Preparation of microcapsules masking the bitter taste of enoxacin by using one continuous process technique of agglomeration and microencapsulation.
In order to mask the bitter taste of drugs, a novel microencapsulation process combined with the wet spherical agglomeration (WSA) technique was developed by using a modified phase separation method. The spherical agglomerates of enoxacin (ENX) with various additives including disintegrants were successfully produced in the system of acetone-n-hexane-ammonia water or acetone-n-hexane-distilled water by the WSA, using flocculation phenomena of particles in liquid. Resultant agglomerates could be microencapsulated continuously with Eudragit RS utilizing the phase separation method in the same system as agglomeration under stirring. 'Explosible' microcapsules which were free from the bitter taste could be produced in formulating finer particle size of ENX and 50 per cent of Primojel in core agglomerates, using distilled water as a bridging liquid, and treating with 20 per cent polymer coating level. These microcapsules were bioequivalent to the commercial ENX 100 mg tablets in beagle dogs. One continuous process technique of agglomeration and microencapsulation was useful for the design of ENX powders which masked the bitter taste and controlled the drug release rate.
Ueda
M
M
Pharmaceutical Research Laboratories, Dainippon Pharmaceutical Co., Ltd., Osaka, Japan.
Nakamura
Y
Y
Makita
H
H
Kawashima
Y
Y
D000818:Animals; D001682:Biological Availability; D002214:Capsules; D002626:Chemistry, Pharmaceutical; D004285:Dogs; D004339:Drug Compounding; D015365:Enoxacin / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D005079:Excipients; D006801:Humans; D007408:Intestinal Absorption; D008297:Male; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D013499:Surface Properties; D013649:Taste / Q000187:drug effects*
D002214:Capsules; D005079:Excipients; D015365:Enoxacin