| Preparation and rectal absorption of highly concentrated glycyrrhizin solution. | |
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MedLine Citation:
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PMID: 12951475 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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We developed a simple method for preparing a highly concentrated solution of glycyrrhizin monoammonium salt (GZ) at low viscosity with no surfactants nor organic solvents and investigated the absorption profile after rectal administration to rats. GZ (200 mg/ml) was dissolved in phosphate buffered solution, pH 7.0; over 350 mM concentration was maintained for the aqueous solution without gel-formation. When glycerin was used as a non-aqueous formulation, GZ did not form gel. Apparent permeability coefficients of GZ obtained from 350 mM phosphate buffered solution (pH 7.0) and glycerin solution through rat rectal mucosa estimated by in vitro parallel diffusion chamber technique were 0.686 x 10(-6) and 0.379 x 10(-6) cm/s, respectively. On the other hand, the area under plasma concentration-time curves of GZ in 400 mM phosphate buffer (pH 7.0) and glycerin formulations after rectal administration to the rat were significantly higher than that in polyethylene glycol 400/propylene glycol (55 : 5) formulation. Maximum plasma concentrations of these formulations were dependent on the apparent permeability coefficients of GZ. Increased absorption observed by phosphate buffered formulation accompanied no pronounced histological damage in mucosa. These results demonstrate that addition of a highly concentrated phosphate salts is effective not only for lowering the viscosity of a highly concentration of GZ solution, but also for improving the mucosal GZ absorption. |
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Authors:
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Kenjiro Koga; Susumu Kawashima; Nobuhito Shibata; Kanji Takada; Masahiro Murakami |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Biological & pharmaceutical bulletin Volume: 26 ISSN: 0918-6158 ISO Abbreviation: Biol. Pharm. Bull. Publication Date: 2003 Sep |
Date Detail:
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Created Date: 2003-09-02 Completed Date: 2004-04-09 Revised Date: 2008-11-21 |
Medline Journal Info:
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Nlm Unique ID: 9311984 Medline TA: Biol Pharm Bull Country: Japan |
Other Details:
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Languages: eng Pagination: 1299-305 Citation Subset: IM |
Affiliation:
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Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Hokuriku University, Kanazawa, Japan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Rectal Algorithms Animals Antiviral Agents / administration & dosage, chemistry, pharmacokinetics* Biological Availability Buffers Chemistry, Pharmaceutical Chemistry, Physical Gels Glycyrrhizic Acid / administration & dosage, chemistry, pharmacokinetics* Intestinal Absorption Intestine, Large / metabolism Male Pharmaceutical Solutions Physicochemical Phenomena Rats Rats, Wistar Rectum / metabolism* Solubility Temperature Thermodynamics |
| Chemical | |
Reg. No./Substance:
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0/Antiviral Agents; 0/Buffers; 0/Gels; 0/Pharmaceutical Solutions; 1405-86-3/Glycyrrhizic Acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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