去羥梔子苷之預配方研究

The Preformaulation Studies of Geniposide

梔子係茜草科植物Grardenia Jasminoides ELLIS之果實。亦即為本國生藥中所稱之山梔子。常使用於消炎及利膽，去羥梔于苷(Reniposide)為梔子之主要成分，被認為有緩下、保肝及促進膽汁分泌之作用。去羥梔子芬膠囊劑之配方設計中，其藥物與賦型劑相容性之研究係採選十六種常用的賦型劑，將其與去羥梔子苷混合、分別置於避光、日光燈，紫外光燈照射，及不同之溫度下貯存以觀察去羥梔子苷的含量變化。並依藥物與賦型劑相容性之研究結果，製成8種膠囊劑之配方以研究配方老化對釋溶率之影響。本研究結果發現，去羥梔子苷與羥丙基甲基纖維素，玉米澱粉，及硬脂酸鎂混合所製成之膠囊劑的配方，安定性最好。

The fruit of Gardenia jasminoides E(subscript LLIS) is a well known Chinese herbal drug commonly called Zhizi. It is used as an antiphlogistic and a cholagogue. Geniposide, which was isolated from the fruit of Gardenia jasminoides E(subscript LLIS), has been demonstrated effective as a laxative, hepatoprotective, and choleretic. Lactose, mannitol, microcrystalline cellulose, HPMC 606, PVP 30 K, mobile starch, corn starch, potato starch, kaolin, Mg. stearate, sodium lauryl sulfate, stearic acid, silica, aerosil, talc, and stearyl alcohol have been chosen as excipients to study drug-excipient imcompatibility. Geniposide and the excipients were mixed and stored under the conditions of dark, fluorescent light, and UV light at different temperatures for two months. The drug-excipient imcompatibility was evaluated by their appearance and concentration of geniposide remaining. Eight formulations for capsules had been provided for stability studies. Based on the remaining concentration of geniposide and dissoultion profiles, geniposide-corn starch-HPMC-Mg stearate was so far, the best combination for the geniposide capsule dosage form.