Taste masking microspheres for orally disintegrating tablets.
The purpose of this study was to evaluate the potential of microspheres for taste masking when incorporated into orally disintegrating tablets. The microspheres were produced by spray drying a mixture of the model compound (famotidine) with taste masking material. The spray process was optimized using a central composite design for two variables to obtain microspheres with desirable characteristics. Then the microspheres were mixed with other excipients to form orally disintegrating tablets. The optimal spray-drying process parameters were 34mg/ml for solid concentration and 7ml/min for feed rate. The drug encapsulation efficiency of the spray-dried microspheres ranges from of 37.59 to 61.56%, with a mean diameter of less than 10microm size and low moisture content (less than 4%). Results from an evaluation by a panel of six human volunteers demonstrated that the orally disintegrating tablets with taste masking microspheres improved the taste significantly. Furthermore, an in vivo study in rats showed that the microspheres neither decrease the bioavailability nor retard the release of famotidine significantly. In conclusion, spray-dried microspheres can effectively mask the bitter taste of the active pharmaceutical ingredients in combination with the orally disintegrating tablets.
Xu
Jianchen
J
The College of Pharmaceuticals and Biotechnology, Tianjin University, Tianjin, PR China.
Bovet
Li Li
LL
Zhao
Kang
K
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D015738:Famotidine / Q000737:chemistry* / Q000493:pharmacokinetics; D006635:Histamine H2 Antagonists / Q000737:chemistry* / Q000493:pharmacokinetics; D006801:Humans; D008297:Male; D008863:Microspheres; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D016037:Single-Blind Method; D012995:Solubility; D013607:Tablets; D013649:Taste
D006635:Histamine H2 Antagonists; D013607:Tablets; D015738:Famotidine