CN113476417A - 一种口腔崩解片掩味外层及制备方法 - Google Patents
一种口腔崩解片掩味外层及制备方法 Download PDFInfo
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- CN113476417A CN113476417A CN202110926083.7A CN202110926083A CN113476417A CN 113476417 A CN113476417 A CN 113476417A CN 202110926083 A CN202110926083 A CN 202110926083A CN 113476417 A CN113476417 A CN 113476417A
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- taste
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- orally disintegrating
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Abstract
本发明涉及医药制备领域,具体是一种口腔崩解片掩味外层及制备方法,由掩味剂、填充剂、崩解剂、润滑剂及矫味剂制备而成,其中各组分按重量份计算,掩味剂0.0001~0.05份、填充剂0.2~0.4份、崩解剂0.1~0.5份、润滑剂0.01~0.10份、矫味剂0.01~0.10份。本发明通过将掩味剂与崩解剂、填充剂、润滑剂等加工成药物外层,外层中的掩味剂能作用于口腔黏膜上味蕾细胞或其神经传导细胞使苦味无法感知,可有效降低药物苦味,有助于人们吞咽苦味较重的药物,提高适口性。
Description
技术领域
本发明涉及医药制备领域,具体是一种口腔崩解片掩味外层及制备方法。
背景技术
无论中药、西药,其有效成分中苦味物质甚多,这些成分虽然味苦,但通常与药材的功效直接相关,而其味道苦是影响患者用药依从性的重要因素,药物剂型很多,但口崩片、分散片可以免饮水,对吞咽困难人群有更好的适应性,目前一般常用矫味剂掩味,比如阿司帕坦、安赛蜜、三氯蔗糖、蔗糖等甜味剂与香精等。
现有专利一种麻痹口腔掩味的口崩片及其制备方法(专利号:201410572552X),已经提到了使用花椒提取物掩味的方法,但现有专利中用花椒提取物掩味时容易给人们带来麻辣的不适感,且吞咽不适的患者并不适合适用花椒等刺激性食物,因此现有技术存在一定的局限性。
发明内容
有鉴于此,本发明提供一种口腔崩解片掩味外层及制备方法,本发明通过筛选出五种掩味剂溶液,其可以作用于口腔黏膜上味蕾细胞或其神经传导细胞使苦味无法感知,可有效降低药物苦味,有助于人们吞咽药物,并且适应人群广。
为了实现上述目的,本发明采用以下技术方案:
一种口腔崩解片掩味外层,由掩味剂、填充剂、崩解剂、润滑剂及矫味剂制备而成,其中各组分按重量份计算,掩味剂0.0001~0.05份、填充剂0.2~0.4份、崩解剂0.1~0.5份、润滑剂0.01~0.10份、矫味剂0.01~0.10份。
优选地,所述的填充剂选自甘露醇、微晶纤维素、山梨醇中的一种或多种,更优选为甘露醇和微晶纤维素。
优选地,所述的崩解剂选自交联聚维酮、低取代羟丙纤维素、交联羧甲基纤维素钠、微晶纤维素中的一种或多种;更优选为交联聚维酮。
优选地,所述的润滑剂选自硬脂酸镁、硬脂酸钙、硬脂富马酸钠中的一种或多种;更优选为硬脂酸镁。
优选地,所述的矫味剂为甜味剂和酸味剂的混合。
优选地,所述的矫味剂中的甜味剂选自阿司帕坦、葡萄糖、果糖、蔗糖、麦芽糖、乳糖、甜菊糖、甘草酸类、糖精钠、天门冬酰苯丙氨酸甲酯、甜蜜素、木糖醇、蛋白糖、新甲基橙皮二氢查耳酮中的一种或几种混合液;
优选地,所述矫味剂中的酸味剂为柠檬酸、苹果酸、酒石酸、乳酸、乙酸的一种或几种混合液。
优选地,所述的矫味剂还包括香精若干。
优选地,所述的掩味剂为麻醉剂或遮味剂或麻醉剂与遮味剂、麻醉剂与麻醉剂的混合。
优选地,所述掩味剂中的麻醉剂包括薄荷醇、细辛水提物、阿替卡因、丁香油,所述掩味剂中的遮味剂包括单宁酸,使用时单用其中一种或几种混合使用。
一种口腔崩解片掩味外层的制备方法,包括:
步骤a,称取一定量的填充剂、掩味剂、甜味剂、酸味剂与崩解剂,混合均匀备用;
步骤b,向步骤a的混合物中加入乙醇水溶液制粒,干燥后过筛,干颗粒备用;
步骤c,将被掩味药物与适当助剂混匀压制得到内层片剂;
步骤d,将步骤b得到的颗粒与润滑剂混合均匀后注入压皮机一层,将步骤c得到的内层片剂放入,再将步骤b的颗粒与润滑剂混合物注满压皮机压制即可。
本发明中被掩味的药物包括所有中药提取物和常用苦味化学药,尤其是紫苏、黄连、苦参、麻黄、黄芩、菊花、枇杷叶、防已、龙胆、穿心莲、紫花地丁的提取物,以及抗生素类、肿瘤化疗药、精神类等苦味药。
本发明的有益效果是:本发明通过将被掩味药物与崩解剂、填充剂、润滑剂等加工成药物内核,通过将本发明中的各组分裹一层后压片制成掩味外层,其可以大大降低药物苦味,有助于人们吞咽苦味较重的药物,提高适口性;具体地,筛选出的掩味剂在口腔与味蕾接触时间小于等于六十秒,掩味效果维持在大于等于三十秒并小于三十分钟,通过实验,我们筛选出五种掩味剂的溶液包括薄荷醇水溶液、单宁水溶液、细辛水溶液、阿替卡因水溶液、丁香油醇溶液,它们的浓度范围分别为,薄荷醇水溶液的浓度范围为百万分之一到万分之一、单宁水溶液的浓度范围为千分之二到百分之二、细辛水溶液的浓度范围为十克干品熬制四十到六百四十毫升溶液、阿替卡因水溶液的浓度范围为零点五到五毫克每一百毫升、丁香油醇溶液的浓度范围为百分之一点二五到百分之五,筛选出的上述掩味剂能作用于口腔黏膜上味蕾细胞或其神经传导细胞使苦味无法感知,可有效降低药物苦味,有助于人们吞咽药物。
具体实施方式
下面将结合实施例对本发明的技术方案进行清楚、完整地描述,显然,所描述的实施例仅仅是本发明一部分实施例,而不是全部的实施例。基于本发明中的实施例,本领域普通技术人员在没有做出创造性劳动前提下所获得的所有其他实施例,都属于本发明保护的范围。
实施例1
一种口腔崩解片掩味外层,由掩味剂、填充剂、崩解剂、润滑剂及矫味剂制备而成,其中,各组成成分按重量份计算,掩味剂0.0001~0.05份、填充剂0.2~0.4份、崩解剂0.1~0.5份、润滑剂0.01~0.10份、矫味剂0.01~0.10份;
具体我们选用薄荷醇0.0001份、甘露醇0.3份、交联聚维酮0.3份、交联羧甲基纤维素钠0.2份、柠檬酸0.01份、安赛蜜0.01份、葡萄糖0.1份、微晶纤维素0.07份、硬脂酸镁0.01份。
一种口腔崩解片掩味外层的制备方法,包括:
步骤a,称取甘露醇0.3份、交联聚维酮0.3份、交联羧甲基纤维素钠0.2份、微晶纤维素0.07份,薄荷醇0.0001份、柠檬酸0.01份、安赛蜜0.01份、葡萄糖0.1份,混合均匀备用;
步骤b,将步骤a的混合物加入乙醇水溶液制粒,干燥后过筛,干颗粒备用;
步骤c,将被掩味药物与助剂结合压制得到内层片剂;
步骤d,将步骤b得到的颗粒与硬脂酸镁混合后,注入压皮机一层,将步骤c制得的内层片剂放入,再将步骤b得到的颗粒与硬脂酸镁混合物注满压皮机,压制即可。
本实施例生产的掩味外层其内核适用于苦度值低于3.5度,属于微苦到中等苦度级别的。比如紫苏、麻黄、黄芩、菊花、枇杷叶、防已、紫花地丁的提取物,以及地氯雷他定、阿莫西林等苦味异味药,外壳与内核均适合在5-9秒内崩解完毕。
实施例2
一种口腔崩解片掩味外层,由掩味剂、填充剂、崩解剂、润滑剂及矫味剂制备而成,其中,各组成成分按重量份计算,掩味剂0.0001~0.05份、填充剂0.2~0.4份、崩解剂0.1~0.5份、润滑剂0.01~0.10份、矫味剂0.01~0.10份;
具体我们选用阿替卡因0.001份、甘露醇0.3份、交联聚维酮0.1份、交联羧甲基纤维素钠0.4份、柠檬酸0.01份、三氯蔗糖0.01份、果糖0.1份、微晶纤维素0.07份、硬脂酸镁0.01份。
一种口腔崩解片掩味外层的制备方法,包括:
步骤a,称取甘露醇0.3份、交联聚维酮0.1份、交联羧甲基纤维素钠0.4份、微晶纤维素0.07份、阿替卡因0.001份、柠檬酸0.01份、三氯蔗糖0.01份、果糖0.1份混合均匀备用;
步骤b,将步骤a的混合物加入乙醇水溶液制粒,干燥后过筛,干颗粒备用;
步骤c,将被掩味药物与助剂结合压制得到内层片剂;
步骤d,将步骤b得到的颗粒与硬脂酸镁混合后,注入压皮机一层,将步骤c得到的内层片剂放入,再将步骤b得到的颗粒与硬脂酸镁混合物注满压皮机,压制即可。
本实施例生产的掩味外层其内核适用于苦度值高于3.5度,属于极苦到中等苦度级别的,比如苦参、龙胆、穿心莲、山豆根、黄连的提取物。以及氯霉素、抗肿瘤药等苦味药,内核适合在外层崩解完毕后延迟30-50秒后开始崩解。
实施例3
一种口腔崩解片掩味外层,所由掩味剂、填充剂、崩解剂、润滑剂及矫味剂制备而成,其中,各组成成分按重量份计算,掩味剂0.0001~0.05份、填充剂0.2~0.4份、崩解剂0.1~0.5份、润滑剂0.01~0.10份、矫味剂0.01~0.10份;
具体我们选用单宁酸0.01份、山梨醇0.1份、交联聚维酮0.1份、交联羧甲基纤维素钠0.4份、柠檬酸0.01份、三氯蔗糖0.01份、果糖0.1份、蛋白糖0.02份、微晶纤维素0.27份、香精若干、硬脂酸镁0.01份。
一种口腔崩解片掩味外层的制备方法,其包括:
步骤a、称取山梨醇0.1份、交联聚维酮0.1份、交联羧甲基纤维素钠0.4份、微晶纤维素0.27份、单宁酸0.01份、柠檬酸0.01份、三氯蔗糖0.01份、蛋白糖0.02份、果糖0.1份、香精若干混合均匀备用;
步骤b、将步骤a的混合物加入乙醇水溶液制粒,干燥后过筛,干颗粒备用;
步骤c、将被掩味药物与助剂结合压制得到内层片剂;
步骤d、将步骤b得到的颗粒与润滑剂混合后,注入压皮机一层,将步骤c得到的内层片剂放入,再将步骤b得到的颗粒与润滑剂混合物注满压皮机,压制即可。
本实施例生产的掩味外层其内核适用于苦度值低于3.5度,属于微苦到中等苦度级别的,比如紫苏、麻黄、黄芩、菊花、枇杷叶、防已、紫花地丁的提取物,以及地氯雷他定、阿莫西林等苦味异味药,外层与内核均适合在7-17秒内崩解完毕。
实施例4
一种口腔崩解片掩味外层,由掩味剂、填充剂、崩解剂、润滑剂及矫味剂制备而成,其中,各组成成分按重量份计算,掩味剂0.0001~0.05份、填充剂0.2~0.4份、崩解剂0.1~0.5份、润滑剂0.01~0.10份、矫味剂0.01~0.10份;
具体我们选用细辛提取物0.015份、甘露醇0.25份、交联聚维酮0.4份、交联羧甲基纤维素钠0.2份、柠檬酸0.01份、甘草酸0.01份、蔗糖0.1份、微晶纤维素0.03份、香精若干、硬脂酸镁0.01份。
一种口腔崩解片掩味外层的制备方法,包括:
步骤a,称取甘露醇0.25份、交联聚维酮0.4份、交联羧甲基纤维素钠0.2份、微晶纤维素0.03份、细辛提取物0.015份、柠檬酸0.01份、甘草酸0.01份、蔗糖0.1份、香精若干混合均匀备用;
步骤b,将步骤a的混合物加入乙醇水溶液制粒,干燥后过筛,干颗粒备用;
步骤c,将被掩味药物与助剂结合压制得到内层片剂;
步骤d,将步骤b得到的颗粒与润滑剂混合后,注入压皮机一层,将步骤c得到的内层片剂放入,再将步骤b得到的颗粒与润滑剂混合物注满压皮机,压制即可。
本实施例生产的掩味外层其内核适用于苦度值低于3.5度,属于微苦到中等苦度级别的,比如紫苏、麻黄、黄芩、菊花、枇杷叶、防已、紫花地丁的提取物,以及地氯雷他定、阿莫西林等苦味异味药,内核适合在外层崩解后延迟30-50秒后开始崩解。
实施例5
一种口腔崩解片掩味外层,由掩味剂、填充剂、崩解剂、润滑剂及矫味剂制备而成,其中,各组成成分按重量份计算,掩味剂0.0001~0.05份、填充剂0.2~0.4份、崩解剂0.1~0.5份、润滑剂0.01~0.10份、矫味剂0.01~0.10份;
具体我们选用丁香油0.05份、甘露醇0.3份、交联聚维酮0.4份、交联羧甲基纤维素钠0.1份、柠檬酸0.01份、糖精钠0.01份、葡萄糖0.1份、微晶纤维素0.07份、香精若干、硬脂酸镁0.01份。
一种口腔崩解片掩味外层的制备方法:
步骤a,称取甘露醇0.3份、交联聚维酮0.4份、交联羧甲基纤维素钠0.1份、微晶纤维素0.07份,香精若干、丁香油0.05份、柠檬酸0.01份、糖精钠0.01份、葡萄糖0.1份混合均匀备用;
步骤b,将步骤a的混合物加入50%乙醇溶液制粒,干燥后过筛,干颗粒备用;
步骤c,将被掩味药物与助剂结合压制得到内层片剂;
步骤d,将步骤b得到的颗粒与润滑剂混合后,注入压皮机一层,将步骤c得到的内层片剂放入,再将步骤b得到的颗粒与润滑剂混合物注满压皮机,压制即可;
本实施例生产的掩味外层其内核适用于苦度值高于3.5度,属于极苦到中等苦度级别的,比如苦参、龙胆、穿心莲、山豆根、黄连的提取物,以及氯霉素、抗肿瘤药等苦味药,外层与内核均适合在6-15秒内崩解完毕。
验证实施例
因为我们产品仅仅是外层,为了做这个实验,我们把其作为完整药品成分,压制成片,然后检测,如果符合这些物理指标,就意味着作为外层也符合指标条件。
崩解时限、脆碎度、硬度测定
对本发明实施例1-5制备的片剂,按照崩解时限检查法、脆碎度检查法(中国药典2015年版通则0921、0923)进行测定。
崩解时限检查法
仪器装置主要结构为一能升降的支架与下端镶有筛网的不锈钢管,升降的支架上下移动距离为10mm±lmm,往返频率为每分钟30次,崩解篮不锈钢管,管长30mm,内径13.0mm,不锈钢筛网(镶在不锈钢管底部)筛孔内径710μm。
检查方法将不锈钢管固定于支架上,浸入1000ml杯中,杯内盛有温度为37℃±1℃的水约900ml,调节水位高度使不锈钢管最低位时筛网在水面下15mm±1mm,启动仪器,取本品1片,置上述不锈钢管中进行检查,应在60秒钟内全部崩解并通过筛网,如有少量轻质上漂或黏附于不锈钢管内壁或筛网,但无硬心者,可作符合规定论,重复测定6片,均应符合规定,如有1片不符合规定,应另取6片复试,均应符合规定。
脆碎度检查法
仪器装置内径约为286mm,深度为39mm,内壁抛光,一边可打开的透明耐磨塑料圆筒,筒内有一自中心轴套向外壁延伸的弧形隔片(内径为80mm±1mm,内弧表面与轴套外壁相切),使圆筒转动时,片剂产生滚动,圆筒固定于同轴的水平转轴上,转轴与电动机相连,转速为每分钟25转±1转,每转动一圈,片剂滚动或滑动至筒壁或其他片剂上。
检查法片重为0.65g或以下者取若干片,使其总重约为6.5g,片重大于0.65g者取9-10片,用吹风机吹去片剂脱落的粉末,精密称重,置圆筒中,转动100次,取出,同法除去粉末,精密称重,减失重量不得过1%,且不得检出断裂、龟裂及粉碎的片,本试验一般仅作1次。如减失重量超过1%时,应复测2次,3次的平均减失重量不得过1%,并不得检出断裂、龟裂及粉碎的片。
崩解时限、脆碎度测定试验中实施例1-5崩解时限、脆碎度、硬度,试验结果见表1。
样品 | 崩解时限/S | 脆碎度/% | 硬度/N |
实施例1 | 11-17 | 0.2-0.5 | 66-75 |
实施例2 | 15-26 | 0.2-0.4 | 61-66 |
实施例3 | 14-27 | 0.2-0.3 | 62-72 |
实施例4 | 14-26 | 0.2-0.3 | 59-68 |
实施例5 | 12-24 | 0.2-0.4 | 62-71 |
表1
崩解时限、脆碎度、硬度测定试验结果表明,实施例1-5制备的口崩片剂的崩解时限仅为50s以内,脆碎度为0.5%以下,硬度为59~75N,符合《口腔崩解片的剂型特点和质量控制会议纪要》及中国药典2015版的质量标准要求;
口崩片与漱口液掩味效果比较
将实施例1-5得到的口崩片剂与漱口液掩味效果进行比较,以黄连5g以50ml水浸2小时得到的液体作为苦味剂,对其进行掩味效果的比较,知情同意后筛选20人分为五组参加实验,每组四人,分别测试漱口液掩味后苦度、口崩片使用后苦度,取平均值后数据见表2.
表2
表2数据证明,本发明的实施例1-5的口崩片剂与原始漱口液相比,其效果相当,都可以大大降低药物苦味,同时使其不再具有恶心难咽的感觉,略苦能下咽。
尽管已经示出和描述了本发明的实施例,对于本领域的普通技术人员而言,可以理解在不脱离本发明的原理和精神的情况下可以对这些实施例进行多种变化、修改、替换和变型,本发明的范围由所附权利要求及其等同物限定。
Claims (9)
1.一种口腔崩解片掩味外层,由掩味剂、填充剂、崩解剂、润滑剂及矫味剂制备而成,其特征在于,各组分按重量份计算,掩味剂0.0001~0.05份、填充剂0.2~0.4份、崩解剂0.1~0.5份、润滑剂0.01~0.10份、矫味剂0.01~0.10份。
2.根据权利要求1所述的一种口腔崩解片掩味外层,其特征在于,所述的填充剂选自甘露醇、微晶纤维素、山梨醇中的一种或多种。
3.根据权利要求1所述的一种口腔崩解片掩味外层,其特征在于,所述的崩解剂选自交联聚维酮、低取代羟丙纤维素、交联羧甲基纤维素钠、微晶纤维素中的一种或多种。
4.根据权利要求1所述的一种口腔崩解片掩味外层,其特征在于,所述的润滑剂选自硬脂酸镁、硬脂酸钙、硬脂富马酸钠中的一种或多种。
5.根据权利要求1所述的一种口腔崩解片掩味外层,其特征在于,所述的矫味剂为甜味剂和酸味剂的混合,所述的矫味剂中的甜味剂选自阿司帕坦、葡萄糖、果糖、蔗糖、麦芽糖、乳糖、甜菊糖、甘草酸类、糖精钠、天门冬酰苯丙氨酸甲酯、甜蜜素、木糖醇、蛋白糖、新甲基橙皮二氢查耳酮中的一种或几种混合液;所述矫味剂中的酸味剂为柠檬酸、苹果酸、酒石酸、乳酸、乙酸的一种或几种混合液。
6.根据权利要求1所述的一种口腔崩解片掩味外层,其特征在于,所述的矫味剂还包括香精若干。
7.根据权利要求1所述的一种口腔崩解片掩味外层,其特征在于,所述的掩味剂为麻醉剂或遮味剂,所述掩味剂中的麻醉剂包括薄荷醇、细辛水提物、阿替卡因、丁香油,所述掩味剂中的遮味剂包括单宁酸,使用时单用其中一种或几种混合使用。
8.根据权利要求1-7任一所述的一种口腔崩解片掩味外层,其特征在于,各组成成分按重量份计算,薄荷醇0.0001份、甘露醇0.3份、交联聚维酮0.3份、交联羧甲基纤维素钠0.2份、柠檬酸0.01份、安赛蜜0.01份、葡萄糖0.1份、微晶纤维素0.07份、硬脂酸镁0.01份。
9.一种口腔崩解片掩味外层的制备方法,其特征在于,包括:
步骤a,称取一定量的填充剂、掩味剂、甜味剂、酸味剂与崩解剂,混合均匀备用;
步骤b,向步骤a的混合物中加入乙醇水溶液制粒,干燥后过筛,干颗粒备用;
步骤c,将被掩味药物与适当助剂混匀压制得到内层片剂;
步骤d,将步骤b得到的颗粒与润滑剂混合均匀后注入压皮机一层,将步骤c得到的内层片剂放入,再将步骤b的颗粒与润滑剂混合物注满压皮机压制即可。
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Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20070275067A1 (en) * | 2004-01-09 | 2007-11-29 | Norton Healthcare Ltd. | Compression Coated Tablet Comprising Sumatriptan |
US20120237602A1 (en) * | 2009-12-11 | 2012-09-20 | Yuki Ikeda | Press-coated orally-disintegrating tablets |
CN104383552A (zh) * | 2014-10-23 | 2015-03-04 | 温州芳植生物科技有限公司 | 一种药物掩味剂及其配制方法 |
CN104382869A (zh) * | 2014-10-23 | 2015-03-04 | 温州芳植生物科技有限公司 | 一种麻痹口腔掩味的口崩片及其制备方法 |
US20190350857A1 (en) * | 2018-05-17 | 2019-11-21 | Fertin Pharma A/S | Oral tablet for taste masking of active ingredients |
CN113069550A (zh) * | 2021-04-13 | 2021-07-06 | 福州爱建生物科技有限公司 | 通过提前用药可逆性掩盖口腔苦味的掩味剂配方 |
-
2021
- 2021-08-12 CN CN202110926083.7A patent/CN113476417A/zh active Pending
Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20070275067A1 (en) * | 2004-01-09 | 2007-11-29 | Norton Healthcare Ltd. | Compression Coated Tablet Comprising Sumatriptan |
US20120237602A1 (en) * | 2009-12-11 | 2012-09-20 | Yuki Ikeda | Press-coated orally-disintegrating tablets |
CN104383552A (zh) * | 2014-10-23 | 2015-03-04 | 温州芳植生物科技有限公司 | 一种药物掩味剂及其配制方法 |
CN104382869A (zh) * | 2014-10-23 | 2015-03-04 | 温州芳植生物科技有限公司 | 一种麻痹口腔掩味的口崩片及其制备方法 |
US20190350857A1 (en) * | 2018-05-17 | 2019-11-21 | Fertin Pharma A/S | Oral tablet for taste masking of active ingredients |
CN113069550A (zh) * | 2021-04-13 | 2021-07-06 | 福州爱建生物科技有限公司 | 通过提前用药可逆性掩盖口腔苦味的掩味剂配方 |
Non-Patent Citations (1)
Title |
---|
潘卫三主编: "《工业药剂学》", 31 August 2015, 中国医药科技出版社 * |
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