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Nifedipine 圓粒膠囊劑型之開發與直打用間質性控釋材質之開發研究

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Nifedipine

圓粒膠囊劑型之開發與直打用間質性控釋材質之開發研究

圓粒膠囊劑型無論在增加藥物的安全性,提高其治療效力,或是在製程及

處方的調配上均具有相當多的優點及可變通性。本實驗嘗試將

Nifedipine 及其固體分散系溶液以流動層製造機黏附於糖蕊粒上,再將

高分子材質膜衣 (Surelease) 包覆於藥物圓粒外,以製成膜衣式圓粒控釋

劑型。實驗結果顯示:圓粒成品中 Nifedipine 的回收產率均大於 90% ,

而且不同批次間無論在藥物回收率及藥物溶離情形方面均具有良好的再現

性;以 5% 藥物重量的乙基纖維素進行膜衣包覆時,對於 Nifedipine 即

有明顯的緩釋效果;膜衣處方中添加親水性高分子 HPMC 對於藥物的溶離

有促進作用,而且隨著 HPMC 添加量的增多,藥物的溶出速率愈快;另外

,溶離液中添加的非離子性界面活性劑 Tween 80 含量愈多,

Nifedipine 的溶離會愈快。直接壓錠法為製造間質性控釋劑型中最為快

速、簡單的方法。本實驗以傳統的濕式造粒法將高分子材質 Surelease 包

覆於乳糖及磷酸二鈣賦形劑上,使其成為一直打用間質性控釋材質,再和

水難溶性模式藥 Nifedipine 混合直接打錠。實驗結果顯示:各處方的間

質性顆粒均具有不錯的物理性質,可用於直接壓錠;隨乙基纖維素添加量

的增多,緩釋效果愈好;藥物固體分散系的製備則有助於藥物之溶出;另

外,由於乳糖及磷酸二鈣水溶性的差異,對於藥物亦有不同的緩釋效果,

所以將兩種賦形劑以不同比例相互混合使用時,應該可以進一步地調整藥

物的溶出情形。

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Development of Nifedipin Pellet Dosage Form and Development of Matrix Materials for Direct Compression of Controlled Release

Dosage Form

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