CN114522142A - 纳米稳定剂及其制备方法和应用 - Google Patents

纳米稳定剂及其制备方法和应用 Download PDF

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CN114522142A
CN114522142A CN202210149827.3A CN202210149827A CN114522142A CN 114522142 A CN114522142 A CN 114522142A CN 202210149827 A CN202210149827 A CN 202210149827A CN 114522142 A CN114522142 A CN 114522142A
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Abstract

本发明提供了一种纳米稳定剂及其制备方法和应用，纳米稳定剂包括以重量百分含量计的下列各原料：维生素E聚乙二醇琥珀酸酯35％～50％，甘油三脂或者植物油25％～40％，磷脂8％～15％，山梨酸0.3％～0.6％。该纳米稳定剂能够将脂溶性的活性成分制成半透明的纳米乳液；能够完全实现与水的互溶，同时保持光学透明度和持久的稳定性；能够提高生物利用度并缩短起效时间；能够避免长时间的处方筛选和工艺研究，加快产品开发的速度。

Description

纳米稳定剂及其制备方法和应用
技术领域
本发明涉及纳米乳剂技术领域，特别涉及一种纳米稳定剂及其制备方法和应用。
背景技术
将疏水性生物活性化合物，如植物提取物、维生素、精油、萜烯、营养品或者药物，制成完全亲水性递送体系，一直是处方开发的难题。现有的乳液递送体系的油滴体积大而表面积小，即表面积体积比较小，在体内与体液的接触面积就相对较小，因而不利于被人体吸收；而且现有乳液外观呈白色，导致其加入任何透明液体中都会引起浑浊或透明度的下降，降低产品的外观吸引力。
另外，微乳乳液是在大量乳化剂的存在下，使油水界面的张力降低而自发的形成透明或半透明乳液，又称为自乳化乳液。微乳乳液是热力学稳定系统，油滴粒径不随时间变化而变化，但是如果微乳被稀释、酸化或者加热，则会变得极不稳定，这会给产品的生产带来不便。同时，微乳乳液中存在大量的乳化剂，在食品生产中，大量的乳化剂会给产品带来苦味，很难通过后期的味道调节来纠正，且国内CFDA和美国FDA对很多乳化剂的日摄入量有限量，这也使微乳乳液的使用受到限制。
发明内容
本发明提供了一种纳米稳定剂及其制备方法和应用，以解决现有技术中纳米乳剂在保存和使用中不便的技术问题。
为达到上述目的，本发明的技术方案是这样实现的：
本发明提供了一种纳米稳定剂，包括以重量百分含量计的下列各原料：
维生素E聚乙二醇琥珀酸酯35％～50％，甘油三脂或者植物油25％～40％，磷脂8％～15％，山梨酸0.3％～0.6％。
进一步地，包括以重量百分含量计的下列各原料：维生素E聚乙二醇琥珀酸酯49％，甘油三脂或者植物油36％，磷脂14％，山梨酸1％。
进一步地，所述甘油三脂包括辛酸/癸酸甘油三脂、中链脂肪酸甘油酯中的一种或两种。
进一步地，所述植物油包括葵花籽油、橄榄油、葡萄籽油中的一种或多种。
进一步地，所述磷脂包括葵花籽天然磷脂、合成磷脂中的一种或两种。
根据本发明的另一方面，还提供了一种纳米稳定剂的制备方法，用于制备上述的纳米稳定剂，包括以下步骤：将所述甘油三脂或者所述植物油放置于反应釜中融化，然后向反应釜中加入所述山梨酸，再加入所述磷脂，最后加入所述维生素E聚乙二醇琥珀酸酯，温度升高至50℃～60℃，搅拌，即可得到所述纳米稳定剂。
根据本发明的另一方面，还提供了上述纳米稳定剂在对疏水性生物活性化合物进行纳米乳化中的应用。
进一步地，将所述纳米稳定剂与所述疏水性生物活性化合物混合得到混合液，再向所述混合液中加入水，以实现对所述疏水性生物活性化合物的纳米乳化。
进一步地，所述疏水性生物活性化合物、所述纳米稳定剂的重量比为1∶1～9。
进一步地，所述纳米稳定剂对所述疏水性生物活性化合物进行纳米乳化后，得到的纳米乳液的液滴粒径为50nm～100nm。
本发明提供的纳米稳定剂，属于纳米复合乳化剂，它将纳米乳化剂、助乳化剂、油相和防腐剂按照一定的比例混合，制备更加简便。另外，利用上述纳米稳定剂制备纳米乳液时，只需要将疏水性生物活性化合物与纳米稳定剂按照比例混合，再根据需要加入水，混合形成初乳，然后经过乳匀操作便可制得纳米乳液。此方法避免了长时间的处方比例筛选，提高了产品开发的效率和成功率，扩大了纳米产品的使用范围。
本发明提供的纳米稳定剂，能够将脂溶性的活性成分制成半透明的纳米乳液；能够完全实现与水的互溶，同时保持光学透明度和持久的稳定性；能够提高生物利用度并缩短起效时间；能够避免长时间的处方筛选和工艺研究，加快产品开发的速度。
附图说明
图1为本发明实施例1制备的纳米乳维生素D3浓缩液的典型的粒径分布图；
图2为本发明实施例1中维生素D3在不同溶剂中的溶解度对比图。
具体实施方式
本申请实施例提供了一种纳米稳定剂，包括以重量百分含量计的下列各原料：维生素E聚乙二醇琥珀酸酯35％～50％，甘油三脂或者植物油25％～40％，磷脂8％～15％，山梨酸0.3％～0.6％。
一些实施例中，纳米稳定剂包括以重量百分含量计的下列各原料：维生素E聚乙二醇琥珀酸酯49％，甘油三脂或者植物油36％，磷脂14％，山梨酸1％。
本申请实施例中，维生素E聚乙二醇琥珀酸酯为高生物安全性的高分子聚合物，它具有良好的生物相容性及生物降解性，且因为维生素E的存在，还具有非常好的抗氧化性。在制备纳米稳定剂的原料中，维生素E聚乙二醇琥珀酸酯作为乳化剂，相较于其它乳化剂，其用量更少，所得纳米乳滴的包封率更高；另外，由于纳米乳滴的表面吸附了维生素E聚乙二醇琥珀酸酯，延长了活性物质在血液中存留的时间，促进细胞摄取，能够提高活性物质的生物利用度。
本申请实施例提供的纳米稳定剂，属于纳米复合乳化剂，它将纳米乳化剂、助乳化剂、油相和防腐剂按照一定的比例混合，制备更加简便。另外，利用上述纳米稳定剂制备纳米乳液时，只需要将疏水性生物活性化合物与纳米稳定剂按照比例混合，再根据需要加入水，混合形成初乳，然后经过乳匀操作便可制得纳米乳液。此方法避免了长时间的处方比例筛选，提高了产品开发的效率和成功率，扩大了纳米产品的使用范围。
本申请实施例提供的纳米稳定剂，能够将脂溶性的活性成分制成半透明的纳米乳液；能够完全实现与水的互溶，同时保持光学透明度和持久的稳定性；能够提高生物利用度并缩短起效时间；能够避免长时间的处方筛选和工艺研究，加快产品开发的速度。
一些实施例中，甘油三脂包括辛酸/癸酸甘油三脂、中链脂肪酸甘油酯中的一种或两种。植物油包括葵花籽油、橄榄油、葡萄籽油中的一种或多种。另一些实施例中，磷脂包括葵花籽天然磷脂、合成磷脂中的一种或两种。
本申请实施例的第二方面，提供了一种纳米稳定剂的制备方法，用于制备上述的纳米稳定剂，包括以下步骤：将甘油三脂或者植物油放置于反应釜中融化，然后向反应釜中加入山梨酸，再加入磷脂，最后加入维生素E聚乙二醇琥珀酸酯，温度升高至50℃～60℃，搅拌，即可得到纳米稳定剂。
以上制备方法得到的纳米稳定剂，检测上中下三个不同区域的维生素E聚乙二醇琥珀酸酯的含量，含量均匀度在+/-2％。
本申请实施例的第三方面，提供了上述纳米稳定剂在对疏水性生物活性化合物进行纳米乳化中的应用。
本申请实施例的纳米稳定剂是一种专有的多合一混合物，可配合纳超声设备对疏水性生物活性化合物，如植物提取物、馏出物、分离物、维生素、精油、萜烯、营养品、药物等，进行纳米乳化。一些实施例中，将纳米稳定剂与疏水性生物活性化合物混合得到混合液，再向混合液中加入水，以实现对疏水性生物活性化合物的纳米乳化。其中，疏水性生物活性化合物、纳米稳定剂的重量比为1∶1～9。上述混合液与所需水的重量比为1∶10～99。
上述纳米稳定剂可以快速商业化生产疏水性生物活性提取物或者分离物的纳米乳液，而无需开发配方和加工工艺。利用上述纳米稳定剂制备纳米乳液时，只需要将疏水性生物活性化合物与纳米稳定剂按照比例混合，再根据需要加入水，混合形成初乳，然后经过乳匀操作便可制得纳米乳液。此方法避免了长时间的处方比例筛选，提高了产品开发的效率和成功率，扩大了纳米产品的使用范围。
本申请实施例的纳米稳定剂对疏水性生物活性化合物进行纳米乳化后，得到的纳米乳液的液滴粒径为50nm～100nm。生物活性化合物的浓度可达到50mg/mL。上述纳米乳液的液滴具有永久的水相容性、半透明性和稳定性，表面积体积比增大，在体内与血液的接触面积增大，从而增加了活性物质的吸收效率。上述纳米乳液的外观透明或半透明，向其中加入任何透明液体，都不会导致产品的外观发生剧烈改变；其在稀释或酸化后会保持较好的稳定性。上述纳米乳液的微小液滴大大增加了活性化合物的释药表面积，能够显著加快起效速度，提高生物利用度，并且可以很容易地进行过滤灭菌，消除任何微生物或者微粒的污染。
本申请实施例的纳米稳定剂应用广泛，可以用在食品、药品、化妆品领域。配合超声纳米乳化设备，可将疏水性的活性物质制备成纳米乳液，再通过0.22微米的滤膜过滤灭菌，即可注入各种水基产品中，如水、啤酒、茶、咖啡、碳酸饮料、果汁、软糖、食品、护肤品等，并且不会改变它们的外观。上述纳米乳液也可以作为鼻腔或口腔喷雾剂、舌下滴剂直接使用；或者转化为固体纳米乳剂的形式使用，如喷雾干燥粉剂、片剂、锭剂、舌下贴剂等。
实施例1
一种纳米稳定剂，包括以重量百分含量计的下列各原料：维生素E聚乙二醇琥珀酸酯50％，天然葵花子油36％，葵花籽天然磷脂粉末13％，山梨酸1％。
上述纳米稳定剂的制备方法为：准确称量天然葵花子油放入反应釜中，反应釜温度控制在45摄氏度以下。待食天然葵花子油升温后加入准确称量的山梨酸，搅拌使其溶解；再加入准确称量的葵花籽天然磷脂，搅拌使其溶解；最后加入维生素E聚乙二醇琥珀酸酯，温度升高至50℃～60℃，搅拌至均匀。温度调至室温，保持搅拌并冷却至室温。即可得到纳米稳定剂。
取上述纳米稳定剂7份加1份维生素D3，在60℃水浴加热下混合均匀，加入92份60℃的水，在60℃的水浴加热下搅拌1小时制成初乳；再用超声或者高压乳匀设备制成纳米乳维生素D3浓缩液。上述方法得到纳米乳液初始粒径～54nm，粒径分布图参见图1；HPLC测量显示，纳米乳剂中的维生素D3比其在水中的溶解度显著提高，参见图2。
实施例2
一种纳米稳定剂，包括以重量百分含量计的下列各原料：维生素E聚乙二醇琥珀酸酯47％，中链脂肪酸甘油三脂36％，葵花籽天然磷脂粉末16％，山梨酸1％。
制备方法与实施例1的方法相同。
取上述纳米稳定剂7份加1份维生素D3，在60℃水浴加热下混合均匀，加入92份60℃的水，在60℃的水浴加热下搅拌1小时制成初乳；再用超声或者高压乳匀设备制成纳米乳维生素D3浓缩液。服用时根据需要稀释。
实施例3
一种纳米稳定剂，包括以重量百分含量计的下列各原料：维生素E聚乙二醇琥珀酸酯44％，葵花籽油34％，葵花籽天然磷脂粉末14％，山梨酸0.5％，水7％，苯甲酸钠0.5％。
本申请实施例的纳米稳定剂的制备方法为：准确称量食品级中链脂肪酸甘油三酯放入反应釜中，反应釜温度控制在45摄氏度以下。待中链脂肪酸甘油三酯升温后加入准确称量的山梨酸，搅拌使其溶解；再加入准确称量的葵花籽天然磷脂，搅拌使其溶解；最后加入维生素E聚乙二醇琥珀酸酯，温度升高至50℃～60℃，搅拌至均匀。将配比量的苯甲酸钠溶于60摄氏度的水中，再加入之前的混合物中，水浴60摄氏度，搅拌至均匀。温度调至室温，保持搅拌并冷却至室温，即可得到纳米稳定剂。
取上述纳米稳定剂7份加1份二氢杨梅素，在60℃水浴加热下混合均匀，加入242份60℃的水，在60℃的水浴加热下搅拌1小时制成初乳；再用超声或者高压乳匀设备制成纳米乳液。服用时根据需要稀释。
实施例4
一种纳米稳定剂，包括以重量百分含量计的下列各原料：维生素E聚乙二醇琥珀酸酯46.5％，中链脂肪酸甘油三脂34％，葵花籽天然磷脂粉末11％，山梨酸0.5％，水7％，苯甲酸钠0.5％，皂素0.5％。
本申请实施例的纳米稳定剂的制备方法为：准确称量食品级中链脂肪酸甘油三酯放入反应釜中，反应釜温度控制在45摄氏度以下。待中链脂肪酸甘油三酯升温后加入准确称量的山梨酸，搅拌使其溶解；再加入准确称量的葵花籽天然磷脂，搅拌使其溶解；最后加入维生素E聚乙二醇琥珀酸酯，温度升高至50℃～60℃，搅拌至均匀。将配比量的苯甲酸钠和皂素溶于60摄氏度的水中，再加入之前的混合物中，水浴60摄氏度，搅拌至均匀。温度调至室温，保持搅拌并冷却至室温，即可得到纳米稳定剂。
取上述纳米稳定剂7份加1份二氢杨梅素，在60℃水浴加热下混合均匀，加入242份60℃的水，在60℃的水浴加热下搅拌1小时制成初乳；再用超声或者高压乳匀设备制成纳米乳液。服用时根据需要稀释。
以上所述，仅为本发明的具体实施方式，但本发明的保护范围并不同限于此，任何熟悉本技术领域的技术人员在本发明揭露的技术范围内，可轻易想到变化或替换，都应涵盖在本发明的保护范围之内。并且，本发明各个实施方式之间的技术方案可以相互结合，但是必须是以本领域普通技术人员能够实现为基础，当技术方案的结合出现相互矛盾或无法实现时应当认为这种技术方案的结合不存在，也不在本发明要求的保护范围之内。因此，本发明的保护范围应以所述权利要求的保护范围为准。

Claims (9)

1.一种纳米稳定剂，其特征在于，包括以重量百分含量计的下列各原料：
维生素E聚乙二醇琥珀酸酯35％～50％，甘油三脂或者植物油25％～40％，磷脂8％～15％，山梨酸0.3％～0.6％。
2.根据权利要求1所述的纳米稳定剂，其特征在于，包括以重量百分含量计的下列各原料：维生素E聚乙二醇琥珀酸酯49％，甘油三脂或者植物油36％，磷脂14％，山梨酸1％。
3.根据权利要求1或2所述的纳米稳定剂，其特征在于，所述甘油三脂包括辛酸/癸酸甘油三脂、中链脂肪酸甘油酯中的一种或两种；和/或
所述植物油包括葵花籽油、橄榄油、葡萄籽油中的一种或多种。
4.根据权利要求1或2所述的纳米稳定剂，其特征在于，所述磷脂包括葵花籽天然磷脂、合成磷脂中的一种或两种。
5.一种纳米稳定剂的制备方法，用于制备权利要求1至4任意一项所述的纳米稳定剂，其特征在于，包括以下步骤：
将所述甘油三脂或者所述植物油放置于反应釜中融化，然后向反应釜中加入所述山梨酸，再加入所述磷脂，最后加入所述维生素E聚乙二醇琥珀酸酯，温度升高至50℃～60℃，搅拌，即可得到所述纳米稳定剂。
6.权利要求1至4任意一项所述的纳米稳定剂在对疏水性生物活性化合物进行纳米乳化中的应用。
7.根据权利要求6所述的应用，其特征在于，将所述纳米稳定剂与所述疏水性生物活性化合物混合得到混合液，再向所述混合液中加入水，以实现对所述疏水性生物活性化合物的纳米乳化。
8.根据权利要求7所述的应用，其特征在于，所述疏水性生物活性化合物、所述纳米稳定剂的重量比为1∶1～9。
9.根据权利要求6所述的应用，其特征在于，所述纳米稳定剂对所述疏水性生物活性化合物进行纳米乳化后，得到的纳米乳液的液滴粒径为50nm～100nm。
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