Formulation design of taste-masked particles, including famotidine, for an oral fast-disintegrating dosage form.
In this study, the taste-masking of famotidine, which could apply to any fast-disintegrating tablet, was investigated using the spray-dry method. The target characteristics of taste-masked particles were set as follows: the dissolution rate is not to be more than 30% at 1 min and not less than 85% at 15 min, and the particle size is not to be more than 150 microm in diameter to avoid a gritty feeling in the mouth. The target dissolution profiles of spray-dried particles consisting of Aquacoat ECD30 and Eudragit NE30D or triacetin was accomplished by the screening of formulas and the appropriate lab-scale manufacturing conditions. Lab-scale testing produced taste-masked particles that met the formulation targets. On the pilot scale, spray-dried particles with attributes, such as dissolution rate and particle size, of the same quality were produced, and reproducibility was also confirmed. This confirmed that the spray-dry method produced the most appropriate taste-masked particles for fast-disintegrating dosage forms.
Mizumoto
Takao
T
Pharmaceutical Research and Technology Labs, Astellas Pharma Inc, Shizuoka, Japan. takao.mizumoto@jp.astellas.com
Tamura
Tetsuya
T
Kawai
Hitoshi
H
Kajiyama
Atsushi
A
Itai
Shigeru
S
D000284:Administration, Oral; D002482:Cellulose / Q000031:analogs & derivatives; D002626:Chemistry, Pharmaceutical; D003890:Desiccation; D004304:Dosage Forms; D004339:Drug Compounding; D005079:Excipients; D015738:Famotidine / Q000008:administration & dosage* / Q000737:chemistry*; D006635:Histamine H2 Antagonists / Q000008:administration & dosage* / Q000737:chemistry*; D006801:Humans; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D010968:Plasticizers / Q000737:chemistry; D011109:Polymethacrylic Acids; D011208:Powders; D015203:Reproducibility of Results; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet; D013607:Tablets; D013649:Taste / Q000187:drug effects*; D013652:Taste Threshold / Q000187:drug effects; D014215:Triacetin / Q000737:chemistry; D014961:X-Ray Diffraction
D004304:Dosage Forms; D005079:Excipients; D006635:Histamine H2 Antagonists; D010968:Plasticizers; D011109:Polymethacrylic Acids; D011208:Powders; D013607:Tablets; C038300:methylmethacrylate-methacrylic acid copolymer; D015738:Famotidine; C013517:ethyl cellulose; D002482:Cellulose; D014215:Triacetin