CN110960585A - 大枣活性成分的超微粉分散片及其制备方法 - Google Patents
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Abstract
本发明公开了一种大枣活性成分的超微粉分散片及其制备方法。本发明提供的大枣活性成分分散片,至少包括大枣活性成分和基质材料;其中,所述基质材料为大枣纤维素的部分水解物;所述大枣活性成分均匀分散于所述基质材料中。本发明提供的大枣活性成分分散片是一种可全组分保留大枣活性成分,并且极少采用外加辅料的大枣口服片剂。
Description
技术领域
本发明属于天然产物加工及制剂产品领域,具体涉及一种大枣活性成分的超微粉分散片及其制备方法。
背景技术
红枣是中华民族传统饮食中的瑰宝,是国家卫计委首批公布的药食两用食物之一。红枣的药用的价值被大量记录,其应用的范围被不断拓展。数千年的中华传统医学实践肯定了红枣具有补中益气、养血和营、益胃生津、解毒和药、安神定志的功效。现代医学也确认了红枣具有提高免疫力、胃肠保护、抗氧化、抗衰老、抗肿瘤等生物医学功效。
但目前红枣的使用主要还停留在以直接食用(以干枣、原枣)为主的低级阶段,红枣的生物医学价值和红枣的健康提升价值还远没有发挥出来。特别是红枣中有效成分的制剂产品的开发则相对落后,目前制剂产品主要以红枣中有效成分的口服液以及干粉为主。
片剂是一种方便携带和使用的固体制剂,且固体制剂相对更易于保存和保持天然产物中有效成分的活性。然而红枣中含有的多糖等活性成分,吸湿性强,采用常规方法粉碎得到的大枣微粉颗粒的流动性差,常规湿法压片需要制粒干燥,这些过程使用有机溶解以及加热干燥,造成红枣活性成分的损失,这些因素使得红枣片剂制剂的开发较为困难。此外,通常要达到一定的生物功效,需要使用的枣粉量较大,由于片剂单片质量以及常规制片过程中辅料的添加,使得单片片剂的活性成分含量低,难以满足临床需要。
中国发明专利CN101926433A报道了一种红枣多糖泡腾片及其制备方法,其中活性成分仅为红枣多糖,含量不超过20%片重,适合各类人群食用,携带、食用方便。中国发明专利CN109646607A报道了一种将大枣及山药、山楂水煎后的药汤浓缩而制备咀嚼片的工艺,该途径得到的片剂中所含的红枣的活性成分含量非常低。
红枣中含有的活性成分包括多糖、多酚、环磷酸腺苷等多种水溶性活性成分,同时含有20%左右(依据产地不同而略有变化)的纤维素、半纤维素等水不溶性的成分。由纤维素部分水解得到的微晶纤维素,不仅是一种良好的膳食纤维(益生元),同时也是性能优良的片剂辅料。目前尚无关于红枣全活性成分的片剂的报道及相关专利。如能利用红枣中所含纤维素等大分子为辅料,将水提有效成分分散于辅料中制备片剂,不仅可以实现红枣中活性成分的全组分保留,还可以极大的减少外加辅料的用量,使得片剂成分几乎100%来自大枣本身。
发明内容
本发明的目的是提供一种大枣活性成分的超微粉分散片及其制备方法。
本发明提供的大枣活性成分分散片,至少包括大枣活性成分和基质材料;其中,所述基质材料为大枣纤维素的部分水解物;
所述大枣活性成分均匀分散于所述基质材料中;
上述大枣活性成分分散片中,所述活性成分为水溶性活性成分;
所述大枣纤维素的部分水解物为经水提取的有效成分;具体至少包括多糖和多酚。
所述部分水解物为微粉纤维素颗粒;
所述微粉纤维素颗粒的粒径为20~50μm;平均聚合度为100~200。
所述大枣活性成分与大枣纤维素的部分水解物的质量比为1-2:1;具体为1.3:1或1.25:1;
所述大枣活性成分分散片还包括粘合剂;
所述粘合剂具体选自硬脂酸镁和聚乙烯吡咯烷酮K30中至少一种;
所述硬脂酸镁的质量百分含量为所述大枣活性成分分散片片重的1~3%;
所述聚乙烯吡咯烷酮K30的质量百分含量为所述大枣活性成分分散片片重的1~2%。
本发明提供的制备所述大枣活性成分分散片的方法,如图1所示,包括:
1)将干燥的大枣去皮、切片、粉碎为大枣粉末;
2)以水提取步骤1)所得大枣粉末,将提取液和提取后枣渣分离;
3)将步骤2)所得提取液减压蒸发浓缩,得到浓缩液,干燥得到水提取物粉末;
4)将步骤2)所得枣渣进行酸解,分离所得水解液中的固体颗粒并干燥粉碎;
5)将步骤4)干燥粉碎后的固体颗粒与步骤3)所得水提取物粉末混合制粒,真空干燥后压片,即得。
上述方法的步骤1)中,所述大枣粉末的粒径为80目~270目;
所述步骤2)以水提取步骤中,所述水和大枣粉末的质量比为4:1~10:1;具体为5:1或6:1;
提取温度为10~50℃;具体为30℃;
提取时间为6~12h;具体为8h。
所述步骤4)酸解步骤中,酸解剂为稀盐酸;
所述稀盐酸的质量百分浓度为5%~15%;具体为10%;
酸解温度为80~95℃;具体为90℃;
酸解时间为80~360min;具体为240min;
所述稀盐酸与枣渣的用量比为每1kg枣渣使用稀盐酸3~6L;具体为每1kg枣渣使用稀盐酸2~4L;所述枣渣的质量以干基计;
所述步骤4)粉碎可以通过诸如低温超细粉碎、高速剪切粉碎等技术实现;
所述步骤5)中,所述步骤4)干燥粉碎后的固体颗粒与步骤3)所得水提取物粉末的质量比为1:1-2;
所述步骤5)真空干燥步骤中,干燥温度不超过50℃,干燥后产品中的含水量(质量分数)低于5%(湿基)。
所述方法还包括:在所述步骤4)之后,步骤5)制粒步骤之前,向体系中加入粘合剂的乙醇水溶液;
所述乙醇水溶液中,乙醇的质量百分浓度为20-40%;具体为30%。
本发明中,所述大枣具体可为各种大枣品种,如可为新疆阿克苏灰枣或新疆阿克苏骏枣。
本发明提供的大枣活性成分分散片的食用方法为口服。
本发明提供的大枣活性成分分散片是一种可全组分保留大枣活性成分,并且极少采用外加辅料的大枣口服片剂。
附图说明
图1为本发明大枣活性成分分散片的制备工艺流程图。
具体实施方式
下面结合具体实施例对本发明作进一步阐述,但本发明并不限于以下实施例。所述方法如无特别说明均为常规方法。所述原材料如无特别说明均能从公开商业途径获得。
本发明提供一种大枣活性成分分散片及其制备工艺,可全组分保留大枣活性成分,极少采用外加辅料的大枣口服片剂。
该分散片是以大枣中所含纤维素的部分水解物为骨架,将大枣中所含的多糖、多酚、环磷酸腺苷等水溶性物质负载与纤维素骨架上,制粒压片得到的。除了制粒压片时加入少量的制粒辅料聚乙烯吡咯烷酮(PVP K30)以及润滑剂硬脂酸镁外,片中的其他成分均来自大枣自身。
大枣中所含的纤维素大约有10%~20%左右(依据产地不同而略有变化),通过酸性水解纤维素,可得到平均聚合度100~200的微粉纤维素,粒径大小为20~50μm,这种微粉纤维素的性质类似微晶纤维素,具有较好的颗粒流动性,以及较大的负载表面积,对水溶性物质有很好的吸附能力。同时,这种微粉纤维素可在水中形成稳定的分散体系。
为了制备本发明的分散片,需要先将大枣中的水溶性活性成分提出,而后将提取剩余的枣渣进行酸解并得到含有微粉纤维素的固体。大枣中的水溶性活性成分主要包括多糖(水溶性)、多酚、环磷酸腺苷,为保持这些活性成分的稳定性,本发明采取了将红枣先脱皮、微粉化,而后在较低温度下水提的工艺。在提取之前,需要将脱皮去核后的红枣粉碎到140目以下。这种粉碎可以通过诸如低温超细粉碎,或者气流粉碎等粉碎技术实现。粉碎后的枣粉在温度为30~50℃条件下,以水为提取剂提取。为提高提取率,可采取诸如微波提取等提取技术,依据提取技术不同,水和红枣粉末的用量为4:1~10:1,提取时间为2~12h。提取后的水溶液,经过进一步的减压蒸发浓缩(温度不超过50℃)干燥后得到水溶性提取物粉末。
大枣中水提取物的总量占大枣果肉的20~40%(干基),水提后的枣渣的量占大枣果肉的40~70%(干基)。枣渣主要含有水不溶性物质,包括淀粉、纤维素、果胶等,还含有一些难溶的多聚糖,也具有非常重要的生物活性。本发明中提取剩余的枣渣中绝干固体物质较典型的组成是:多糖及淀粉含量40%~70%,纤维素含量为15%~25%。该枣渣在酸性水高温水解下,可去除大部分淀粉和多糖,并将纤维素水解为低聚合度的纤维素。本发明采用的浓度为5%~15%盐酸,在酸解温度为80~95℃溶解淀粉,同时水解纤维素。盐酸与枣渣的用量比为:1kg枣渣(干基)使用盐酸3~6L;在该条件下,酸解80~360min,可去除70%以上的淀粉和多糖,并将纤维素的平均聚合度降低至100~200,得率为50%~75%。水解枣渣的水解液经离心与过滤分离后,将固体物质干燥以脱出其中的水分和酸,使其中的水分降低到5%(湿基)以下,而后进一步粉碎至20~50μm,制得微细纤维素粉。粉碎可以通过诸如低温超细粉碎、高速剪切粉碎等技术实现。
将微细纤维素粉与水溶性提取物粉末以1:1~1:2的比例(质量比)混合,以含有10%聚乙烯吡咯烷酮的水-乙醇溶液(乙醇质量分数为30%)为粘合剂,高速剪切搅拌制粒;制粒经真空干燥后压片。制粒真空干燥条件为,干燥温度不超过50℃,最终含水量(质量分数)低于5%(湿基)。
下面通过具体实施例对本发明进行说明,但本发明并不局限于此,凡在本发明的精神和原则之内所做的任何修改、等同替换和改进等,均应包含在本发明的保护范围之内。
下述实施例中所使用的实验方法如无特殊说明,均为常规方法。
下述实施例中所用的材料、试剂等,如无特殊说明,均可从商业途径得到。
实施例1
本实施例以新疆阿克苏灰枣为原料,提取大枣活性成分并制备微细纤维素。所采用的新疆阿克苏灰枣的主要成分如表1所示(均以绝干枣计)。
将1kg脱皮去核的干枣,通过低温超细粉碎粉碎到140目。
将粉碎后的枣粉分散到纯水中,在30℃条件下,以100r/min的搅拌提取水溶性成分。水和红枣粉末的用量为6:1(质量比),提取时间为12h。提取后的水溶液,经过进一步的减压浓缩(温度40℃)后得到水溶性提取物的浓缩液,浓缩液干燥后得到水溶性提取物粉末324g。水提后的枣渣干重为528g,组成是(占绝干固体枣渣的质量分数):多聚糖及淀粉含量65%,纤维素含量为20%。上述枣渣分散于2L浓度为10%的盐酸中,温度为90℃溶解淀粉,同时水解纤维素,酸解时间240min,淀粉去除率72%,纤维素的平均聚合度降低至180,得率为71%。水解枣渣的水解液经离心与过滤分离后,将固体物质干燥以脱出其中的水分和酸,水分降低到5%(湿基)以下,低温超细粉碎粉粉碎至50μm,得到微细纤维素粉182g。
表1原料(新疆阿克苏灰枣)的主要成分
*注:按绝干枣计
实施例2
本实施例以实施例1中得到的水溶性提取物和微细纤维素粉为原料制备分散片。将实施例1中得到的微细纤维素粉180g与240g水溶性提取物混合后,以含有10%聚乙烯吡咯烷酮(K30,国药集团化学试剂有限公司生产)的水-乙醇溶液(乙醇质量分数为30%)为粘合剂,使用高速剪切搅拌制粒机进行制粒。粘合剂的用量为80g。所得湿粒在40℃下真空干燥48h,至最终湿含量(质量分数)低于5%(湿基)。干燥后的颗粒过80目筛网,并加入1%硬脂酸镁(质量比)作为润滑剂,以单冲压片机进行压片,得到大枣活性成分分散片。该分散片的最终组成及含量如表2所示。对该分散片中所含的红枣主要活性物质进行分析,结果如表3所示,可见该分散片包含了红枣的主要活性成分,且含量基本与红枣本身相当。
表2分散片的组成及含量
*注:按绝干片重计
表3分散片的有效成分分析
*注:按绝干片重计
实施例3
本实施例以新疆阿克苏骏枣为原料,得到水溶性提取物和微细纤维素粉,并依此原料制备分散片。所采用的新疆阿克苏骏枣的主要成分如表4所示(均以绝干枣计)。将1kg干枣脱皮去核后,通过低温超细粉碎粉碎到140目。将粉碎后的枣粉分散到纯水中,在50℃条件下,以100r/min的搅拌提取水溶性成分。水和红枣粉末的用量为5:1(质量比),提取时间为8h。提取后的水溶液,经过进一步的减压浓缩(温度50℃)后得到水溶性提取物的浓缩液,浓缩液干燥得到水溶性提取物粉末330g;水提后的枣渣干重为548g,组成是(占绝干固体枣渣的质量分数):多聚糖及淀粉含量56%,纤维素含量为24%。上述枣渣分散于2.5L浓度为10%的盐酸中,温度为90℃溶解淀粉与多糖,同时水解纤维素,酸解时间240min,淀粉与多糖去除率79%,纤维素的平均聚合度降低至160,得率为68%。水解枣渣的水解液经离心与过滤分离后,将固体物质干燥以脱出其中的水分和酸,水分降低到5%(湿基)以下,低温超细粉碎粉碎至50μm,得到微细纤维素粉176g。
将上述微细纤维素粉200g与250g水溶性提取物混合后,以含有10%聚乙烯吡咯烷酮的水-乙醇溶液(乙醇质量分数为30%)为粘合剂,使用高速剪切搅拌制粒机进行制粒。粘合剂的用量为100g。所得湿粒在40℃下真空干燥48h,至最终湿含量(质量分数)低于5%(湿基)。干燥后的颗粒过80目筛网,并加入1%硬脂酸镁(质量比)作为润滑剂,以单冲压片机进行压片,得到大枣活性成分分散片。对该分散片中所含的红枣主要活性物质进行分析,结果如表5所示。
表4原料(新疆阿克苏骏枣)的主要成分
*注:按绝干枣计
表5分散片的有效成分分析
*注:按绝干片重计。
Claims (9)
1.一种大枣活性成分分散片,至少包括大枣活性成分和基质材料;其特征在于:所述基质材料为大枣纤维素的部分水解物;
所述大枣活性成分均匀分散于所述基质材料中。
2.根据权利要求1所述的大枣活性成分分散片,其特征在于:所述活性成分为水溶性活性成分;
所述大枣纤维素的部分水解物为经水提取的有效成分;具体至少包括多糖和多酚。
3.根据权利要求1或2所述的大枣活性成分分散片,其特征在于:所述部分水解物为微粉纤维素颗粒;
所述微粉纤维素颗粒的粒径为20~50μm;平均聚合度为100~200。
4.根据权利要求1-3任一所述的大枣活性成分分散片,其特征在于:所述大枣活性成分与大枣纤维素的部分水解物的质量比为1-2:1。
5.根据权利要求1-4任一所述的大枣活性成分分散片,其特征在于:所述大枣活性成分分散片还包括粘合剂;
所述粘合剂具体选自硬脂酸镁和聚乙烯吡咯烷酮K30中至少一种;
所述硬脂酸镁的质量百分含量为所述大枣活性成分分散片片重的1~3%;
所述聚乙烯吡咯烷酮K30的质量百分含量为所述大枣活性成分分散片片重的1~2%。
6.一种制备权利要求1-5任一所述大枣活性成分分散片的方法,包括:
1)将干燥的大枣去皮、切片、粉碎为大枣粉末;
2)以水提取步骤1)所得大枣粉末,将提取液和提取后枣渣分离;
3)将步骤2)所得提取液减压蒸发浓缩,得到浓缩液,干燥得到水提取物粉末;
4)将步骤2)所得枣渣进行酸解,分离所得水解液中的固体颗粒并干燥粉碎;
5)将步骤4)干燥粉碎后的固体颗粒与步骤3)所得水提取物粉末混合制粒,真空干燥后压片,即得。
7.根据权利要求6所述的方法,其特征在于:所述步骤1)中,所述大枣粉末的粒径为80目~270目;
所述步骤2)以水提取步骤中,所述水和大枣粉末的质量比为4:1~10:1;
提取温度为10~50℃;
提取时间为6~12h。
8.根据权利要求6或7所述的方法,其特征在于:所述步骤4)酸解步骤中,酸解剂为稀盐酸;
所述稀盐酸的质量百分浓度为5%~15%;
酸解温度为80~95℃;
酸解时间为80~360min;
所述稀盐酸与枣渣的用量比为每1kg枣渣使用稀盐酸3~6L;所述枣渣的质量以干基计;
所述步骤5)中,所述步骤4)干燥粉碎后的固体颗粒与步骤3)所得水提取物粉末的质量比为1:1-2;
所述真空干燥步骤中,干燥温度不超过50℃,干燥后产品中的含水量低于5%。
9.根据权利要求6-8中任一所述的方法,其特征在于:所述方法还包括:在所述步骤4)之后,步骤5)制粒步骤之前,向体系中加入粘合剂的乙醇水溶液;
所述乙醇水溶液中,乙醇的质量百分浓度为20-40%。
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