| Clarithromycin is a semisynthetic macrolides antibiotic with a broad and essentially bateriostatic action against many Gram-positive and some Gram- negative bacteria, as well as some anaerobes. It has been widely used clinically to treat respiratory tract infection, urogenifal infection, skin and soft tissue infections etc, especially as the first picked medicine to therapy pediatric respiratory tract infection. Its side effect incidence is low. The purpose of the study was to develop two kinds of Clarithromycin sustained release pellets with 400～ 600um and 0.8～1.5mm diameters respectively and the former will be made into granule and the later, capsule which would improve its action,reduce adverse effects and increase patients' compliance.Through physico-chemical property investigation HPLC was established to determine Clarithromycin content in pellets, colorimetry for assaying release of sustained release pellets and microbioassay method to determine the plasma concentration in dogs.400～600um diameter Clarithromycin pellets were prepared by means of powder layering in a centrifugal granulation equipment. 0.8～1.5mm diameter pellets were prepared by means of extrusion-spheronization method .Multifunction particle machine was usded for coating. Different Categories,amounts and matches Acrylic resins as the coating material were investigated.The yield,appearance,contents and release of the objective pellets all reached the prospective goals.Pharmacokinetic study of 400～600um diameter sustained release pellets was conducted as a single-dose,randomaised,four-period,crossover design in 6 healthy dogs under fed and fasted conditions with one week washout period. The plasma concentration of Clarithromycin were tested by bioassay. The pharmacokinetic parameters , relative bioavailability and food effects were studied. Pharmacokinetic parameters of Clarithromycin in reference tablets under...
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