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Absorption-enhancing effect of glycyrrhizin induced in the presence of capric acid.
Int J Pharm. 2005 Apr 27; 294(1-2):11-21.IJ

Abstract

The absorption-enhancing effect of the simultaneous administration of sodium caprate (Cap-Na) and dipotassium glycyrrhizinate (Grz-K) was investigated to clarify an effect of Grz-K. A combination of 0.1% (w/v) Cap-Na and 2% (w/v) Grz-K had a rapid and long-lasting absorption-enhancing activity in Caco-2 cell monolayers under conditions where Cap-Na and Grz-K showed a weak and no activity, respectively. The simultaneous treatment of a Caco-2 cell monolayer with Cap-Na and Grz-K showed no change in intracellular calcium ion level, although a major mechanism of absorption-enhancing effect for Cap-Na was elevation of intracellular calcium ion level. On the other hand, the simultaneous enhancing effect of Cap-Na and Grz-K was inhibited by H7, a PKC inhibitor. Possibly, Grz-K showed an absorption-enhancing effect via PKC cellular signaling pathway after penetration into cell according to increasing membrane permeability by Cap-Na. The absorption of sCT by the rat colon was enhanced by a combination of 0.1% (w/v) Cap-Na and 2% (w/v) Grz-K, and its effect continued even 9h after the onset of the experiment. Furthermore, the simultaneous treatment of 0.1% (w/v) Cap-Na and 2% (w/v) Grz-K showed a negligible histological changes to the colon mucosal membrane and a negligible toxicity on Caco-2 cell monolayer. A combination of Cap-Na and Grz-K shows a synergistic absorption-enhancing effect with little mucosal injury, which is applicable to colon-specific delivery.

Authors+Show Affiliations

Graduate School of Pharmaceutical Sciences, Kumamoto University, 5-1 Oe-honmachi, Kumamoto 862-0973, Japan. iteruko@gpo.kumamoto-u.ac.jpNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

15814227

Citation

Imai, Teruko, et al. "Absorption-enhancing Effect of Glycyrrhizin Induced in the Presence of Capric Acid." International Journal of Pharmaceutics, vol. 294, no. 1-2, 2005, pp. 11-21.
Imai T, Sakai M, Ohtake H, et al. Absorption-enhancing effect of glycyrrhizin induced in the presence of capric acid. Int J Pharm. 2005;294(1-2):11-21.
Imai, T., Sakai, M., Ohtake, H., Azuma, H., & Otagiri, M. (2005). Absorption-enhancing effect of glycyrrhizin induced in the presence of capric acid. International Journal of Pharmaceutics, 294(1-2), 11-21.
Imai T, et al. Absorption-enhancing Effect of Glycyrrhizin Induced in the Presence of Capric Acid. Int J Pharm. 2005 Apr 27;294(1-2):11-21. PubMed PMID: 15814227.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Absorption-enhancing effect of glycyrrhizin induced in the presence of capric acid. AU - Imai,Teruko, AU - Sakai,Michinori, AU - Ohtake,Hiroshi, AU - Azuma,Hidekazu, AU - Otagiri,Masaki, PY - 2004/07/25/received PY - 2004/12/08/revised PY - 2004/12/08/accepted PY - 2005/4/9/pubmed PY - 2005/8/19/medline PY - 2005/4/9/entrez SP - 11 EP - 21 JF - International journal of pharmaceutics JO - Int J Pharm VL - 294 IS - 1-2 N2 - The absorption-enhancing effect of the simultaneous administration of sodium caprate (Cap-Na) and dipotassium glycyrrhizinate (Grz-K) was investigated to clarify an effect of Grz-K. A combination of 0.1% (w/v) Cap-Na and 2% (w/v) Grz-K had a rapid and long-lasting absorption-enhancing activity in Caco-2 cell monolayers under conditions where Cap-Na and Grz-K showed a weak and no activity, respectively. The simultaneous treatment of a Caco-2 cell monolayer with Cap-Na and Grz-K showed no change in intracellular calcium ion level, although a major mechanism of absorption-enhancing effect for Cap-Na was elevation of intracellular calcium ion level. On the other hand, the simultaneous enhancing effect of Cap-Na and Grz-K was inhibited by H7, a PKC inhibitor. Possibly, Grz-K showed an absorption-enhancing effect via PKC cellular signaling pathway after penetration into cell according to increasing membrane permeability by Cap-Na. The absorption of sCT by the rat colon was enhanced by a combination of 0.1% (w/v) Cap-Na and 2% (w/v) Grz-K, and its effect continued even 9h after the onset of the experiment. Furthermore, the simultaneous treatment of 0.1% (w/v) Cap-Na and 2% (w/v) Grz-K showed a negligible histological changes to the colon mucosal membrane and a negligible toxicity on Caco-2 cell monolayer. A combination of Cap-Na and Grz-K shows a synergistic absorption-enhancing effect with little mucosal injury, which is applicable to colon-specific delivery. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/15814227/Absorption_enhancing_effect_of_glycyrrhizin_induced_in_the_presence_of_capric_acid_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(05)00081-5 DB - PRIME DP - Unbound Medicine ER -