盐酸地芬尼多口崩片的制备  

Preparation of difenidol hydrochloride orally disintegrating tablets

作　　者：曾媛 廖翔茹 刘辉 熊菁 胡华 ZENG Yuan;LIAO Xiangru;LIU Hui;XIONG Jing;HU Hua(Department of Pharmacy,Medical Security Center,General Hospital of Central Theater Command,Hubei Wuhan 430070,China)

机构地区：[1]中部战区总医院医疗保障中心药剂科,湖北武汉430070

出　　处：《中国医院药学杂志》2024年第10期1169-1173,1191,共6页Chinese Journal of Hospital Pharmacy

摘　　要：目的:制备盐酸地芬尼多口崩片并进行处方优化。方法:分别采用粉末直接压片法、内外加崩解剂湿法制粒法、内加崩解剂湿法制粒法制备盐酸地芬尼多口崩片,以口崩片的崩解时限、口感、可压性为考察指标,通过单因素试验考察筛选填充剂、崩解剂、润滑剂的种类和用量,获得各组分用量优选范围。然后以口崩片的崩解时限、硬度、30 min溶出百分率作为评价指标,采用Box-Behnken响应面法优化盐酸地芬尼多口崩片的处方。结果:选用粉末直压工艺,优化所得处方为盐酸地芬尼多25 mg、硬脂酸25 mg、甘露醇70 mg、微晶纤维素180 mg、阿司帕坦35 mg、蓝莓香精8 mg、碳酸氢钠5 mg、柠檬酸6 mg、交联羧甲基纤维素钠19 mg、十二烷基硫酸钠5 mg、硬脂酸镁3 mg。最优处方制备的口崩片崩解时间在40 s以内,且30 min溶出百分率达到90%以上。结论:筛选优化获得的最优处方制备的盐酸地芬尼多口崩片符合《中国药典》关于口崩片的质量要求,且口感良好,工艺重现性良好。OBJECTIVE To prepare difenidol hydrochloride(DH)orally disintegrating tablets(ODT)and optimize its formulation.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 evaluators.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 percentage 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 hydrochloride 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 magnesium 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 preparation of DH ODT.Meeting the quality requirements of Chinese Pharmacopoeia for ODT,it has a decent taste and process reproducibility.

关 键 词：盐酸地芬尼多 口崩片 单因素 Box-Behnken 制备 

分 类 号：A944.4[哲学宗教—马克思主义哲学]