Stabilization mechanism of clarithromycin tablets under gastric pH condition
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- Fujiki Sadahiro
- School of Pharmaceutical Sciences, University of Shizuoka
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- Iwao Yasunori
- School of Pharmaceutical Sciences, University of Shizuoka
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- Kobayashi Mika
- School of Pharmaceutical Sciences, University of Shizuoka
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- Miyagishima Atsuo
- School of Pharmaceutical Sciences, University of Shizuoka
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- Itai Shigeru
- School of Pharmaceutical Sciences, University of Shizuoka
書誌事項
- タイトル別名
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- Stabilization Mechanism of Clarithromycin Tablets under Gastric pH Conditions
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It has been reported that tablets of clarithromycin (CAM), a 14-membered macrolide antibiotic, are especially stable under low pH conditions such as in gastric fluid, and showed excellent antibacterial efficiency even though CAM molecules themselves are rapidly decomposed. Therefore, we aimed to clarify the stabilization mechanism of CAM tablets under low pH conditions. From the results of stability and dissolution tests, the optimal decomposition rate constant (Kdec) and dissolution rate constant (Kdis) at various pH values were calculated by curve-fitting to consecutive reactions. Consequently, log(Kdec) increased as pH decreased. On the other hand, log(Kdis) increased as pH decreased from 3.0 to 1.5, but decreased as pH decreased from 1.5 to 1.0. In addition, the disintegration time of commercially available tablets at pH 1.0 and 1.2 was found to be delayed, resulting in a decrease of Kdis. Furthermore, from powder X-ray diffraction, HPLC and elemental analysis, the delay in disintegration time might be attributable to the formation of a transparent gel, formed by the reaction between CAM molecule and hydrochloric acid under low pH conditions, on the surface of CAM tablet. On the basis of these results, this report can be considered the first case where a transparent gel prevents gastric fluid from penetrating the tablet, resulting in reduced decomposition of CAM following oral administrating.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 59 (5), 553-558, 2011
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679150046848
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- NII論文ID
- 130000648868
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 11057944
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
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