Improving Relative Bioavailability of Oral Imidazolidinedione by Reducing Particle Size Using Homogenization and Ultra-Sonication
| العنوان: | Improving Relative Bioavailability of Oral Imidazolidinedione by Reducing Particle Size Using Homogenization and Ultra-Sonication |
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| المؤلفون: | Jing Zhang, Brittney Potter, Chad C. Black, Samantha O. Aylor, Lisa Xie, Chau Vuong, Jason C. Sousa, Qigui Li, Qiang Zeng |
| المصدر: | Military Medicine. 184:106-113 |
| بيانات النشر: | Oxford University Press (OUP), 2019. |
| سنة النشر: | 2019 |
| مصطلحات موضوعية: | Chromatography, Chemistry, Sonication, Public Health, Environmental and Occupational Health, Biological Availability, 02 engineering and technology, General Medicine, Imidazolidines, 021001 nanoscience & nanotechnology, 030226 pharmacology & pharmacy, Homogenization (chemistry), Bioavailability, 03 medical and health sciences, 0302 clinical medicine, Pharmacokinetics, Particle diameter, Humans, Homogenizer, Particle size, Particle Size, Microparticle, 0210 nano-technology |
| الوصف: | Particle size is an important determinant of gastrointestinal absorption of compounds administrated orally. The present study evaluates the effect of a reduction in particle size assessed by homogenization, sonication, and homogenization plus sonication on the bioavailability of imidazolidinedione (IZ), an antimalarial compound with known causal prophylactic activity and radical cure of relapsing malaria. Formulations were administrated intragastrically to mice, and blood samples were collected for LC-MS/MS analysis. The homogenization method manually decreased particle size with minimal variance, resulting in a mean particle diameter of 42.22 μm, whereas the probe sonication method evenly distributed pulses of sound to break apart particles, resulting in a mean diameter of 1.50 μm. Homogenization plus sonication resulted in a mean particle diameter of 1.44 μm, which was similar to that of the sonication method alone. The compound suspensions did not show a significant difference in mean particle size between the different vehicles. The sonically engineered microparticle delivers high sonic energy to the suspension leads to faster breakdown and stabilizing of the micronized particles when compared with homogenizer. The bioavailability of the small particle IZ formulation was 100%, compared to the 55.79% relative bioavailability of IZ with larger particle size. These initial data clearly show that a reduction in particle size of orally administered IZ with probe sonication could significantly increase bioavailability in rodent animals that is affected by a high first-pass effect. |
| تدمد: | 1930-613X 0026-4075 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a1d1c80eb4a317145e10ade4ad051157 https://doi.org/10.1093/milmed/usy368 |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....a1d1c80eb4a317145e10ade4ad051157 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 1930613X 00264075 |
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