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    題名: Lansoprazole腸溶圓粒膠囊劑之配方設計與研究;Formulation designs and studies of Lansoprazole enteric coating pellet capsules
    作者: 陳健傑;Chien-Chieh Chen
    貢獻者: 中國醫藥大學:藥學系碩士班
    關鍵詞: 腸溶;圓粒;膠囊劑;Lansoprazole
    日期: 2007-06-02
    上傳時間: 2009-08-13 10:54:06 (UTC+8)
    摘要: Lansoprazole為一種benzimidazole類的質子幫浦抑制劑(Proton Pump Inhibitor),可以專一性的作用於胃壁細胞分泌胃酸的最後一個酵素(H+/K+-ATPase),使之去活化,減少胃酸的分泌。臨床上廣泛應用於胃潰瘍、十二指腸潰瘍、逆流性食道炎、Zollinger-Ellison症候群等各種抗酸分泌的治療。

    圓粒(Pellet)可以打成錠劑或填充成膠囊劑,然而圓粒的特色是能克服胃腸道轉移之時間差異,而在胃腸道內的轉移是不受食物輸送規律的影響,也不受胃排空的影響。另外圓粒能夠均勻的分佈在胃腸道內,增加吸收面積,可以大大的提升身體可用率,並且可以減少藥物對胃腸道黏膜的刺激。

    將Lansoprazole製備成腸溶圓粒劑型以避免胃酸的破壞,使用伍斯特式流動床來製備腸溶圓粒,利用不同賦形劑進行配方設計並以HPLC作含量測定及相關的評估。由實驗結果發現,在藥物層中,使用Polyvinyl Alcohol(PVA)當黏合劑效果最佳。因Lansoprazole在溶液中易被破壞而PVA有安定效果可避免Lansoprazole被破壞。在腸衣層中,隨著Eudragit® L30 D-55不同比例濃度的增加而延遲藥物自圓粒釋放。當腸衣層的濃度過高時,會影響溶離速率抑制藥物的釋放。另外做圓粒物性、膠囊物性評估測定,包括顆粒密度、顆粒粒徑分佈、顆粒含水量、單位劑量含量均一度。再以體外溶離試驗,評估不同比例腸衣層的濃度對Lansoprazole溶離的影響。因為形成的包覆厚度太厚會延遲藥物釋放,甚至阻止藥物釋放,然而太薄會太早釋放,使藥物受到胃酸破壞,也會刺激胃部。

    Lansoprazole is the proton pump inhibitor of a kind of benzimidazoles,It last coat of the stomach the cells not secreting uniqueness not all right ferment of hydrochloric acid in gastric juice (H + /K + the - ATPase) ,Make it activate,reduce the secretion of the hydrochloric acid in gastric juice。Apply to such various kinds of treatment resisting acid and secreting as the gastric ulcer、duodenal ulcer、adverse current esophagitis、Zollinger-Ellison disease groupetc。

    Pellet can hit into the lozenge or pack into the capsule pharmaceutical, but the characteristic of the round one can overcome the time that the intestines and stomach shift difference,transformation in intestines and stomach to transport food influence of law,influence not emptied by the stomach either。The round one can be distributed evenly in the intestines and stomach,increase the area of absorbing in addition,improvement body availability on can big,can reduce between medicine and stimulus, intestines and stomach of mucous membrane.

    Prepare Lansoprazole into the intestines to dissolve the destruction in
    order to avoid the hydrochloric acid in gastric juice of round grains of form of a drug,use Wooster type flow bed is it prepare intestines dissolve round grain,is it design and act as content determining and relevant assessment with excipient so as to HPLC to fill a prescription to go on to utilize to come。Found by the experimental result,in the medicine floor, use Polyvinyl Alcohol (PVA) The best as binding the pharmaceutical result。 Because Lansoprazole easy to destroy PVA have stable result can prevent Lansoprazole from destroy among solution。In the casing floor, postpone medicines and justify one oneself to release with increase of the thickness of Eudragit® L30 D-55 different proportions。 When the thickness of floor of casing is too high,will influence and dissolve and leave the release that the speed suppresses the medicine。Make round grains of thing in addition,capsule thing assessment determine,including particle density,particle grain distribute directly,for a time content,water content of particle and dosage of unit。It is and then by body dissolve from testing,assess proportion thickness,the casings of layer not different dissolve to Lansoprazole from influence。Because the bag formed will postpone medicines to release to cover the thickness too thick,even prevent the medicine from releasing,but too thin to will release early too, make medicine destroy hydrochloric acid in gastric juice,can stimulate stomach too。
    顯示於類別:[藥學系暨碩博士班] 博碩士論文

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