Comparative study of different approaches for preparation of chlorzoxazone orodispersible tablets.
CONTEXT
Muscle spasm is a painful involuntary contraction of muscles, which causes involuntary movement and distortion. Chlorzoxazone is a centrally acting muscle-relaxant with sedative properties, but given orally, it is hepatically metabolized leading to decreased bioavailability.


OBJECTIVE
Orodispersible tablets (ODTs) of chlorzoxazone were formulated using two different approaches; by coprocessed excipients (CE) or by liquisolid (LS) technique.


MATERIALS AND METHODS
Pharmaburst® 500, Starlac®, Pearlitol flash®, Prosolv® odt and F-melt® were used as coprocessed superdisintegrants, whereas in LS, Avicel® PH101, Microcelac® 100 and Cellactose® 80 were used as carriers, while Aerosil® 200 was the coating material. ODTs were evaluated in terms of weight and thickness variations, drug content, hardness, friability, wetting time, dissolution, disintegration time (DT) and palatability.


RESULTS
In vitro DT of CE-ODTs ranged from 26.43 ± 1.693 s to >180 s, whereas it was between 25.42± 0.203 s to >180 s in LS-ODTs. Complete drug release within 15 min was attained by CE1 prepared with 92.5 mg Pharmaburst® 500. In vivo DT of CE1 and LS3 were 19.779 ± 0.810 and 18.105 ± 0.423 s, respectively, using six volunteers. Volunteers found that CE1 had more acceptable taste and was more palatable than LS3.


CONCLUSION
It was concluded that chlorzoxazone ODTs could be successfully formulated using either CE or LS techniques and be used as novel dosage forms for pediatrics and geriatrics showing improved drug release. Moreover, CE technique was superior to LS technique in terms of palatability.
['Moqbel|Helal Abdo|HA|', 'ElMeshad|Aliaa Nabil|AN|', 'El-Nabarawi|Mohamed Ahmed|MA|']
D000284:Administration, Oral D000328:Adult D001682:Biological Availability D002626:Chemistry, Pharmaceutical D002753:Chlorzoxazone D004339:Drug Compounding D065546:Drug Liberation D005079:Excipients D005260:Female D006244:Hardness D006801:Humans D008297:Male D012995:Solubility D013607:Tablets D013649:Taste D055697:Taste Perception D017155:Wettability
chlorzoxazone Orodispersible tablet coprocessed superdisintegrant dissolution disintegration time liquisolid technique