CN110960516B - 一种姜黄素复合物及其制备方法 - Google Patents
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Abstract
本发明公开一种姜黄素复合物，包括姜黄素20‑30份、儿茶素5‑10份、杨梅素5‑10份、椰子油0.5‑2份、棕榈仁油0.5‑2份、巴沙鱼油1‑4份、磷脂2‑40份、HLB值为1‑2的蔗糖脂肪酸酯0.5‑2份。本发明选择椰子油、棕榈仁油和巴沙鱼油作为油性溶剂，来提高姜黄素、儿茶素和杨梅素的稳定性和吸收率。OPO可以促进机体对能量或营养的吸收，改善消化的能力，而且中链和短链脂肪酸的结构一方面吸收性比长链要好，且能够在一定程度上改变微生物的菌群。本发明选择使用相对量较大的磷脂和一定HLB值下的蔗糖脂肪酸酯配合促进在本发明的体系下结构的均匀性，提高姜黄素复合物的稳定性和吸收率。
Description
技术领域
本发明属于医药和保健食品领域，具体涉及一种姜黄素复合物及其制备方法。
背景技术
人体衰老和疾病的发生于体内氧化和抗氧化的动态平衡被打破有关，人体内在氧的利用过程中，会因各种内在性和外在性的原因而产生各种活性氧和自由基，虽然机体自身具有消除活性氧和自由基的防御体系，然而当出现超负荷状态时，就会导致平衡丧失，诱发各种组织损伤和疾病。
如血液中的不饱和脂肪酸因氧化而成为过氧化物质，经小肠系搜狐，进入各个组织，进而发生有害作用，特别是过氧化脂质可直接攻击血管内壁，成为脑出血、动脉硬化的初期病变。另外研究认为自由基攻击生命大分子造成组织损伤，是引起机体衰老的原因，也是引发一些恶性疾病的重要原因。因此，抗氧化物质的补充就会发挥比较好的作用。比如茶多酚、儿茶素、谷胱甘肽、黄铜等物质，已广泛的用于健康食品或者药品的开发，由于上述的成分主要都是天然活性成分，十分受欢迎，抗氧化活性是保健食品的保健功能之一，能够有效清除体内有害自由基，防止脂质过氧化，防止自由基对生物大分子的氧化损伤，保证细胞结构和功能的正常。
姜黄（Curcuma longa L.）为姜科（Zingiberaceae）姜黄属（Curcuma）植物，主产于印度、中国等亚洲国家。据明代李时珍《本草纲目》记载，唐代药学专著《唐本草》就已有姜黄入药的记录，姜黄素具有抑制低密度脂蛋白、脂质、蛋白质氧化的作用。姜黄素具有很强的抗炎活性，可抑制诱导型一氧化氮合酶、还原型辅酶Ⅱ（NADPH）氧化酶催化结构域的表达，减少心肌内质网压力信号蛋白，改善实验性自身免疫性心肌炎大鼠心肌功能。对于姜黄素而言，稳定性、吸收率是其很受制约的因素，在肠道中容易转化为葡糖苷醛酸和磺酸等复合物，代谢快、半衰期段导致了生物利用率低，限制了在食品或药品领域的应用。
发明内容
基于现有技术中存在的问题，本发明提供一种姜黄素复合物及其制备方法，改善其稳定性差和吸收率低等问题。本发明的技术方案如下。
一种姜黄素复合物，包括以下的组分：姜黄素20-30份、油脂1-8份、磷脂2-40份、HLB值为1-2的蔗糖脂肪酸酯0.5-2份。
进一步地，油脂包括椰子油、棕榈仁油、淡水鱼油中的一种或多种。
进一步地，所述油脂具体为椰子油、棕榈仁油和巴沙鱼油，三者质量配比为1-3:1-3:3-6。
一种姜黄素复合物，包括以下的原料：姜黄素20-30份、儿茶素5-10份、杨梅素5-10份、椰子油0.5-2份、棕榈仁油0.5-2份、巴沙鱼油1-4份、磷脂2-40份、HLB值为1-2的蔗糖脂肪酸酯0.5-2份。
进一步地，姜黄素复合物的各组分的用量配比为：姜黄素25-30份、儿茶素5-8份、杨梅素5-8份、椰子油0.5-1份、棕榈仁油0.5-1份、巴沙鱼油1-4份、磷脂15-40份、HLB值为1-2的蔗糖脂肪酸酯0.5-1.5份。
进一步优选地，上述的复合物的组分用量选择为姜黄素25-30份、儿茶素8-10份、杨梅素8-10份、椰子油1-2份、椰子油1-2份、巴沙鱼油2-4份、磷脂15-40份、HLB值为1-2的蔗糖脂肪酸酯1-2份。
进一步地，所述的原料还包括常规的辅料或载体。
进一步地，所述的磷脂可以是大豆磷脂、卵磷脂、磷脂酰胆碱中的一种或多种。
提高姜黄素的生物利用度，现在的研究方向包括与适当的药用辅料配合使用，或制成带金属离子的螯合物，或者改变产品的剂型。比如聚乙二醇或聚乙烯吡咯烷酮固体分散体等。
本发明旨在提高姜黄素的生物利用度，本发明的改进之处主要为：将姜黄素、儿茶素和杨梅素相互配伍使用，实验证明，三者的相互促进作用能够较为明显的提高生物利用度，提高吸收率。另外在原料配伍中，本发明选择椰子油、棕榈仁油和巴沙鱼油作为油性溶剂，来提高姜黄素、儿茶素和杨梅素的稳定性和吸收率。我们知道对于椰子油和棕榈仁油而言，二者的中链脂肪酸和短链脂肪酸含量比其他油脂含量高，巴沙鱼油含有较多地OPO结构类油脂，OPO可以促进机体对能量或营养的吸收，改善消化的能力，而且中链和短链脂肪酸的结构一方面吸收性比长链要好，且能够在一定程度上改变微生物的菌群。然而姜黄素的脂溶性并不理想，因此本发明选择使用相对量较大的磷脂和一定HLB值下的蔗糖脂肪酸酯配合促进在本发明的体系下结构的均匀性。上述油脂的组合与乳化剂的配伍能够提高姜黄素复合物的稳定性和吸收率。
姜黄素复合物的制备方法，包括如下的步骤：（1）按照质量份数称取各原料，将姜黄素、儿茶素和杨梅素与磷脂初步混合，添加至溶剂中，加热搅拌回流处理1-2h，回流处理完后，回收溶剂得到混合物A；
（2）准备油相，将椰子油、棕榈仁油、巴沙鱼油和蔗糖脂肪酸酯混合，加热至70-80℃，搅拌处理20-30min得到油相混合物B；
（3）采用梯度混合的方式，先将等量的混合物A和油相混合物B混合剪切，混合温度控制在45-80℃，剪切处理10-40min，然后添加剩余的混合物A在温度条件为45-80℃下，剪切处理30-60min即得到姜黄素复合物。
进一步地，步骤（1）中所述的溶剂可以是乙醇、丙酮、乙酸乙酯的一种或多种。
进一步地，所述的姜黄素复合物可以通过常规的处理方式得到软胶囊。
进一步地，所述的加热搅拌回流时间为1.5h。
进一步地，所述的步骤（2）中加热温度为75℃，搅拌处理时间为27min。
进一步地，步骤（3）的混合温度为60-75℃，剪切处理时间为25-35min；添加剩余的混合物A后的处理温度为50-75℃，剪切处理时间为40-50min。
进一步地，所述的蔗糖脂肪酸酯HLB值为1-2。
本发明的有益效果包括：（1）改善了姜黄素复合物的稳定性和生物利用度，提高吸收利用率。（2）姜黄素、儿茶素和杨梅素相互促进，增进抗氧化的效果。（3）通过在原料中增加短链、中链脂肪酸的油脂和OPO结构油脂，促进姜黄素、儿茶素和杨梅素的吸收能力。
具体实施方式
实施例1
含有姜黄素的复合物，原料包括：姜黄素30份、儿茶素8份、杨梅素6份、椰子油0.5份、棕榈仁油0.5份、巴沙鱼油1份、磷脂30份、HLB值为1-2的蔗糖脂肪酸酯1份。
实施例2
含有姜黄素的复合物，原料包括：姜黄素25份、儿茶素5份、杨梅素5份、椰子油1份、棕榈仁油0.5份、巴沙鱼油2份、磷脂40份、HLB值为1-2的蔗糖脂肪酸酯2份。
实施例3
含有姜黄素的复合物，原料包括：姜黄素30份、儿茶素6份、杨梅素6份、椰子油1份、棕榈仁油0.5份、巴沙鱼油2份、磷脂28份、HLB值为1-2的蔗糖脂肪酸酯1.5份。
实施例4
含有姜黄素的复合物的制备方法，包括（1）按照质量份数称取各原料（实施例1），将姜黄素、儿茶素和杨梅素与磷脂初步混合，添加至溶剂中，溶剂为乙醇和丙酮的混合物；加热搅拌回流处理2h，回流处理完后，回收溶剂得到混合物A；
（2）准备油相，将椰子油、棕榈仁油、巴沙鱼油和蔗糖脂肪酸酯混合，加热至75℃，搅拌处理30min得到油相混合物B；
（3）采用梯度混合的方式，先将等量的混合物A和油相混合物B混合剪切，混合温度控制在70℃，剪切处理35min，然后添加剩余的混合物A在温度条件为65℃下，剪切处理50min即得到姜黄素复合物。
对比例1
含有姜黄素的复合物，包括姜黄素44份、椰子油0.5份、棕榈仁油0.5份、巴沙鱼油1份、磷脂30份、HLB值为1-2的蔗糖脂肪酸酯1份。
对比例2含有姜黄素的复合物，包括姜黄素30份、儿茶素8份、杨梅素6份、大豆油2份、磷脂30份、HLB值为1-2的蔗糖脂肪酸酯1份。
对比例3
含有姜黄素的复合物，原料包括：姜黄素30份、儿茶素8份、杨梅素6份、椰子油0.5份、棕榈仁油0.5份、巴沙鱼油1份、磷脂30份。
对比例4
含有姜黄素的复合物，原料包括：姜黄素30份、儿茶素8份、杨梅素6份、磷脂30份、HLB值为1-2的蔗糖脂肪酸酯1份。
对比例5
含有姜黄素的复合物，原料包括：姜黄素30份、儿茶素8份、杨梅素6份、椰子油0.5份、棕榈仁油0.5份、巴沙鱼油1份、磷脂10份、HLB值为1-2的蔗糖脂肪酸酯1份。
对比例6
含有姜黄素的复合物，原料包括：姜黄素15份、儿茶素15份、杨梅素14份、椰子油0.5份、棕榈仁油0.5份、巴沙鱼油1份、磷脂30份、HLB值为1-2的蔗糖脂肪酸酯1份。
对比例7
含有姜黄素的复合物，原料包括：姜黄素30份、儿茶素8份、杨梅素6份、椰子油3份、棕榈仁油3份、巴沙鱼油4份、磷脂30份、HLB值为1-2的蔗糖脂肪酸酯1份。
对比例8
含有姜黄素的复合物的制备方法，包括按照质量份数称取各原料（实施例1），混合，添加至溶剂中，溶剂为乙醇和丙酮的混合物；加热搅拌回流处理2h，回流处理完后，回收溶剂得到混合物A；将混合物的混合温度控制在70℃，剪切处理60min，即得到姜黄素复合物。
稳定性
将待测样品贮藏在温度为60℃、湿度为75%的环境下（加速试验），测试周期为6个月，分别在第1、3和6月各测一定活性稳定性的情况，分别测定实施例1、和对比例1-7的活性稳定情况。
稳定性测定方法参照现有技术中已有的方法进行，测定对活性自由基的清除率。DPPH自由基在517nm波长附近有最大吸收峰，当DPPH自由基与抗氧化剂反应后，517nm波长处的吸收值降低，其降低的程度与接收的电子（抗氧化剂清除自由基活性）呈定量的关系，通过分光光度计检测，DPPH自由基清除公式一般为：DPPH自由基清除率/%=（A对照-A样品）/A对照*100%。
其中A对照为未加样品的DPPH自由基吸光度，A样品为加入样品反应后的DPPH自由基吸光度。
DPPH自由基清除率在第1、3和6个月的时候如下表所示。
| 第1个月 | 第3个月 | 第6个月 | |
| 实施例1 | 95.3% | 95.1% | 94.9% |
| 对比例1 | 75.3% | 74.2% | 74.0% |
| 对比例2 | 94.8% | 86.4% | 79.5% |
| 对比例3 | 94.7% | 83.2% | 78.2% |
| 对比例4 | 95.1% | 78.4% | 67.3% |
| 对比例5 | 94.2% | 84.7% | 79.7% |
| 对比例6 | 94.6% | 90.4% | 84.3% |
| 对比例7 | 94.8% | 88.1% | 77.8% |
根据检测的DPPH自由基清除率结果来看，姜黄素、儿茶素和杨梅素三者具有一定的协同促进的作用，三者配伍效果更为明显。同时根据贮藏的稳定性来看，本发明的体系下在第3和6个月时更加的稳定。
显然，本发明的上述实施例仅仅是为清楚地说明本发明所作的举例，而并非是对本发明的实施方式的限定。对于所属领域的普通技术人员来说，在上述说明的基础上还可以做出其它不同形式的变化或变动。这里无需也无法对所有的实施方式予以穷举。凡在本发明的精神和原则之内所作的任何修改、等同替换和改进等，均应包含在本发明权利要求的保护范围之内。
Claims (2)
1.一种含有姜黄素的复合物，其特征在于由以下原料制成：姜黄素30份、儿茶素8份、杨梅素6份、椰子油0.5份、棕榈仁油0.5份、巴沙鱼油1份、磷脂30份、HLB值为1-2的蔗糖脂肪酸酯1份；
制备方法为（1）按照质量份数称取各原料，将姜黄素、儿茶素和杨梅素与磷脂初步混合，添加至溶剂中，溶剂为乙醇和丙酮的混合物；加热搅拌回流处理2h，回流处理完后，回收溶剂得到混合物A；
（2）准备油相，将椰子油、棕榈仁油、巴沙鱼油和蔗糖脂肪酸酯混合，加热至75℃，搅拌处理30min得到油相混合物B；
（3）采用梯度混合的方式，先将等量的混合物A和油相混合物B混合剪切，混合温度控制在70℃，剪切处理35min，然后添加剩余的混合物A在温度条件为65℃下，剪切处理50min即得到含有姜黄素的复合物。
2.一种权利要求1所述的含有姜黄素的复合物制备方法，其特征在于制备方法为：（1）按照质量份数称取各原料，将姜黄素、儿茶素和杨梅素与磷脂初步混合，添加至溶剂中，溶剂为乙醇和丙酮的混合物；加热搅拌回流处理2h，回流处理完后，回收溶剂得到混合物A；
（2）准备油相，将椰子油、棕榈仁油、巴沙鱼油和蔗糖脂肪酸酯混合，加热至75℃，搅拌处理30min得到油相混合物B；
（3）采用梯度混合的方式，先将等量的混合物A和油相混合物B混合剪切，混合温度控制在70℃，剪切处理35min，然后添加剩余的混合物A在温度条件为65℃下，剪切处理50min即得。
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