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Mar. Drugs 2017, 15(9), 279;

Pharmacokinetics of Jaspine B and Enhancement of Intestinal Absorption of Jaspine B in the Presence of Bile Acid in Rats

College of Pharmacy, Dankook University, Cheon-an 31116, Korea
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 41566, Korea
College of Pharmacy, Ajou University, Suwon 16499, Korea
Author to whom correspondence should be addressed.
Received: 13 July 2017 / Revised: 13 August 2017 / Accepted: 30 August 2017 / Published: 1 September 2017
(This article belongs to the Special Issue Development and Application of Herbal Medicine from Marine Origin)
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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. View Full-Text
Keywords: Jaspine B; bile salts; intestinal permeability; bioavailability; metabolic instability Jaspine B; bile salts; intestinal permeability; bioavailability; metabolic instability

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Choi, M.-K.; Lee, J.; Nam, S.J.; Kang, Y.J.; Han, Y.; Choi, K.; Choi, Y.A.; Kwon, M.; Lee, D.; Song, I.-S. Pharmacokinetics of Jaspine B and Enhancement of Intestinal Absorption of Jaspine B in the Presence of Bile Acid in Rats. Mar. Drugs 2017, 15, 279.

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