Biopharmaceutical evaluation of sustained-release ethylcellulose microcapsules containing amoxicillin using beagle dogs.
A beta-lactam antibiotic, amoxicillin, was microencapsulated with ethylcellulose using a solvent evaporation process in liquid paraffin containing sorbitan tristearate as a dispersing agent, and the microcapsules obtained showed first-order drug release. Usage of the previous log-log relationship of cefadroxil between in vitro dissolution half-lives (T50) and the experimental release rate constants (k'r) of the drug in vivo, and the nomogram for the design of satisfactory sustained-release preparations resulted in the prediction that ethylcellulose microcapsules containing 60% amoxicillin would show the most effective sustained-release pattern. Prepared microcapsules containing various amounts of amoxicillin were administered to beagle dogs and it was found that above prediction was correct. In addition, a more precise log-log correlation concerning amoxicillin was also undertaken, good linearity was observed and the decline was very similar to that of cefadroxil.
Uchida
T
T
Fujimoto
I
I
Goto
S
S
D000658:Amoxicillin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000818:Animals; D001702:Biopharmaceutics; D002214:Capsules; D002482:Cellulose / Q000031:analogs & derivatives; D003692:Delayed-Action Preparations; D004285:Dogs; D008297:Male
D002214:Capsules; D003692:Delayed-Action Preparations; C013517:ethyl cellulose; D000658:Amoxicillin; D002482:Cellulose