填充剂及崩解剂对尼莫地平固体分散体片剂溶出行为的影响  

Effects of Fillers and Disintegrants on Dissolution Behavior of Nimodipine Solid Dispersion Tablets

作　　者：陈梦娇 戴安印 尚龙宇 陈丽娜[1] 王文喜[1] CHEN Mengjiao;DAI Anyin;SHANG Longyu;CHEN Lina;WANG Wenxi(College of Pharmaceutical Science,Zhejiang University of Technology,Hangzhou 310014;The 903rd Hospital of Joint Logistic Support Force of the Chinese People's Liberation Army,Hangzhou 310013)

机构地区：[1]浙江工业大学药学院,浙江杭州310014 [2]中国人民解放军联勤保障部队第九〇三医院,浙江杭州310013

出　　处：《中国医药工业杂志》2025年第1期66-72,共7页Chinese Journal of Pharmaceuticals

摘　　要：该研究采用热熔挤出法制备了尼莫地平(1)固体分散体(SD),并以粉末直接压片法压制成1-SD片剂。以体外溶出度为指标,考察了填充剂类型、崩解剂种类及用量对1-SD片剂中1溶出行为的影响。结果显示,以磷酸二氢钾为填充剂、泡腾剂[m(碳酸氢钠)∶m(枸橼酸)=5∶4]为崩解剂时,所得片剂的溶出度较好。以优化处方(含1-SD 240 mg、磷酸二氢钾124 mg、崩解剂32 mg和硬脂酸镁4 mg)制备的1-SD片剂5 min即可崩解,10 min时1的溶出率可超过95%。该研究制备的1-SD片剂溶出性能良好,有效克服了由亲水性载体所产生的凝胶屏障,为SD片剂的开发提供了参考。Nimodipine(1) solid dispersion(SD) was prepared by hot melt extrusion, and the tablets based on 1-SD were prepared by direct compression method. Taking the in vitro dissolution as an indicator, the impacts of filler type,type and amount of disintegrants on drug dissolution of 1-SD tablets were investigated. The results showed that the tablets prepared with potassium dihydrogen phosphate as the filler and the effervescent agent[m(sodium bicarbonate) ∶ m(citric acid)=5 ∶ 4] as the disintegrant exhibited a favorable dissolution behavior. The 1-SD tablets prepared with the optimized formulation(containing 240 mg of 1-SD, 124 mg of potassium dihydrogen phosphate, 32 mg of above disintegrant, and 4 mg of magnesium stearate) disintegrated in 5 min, and their dissolution rate at 10 min could be over 95%. The 1-SD tablets prepared in this study effectively overcame the gel barrier produced by the hydrophilic carrier and had a good dissolution performance, which provided a reference for the development of SD tablets.

关 键 词：尼莫地平 难溶性药物 固体分散体 片剂 溶出度 崩解 

分 类 号：R944.4[医药卫生—药剂学] R944.9[医药卫生—药学]