Preparation of amoxicillin intragastric buoyant sustained-release tablets and the dissolution characteristics.
An intragastric buoyant sustained-release tablet (IGB-T) containing 100 mg of amoxicillin (AMX) was prepared to eradicate gastric Helicobacter pylori. A tablet prepared by compressing the mixture of hydroxypropylcellulose-H (HPC-H), citric acid (17.2 mg), sodium hydrogen carbonate (22.8 mg) and AMX was employed as the basic system for preparing IGB-T. The weight and diameter of the tablets were designed to be about 300 mg and 10 mm, respectively. IGB-T containing 5 mg of AMX and HPC-H (255 mg) was buoyant and showed a sustained-release pattern in water. However, when AMX was increased and HPC-H decreased to maintain the tablet weight (300 mg), there was no apparent sustained-release pattern. To prepare IGB-T containing 50 mg of AMX, the surface of the tablet was coated with HPC-H after a tablet was prepared from the mixture of AMX (50 mg), HPC-H (210 mg), citric acid (17.2 mg), and sodium hydrogen carbonate (22.8 mg). This tablet (IGB-T50-Coating) was buoyant and showed a sustained-release pattern in water. However, to complete IGB-T with 100 mg of AMX, it was necessary not only to coat the surface of the tablet but also to use granulated AMX with a particle size of 300-500 microm (IGB-T100-Coating-300-500G). IGB-T100-Coating-300-500G was confirmed to be buoyant for 24 h while maintaining a tablet shape and showed a sustained-release pattern in water and buffer solutions of pH 1.2 and 6.8.
Tokumura
Tadakazu
T
Department of Drug Delivery Research, Hoshi University, Ebara, Shinagawa, Tokyo, Japan. tokumura@pep.ne.jp <tokumura@pep.ne.jp>
Machida
Yoshiharu
Y
D000658:Amoxicillin / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003692:Delayed-Action Preparations / Q000138:chemical synthesis / Q000493:pharmacokinetics; D012995:Solubility; D013608:Tablets, Enteric-Coated
D003692:Delayed-Action Preparations; D013608:Tablets, Enteric-Coated; D000658:Amoxicillin