Roxithromycin Coated Pellets

Roxitbromycin is a macrolides antibiotic with a broad and essentially bateriostatic action against ststaphylococcus,streptococcus,gonococcus,Chlamydia,legionella,manyGrampositivebacteria, as well as some other organisms.Roxitbromycin has been widely used clinically to treat respiratory tract bacterial infection,pneumonia bacteroidal,lung abscess,for acute or chronic bronchitis and bronchiectasis,skin and soft tissue infections etc.The purpose of this paper was to develop roxitbromycin coated pellets which would decrease adverse effects and improve its bioavailability,and be more convenient for patients to use.To study the compatibility between Roxitbromycin and excipients in coated pellets of Roxitbromycin,thermal analysis technique(DSC)was used in the study.It was indicated that Roxitbromycin was compatible with lactose,microcrystalline cellulose,HPMCand Eudragit EPO.HPLC was utilized to determine the Roxitbromycin content and impurity in the pellets, colorimetry for determining the dissolution of Roxitbromycin from pellets.Roxitbromycin pellets were prepared by means of power layering with the centrifugal granulation equipment,with MCC and lactose as the core excipients,Eudragit EPO as the coat.By formulation screen,the final formulation was obtained.It was demonstrated that the product was confirmed with the compendia standard and had good stability.The plasma concentration of Roxitbromycin in 18 volunteers was determined by a method of HPLC after a single oral administration of commercial pellets(reference)and the coated pellets (test).The pharmacokinetics parameters and the relative bioavailability were measured.The pharmacokinetics parameters(C_max,AUC_0-48AUC_0-∞)of Roxitbromycin between test and reference preparations was not significantly different.It was indicated that commercial pellets (reference)and the coated pellets(test)was bio-equivalent by double one side test,with 90% confidence limit for AUC_0-48being 93.73%～98.82%,for AUC_0-∞being 95.40%～100.14%and for C_maxbeing95.62%～101.99%.