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A Novel Evaluation Method of Gastric Mucoadhesive Property in Vitro and the Mucoadhesive Mechanism of Tetracycline-Sucralfate Acidic Complex for Eradication of Helicobacter pylori

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Abstract

Purpose. The gastric mucoadhesive property of tetracycline-sucralfate acidic complex (CO) was evaluated by using a novel method in vitro to compare with the in vivo test. The mucoadhesive mechanism of the acidic complex was also studied.

Methods. The gastric mucosa removed from a rat was placed covering the end of a plunger and secured in a disposable syringe. The acidic test medium was gradually infused in and then flowed out. Two different kinds of CO, tetracycline, or a physical mixture (PM) were introduced into the device to compare their mucoadhesive properties. The tetracycline content in the residue on the mucosa was measured. The results were compared with those of the in vivo test. The acidic response of CO and the protein binding capacity of a sucrose octa-sulfate group (SOS) in sucralfate or CO were evaluated.

Results. The mucoadhesive properties of CO were clearly superior to those of PM. The remaining amounts of tetracycline in each test sample, determined by the in vitro test, were in agreement with those of the in vivo test. The excellent mucoadhesive property of CO appeared to be caused by the rapid response to the acid and resulting mucoadhesive gel formation. Furthermore, the binding capacity of SOS to the protein was clearly greater than that of PM. The excessive acid treatment during the preparation of CO tended to decrease the mucoadhesive property.

Conclusions. CO appeared to be potentially useful for the eradication of Helicobacter pylori because of the direct delivery of tetracycline to the gastric mucosa for an extended period of time.

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Authors and Affiliations

  1. Product Research Department, Chugai Pharmaceutical Co. Ltd., 1-135 Komakado, Gotemba, Shizuoka, 412-8513, Japan

    Shoichi Higo & Kazutomo Ori

  2. Department of Pharmaceutical Engineering, Gifu Pharmaceutical University, 5-6-1 Mitahora-higashi, Gifu, 502-0003, Japan

    Hirofumi Takeuchi, Hiromitsu Yamamoto, Tomoaki Hino & Yoshiaki Kawashima

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  1. Shoichi Higo
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  2. Kazutomo Ori
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  3. Hirofumi Takeuchi
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  4. Hiromitsu Yamamoto
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  5. Tomoaki Hino
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  6. Yoshiaki Kawashima
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Correspondence to Shoichi Higo.

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Higo, S., Ori, K., Takeuchi, H. et al. A Novel Evaluation Method of Gastric Mucoadhesive Property in Vitro and the Mucoadhesive Mechanism of Tetracycline-Sucralfate Acidic Complex for Eradication of Helicobacter pylori . Pharm Res 21, 413–419 (2004). https://doi.org/10.1023/B:PHAM.0000019293.57927.7f

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