Разработка эмульсионной лекарственной формы 2,6-диизоборнил-4-метилфенола: скрининг компонентов, физико-химические свойства и апробация in vivo
Dibornol (2,6-diisobornyl-4-methylphenol, IBP) is a semi-synthetic phenolic antioxidant with cardio-, neuro-, and retinoprotective properties; therefore, it has attracted considerable attention in recent years in Russia. Nevertheless, the drug had low bioavailability after oral administration due to...
| Published in: | Перспективы развития фундаментальных наук. Т. 2 : сборник научных трудов XX Международной конференции студентов, аспирантов и молодых ученых, 25–28 апреля 2023 г. Т. 2 : Химия. С. 124-126 |
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| Main Author: | |
| Format: | Book Chapter |
| Language: | Russian |
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| Online Access: | http://vital.lib.tsu.ru/vital/access/manager/Repository/koha:001146742 |
| Summary: | Dibornol (2,6-diisobornyl-4-methylphenol, IBP) is a semi-synthetic phenolic antioxidant with cardio-, neuro-, and retinoprotective properties; therefore, it has attracted considerable attention in recent years in Russia. Nevertheless, the drug had low bioavailability after oral administration due to its insufficient gastric residence time, low permeability, and water-solubility (logP = 8.14). It is well known that emulsions are considered as one of the most promising encapsulation and delivery systems for such compounds. Hence, the aim of the present study was to develop an oil-in-water microemulsion that contained lauryl alcohol ethoxylate 24 moles as a surfactant and ethyl alcohol as a co-surfactant to enhance the oral absorption of IBP. The prepared microemulsion was evaluated for its particle size, viscosity, and stability (thermo- and long-term stability, stability after dilution with simulated gastric fluid). The obtained microemulsion had a particle size of <100 nm. Stability testing indicated that this microemulsion was stable at room temperature and at 37°C for at least 31 days. The results of pharmacokinetic studies showed that Cmax and AUC0–72 parameters increased by 2 and 2.7 times for microemulsion compared to the oil dosage form. As a result, the IBP relative bioavailability also increased by 273%. Thus, in this study, the prospects of using microemulsion to obtain IBP dosage form with enhanced oral bioavailability were demonstrated. |
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| Bibliography: | Библиогр.: 3 назв. |
| ISBN: | 9785438711384 9785438711360 |