Preparation of roxithromycin-polymeric microspheres by the emulsion solvent diffusion method for taste masking.
Microspheres of roxithromycin with Eudragit S100 and silica were prepared by the emulsion solvent diffusion method to mask the bitter taste of the antibiotic. The effect of different polymers and drug-polymer ratios on the taste masking and the characteristics of the microspheres were investigated. It was found that Eudragit S100 was the best for masking the unpleasant taste of roxithromycin among the six kinds of polymers investigated. The results of DSC, X-ray diffraction and IR showed that there were several combinations of roxithromycin and Eudragit S100. The influence of other formulation factors, i.e. dichloromethane-acetone ratios and silica-polymer ratios on the properties of the microspheres were also examined. In conclusion, the results of the present study will be helpful for the preparation of oral forms of roxithromycin with an acceptable taste.
Gao
Yan
Y
Department of Pharmaceutics, Shenyang Pharmaceutical University, No. 103 Wenhua Road, Shenhe District, Shenyang City, Liaoning Province 110016, China.
Cui
Fu-de
FD
Guan
Ying
Y
Yang
Lei
L
Wang
Yong-sheng
YS
Zhang
Li-na
LN
D000096:Acetone; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D002681:China; D004058:Diffusion; D004655:Emulsions; D005260:Female; D006801:Humans; D008297:Male; D008752:Methylene Chloride; D008863:Microspheres; D010602:Pharmacopoeias as Topic; D011108:Polymers; D015575:Roxithromycin / Q000008:administration & dosage* / Q000009:adverse effects / Q000737:chemistry; D012822:Silicon Dioxide; D012997:Solvents; D013055:Spectrophotometry, Infrared; D013649:Taste / Q000187:drug effects*; D013652:Taste Threshold; D014961:X-Ray Diffraction
D000900:Anti-Bacterial Agents; D004655:Emulsions; D011108:Polymers; D012997:Solvents; D000096:Acetone; D015575:Roxithromycin; D008752:Methylene Chloride; D012822:Silicon Dioxide