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Mar. Drugs 2017, 15(9), 279; doi:10.3390/md15090279

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

1
College of Pharmacy, Dankook University, Cheon-an 31116, Korea
2
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 41566, Korea
3
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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Abstract

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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MDPI and ACS Style

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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