CN103520134B - 一种十二指肠靶向空心胶囊 - Google Patents
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Abstract
一种十二指肠靶向空心胶囊,由明胶或植物胶的囊材和表材外的包衣层所构成,其特征是所述包衣层为聚乙烯醇醋酸苯二甲酸酯,囊材和包衣层的质量百分比分别为70-80%和20-30%。本空心胶囊在pH值2的人工胃液中2小时以上不崩解,在pH值4的人工十二指肠液中30min内崩解,在pH值6.8的人工肠液中10-15min内崩解。本空心胶囊在人体特定的十二指肠部位崩解释放囊内药物。
Description
一、技术领域
本发明涉及一种药用辅料空心胶囊,具体地说是一种在人体胃部不允许崩解,而在人体特定的十二指肠部位要迅速崩解的靶向性空心胶囊。
二、背景技术
肠溶空心胶囊(囊壳)是指按《中国药典》2010版规定:囊壳在人工胃液(pH值2)2小时以上不能崩解,但在人工肠液(pH值6.8)中1小时内能崩解或溶化。目前使用的肠溶空心胶囊都是由明胶或植物胶加工成型后外包抗胃酸的肠溶包衣材料。生产工艺是明胶或植物胶溶成胶液后送胶囊生产线经蘸胶成型、固化干燥得到空心胶囊囊材,再在囊材表面进行肠溶包衣处理后,经干燥、切割、套合等工序得到肠溶空心胶囊(囊壳)。目前使用的抗胃酸的肠溶包衣材料很多,如有纤维醋法酯(CAP);甲基丙烯酸和丙烯酸乙酯(1:1)共聚物,甲基丙烯酸和甲基丙烯酸甲酯(1:1)共聚物;邻苯二甲酸羟丙基纤维素酯(简称HPMCP);羟丙基甲基纤维素醋酸琥珀酸盐(简称AS)。这些肠溶包衣材料使用都较好的抗胃酸,但都是在人工肠液中(pH值6.8)崩解或溶化,并且崩解或溶化时间长,只能在人体小肠部位释放囊内药物等。人体特定部位十二指肠的pH值在4左右,上述肠溶包衣材料均具有抗该pH值的特性。
三、发明内容
本发明旨在提供一种除在肠液崩解规定外其它各项理化性能都符合《中国药典》2010版规定的十二指肠靶向空心胶囊,所要解决的技术问题是遴选适合的具有在人体胃液pH值2以内能抗胃酸又能在十二指肠液pH值4左右能崩解或溶化的包衣材料。
申请人在众多的包衣材料中进行了品种、用量及包衣工艺的筛选,唯聚乙烯醇醋酸苯二甲酸酯(简称PVAP)符合在十二指肠崩解的要求,此外,与明胶或植物胶的囊材有很好的相容性,利用现有的包衣工艺和装置即可进行包衣。
本十二指肠靶向空心胶囊由明胶或植物胶在胶囊生产线上加工的囊材和囊材外的包衣层所构成,与现有技术的区别是所述的包衣层为PVAP材料,囊材和包衣层的质量百分比分别为70-80%和20-30%。优选75%和25%。
本空心胶囊同胃溶或肠溶空心胶囊一样,可根据试剂需要添加食用色素和遮光剂二氧化钛等。
所述的明胶由动物的皮、骨、肌腱、韧带等结缔组织中的胶原蛋白经水解得到的水溶性蛋白质。所述的植物胶羟丙基甲基纤维素、普鲁兰多糖等,是加工胃溶胶囊的主要原料。也是加工本囊材的主要原料,囊材的加工同现有技术。
包衣时以乙醇或/和丙酮为溶剂,将PVAP制成包衣液,经至少一次包衣,再烘干、脱模、切割、套合,加工成十二指肠靶向空心胶囊。
本空心胶囊按药典规定的方法进行崩解试验,结果如下:
1、在pH值2的人工胃液中2小时以上不崩解。
2、在pH值4的人工十二指肠液中30min内崩解。
3、在pH值6.8的人工肠液中10-15min内崩解。
崩解试验表明,本空心胶囊能在人体特定的十二指肠部位崩解(溶解)以释放囊内的药物。
四、具体实施方式
1、囊材的制备
将明胶或植物胶和水投入混合釜中加热搅拌溶解后过滤、调比重(即胶液的浓度),根据用户的不同需求加入各种颜色的食用色素,和加一定量的遮光剂二氧化钛等,静置保温后除气泡,再放入胶囊生产线上经胶囊帽体模具蘸胶、固化和烘干得到囊材。
2、包衣
以乙醇或/和丙酮为溶剂,将聚乙烯醇醋酸苯二甲酸酯(简称PVAP)配制成浓度为10%的包衣液,在包衣流水线上经至少一次包衣后,再烘干、脱模、切割、套合制成十二指肠靶向空心胶囊。
Claims (1)
1.一种十二指肠靶向空心胶囊,由明胶或植物胶加工的囊材和囊材外的包衣层所构成,其特征在于:所述的包衣层为聚乙烯醇醋酸苯二甲酸酯,囊材和包衣层的质量百分比分别为75%和25%。
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Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
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CN1596902A (zh) * | 2004-07-20 | 2005-03-23 | 王永发 | 三七总皂甙肠溶型制剂 |
CN1682699A (zh) * | 2005-02-28 | 2005-10-19 | 潮州市强基制药厂 | 结肠溶肠溶空心硬胶囊及生产工艺 |
CN101317830A (zh) * | 2008-07-10 | 2008-12-10 | 青岛益青药用胶囊有限公司 | 一种肠溶空心胶囊及其制备方法 |
CN101732281A (zh) * | 2010-01-26 | 2010-06-16 | 安徽黄山胶囊有限公司 | 一种肠溶空心胶囊的生产工艺 |
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Publication number | Priority date | Publication date | Assignee | Title |
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CN1596902A (zh) * | 2004-07-20 | 2005-03-23 | 王永发 | 三七总皂甙肠溶型制剂 |
CN1682699A (zh) * | 2005-02-28 | 2005-10-19 | 潮州市强基制药厂 | 结肠溶肠溶空心硬胶囊及生产工艺 |
CN101317830A (zh) * | 2008-07-10 | 2008-12-10 | 青岛益青药用胶囊有限公司 | 一种肠溶空心胶囊及其制备方法 |
CN101732281A (zh) * | 2010-01-26 | 2010-06-16 | 安徽黄山胶囊有限公司 | 一种肠溶空心胶囊的生产工艺 |
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Effective date of registration: 20160719 Address after: 242600, Xuancheng County, Anhui City, Jingde Province, white land town of Hong Chuan Patentee after: Anhui Huangshan Capsule Co.,Ltd. Address before: 242600 Anhui Province, Xuancheng City Jingyang town Jingde County Liang Jia No. 5 Patentee before: Liu Songlin |