CN112469445A - 包含崩解剂成分和微小纤维状纤维素的崩解性固体物 - Google Patents
包含崩解剂成分和微小纤维状纤维素的崩解性固体物 Download PDFInfo
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- CN112469445A CN112469445A CN201980050840.XA CN201980050840A CN112469445A CN 112469445 A CN112469445 A CN 112469445A CN 201980050840 A CN201980050840 A CN 201980050840A CN 112469445 A CN112469445 A CN 112469445A
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- disintegrating
- starch
- disintegrating solid
- cellulose
- tablet
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Abstract
本发明的课题在于,提供一种在使用时需要溶解于液体中的固体物(片剂等)中无需使用发泡剂和酸性成分等即可加速崩解的技术。本发明的解决手段:提供包含微小纤维状纤维素的崩解性粒子组合物和包含该组合物的崩解性固体物等。
Description
技术领域
本发明涉及包含崩解剂成分和微小纤维状纤维素、且形状和重量相对较大的崩解性固体物等。
背景技术
以往,关于例如洗涤剂、消毒剂、杀虫剂、调味料加工食品、固体调味料、粉末饮料、入浴剂、含漱剂、水质调整剂、矿物质增强剂等在使用时需要溶解于液体中的固体物(片剂等),为了加速该固体物的崩解,一直使用糖或糖醇、淀粉等一般的添加剂和碳酸盐等发泡剂以及柠檬酸、抗坏血酸、琥珀酸、富马酸、苹果酸等酸性成分。或者,使用冷冻干燥等特殊的方法,降低片剂密度,加速崩解。
在专利文献1中记载了包含崩解剂成分和微小纤维状纤维素的崩解性粒子组合物以及包含该组合物的崩解剂。
由植物纤维制备且纤维的直径(短径)或粗细为数nm~数μm左右的纤维素,通常被称为“微细纤维状纤维素”或“微小纤维状纤维素”。关于这样的微小纤维状纤维素的制备例及其结构/特性/功能等,记载于专利文献2和专利文献3中。
这些微细化或微小纤维化的纤维素不损害作为原料的纤维素的基本特性(物理和化学稳定性、晶形(I型)等),而表面积显著增大,在作为纤维素原本的特征的亲水性显著增强的同时,形成由微小纤维的相互缠绕而构成的三维网状结构。其结果,在配合到糊状/膏状的商品中的情况下,通过与水/油滴、微粒等的相互作用而发挥保水(防止脱水)或保型的效果。而且,由于三维网状结构,可用于胶状商品的强度提高等的改性。
因此,到目前为止,这些纤维素以各种各样的用途被广泛用于各种的粉体(粉末)/纤维状物的粘结剂、砂纸的纸力强化剂、改良食品口感的增稠剂、提高食品保水性的保水剂、酒类的过滤助剂等。
作为这样的微细纤维状纤维素的利用例,例如,在专利文献4中记载了以特定比例含有水分散性复合物、胶凝剂以及水的凝胶状组合物,所述复合物以特定比例含有微细纤维状纤维素和在温水中溶解的亲水性高分子。作为该组合物的特性,在加热或加温处理时,抑制蛋白质的变性或水不溶性成分的沉淀,口感和口感良好。
另外,在专利文献5中记载了以特定比例含有高分散性纤维素复合物以及特定种类的多糖类的胶凝剂,所述复合物以特定比例包含微细纤维状纤维素、水溶性高分子和亲水性物质。其特征在于,与以往技术的高分散性纤维素复合物相比,在水中的崩解/分散性优异,可在工业上实用的分散条件下使用。
如上所述,即使在专利文献4或5的任一文献所记载的发明中,最终也将微细纤维状纤维素用作凝胶状组合物或胶凝剂的一种成分。而且,在专利文献3所记载的水分散性复合物中亲水性高分子为必需的成分,而且在专利文献4所记载的高分散性纤维素复合物中水溶性高分子也为必需的成分。
而且,在专利文献6中记载了重量较大(直径:12~18mm、重量:15~250mg左右)且相对较薄的片剂,其为具有极短的口腔内崩解时间和/或水中崩解时间的口腔内崩解片剂。然而,在该文献的实施例所记载的口腔内崩解片剂中不含微小纤维状纤维素。
现有技术文献
专利文献
专利文献1:国际公开第WO2015/163135号小册子;
专利文献2:日本特开昭56-100801号公报;
专利文献3:日本特开2009-203559号公报;
专利文献4:日本特开2004-283135号公报;
专利文献5:日本特开2006-290972号公报;
专利文献6:国际公开第WO2016/073917号小册子。
发明内容
发明所要解决的课题
在以往的技术中,为了加速如上所述的固体物的崩解,由于在该固体物中含有发泡剂和酸性成分,因此需要考虑该固体物的包装或内部状态、相对于装入有该固体物的体系的pH变化。例如,存在着下述的各种各样的问题:在包装内因来自发泡剂的二氧化碳气体的产生而导致包装体的膨胀或破裂;难以适用于对酸性不稳定的有效成分;伴随投入有该固体物的液体(例如锅中的汤等)的pH的变化,各种成分会发生变性;以及洗剂的活性降低等。
因此,需求一种无需使用发泡剂和酸性成分等即可加速如上所述的固体物的崩解的技术。
本发明的目的在于解决这样的课题,提供包含微小纤维状纤维素的崩解性固体物等。
用于解决课题的手段
本发明人为了解决上述课题而进行深入研究,结果发现以下预想之外的效果,从而完成了本发明:通过在具有作为崩解剂用途的以往公知的组合物中追加微小纤维状纤维素,由于该两者产生的协同效应,包含该组合物的各种崩解片剂中的片剂硬度增大,另一方面水中崩解时间更加缩短。
更具体而言,本发明提供以下的方案。
[方案1] 崩解性固体物,其包含崩解剂成分和微小纤维状纤维素。
[方案2] 方案1所述的崩解性固体物,其中,密度为0.80~3.00mg/mm3,重量为1000mg以上。
[方案3] 方案1或2所述的迅速崩解片剂,其中,直径为14mm以上。
[方案4] 方案1~3中所述的崩解性固体物,其中,片剂的绝对硬度为0.01N/mm2~4.00N/mm2。
[方案5] 方案1~4中任一项所述的崩解性固体物,其中,水中崩解时间为4分钟以下。
[方案6] 方案1所述的崩解性固体物,其中,微小纤维状纤维素的平均纤维长度为0.01~2mm和平均纤维直径为0.001~1μm。
[方案7] 方案1~6中任一项所述的崩解性固体物,其中,崩解剂成分为选自下述的1种成分以上:交聚维酮、交联羧甲纤维素钠、低取代羟丙基纤维素、羧甲基纤维素钙、淀粉和加工淀粉。
[方案8] 方案7所述的崩解性固体物,其中,淀粉为玉米淀粉、马铃薯淀粉、蜡质玉米淀粉、部分预胶化淀粉或预胶化淀粉,加工淀粉为羟基乙酸淀粉钠或羟丙基淀粉。
[方案9] 方案1~6中任一项所述的崩解性固体物,其进一步包含糖醇或糖。
[方案10] 方案1~6中任一项所述的崩解性固体物,其进一步包含赋形助剂(赋形辅助剂)。
[方案11] 方案10所述的崩解性固体物,其中,赋形助剂为晶体纤维素和/或粉末纤维素。
[方案12] 方案1~11中任一项所述的崩解性固体物的制备方法,其包括:将包含崩解剂成分和微小纤维状纤维素的崩解性粒子组合物与有效成分混合,并将所得的混合物进行压片。
[方案13] 方案12所述的制备方法,其中,施加10~100kN的压片压缩力进行压片。
发明效果
尽管本发明的崩解性固体物的形状和重量相对较大,但通过含有崩解剂成分和微小纤维状纤维素,由于它们的协同效应,可赋予各种崩解性固体物所要求的优异的崩解性。
由于这样的本发明的崩解性固体物所具有的优异的崩解性,例如,提高洗涤剂等固体物中所含有的有效成分的分散性,因此可缩短达到效果显现的时间。在有效成分为调味料的情况下,由于崩解迅速进行,因此具有烹调时间缩短等的优点。另外,在崩解性固体物为粉末饮料的情况下,崩解迅速进行的结果,在极短的时间内得到饮料。而且,在本发明的崩解性固体物中,为了加速固体物的崩解,由于不需要如以往那样含有碳酸盐等发泡剂和酸性成分,因此不易引起有效成分的pH变化或与之相伴的味道的变质、有效成分的活性降低。
附图说明
[图1] 显示出本发明的崩解性固体物(具有R面的片剂)的体积的计算方法。
具体实施方式
本发明涉及包含崩解剂成分和微小纤维状纤维素的崩解性固体物。作为微小纤维状纤维素,可使用以往公知的被称为“微细纤维状纤维素”或“微小纤维状纤维素”的任意纤维素。
本发明的崩解性固体物特别是不像口腔内崩解片剂那样直接给予/摄取到体内,而是具有在使用时需要溶解于液体中的、例如洗涤剂、消毒剂、杀虫剂、调味料加工食品、固体调味料、粉末饮料、入浴剂、含漱剂、水质调整剂、矿物质增强剂等的用途。
如上所述,“微小纤维状纤维素”通常是指由植物纤维制备且纤维的直径(短径)或粗细为数nm~数μm左右的纤维素,其不损害作为原料的纤维素的基本特性(物理和化学稳定性等),而表面积显著增大,在作为纤维素原本的特征的亲水性显著增强的同时,形成由微小纤维的相互缠绕而构成的三维网状结构。
纤维素的晶体结构可大致分类为I型~IV型。只有天然纤维素具有I型纤维素。由生物组织产生的纤维素是单晶纤维的聚集体,在单晶纤维内所有纤维素分子链均具有相同的平行链,并朝向相同的方向。II型纤维素是通过将天然纤维素纤维用浓碱溶液处理后进行水洗、干燥而得到。分子的填充方式为反平行链,且相邻的分子链朝向反方向。纤维素III型是通过将天然纤维素纤维或II型纤维素利用液体氨处理并进行洗涤、干燥而得到。纤维素IV型是通过将天然纤维素纤维或纤维素II型在甘油中加热至280℃而得到。不会从纤维素II型、III型、IV型再转变为作为天然纤维素纤维的I型,该过程是不可逆的过程。本发明中使用的微小纤维状纤维素优选具有纤维素I型的晶体结构。
这样的微小纤维状纤维素的干燥物可利用以往公知的任意技术、例如将直接干燥状态的纤维素纤维利用球磨机粉碎而直接以干燥状态得到(专利文献2)。或者,在置换工序中对由通过高压均化器将纤维素纤维的水分散液进行微原纤化而得到的微小纤维状纤维素构成的水悬浮状态的微小纤维状纤维素进行溶剂置换后,通过干燥工序除去溶剂,进一步在粉碎工序中进行粉碎,由此可得到微小纤维状纤维素的干燥物(专利文献3)。
作为本发明的崩解性粒子组合物所含的微小纤维状纤维素的适合例,可举出:作为纤维集合体且平均纤维长度为约0.01~2mm和平均纤维直径为约0.001~1μm、优选平均纤维直径为约0.01~0.1μm的微小纤维状纤维素(专利文献2)。例如,这样的微小纤维状纤维素(固体成分为10~35%的含水状态)以“CELISH”系列的商品名(平均纤维直径为约0.01~0.1μm)由Daicel Fine Chem株式会社销售各种等级的制品(产品)。
作为本发明的崩解性固体物所含的崩解剂成分,可使用本领域技术人员所公知的任意物质。例如可含有选自下述的任意的一种成分以上:交聚维酮、交联羧甲纤维素钠、低取代羟丙基纤维素、羧甲基纤维素钙、玉米淀粉、马铃薯淀粉、蜡质玉米淀粉、部分预胶化淀粉、和预胶化淀粉等淀粉、以及羟基乙酸淀粉钠和羟丙基淀粉等加工淀粉。尚需说明的是,交聚维酮是1-乙烯基-2-吡咯烷酮的交联聚合物的统称,交联羧甲纤维素钠是羧甲基纤维素钠的交联物的统称。
尚需说明的是,在这样的崩解剂成分中,例如,交聚维酮、交联羧甲纤维素钠、低取代羟丙基纤维素、羧甲基纤维素钙等均为对水不溶性的高分子。另外,作为淀粉,例如玉米淀粉、马铃薯淀粉、蜡质玉米淀粉、水不溶性部分预胶化淀粉、和水不溶性预胶化淀粉等为水不溶性的高分子,作为加工淀粉,例如羟基乙酸淀粉钠和羟丙基淀粉等的加工淀粉等为水不溶性的高分子。
在本发明的崩解性固体物中可进一步包含本领域技术人员所公知的任意的糖醇或糖作为赋形剂。
作为糖醇或糖的代表例,可举出:甘露糖醇、赤藓糖醇、木糖醇、海藻糖、乳糖、麦芽糖、麦芽糖醇、葡萄糖、蔗糖、果糖、甘露糖、和山梨糖醇等。而且,作为适合例,可举出:甘露糖醇、赤藓糖醇、木糖醇、海藻糖、乳糖。另外,糖或糖醇可为1种,还可使用从这些之中适当选择的2种以上的化合物。
而且,通过在本发明的崩解性固体物中含有晶体纤维素和/或粉末纤维素作为赋形助剂,可对崩解片剂赋予更优异的片剂硬度和崩解性。晶体纤维素和粉末纤维素是用酸将由纤维性植物所得的α-纤维素部分地解聚并纯化而得到的白色粉末状且不溶于水的物质。由于无味且为化学惰性,所以即使与药物混合也无变化,可用于医药品添加物、特别是配制片剂时的赋形助剂、粘合剂或崩解剂等用途。而且,除了医药品以外,还可作为乳化稳定剂等而用于化妆品和乳制品等食品中。
可使用本领域技术人员所公知的任意晶体纤维素和/或粉末纤维素,作为该晶体纤维素的代表例,可举出:AVICEL (FMC Corporation)、CEOLUS (旭化成Chemicals株式会社)、VIVAPUR (Rettenmaier)等市售品,作为粉末纤维素的代表例,可举出:KC FLOCK (日本造纸Chemical)、ARBOCEL (Rettenmaier)、SOLKA FLOC (木村产业)。
在本发明的固体物中,根据其目的/用途,能够以任意的含量包含各种各样的有效成分(活性成分)。
作为这样的有效成分的实例,例如可举出:如上所述的作为本发明的固体物的主要用途的洗涤剂、消毒剂、杀虫剂、调味料加工食品、固体调味料、粉末饮料、入浴剂、含漱剂、水质调整剂、矿物质增强剂等中所含的、本领域技术人员所公知的任意的各种成分。
而且,在本发明的崩解性固体物中,例如为了调整崩解力、粘合力和片剂的服用感等诸特性,可将本领域技术人员所公知的各种任意成分以不会因上述成分而损及本发明效果的范围内,进行适宜添加混合。作为这样的成分的实例,可举出:本领域技术人员所公知的赋形剂、崩解剂、赋形助剂、助流剂、润滑剂、甜味剂、矫味剂、香料和着色料等。
本发明的崩解性固体物中的各成分的配合量,可根据该固体成分和各成分的种类和用途等,由本领域技术人员适宜确定。通常,相对于崩解性固体物总重量,微小纤维状纤维素(换算为干燥物)为1~50重量%、崩解剂成分为1~30重量%、糖或糖醇(在含有的情况下)为20~98重量%的范围、以及晶体纤维素和/或粉末纤维素等赋形助剂(在含有的情况下)为1~40重量%的范围。
本发明的崩解性固体物,例如与在体内直接摄取的药用片剂和食品用片剂相比,具有相对较大的形状(尺寸)和重量。尚需说明的是,对固体物的形态/结构没有特别限制,例如,可获取片剂、薄片、胶囊、颗粒等本领域技术人员所公知的任意形态/结构。
本发明的崩解性固体物,其形状和重量是相对较大。即,重量通常为1000mg以上、优选为1500mg以上。而且,其密度通常为0.80~3.00mg/mm3、优选为1.1~2.00mg/mm3的范围。
在本发明的崩解性固体物为片剂的情况下,可获取本领域技术人员所公知的任意形状(例如,正平片、标准R面、糖衣R面、圆角片(平面)、平角片(平面)和两阶段R面等)。另外,片剂的直径可适时设定,通常,其直径为14mm以上、优选为20mm以上,厚度通常为4mm以上、优选为6mm以上。
而且,本发明的崩解性固体物具有优异的片剂硬度和崩解性。例如,在施加10~100kN的压片压缩力进行压片的情况下,崩解性固体物的绝对硬度为0.01N/mm2~4.00N/mm2、优选为0.05N/mm2~2.50N/mm2、进一步优选为0.10N/mm2~2.50N/mm2,且水中崩解时间为4分钟以下、优选为3分钟以下、特别优选为1分钟以下。
本发明的崩解性固体物可通过本领域技术人员所公知的任意的方法/手段来制备。例如,可通过包括下述工序的制备方法进行制备:将包含崩解剂成分和微小纤维状纤维素的崩解性粒子组合物与有效成分混合,并将所得的混合物施加例如10~100kN的压片压缩力进行压片的工序。
本发明的崩解性粒子组合物可通过本领域技术人员所公知的任意方法来制备。
例如,上述的崩解性粒子组合物可通过一次混合该组合物所含的各种成分来制备。
或者,也可通过各种的制粒工序法来制备。作为制粒手段,无特殊限定,也可通过干式制粒法或湿式制粒工序法等进行制备。
干式制粒法包括下述工序:将崩解性粒子组合物所含的各种成分粉末直接或与适当的粘合剂等混合且通过强压制成小块,并将其适当地破碎而进行制粒的工序。作为干式制粒法的具体实例,可举出:破碎制粒法或辊压缩法等。
湿式制粒法是通过在水的存在下使各成分分散并干燥而形成复合物的方法,作为湿式制粒法的具体例,可举出:喷雾干燥、滚动制粒、搅拌制粒和流化床制粒等喷雾法,冷冻干燥法,以及捏合制粒等,可通过这些的本领域技术人员所公知的任意方法进行制备。
在通过湿式制粒工序法进行制备的情况下,可通过同时使用崩解性粒子组合物所含的所有成分的一阶段制粒工序来制备本发明的崩解性粒子组合物,或者也可在多个阶段的湿式制粒工序中进行添加混合。
例如,可通过下述工序进行制备:使用任意的一种成分或两种成分的第一湿式制粒工序、包括至少使用第一湿式制粒工序中所得的制粒物和剩余成分的第二湿式制粒工序的二阶段制粒工序、或者包括在第二湿式制粒工序中所得的制粒物中进一步混合成分的第三工序的三阶段制粒工序等。
尚需说明的是,在上述制备方法的多个湿式制粒工序中,是否使用崩解性粒子组合物所含的各成分中的任意的一种或两种成分,可根据它们的种类/量等,由本领域技术人员适宜确定。
而且,在各制粒工序中,喷雾(spray)速度或气体供给温度、排气温度、气体供给量等诸条件,可根据各成分的种类/量等,由本领域技术人员适宜确定。
在各制粒工序的任一工序中,作为喷雾液的介质,例如可举出:水、乙醇、甲醇和丙酮等在医药品或食品中可接受的溶剂。或者,作为喷雾液,可举出:溶解有低于10%的该崩解性粒子组合物的成分的水溶液等,特别优选为水或该水溶液。
例如,可通过对投入有微小纤维状纤维素以外的成分的流化床制粒机喷雾微小纤维状纤维素的分散液(浆料),来制备本发明的崩解性粒子组合物。
需要说明的是,本发明的崩解性粒子组合物中可适宜含有的上述的各种任意成分,可在各制粒工序中进行适宜添加。或者,也可另外进一步设置湿式制粒工序,并在该阶段添加混合这些任意成分。
尚需说明的是,优选通过这样的湿式制粒工序法而制备的本发明的崩解性粒子组合物具有如下的物性。
(1) 平均粒径:50~200微米、(2) 水分:0.5~7重量%。
尚需说明的是,这些物性值通过以下的条件/方法进行测定。
平均粒径:使用φ75mm自动振荡筛(M-3T型,筒井理化学器械株式会社)对2g崩解性粒子组合物进行测定。
水分:使用卤素水分测定器(MX-50、株式会社A & D)对5g崩解性粒子组合物进行测定。
尚需说明的是,将在本说明书中引用的所有现有技术文献的记载内容作为参照而纳入本说明书中。
以下,通过实施例来更具体地说明本发明,但本发明并不限于这些实施例。
实施例1
[崩解性粒子组合物的制备1]
向流化床制粒机(FL-LABO、FREUND产业株式会社)中投入270g乳糖一水合物(GranuLac、Meggle Japan株式会社)、80g玉米淀粉(Cornstarch、日本食品化工株式会社)、20g部分预胶化淀粉(PCS PC-10、旭化成Chemicals株式会社),以12g/分钟的速度喷雾600g用水将微小纤维状纤维素的润湿物(CELISH FD200L、Daicel Fine Chem株式会社)稀释成5%的CELISH悬浮液,由此进行制粒,得到崩解性粒子组合物1。尚需说明的是,所得的崩解性粒子组合物1具有以下的物性。(1) 平均粒径:135微米、(2) 水分:2.5重量%。
[崩解性固体物的制备1]
在99.5重量份所得的崩解性粒子组合物1中加入0.5重量份硬脂酸钙(太平化学产业株式会社)并混合,使用简易片剂成型机(HANDTAB-100、市桥精机株式会社),在25kN的压片压缩力下进行压片,得到直径14.0mm、平角片、重量1500mg、厚度7.4mm的片剂。
实施例2
[崩解性固体物的制备2]
将所得的崩解性粒子组合物1与实施例1同样地进行压片,得到直径20.0mm、平角片、重量2500mg、厚度6.8mm的片剂。
实施例3
[崩解性固体物的制备3]
在49.5重量份所得的崩解性粒子组合物1、50重量份作为有效成分的汤料(粉末、株式会社SHIMAYA)中加入0.5重量份硬脂酸钙(太平化学产业株式会社)并混合,使用简易片剂成型机(HANDTAB-100、市桥精机株式会社),在15kN的压片压缩力下进行压片,得到直径20.0mm、平角片、重量2500mg、厚度7.4mm的片剂。
实施例4
[崩解性固体物的制备4]
在49.5重量份所得的崩解性粒子组合物1、50重量份作为有效成分的汤料(粉末、株式会社SHIMAYA)中加入0.5重量份硬脂酸钙(太平化学产业株式会社)并混合,使用简易片剂成型机(HANDTAB-100、市桥精机株式会社),在25kN的压片压缩力下进行压片,得到直径20.0mm、平角片、重2500mg、厚度6.3mm的片剂。
实施例5
[崩解性固体物的制备5]
在49.5重量份所得的崩解性粒子组合物1、50重量份作为有效成分的抗坏血酸(Vitamin C、Eisai Food Chemical株式会社)中加入0.5重量份硬脂酸钙(太平化学产业株式会社)并混合,使用简易片剂成型机(HANDTAB-100、市桥精机株式会社),在25kN的压片压缩力下进行压片,得到直径20.0mm、平角片、重量2500mg、厚度6.8mm的片剂。
实施例6
[崩解性固体物的制备6]
在49.5重量份所得的崩解性粒子组合物1、50重量份作为有效成分的氯化钠(和光纯药株式会社)中加入0.5重量份硬脂酸钙(太平化学产业株式会社)并混合,使用简易片剂成型机(HANDTAB-100、市桥精机株式会社),在25kN的压片压缩力下进行压片,得到直径20.0mm、平角片、重量2500mg、厚度5.7mm的片剂。
[比较例1]
将300g乳糖一水合物(GranuLac、Meggle Japan株式会社)、80g玉米淀粉(Cornstarch、日本食品化工株式会社)、20g部分预胶化淀粉(PCS PC-10、旭化成Chemicals株式会社)混合,得到混合物1。
将所得的混合物1与实施例4同样地进行压片,得到直径20.0mm、平角片、重量2500mg、厚度7.5mm的片剂。
[硬度和崩解性试验的评价]
对于以上的实施例和比较例中得到的各片剂,通过以下的方法测定硬度(和绝对硬度)和水中崩解时间。将硬度和崩解时间的测定结果示于表1中。
尚需说明的是,这些物性值通过以下的条件/方法进行测定。
密度:是“片剂重量/片剂体积”。密度可通过通常进行的一般方法来求出。例如,在平片的情况下,假定为圆柱,可由片剂的底面积和片剂厚度求出片剂体积,并计算密度,在立方体片的情况下,假定为立方体或长方体,可求出片剂体积,并计算密度。另外,在具有R面的片剂的情况下,可通过图1的方法求出片剂体积,并计算密度。
硬度:使用数字木屋式硬度计(株式会社藤原制作所),测定硬度(N)。
绝对硬度:是不依赖于片剂的厚度或片剂的直径的硬度。可根据利用数字木屋式硬度计而得到的硬度(N)来计算。例如,在平片的情况下,可由绝对硬度(N/mm2)=(2×硬度(N))/(π×片剂直径(mm)×片剂厚度(mm))来计算绝对硬度。
水中崩解时间:通过使用日本药典记载(其中,无辅助盘)的辅助筒的方法,并使用崩解试验器(NT-400、富山产业株式会社),测定水中崩解时间。
硬度(和绝对硬度)以及崩解时间分别进行6次的测定,将它们的平均值作为测定结果。
[表1]
崩解性固体物 | 实施例1 | 实施例2 | 实施例3 |
压片压缩力(kN) | 25 | 25 | 15 |
密度(mg/mm<sup>3</sup>) | 1.31 | 1.17 | 1.32 |
硬度(N) | 295 | 157 | 14 |
绝对硬度(N/mm<sup>2</sup>) | 1.80 | 0.74 | 0.20 |
水中崩解时间(秒) | 50 | 34 | 38 |
[表2]
崩解性固体物 | 实施例4 | 实施例5 | 实施例6 | 比较例1 |
压片压缩力(kN) | 25 | 25 | 25 | 25 |
密度(mg/mm<sup>3</sup>) | 1.27 | 1.17 | 1.39 | 1.07 |
硬度(N) | 31 | 24 | 42 | 12 |
绝对硬度(N/mm<sup>2</sup>) | 0.16 | 0.11 | 0.23 | 0.05 |
水中崩解时间(秒) | 34 | 53 | 39 | 290 |
由表1所示的结果证实了:在实施例1~6中,使用微小纤维状纤维素而得到的崩解性固体物,与使用不含微小纤维状纤维素的组合物而得到的固体物(比较例1)进行比较,具有更优异的崩解性、成形性,而且即使不含为了促进崩解等而使用的作为添加剂的碳酸盐等发泡剂,也显示出迅速的崩解时间。
实施例7
[崩解性固体物的制备7]
在49.5重量份所得的崩解性粒子组合物1、50重量份作为有效成分的硫酸钠(入浴剂的主要成分)中加入0.5重量份硬脂酸钙(太平化学产业株式会社)并混合,使用简易片剂成型机(HANDTAB-100、市桥精机株式会社),在15kN的压片压缩力进行压片,得到直径20.0mm、平角片、重量2500mg、厚度5.4mm的片剂。
实施例8
[崩解性固体物的制备8]
在49.5重量份所得的崩解性粒子组合物1、50重量份作为有效成分的碳酸氢钠(洗涤剂的主要成分)中加入0.5重量份硬脂酸钙(太平化学产业株式会社)并混合,使用简易片剂成型机(HANDTAB-100、市桥精机株式会社),在15kN的压片压缩力下进行压片,得到直径20.0mm、平角片、重量2500mg、厚度6.2mm的片剂。
将使用与实施例1~6同样的方法而评价的结果示于表3中。
证实了:即使在使用入浴剂或洗涤剂中通常所用的有效成分的情况下,也可显示出迅速的崩解时间。
[表3]
崩解性固体物 | 实施例7 | 实施例8 |
压片压缩力(kN) | 15 | 15 |
密度(mg/mm<sup>3</sup>) | 1.47 | 1.28 |
硬度(N) | 27 | 25 |
绝对硬度(N/mm<sup>2</sup>) | 0.16 | 0.13 |
水中崩解时间(秒) | 37 | 38 |
产业上的可利用性
本发明对具有优异的片剂硬度和崩解性的各种崩解性固体物等的研究/开发大有裨益。
Claims (13)
1.崩解性固体物,其包含崩解剂成分和微小纤维状纤维素。
2.权利要求1所述的崩解性固体物,其中,密度为0.80~3.00mg/mm3,重量为1000mg以上。
3.权利要求1或2所述的迅速崩解片剂,其中,直径为14mm以上。
4.权利要求1~3中所述的崩解性固体物,其中,片剂的绝对硬度为0.01N/mm2~4.00N/mm2。
5.权利要求1~4中任一项所述的崩解性固体物,其中,水中崩解时间为5分钟以下。
6.权利要求1所述的崩解性固体物,其中,微小纤维状纤维素的平均纤维长度为0.01~2mm和平均纤维直径为0.001~1μm。
7.权利要求1~6中任一项所述的崩解性固体物,其中,崩解剂成分为选自下述的1种成分以上:交聚维酮、交联羧甲纤维素钠、低取代羟丙基纤维素、羧甲基纤维素钙、淀粉和加工淀粉。
8.权利要求7所述的崩解性固体物,其中,淀粉为玉米淀粉、马铃薯淀粉、蜡质玉米淀粉、部分预胶化淀粉或预胶化淀粉,加工淀粉为羟基乙酸淀粉钠或羟丙基淀粉。
9.权利要求1~6中任一项所述的崩解性固体物,其进一步包含糖醇或糖。
10.权利要求1~6中任一项所述的崩解性固体物,其进一步包含赋形助剂。
11.权利要求10所述的崩解性固体物,其中,赋形助剂为晶体纤维素和/或粉末纤维素。
12.权利要求1~11中任一项所述的崩解性固体物的制备方法,其包括:将包含崩解剂成分和微小纤维状纤维素的崩解性粒子组合物与有效成分混合,并将所得的混合物进行压片。
13.权利要求12所述的制备方法,其中,施加10~100kN的压片压缩力进行压片。
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