEDDS) of adamantylbromophenylamine in the form of a pre-emulsion concentrate.Materials and methods. To develop model formulations of adamantylbromophenylamine SEDDS pre-emulsion concentrate, excipients including oils, emulsifiers (surfactants), and cosolvents were used. A (pseudo)ternary phase diagram was constructed to optimize the quantitative ratio of the model component composition of the SEDDS. The selected model formulations of the SEDDS were evaluated for their emulsification ability. A series of stability tests were also conducted for the model formulations of the SEDDS, including stability at various pH levels and dilution volumes, stability under six cycles of heating to 45±0,5 °C and cooling to 4 °C, and four cycles of freezing to −20±0,5 °C and thawing.Results. During the study, solubilization of adamantylbromophenylamine in purified water using the SEDDS approach was achieved. The composition of liquid SEDDS adamantylbromophenylamine in the form of a pre-emulsion concentrate has been developed and optimized. It was found that the liquid SESD of adamantylbromophenylamine of the final composition is resistant to various pH of the medium and dilution volumes and remains stable after six cycles of heating to 45±0.5 °C − cooling to 4±0.5 °C and four cycles of freezing to −20±0.5 °C − thawing.Conclusions. The composition of liquid SEDDS adamantylbromophenylamine in the form of a pre-emulsion concentrate has been developed: API: adamantylbromophenylamine − 10.0 mg; BB: Cremophor® EL − 135.0 mg; Labrafac™ PG − 15.0 mg. Based on the results of the study of the emulsification ability and stability of the developed composition, it was concluded that the further development of the composition of an oral medicinal product based on SEDDS adamantylbromophenylamine is promising.
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