التفاصيل البيبلوغرافية
| العنوان: |
Pharmacokinetics of Jaspine B and Enhancement of Intestinal Absorption of Jaspine B in the Presence of Bile Acid in Rats |
| المؤلفون: |
Min-Koo Choi, Jihoon Lee, So Jeong Nam, Yun Ju Kang, Youjin Han, Kwangik Choi, Young A. Choi, Mihwa Kwon, Dongjoo Lee, Im-Sook Song |
| المصدر: |
Marine Drugs, Vol 15, Iss 9, p 279 (2017) |
| بيانات النشر: |
MDPI AG, 2017. |
| سنة النشر: |
2017 |
| المجموعة: |
LCC:Biology (General) |
| مصطلحات موضوعية: |
Jaspine B, bile salts, intestinal permeability, bioavailability, metabolic instability, Biology (General), QH301-705.5 |
| الوصف: |
We aimed to investigate the pharmacokinetics and the underlying mechanisms of the intestinal absorption, distribution, metabolism, and excretion of Jaspine B in rats. The oral bioavailability of Jaspine B was 6.2%, but it decreased to 1.6% in bile-depleted rats and increased to 41.2% (normal) and 23.5% (bile-depleted) with taurocholate supplementation (60 mg/kg). Consistent with the increased absorption in the presence of bile salts, rat intestinal permeability of Jaspine B also increased in the presence of 10 mM taurocholate or 20% bile. Further studies demonstrated that the enhanced intestinal permeability with bile salts was due to increased lipophilicity and decreased membrane integrity. Jaspine B was designated as a highly tissue-distributed compound, because it showed large tissue to plasma ratios in the brain, kidney, heart, and spleen. Moreover, the recovery of Jaspine B from the feces and urine after an intravenous administration was about 6.3%, suggesting a substantial metabolism of Jaspine B. Consistent with this observation, 80% of the administered Jaspine B was degraded after 1 h incubation with rat liver microsomes. In conclusion, the facilitated intestinal permeability in the presence of bile salts could significantly increase the bioavailability of Jaspine B and could lead to the development of oral formulations of Jaspine B with bile salts. Moreover, the highly distributed features of Jaspine B in the brain, kidney, heart, and spleen should be carefully considered in the therapeutic effect and toxicity of this compound. |
| نوع الوثيقة: |
article |
| وصف الملف: |
electronic resource |
| اللغة: |
English |
| تدمد: |
1660-3397 |
| Relation: |
https://www.mdpi.com/1660-3397/15/9/279; https://doaj.org/toc/1660-3397 |
| DOI: |
10.3390/md15090279 |
| URL الوصول: |
https://doaj.org/article/5a86dac584ad4c04a44f77da7712e202 |
| رقم الانضمام: |
edsdoj.5a86dac584ad4c04a44f77da7712e202 |
| قاعدة البيانات: |
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