Asian Journal of Pharmaceutical Sciences    2009, 4(1): 32-38   ISSN: 1818-0876   CN:    

 
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Antibiotic activity of tetracycline released from a mucoadhesive
complex with sucralfate against Helicobacter pylori
Shoichi Higo1*, Hirofumi Takeuchi2, Hiromitsu Yamamoto2, Tomoaki Hino2, Machiko Miyata3, Hiroshi Mori3, Yoshiaki Kawashima2
1 Discovery Platform Technology Department, Chugai Pharmaceutical Co. Ltd.; Shizuoka 412-8513, Japan
2 NLaboratory of Pharmaceutical Engineering, Gifu Pharmaceutical University, Gifu 502-8585, Japan
3 Laboratory of Medical Microbiology, Gifu Pharmaceutical University, Gifu 502-8585, Japan
Received 2008-7-15 ; Revised 2008-10-6 ; Accepted 2008-11-23 ; Online 2009-3-10

Abstract

Purpose: To evaluate the antibiotic activity and possible loss of antibiotic activity due to the complexation process and to confirm the synergistic effect of the tetracycline-sucralfate acidic complex. Method: Tetracycline-sucralfate complexes were prepared and their antibiotic activity against two bacteria was investigated. Staphylococcus aureus was used to evaluate the reported loss of activity following complexation with a metal, and H. pylori was used as the bacterial target. All test solutions were prepared using an acidic medium because the drug is expected to be released under acidic conditions in the stomach. Results: While sucralfate exhibited no antibiotic activity, the tetracycline released from the complex exhibited antibiotic activity even after complexation under acid conditions. The antibiotic activity of tetracycline against H. pylori was far greater than that against Staphylococcus aureus. Conclusion: The adhesion of the orally administered complex to the gastric mucosa produces sustained activity against H. pylori infection and its eradication in spite of chelation due to complexation with sucralfate.


Keywords:  Tetracycline   Sucralfate   Complexation   Helicobacter pylori   Antibiotic activity  

DOI: 

Correponding author: Shoichi Higo; Email: higosui@chugai-pharm.co.jp