CN107252112A - 一种含egcg的片剂 - Google Patents
一种含egcg的片剂 Download PDFInfo
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- CN107252112A CN107252112A CN201710426159.3A CN201710426159A CN107252112A CN 107252112 A CN107252112 A CN 107252112A CN 201710426159 A CN201710426159 A CN 201710426159A CN 107252112 A CN107252112 A CN 107252112A
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- egcg
- quercetin
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- water
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Abstract
本发明涉及健康制品技术领域,具体涉及一种含EGCG的片剂。所述片剂为包括EGCG与槲皮素或槲皮素糖苷衍生物的复合制剂,EGCG与槲皮素或槲皮素糖苷衍生物的比例为3‑8:0.3‑1。该片剂将EGCG与槲皮素或槲皮素糖苷衍生物配制成复合制剂,能够促进协同相互促进,特别是促进槲皮素或槲皮素糖苷衍生物的吸收;同时,在片剂中加入白藜芦醇和山梨醇能够提高EGCG的吸收效率和吸收速率。
Description
技术领域
本发明涉及健康制品技术领域,具体涉及一种含EGCG的片剂。
背景技术
茶,是中国特有的一种著名饮品,遍销海内外。茶多酚(Tea Polyphenols)是茶叶中多酚类物质的总称,包括黄烷醇类、花色苷类、黄酮类、黄酮醇类和酚酸类等。主要为黄烷醇(儿茶素)类,儿茶素占60~80%。类物质茶多酚又称茶鞣或茶单宁,是形成茶叶色香味的主要成份之一,也是茶叶中有保健功能的主要成份之一。
茶多酚是一种稠环芳香烃,可分为黄烷醇类、羟基-[4]-黄烷醇类、花色苷类、黄酮类、黄酮醇类和酚酸类等。儿茶素又称儿茶精,茶单宁,为黄烷醇的衍生物,是茶多酚最为重要组分,约占多酚类总量 的60%-80%;儿茶素类主要由EGC、DLC、EC、EGCG、GCG、ECG等几 种单体组成,EGCG中文名表没食子儿茶素没食子酸酯,是茶多酚的主要组成成分。
表没食子儿茶素没食子酸酯 (EGCG)是绿茶中最有效的抗氧化多酚,具有抗氧化、抗癌、抗突变等活性。抗氧化活性至少是维生素C的100多倍,是维生素E的25倍,能够保护细胞和DNA受损害,这种损害相信与癌症、心脏疾病和其他重大疾病有关,EGCG的这些功效归结于他们对氧自由基的清除(抗氧化 )能力。
研究表明 EGCG可以提高癌细胞对化疗的敏感性,同时降低化疗对心脏的毒性。同时 EGCG 具有抗自由基 DNA 损害,抗辐射和紫外线,阻止油脂过氧化,减少血清中低密度胆固醇、超低密度胆固醇和甘油三酯的含量,干扰癌细胞生存所需的信号传递,抑制饮食中的致癌物质,与肠、肝、和肺中的其他酶和抗氧化剂作用共同阻止某些致癌物质的活力,清除自由基,抵御污染、日晒和吸烟的影响,防治皮肤老化和起皱等作用。
但是,EGCG 的稳定性较差,易受到温度、水、pH 等因素的影响,尤其在液体环境中其水解/降解严重,即使在固体状态下,虽然稳定性相对会提高,但是对于温度较敏感,会在热环境下逐步降解,严重影响产品品质和EGCG产品的开发,对于产品的制备、储存、流通等带来严重不良影响,对制剂的使用安全带来不利与隐患。
发明内容
本发明的目的是为了解决上述问题,提供一种含EGCG的片剂。
为了达到上述发明目的,本发明采用以下技术方案:
一种含EGCG的片剂,所述片剂为包括EGCG与槲皮素或槲皮素糖苷衍生物的复合制剂,EGCG与槲皮素或槲皮素糖苷衍生物的比例为3-8:0.3-1。
进一步的优选方案,所述片剂还包括白藜芦醇和山梨醇,EGCG与白藜芦醇和山梨醇的重量比为1:0.1-0.5:0.1-0.5。
白藜芦醇和山梨醇的配合,以辅助配合EGCG,提高EGCG的吸收速率和吸收率,从而提高EGCG的效果。
进一步的优选方案,所述槲皮素糖苷衍生物为槲皮素-3-O-葡萄糖苷、槲皮苷或槲皮素-3-O-α-L-鼠李糖苷。
进一步的优选方案,所述片剂由片芯和包裹在片芯外的包衣组成,所述片芯包括EGCG、槲皮素或槲皮素糖苷衍生物、白藜芦醇、山梨醇和其他助剂;EGCG与槲皮素或槲皮素糖苷衍生物的比例为3-8:0.3-1,EGCG与白藜芦醇和山梨醇的重量比为1:0.1-0.5:0.1-0.5;
所述包衣按重量份数计包括羧甲基淀粉钠20-25份,微晶纤维素3-8份、环糊精5-10份、碳酸氢钠2-5份、碳酸钙1-3份、聚乙烯吡咯烷酮5-8份、味色剂1-3份和润滑剂1-3份;
味色剂选自β胡萝卜素、甜菊素、甜菊糖甙、三氯蔗糖或果味香精中的一种或两种以上;
润滑剂选自亮氨酸、PEG 6000、氢化植物油、硬脂酸或硬脂酸盐。
进一步的优选方案,还包括芦丁,芦丁与EGCG的重量比为0.1-0.3:1-10。
芦丁能够抑制EGCG,防止其氧化酶解,提高EGCG的存放时间,配合包衣使其能够在外界开放环境下长时间保存。
同时,为了解决目前的EGCG提纯度不高工艺复杂不易规模化的问题,提供了一种上述所述的EGCG的提取方法,包括以下步骤:
(1)将茶叶原料去除杂质,然后清洗干净;然后采用冷冻粉碎机中粉碎,过筛,目数为20-50目;
(2)然后将粉碎后的原料烘干至含水量在10%以下;
在步骤(2)中采用一种优选的方案为:然后进行辐照处理,辐照的剂量为3-6kGy;
(3)然后进行超临界CO2流体萃取,并收集萃取液;
(4)将萃取后的茶渣首先加入水,加水量为每千克茶渣加水1-1.5L,然后煮沸10-30min,再进行浸提处理,具体为继续在其中加入水、乙醇,水和乙醇的比例为1-3:1,每千克茶渣加入液体的量为3-5L,并在混合液体中加入柠檬酸钠,使得混合液中柠檬酸钠的重量百分比为1-3%,然后,升温至60-70℃,浸提20-30min,收集浸提液;
步骤(4)采用的另一种优选的方案为:茶渣中加水后然后采用辐照处理,辐照剂量为2-3kGy,
(5)然后将收集到的两种液体混合并浓缩,得到浓缩液;
(6)最后将浓缩液进行干燥处理。
作为进一步的优选方案,步骤(6)的干燥处理为喷雾干燥。
作为进一步的优选方案,步骤(4)的茶渣首先采用微波处理20-40s,微波功率为500-600W。
本发明与现有技术相比,有益效果是:该片剂将EGCG与槲皮素或槲皮素糖苷衍生物配制成复合制剂,能够促进协同相互促进,特别是促进槲皮素或槲皮素糖苷衍生物的吸收;同时,在片剂中加入白藜芦醇和山梨醇能够提高EGCG的吸收效率和吸收速率。同时,将片剂分苇片芯和包衣,在模拟胃酸环境下,本发明片剂在3分钟内完全分解,提高片剂在体内的。
具体实施方式
下面通过具体实施例对本发明的技术方案作进一步描述说明。
如果无特殊说明,本发明的实施例中所采用的原料均为本领域常用的原料,实施例中所采用的方法,均为本领域的常规方法。
关于EGCG的提取方法,具体如下:
实施例1:
一种上述所述的EGCG的提取方法,包括以下步骤:
(1)将茶叶原料去除杂质,然后清洗干净;然后采用冷冻粉碎机中粉碎,过筛,目数为20-50目;
(2)然后将粉碎后的原料烘干至含水量在10%以下;
(3)然后进行超临界CO2流体萃取,并收集萃取液;
(4)将萃取后的茶渣首先加入水,加水量为每千克茶渣加水1L,然后煮沸10min,再进行浸提处理,具体为继续在其中加入水、乙醇,水和乙醇的比例为3:1,每千克茶渣加入液体的量为3L,并在混合液体中加入柠檬酸钠,使得混合液中柠檬酸钠的重量百分比为3%,然后,升温至60℃,浸提30min,收集浸提液;
(5)然后将收集到的两种液体混合并浓缩,得到浓缩液;
(6)最后将浓缩液进行干燥处理,具体采用喷雾干燥处理,喷雾干燥工艺的进风温度为195℃,出风温度为155℃。
实施例2:
一种上述所述的EGCG的提取方法,包括以下步骤:
(1)将茶叶原料去除杂质,然后清洗干净;然后采用冷冻粉碎机中粉碎,过筛,目数为20-50目;
(2)然后将粉碎后的原料烘干至含水量在10%以下;
(3)然后进行超临界CO2流体萃取,并收集萃取液;首先采用微波处理20-40s,微波功率为500-600W;
(4)将萃取后的茶渣首先加入水,加水量为每千克茶渣加水1.5L,然后煮沸30min,再进行浸提处理,具体为继续在其中加入水、乙醇,水和乙醇的比例为1:1,每千克茶渣加入液体的量为5L,并在混合液体中加入柠檬酸钠,使得混合液中柠檬酸钠的重量百分比为1%,然后,升温至70℃,浸提20min,收集浸提液;
(5)然后将收集到的两种液体混合并浓缩,得到浓缩液;
(6)最后将浓缩液进行干燥处理,具体采用喷雾干燥处理,喷雾干燥工艺的进风温度为205℃,出风温度为145℃。
实施例3:
一种上述所述的EGCG的提取方法,包括以下步骤:
(1)将茶叶原料去除杂质,然后清洗干净;然后采用冷冻粉碎机中粉碎,过筛,目数为20-50目;
(2)然后将粉碎后的原料烘干至含水量在10%以下,然后进行辐照处理,辐照的剂量为3-6kGy;
(3)然后将辐照后进行超临界CO2流体萃取,并收集萃取液;
(4)将萃取后的茶渣首先加入水,加水量为每千克茶渣加水1L,然后采用辐照处理,辐照剂量为3kGy,然后煮沸10min,再进行浸提处理,具体为继续在其中加入水、乙醇,水和乙醇的比例为3:1,每千克茶渣加入液体的量为3L,并在混合液体中加入柠檬酸钠,使得混合液中柠檬酸钠的重量百分比为3%,然后,升温至60℃,浸提30min,收集浸提液;
(5)然后将收集到的两种液体混合并浓缩,得到浓缩液;
(6)最后将浓缩液进行干燥处理,具体采用喷雾干燥处理,喷雾干燥工艺的进风温度为195℃,出风温度为155℃。
实施例4:
一种上述所述的EGCG的提取方法,包括以下步骤:
(1)将茶叶原料去除杂质,然后清洗干净;然后采用冷冻粉碎机中粉碎,过筛,目数为20-50目;
(2)然后将粉碎后的原料烘干至含水量在10%以下,然后进行辐照处理,辐照的剂量为3-6kGy;
(3)然后将辐照后的物质进行超临界CO2流体萃取,并收集萃取液;首先采用微波处理20-40s,微波功率为500-600W;
(4)将萃取后的茶渣首先加入水,加水量为每千克茶渣加水1.5L,然后采用辐照处理,辐照剂量为2kGy,然后煮沸30min,再进行浸提处理,具体为继续在其中加入水、乙醇,水和乙醇的比例为1:1,每千克茶渣加入液体的量为5L,并在混合液体中加入柠檬酸钠,使得混合液中柠檬酸钠的重量百分比为1%,然后,升温至70℃,浸提20min,收集浸提液;
(5)然后将收集到的两种液体混合并浓缩,得到浓缩液;
(6)最后将浓缩液进行干燥处理,具体采用喷雾干燥处理,喷雾干燥工艺的进风温度为205℃,出风温度为145℃。
采用上述方法提纯得到的产物,EGCG的含量在85%以上。
关于上述提取方法,操作简单,避免了有害物质的残留,有效节约成本,能够大规模实施操作。EGCG 的含量较对照组增加了30-40%,表面的菌落总数则明显下降,具有良好的保鲜抑菌效果。
关于含EGCG的片剂,具体如下(对于配比,具体按照重量份数进行配制):
实施例5:
一种含EGCG的片剂,所述片剂为包括EGCG与槲皮素的复合制剂,EGCG与槲皮素或槲皮素糖苷衍生物的比例为8:0.3。
实施例6:
一种含EGCG的片剂,所述片剂为包括EGCG与槲皮素糖苷衍生物的复合制剂,EGCG与槲皮素或槲皮素糖苷衍生物的比例为3:1。槲皮素糖苷衍生物为槲皮素-3-O-葡萄糖苷、槲皮苷或槲皮素-3-O-α-L-鼠李糖苷。
实施例7:
在实施例3或4的基础上,在片剂中加入白藜芦醇和山梨醇,EGCG与白藜芦醇和山梨醇的重量比为1:0.1:0.5。
实施例8:
在实施例3或4或5的基础上,在片剂中加入白藜芦醇和山梨醇,EGCG与白藜芦醇和山梨醇的重量比为1:0.5:0.5。
所述槲皮素糖苷衍生物为槲皮素-3-O-葡萄糖苷、槲皮苷或槲皮素-3-O-α-L-鼠李糖苷。
实施例9:
一种含EGCG的片剂,所述片剂由片芯和包裹在片芯外的包衣组成,所述片芯包括EGCG、槲皮素或槲皮素糖苷衍生物、白藜芦醇、山梨醇和其他助剂;EGCG与槲皮素或槲皮素糖苷衍生物的比例为3:1,EGCG与白藜芦醇和山梨醇的重量比为1:0.1:0.5;
所述包衣按重量份数计包括羧甲基淀粉钠20份,微晶纤维素8份、环糊精5份、碳酸氢钠5份、碳酸钙1份、聚乙烯吡咯烷酮8份、味色剂1份和润滑剂3份;
其中,味色剂选自β胡萝卜素、甜菊素、甜菊糖甙、三氯蔗糖或果味香精中的一种或两种以上;润滑剂选自亮氨酸、PEG 6000、氢化植物油、硬脂酸或硬脂酸盐中的一种。
实施例10:
一种含EGCG的片剂,所述片剂由片芯和包裹在片芯外的包衣组成,所述片芯包括EGCG、槲皮素或槲皮素糖苷衍生物、白藜芦醇、山梨醇和其他助剂;EGCG与槲皮素或槲皮素糖苷衍生物的比例为8:0.3,EGCG与白藜芦醇和山梨醇的重量比为1:0.5:0.1;
所述包衣按重量份数计包括羧甲基淀粉钠25份,微晶纤维素3份、环糊精10份、碳酸氢钠2份、碳酸钙3份、聚乙烯吡咯烷酮5份、味色剂3份和润滑剂1份;
其中,味色剂选自β胡萝卜素、甜菊素、甜菊糖甙、三氯蔗糖或果味香精中的一种或两种以上;润滑剂选自亮氨酸、PEG 6000、氢化植物油、硬脂酸或硬脂酸盐中的一种。
实施例11:
在实施例3或4或5或6或7或8的基础上,再加入芦丁,芦丁与EGCG的重量比为0.3:10。
实施例12:
在实施例3或4或5或6或7或8的基础上,再加入芦丁,芦丁与EGCG的重量比为0.1:1。
以上所述的实施例只是本发明的一种较佳的方案,并非对本发明作任何形式上的限制,在不超出权利要求所记载的技术方案的前提下还有其它的变体及改型。
Claims (8)
1.一种含EGCG的片剂,其特征在于,所述片剂为包括EGCG与槲皮素或槲皮素糖苷衍生物的复合制剂,EGCG与槲皮素或槲皮素糖苷衍生物的比例为3-8:0.3-1。
2.根据权利要求1所述的一种EGCG的片剂,其特征在于,所述片剂还包括白藜芦醇和山梨醇,EGCG与白藜芦醇和山梨醇的重量比为1:0.1-0.5:0.1-0.5。
3.根据权利要求1或2所述的一种EGCG的片剂,其特征在于,所述槲皮素糖苷衍生物为槲皮素-3-O-葡萄糖苷、槲皮苷或槲皮素-3-O-α-L-鼠李糖苷。
4.根据权利要求1所述的一种EGCG的片剂,其特征在于,所述片剂由片芯和包裹在片芯外的包衣组成,所述片芯包括EGCG、槲皮素或槲皮素糖苷衍生物、白藜芦醇、山梨醇和其他助剂;EGCG与槲皮素或槲皮素糖苷衍生物的比例为3-8:0.3-1,EGCG与白藜芦醇和山梨醇的重量比为1:0.1-0.5:0.1-0.5;
所述包衣按重量份数计包括羧甲基淀粉钠20-25份,微晶纤维素3-8份、环糊精5-10份、碳酸氢钠2-5份、碳酸钙1-3份、聚乙烯吡咯烷酮5-8份、味色剂1-3份和润滑剂1-3份;
味色剂选自β胡萝卜素、甜菊素、甜菊糖甙、三氯蔗糖或果味香精中的一种或两种以上;
润滑剂选自亮氨酸、PEG 6000、氢化植物油、硬脂酸或硬脂酸盐。
5.根据权利要求1或2或4所述的一种EGCG的片剂,其特征在于,还包括芦丁,芦丁与EGCG的重量比为0.1-0.3:1-10。
6.一种上述所述的EGCG的提取方法,其特征在于,包括以下步骤:
(1)将茶叶原料去除杂质,然后清洗干净;然后采用冷冻粉碎机中粉碎,过筛,目数为20-50目;
(2)然后将粉碎后的原料烘干至含水量在10%以下;
(3)然后进行超临界CO2流体萃取,并收集萃取液;
(4)将萃取后的茶渣首先加入水,加水量为每千克茶渣加水1-1.5L,然后煮沸10-30min,再进行浸提处理,具体为继续在其中加入水、乙醇,水和乙醇的比例为1-3:1,每千克茶渣加入液体的量为3-5L,并在混合液体中加入柠檬酸钠,使得混合液中柠檬酸钠的重量百分比为1-3%,然后,升温至60-70℃,浸提20-30min,收集浸提液;
(5)然后将收集到的两种液体混合并浓缩,得到浓缩液;
(6)最后将浓缩液进行干燥处理。
7.根据权利要求6所述的一种上述所述的EGCG的提取方法,其特征在于,步骤(6)的干燥处理为喷雾干燥。
8.根据权利要求6所述的一种上述所述的EGCG的提取方法,其特征在于,步骤(4)的茶渣首先采用微波处理20-40s,微波功率为500-600W。
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