Preparation of difenidol hydrochloride orally disintegrating tablets
OBJECTIVE To prepare difenidol hydrochloride(DH)orally disintegrating tablets(ODT)and optimize its for mulation.METHODS DH ODT was prepared through the methods of internal/external addition disintegrant,internal addition disintegrant and powder direct compression.Disintegration time limit,taste and compressibility of ODT were utilized as evalua-tors.Single factor experiments were conducted for screening the types and amounts of fillers,disintegrants and lubricants.An optimal range of dosage for each component was obtained.Then disintegration time limit,hardness and 30 min dissolution percent-age of ODT were employed as evaluators.Box Behnken response surface method was utilized for optimizing the prescription of DH ODT.RESULTS Direct compression process was selected.The optimized formula was composed of difenidol hydrochlo-ride 25 mg,stearic acid 25 mg,mannitol 70 mg,microcrystalline cellulose 180 mg,aspartame 35 mg,blueberry essence 8 mg,sodium bicarbonate 5 mg,citric acid 6 mg,cross-linked carboxymethyl cellulose 19 mg,sodium dodecyl sulfate 5 mg and magne-sium stearate 3 mg.The optimal prescription for preparing ODT had a disintegration time of ＜40 seconds and a dissolution rate of ＞90％ within 30 min.CONCLUSION An optimal prescription may be obtained through screening and optimizing the prepara-tion of DH ODT.Meeting the quality requirements of Chinese Pharmacopoeia for ODT,it has a decent taste and process reproducibility.
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