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KMID : 0043320160390060811
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Archives of Pharmacal Research
2016 Volume.39 No. 6 p.811 ~ p.824
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pH-dependent release of platycodin mitigates its gastrointestinal mucosa irritation after oral administration in rats
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Chen Qin
Yang Wen Wen
Shen Pan
Cao Qing Ri
Lee Beom-Jin
Cui Jing Hao
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Abstract
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The present study aimed to evaluate the gastrointestinal mucosa irritation of three platycodin formulations. Platycodin-loaded core pellets were prepared via extrusion?spheronization method and coated with Eudragit® L100-55 (L100) or Eudragit® S100 (S100) for pH-dependent release. The release of platycodin D from coated pellets exhibited pH dependent release profiles. The pharmacokinetic study in rats showed that Tmax of the coated pellets were prolonged as compared to that of un-coated pellets. The S100-coated pellets possess a lower Cmax and decreased AUC0?24h as compared to the L100-coated and uncoated pellets. Hematoxylin-eosin staining and nuclear factor Kappa B (NF-κB) measurement were carried out to observe the gastrointestinal mucosa irritations. The results revealed that the irritations of platycodin on the upper gastrointestinal mucosa are dose-dependent. However, no obvious irritation effect on the gastrointestinal tissues of rats was detected after oral administration of the coated pellets. In addition, the amount of NF-κB in the stomach of rats treated with the uncoated pellets was about fivefold higher as compared to that of the coated pellets. In summary, the L100-coated platycodin pellets exhibited higher oral bioavailability and less gastrointestinal mucosa irritations as compared to the other two formulations.
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KEYWORD
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Platycodin D, PH dependent release, Pharmacokinetics, Gastrointestinal mucosa, Irritation
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