ABSTRACT
OBJECTIVE:To optimize the formulation of azithromycin sustained-release vaginal suppository(ASVS).METHODS:The ASVS was prepared using S-40 as suppository base,HPMC as sustained-release material and glycerine as humectant.The formulation of ASVS was optimized by orthogonal design with accumulated release percentage and hardness as indexes and the amount of 8% HPMC and glycerol as factors;meanwhile,a verification test and the fitting of in vitro drug release model were performed.RESULTS:The optimized formulation ASVS was as follows:azithromycin 6 g,8% HPMC 23.52 g,glycerol 29.40 g,ethanol absolute 3 g,ethylparaben 0.59 g,and S-40 294 g.Three batches of suppositories prepared under the optimized formulation reached a mean content of 99.5%,with hardness up to the standard,showing good reproducibility and homogenicity in drug release in vitro.The accumulative release rates of all samples were greater than 98% at 180 min,and the release dynamics in vitro were in line with Higuchi equations.CONCLUSION:The optimized ASVS is feasible in formulation,stable and reproducible in preparation technology and up to the standard for sustained-release preparation.
ABSTRACT
OBJECTIVE:Study on the efficiency of azithromycin sustained-release vaginal suppository in inhibiting ureaplasma urealyticum(Uu)in vitro.METHODS:The method of microdilution was used to determine the minimal inhibitory concentration(MIC)for Uu that azithromycin sustained-release vaginal suppository campared with azithromycin dried suspension. RESULTS:The MIC for Uu that both azithromycin sustained-release vaginal suppository and azithromycin dried suspension is lower than 0.125?g?mL~(-1).CONCLUSION:Azithromycin sustained release vaginal suppository has significant inhibitive effects on Uu under the experiment condition.