Utility of mixture of commercially available polymers as constituents of sustained-release microcapsules containing cefadroxil or theophylline.
Hydroxy propyl methyl cellulose acetate succinate high grade (AS-HG) and ethyl cellulose (EC) mixture microcapsules containing cefadroxil or theophylline were prepared by a solvent evaporation method in liquid paraffin dissolved sorbitan tri-stearate as a dispersing agent, and their sustained-release properties were evaluated. The microcapsules prepared with AS-HG:EC (in a 2:5 weight ratio) mixture containing 20% of cefadroxil or theophylline exhibited apparent zero-order releasing pattern in pH 6 to 8, at 50 rpm and 37 degrees C (paddle method). These microcapsules were administered orally to beagle dogs and the plasma concentrations of cefadroxil or theophylline were measured periodically. As a result of in vivo investigation, a satisfactory sustained-release plasma pattern and an apparent zero-order process in the gastrointestinal absorption were confirmed by deconvolution analysis of both drugs.
Uchida
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T
Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
Yasutake
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T
Goto
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S
D000284:Administration, Oral; D000818:Animals; D002434:Cefadroxil / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D002482:Cellulose / Q000031:analogs & derivatives*; D003692:Delayed-Action Preparations; D004285:Dogs; D004339:Drug Compounding; D007408:Intestinal Absorption; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives*; D013806:Theophylline / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
D003692:Delayed-Action Preparations; D002434:Cefadroxil; C048331:hydroxypropylmethylcellulose acetate succinate; C013517:ethyl cellulose; D002482:Cellulose; D008747:Methylcellulose; D013806:Theophylline