The acidic complexation of tetracycline with sucralfate for its mucoadhesive preparation.
The complex of antibiotics with sucralfate (SF) was prepared with acid. The mechanism of the complexation and some factors concerning the preparation, which influence the mucoadhering property, were studied. The complexation was confirmed by the change in color and instrumental analysis. The acidic complex appeared to be produced by reagglomeration of SF preliminary particles. It was suggested that the amide or amine groups of tetracycline (TC) and aluminum moieties of SF serve as the binding sites. The potential of multiple binding sites and a priority in them were suggested by the Scatchard plot analysis. The additional amounts of acid and the increase in the surface area increased the number of sites. The amount of the additional acid appeared to be the most important factor during the preparation of the acidic complex. The appropriate amount of acid added appeared to produce a complex rich in TC. However, an excess amount might cause the excess dissociation of aluminum moieties, which destroys the mucoadhesive paste-forming property.
Higo
Shoichi
S
Product Research Department, Chugai Pharmaceutical Co. Ltd., Gotemba, Shizuoka, Japan. higosui@chugai-pharm.co.jp
Takeuchi
Hirofumi
H
Yamamoto
Hiromitsu
H
Hino
Tomoaki
T
Kawashima
Yoshiaki
Y
D000143:Acids / Q000737:chemistry; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D000897:Anti-Ulcer Agents / Q000737:chemistry / Q000494:pharmacology*; D001665:Binding Sites / Q000187:drug effects*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D016503:Drug Delivery Systems; D016480:Helicobacter pylori / Q000187:drug effects; D013392:Sucralfate / Q000737:chemistry / Q000494:pharmacology*; D013752:Tetracycline / Q000737:chemistry / Q000494:pharmacology*
D000143:Acids; D000900:Anti-Bacterial Agents; D000897:Anti-Ulcer Agents; D013392:Sucralfate; D013752:Tetracycline