CN102138915A - 一种口服药物制剂及其制备方法 - Google Patents
一种口服药物制剂及其制备方法 Download PDFInfo
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- Medicinal Preparation (AREA)
Abstract
本发明公开了一种口服药物制剂及其制备方法，它是由药物有效量的活性药物和辅料的均匀水分散液以溶液涂布法在涂布机上制备的膜剂，其中辅料含有至少一种水溶性高分子聚合物，离子交换树脂以及其它助剂。本发明与现有技术相比，所制备的口腔速溶膜制剂，在口腔中遇到唾液时能迅速溶解。在药物变成液体后，可迅速经口腔黏膜和胃肠道吸收进入体循环，口感良好，无砂粒感和苦涩感。这本发明采用的溶液涂布法为国内制药行业首创的生产工艺，生产的药物质量稳定，生产效率高，成本低，市场前景极为广阔。
Description
技术领域
本发明涉及一种新型口服药物制剂及其制备方法，特别是一种口腔速溶膜制剂及其制备方法。
背景技术
药剂学上对药物制剂按给药途径分为口服药物制剂和非口服药物制剂。口服药物制剂经口服给药，经胃肠道吸收发挥作。如：口服溶液剂、乳剂、混悬剂、颗粒剂、胶囊剂、片剂等。其中属于液体剂型的有口服溶液剂，乳剂，混悬剂等，而颗粒剂，胶囊剂和片剂则属于固体剂型。
液体口服药剂的优点在于服用容易简便，不需要用水送服；其缺点在于体积较大，不易携带，服用时需要容器计量，剂量不精确等。而固体口服药剂的优点在于包装体积小，容易携带，服用剂量准确；其缺点在于需要用水送服，对吞咽有困难的患者如老人和儿童等造成不便。
发明内容
本发明的目的是提供一种服用方便，溶解迅速且生物利用度高的口服制剂，该制剂在口腔中能迅速溶解于唾液而无需饮水，药物在溶解后可迅速经口腔黏膜和胃肠道进入体循环，增大药物的生物利用度，加快药物起效时间。
本发明的另一目的是提供一种上述制剂的制备方法。
本发明的上述目的通过如下过程来实现：
一种口服药物制剂，它是由药物有效量的活性药物和辅料的均匀水分散液以溶液涂布法在涂布机上制备的膜剂，其中辅料含有至少一种水溶性高分子聚合物，离子交换树脂以及其它助剂。
所述活性药物成分包括但不限于化学药物，中药提取剂和生物活性成分。
活性药物的具体例子包括但不限于硝酸甘油，阿立必利，头孢克洛，苯坐卡因，咖啡碱，氢溴酸石美沙芬，愈创木酚甘油醚，氯雷他定，L-茶氨酸，奥美拉唑，盐酸伪麻黄碱和维生素，如烟酸或视黄醇。
辅料包括至少一种水溶性聚合物做为成膜物质；离子交换树脂用于络合口感不好的活性药物，使之在口腔中释放后无明显异味；其它助剂通常包括口服药物制剂常用的掩味剂，增塑剂，食用色素等。
所述水溶性高分子聚合物包括但不限于天然高分子聚合物，改性天然高分子聚合物和合成高分子聚合物。
水溶性聚合物包括但不显普鲁兰多糖，羟丙基甲基纤维素，羟乙基纤维素，羟丙基纤维素，聚乙烯吡咯烷酮，羧甲基纤维素，聚乙烯醇，藻酸钠，聚乙二醇，黄X胶，瓜耳胶，金合欢胶，阿拉伯树胶，聚丙烯酸，甲基丙烯酸甲酯共聚物，羧基乙烯基聚合物，直链淀粉，高直链淀粉，羟丙基化高直链淀粉，糊精，果胶，甲壳质，脱乙酰壳多糖，果聚糖，骨胶原，明胶，玉米蛋白，谷蛋白，大豆蛋白分离物，乳清蛋白分离物，酪蛋白及它们的混合物。
所述离子交换树脂是药用阴离子交换树脂如磺酸基聚苯乙烯-丁二烯共聚树脂和药用阳离子交换树脂如季胺基聚苯乙烯-丁二烯共聚树脂。
掩味剂中包括代表性的食用油质香精，如：薄荷油，肉桂油，胡椒薄荷油，丁香油，月桂油，百里香油，香柏叶油，肉豆蔻油，鼠尾草油和苦杏仁油。同样有用的是人造的，天然的或合成的水果香料，例如香草，巧克力，咖啡，可可豆和柑橘树油，包括柠檬，橙，葡萄，酸橙和柚子，以及水果香精，包括苹果，梨，桃，草莓，树莓，樱桃，李子，杏。
增塑剂包括代表性的乙二醇，丙二醇，木糖醇，山梨醇，甘露糖醇，麦芽糖醇，乳糖醇，果糖，葡萄糖，蔗糖，麦芽糖，甘油，聚乙二醇。
本发明制剂的制备工艺，按以下步骤进行：
a)活性药物与离子交换树脂通过现有工艺制成无明显口腔异味的复合物；
b)水溶性高分子聚合物和其它辅料溶于适量水中成均匀水溶液；
c)调节该水溶液粘度至1000～30000cps；
d)搅拌下将复合物1加入溶液3，搅拌均匀；
e)减压脱去气泡，待用；
f)将溶液5转移至涂布机机头，涂布在作为基质的聚酯剥离膜或防粘纸表面成均匀的膜；
g)传送进入鼓风烘箱，在50～80℃温度下除去水分，制成厚度为25～250微米的固体薄膜；
e)将薄膜切割成合适大小，每片薄膜重量约为50～200毫克。
本发明的使用方法为：将口腔速溶药膜置于舌上或舌下，1分钟内迅速溶解于唾液，完成服药过程。
本发明的优点在于：本发明制备的口腔速溶膜制剂，在口腔中遇到唾液时能迅速溶解。在药物变成液体后，可迅速经口腔黏膜和胃肠道吸收进入体循环，口感良好，无砂粒感和苦涩感，采用的溶液涂布法为国内制药行业首创的生产工艺，生产的药物质量稳定，生产效率高，成本低，市场前景极为广阔。
具体实施例：
下面结合实施例对本发明作详细的说明。
实施例1：
处方：
本实施例主药为头孢克洛，高分子聚合物成膜剂为聚乙烯基吡咯烷酮和羟乙基纤维素，聚乙二醇400是增塑剂，阴离子交换树脂，薄荷醇和三氯蔗糖是掩味剂，FD&C食用红色色素40号是用于增加膜剂的外观美感。
本实施例的制备工艺，通过以下步骤进行：
1.按上述处方中主药15g头孢克洛溶于1800g 40℃水中，加入阴离子交换树脂，搅拌24小时；
2.减压抽滤除去水分，制成头孢克洛/阴离子交换树脂复合物；
3.上述辅料10.4g聚乙烯基吡咯烷酮和11.3g羟乙基纤维素加入180g 40℃水中搅拌2小时；
4.加入20g 40℃水调节该水溶液粘度至3500cps；
5.剧烈搅拌下将复合物2加入溶液4，继续搅拌2小时；
6.搅拌下加入1.5g薄荷醇，11.1g三氯蔗糖FD&C食用红色色素40号搅拌30分钟；
7.减压脱去气泡，待用；
8.将溶液7转移至涂布机机头，涂布在作为基质的防粘纸表面成均匀的膜；
9.传送进入鼓风烘箱，在50～80℃温度下除去水分，制成厚度为25微米的固体薄膜；
10.将薄膜切割成长25毫米，宽15毫米的小片，每片薄膜重量约为50毫克。
实施例2：
处方：
本实施例主药为阿立必利，高分子聚合物成膜剂为聚乙烯基吡咯烷酮和羟丙基纤维素，聚乙二醇400是增塑剂，阳离子交换树脂(美国罗门哈斯公司Amberlite IRA400)和木糖醇是掩味剂，FD&C食用蓝色色素1号和红色色素40号是用于增加膜剂的外观美感。
本实施例的制备工艺，通过以下步骤进行：
1.按上述处方中主药5g阿立必利溶于100g无水乙醇，加入阳离子交换树脂，搅拌4小时；
2.旋转减压蒸馏出去无水乙醇，制成阿立必利/阳离子交换树脂复合物；
3.上述辅料12.7g聚乙烯基吡咯烷酮和17.9g低分子量的羟丙基纤维素加入180g 40℃水中搅拌2小时；
4.加入20g 40℃水调节该水溶液粘度至8400cps；
5.剧烈搅拌下将复合物2加入溶液4，继续搅拌2小时；
6.搅拌下加入7.6g木糖醇，0.02g FD&C食用蓝色色素1号和FD&C食用红色色素40号搅拌30分钟；
7.减压脱去气泡，待用；
8.将溶液7转移至涂布机机头，涂布在作为基质的防粘纸表面成均匀的膜；
9.传送进入鼓风烘箱，在50～80℃温度下除去水分，制成厚度为50微米的固体薄膜；
10.将薄膜切割成长25毫米，宽15毫米的小片，每片薄膜重量为75毫克。
实施例1、2的技术指标如下：
将口腔速溶药膜放入37℃的50ml恒温水浴中，秒表计时，完全溶解时间小于1分钟。
Claims (6)
1.一种口服药物制剂，其特征在于：它是由药物有效量的活性药物和辅料的均匀水分散液以溶液涂布法在涂布机上制备的膜剂，其中辅料含有至少一种水溶性高分子聚合物，离子交换树脂以及其它助剂。
2.根据权利要求1所述的一种口服药物制剂，其特征在于：所述活性药物成分包括但不限于化学药物，中药提取剂和生物活性成分。
3.根据权利要求1所述的一种口服药物制剂，其特征在于：所述水溶性高分子聚合物包括但不限于天然高分子聚合物，改性天然高分子聚合物和合成高分子聚合物。
4.根据权利要求1所述的一种口服药物制剂，其特征在于：所述离子交换树脂是药用阴离子交换树脂和药用阳离子交换树脂。
5.根据权利要求1所述的一种口服药物制剂，其特征在于：所述活性药物成分含量为1％～50％。
6.权利要求1所述的一种口服药物制剂的制备方法，其特征在于：将活性药物和离子交换树脂通过适当的工艺制成活性药物/离子交换树脂复合物；该复合物与其它辅料混合于水中成为均匀的分散溶液，以溶液涂布法在涂布机上将该分散溶液均匀涂布于聚酯剥离薄膜或防粘纸表面形成薄膜，在50℃～80℃烘干并切割成药膜。
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| CN103340841A (zh) * | 2013-07-02 | 2013-10-09 | 康美药业股份有限公司 | 一种中药膜剂、其制备方法和用途 |
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