CN111956535A - 一种调理剂组合物及其制备方法与应用 - Google Patents
一种调理剂组合物及其制备方法与应用 Download PDFInfo
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- CN111956535A CN111956535A CN201911405762.9A CN201911405762A CN111956535A CN 111956535 A CN111956535 A CN 111956535A CN 201911405762 A CN201911405762 A CN 201911405762A CN 111956535 A CN111956535 A CN 111956535A
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Abstract
本发明公开了一种调理剂组合物及其制备方法与应用。本发明公开的组合物包含工业***提取物或***二酚、维生素E、视黄醇、大豆卵磷脂、辅酶Q10和植物油等。本发明的组合物主要成分配伍后具有协同增效作用,其生物利用度高,并且抗氧化性能显著提高,具有很好的抗衰老功效,并能有效缓解皮肤炎症,修复肌肤光损伤。可制成软胶囊,其质量稳定,安全无毒副作用,可内服可外用,可以作为调理剂长期使用。
Description
技术领域
本发明属于化妆品领域,涉及一种调理剂组合物及其制备方法与应用。
背景技术
***经常被用来辅助某些晚期绝症(癌症、艾滋病)的治疗,用来增进食欲、减轻疼痛,可用来缓解青光眼和癫痫、偏头痛等神经症状,以及两极情绪不稳,可以减轻化疗病人的恶心症状。
人的一生普遍要经历生长期、成熟期和老年期(衰老期)三个阶段。老年期是人生最后一个阶段,是走下坡路的历程。在人体衰老阶段,各器官、组织和***都会发生变化。但是从外观上最容易发生变化的就是皮肤及附属器官。人在40-50岁后发生衰老的最明显变化就是毛发由黑变为灰白,皮肤由光洁变为暗淡、松弛,出现老年斑,皮下脂肪变少、变性,皮肤弹性降低,皮肤干枯、变薄。皮肤衰老分为两种,一种是固有的老化,又称自然老化或内源性老化,是由于遗传因素和不可抗因素(机体内分泌及免疫功能随着机体衰老所发生的改变)所引起的;另一种是由于环境因素如紫外线、吸烟、风吹、接触化学物等引起的外源性老化,其中因日光中的紫外线长期反复照射是环境中影响皮肤老化的最重要因素,又称为光老化。
内源性老化是人体发育过程中无法避免的,目前尚无法对其采取有效措施,我们可以预防外源性的、紫外线引起的皮肤衰老。光老化的最主要机理是,皮肤中的各种成分在吸收了紫外线的能量后,可诱导产生活性氧化物,直接攻击细胞膜,引起脂质过氧化,并且耗竭细胞内的抗氧化酶,加速皮肤老化过程。同时,活性氧化物还可以激发细胞内的信号传导,诱导皮肤成纤维细胞合成基质金属蛋白酶,降解包括胶原蛋白、弹性蛋白在内的多种基质成分,从而形成光老化皮肤特有的临床表现和病理改变。
日光除引起光老化外,还会引起皮肤损伤。其中,红外线引起的生物效应主要是热效应,皮肤受红外线照射后可出现充血,形成红斑,温度升至45℃时即有灼痛感。红斑可快速消退,反复多次后可发生色素沉着;紫外线的生物效应主要属于光化学效应,能级较高的光子流引起细胞内的核蛋白和一些酶的变性。照射后要经过6-8小时的潜伏期后发生细胞的改变并出现症状,包括皮肤干痛、表皮皱缩,甚至起泡脱落。长期、多次的曝晒可造成皮肤和粘膜的日光性角化症(光照性角化症),表现在暴露部位如额部、颊部、鼻尖、唇、眼睑、结膜、出现单个或多个平顶形角化层增厚,有时可呈结节样、雀斑样或皮角样,组织病理学检查发现上皮层呈角化不全、过度角化和异常角化,细胞排列失去极性(见日光性皮炎)。这是一种癌前期变化,可能发展为皮肤癌。
减轻光老化及光损伤的主要方法就是抗氧化:清除体内自由基阻断抗氧化的途径。
目前市面上的抗衰老产品多数为食品或中药的提取物组合而成,一定程度上具有增强人体机能的作用,但是使用效果并不理想,抗衰老效果有待加强。现在的抗衰产品有的为了达到很好的抗衰老效果使用了抗氧化性强的工业成分、短时见效快,但是长时间使用对人体危害极大;有的抗衰产品添加维生素类抗氧化剂,但是这类产品稳定性差,且长期使用也有副作用,如维生素E虽然有抗衰老作用,但是每日口服超过100毫克,连续应用6个月以上者,可出现胃肠道功能紊乱、口角炎、肌无力、唇炎,并可能会引起低血糖、血栓性静脉炎、血脂和胆固醇升高等。另一方面,目前市场上已有产品,大多功能单一,大部分产品虽具有一定的抗氧化、抗衰老作用,如含有维生素E、维生素C、超氧化物歧化酶、蛋氨酸亚砜还原酶A、人类细胞保护蛋白、重组Trx-TAT-hMsrA融合蛋白等成分的产品,虽有一定的抗氧化作用,但这类产品无法对损伤的肌肤进行修复。皮肤受光损伤较重时,常用尿素软膏、尤卓尔,但这类药物副作用大,无法长时间使用。因此需要开发一种有效、可长期使用、抗氧化性能高并能够修复光损伤肌肤的产品。
***二酚(CBD)是从***花叶中萃取的一种无毒的可用于药品、化妆品、保健食品的一种高附加值的酚类物质。目前,以色列、美国、英国等发达国家已用其做原料并开发出多种特效药品和化妆品。CBD是***中的非成瘾性成分,能阻碍THC对人体神经***影响,并具有抗痉挛、抗风湿性关节炎、抗焦虑等药理活性,亦有在抗氧化、抗衰老、光损伤修复方面的报道,但单独使用***二酚(CBD)的效果不理想。
发明内容
本发明旨在提供一种调理剂组合物,该组合物抗氧化性能高并能够有效修复肌肤光损伤,可内服,可外用,具有很好的抗衰老、淡化黑色素、抗炎、光损伤修复、改善睡眠等作用。
鉴于以上目的,本发明提供一种组合物,其包含工业***提取物或***二酚、维生素E、视黄醇、大豆卵磷脂、辅酶Q10和植物油。
在一些实施方案中,上述组合物中,所述组合物以质量百分含量计包含:
以上述各组分的总和为100wt%计;
所述***二酚(CBD)可以是化学合成产物、生物合成产物、植物提取物或采用其他方式制备得到;优选地,本发明所述的***二酚是植物提取物,所述的植物提取部位可以为工业***Cannabis sativa L.的秆芯、花、叶、根和/或籽的外壳;
所述工业***提取物中按质量百分比含有30%-99%的***二酚;
优选地,所述工业***提取物中按质量百分比含有50%-99%的***二酚,更优选地,所述工业***提取物中按质量百分比含有60%-99%的***二酚,特别优选地,所述工业***提取物中按质量百分比含有95%-99%的***二酚。
优选地,所述工业***提取物为广谱系***油,所述广谱系***油为以***二酚、次***二酚、***萜酚、四氢***素等***素为主,同时涵盖黄酮、萜类等活性成分的工业***油,可直接从市场购买得到;
所述工业***提取物和***二酚均含THC,不含任何违禁物质,可直接从市场购买得到。
在一些实施方案中,上述组合物中,所述植物油为火麻仁油、向日葵籽油、橄榄油、山茶油、小麦胚芽油、甜杏仁油中的一种或多种,优选地,所述植物油为火麻仁油。
在一些实施方案中,上述组合物中,根据效用和成本,所述组合物包含以下质量百分含量的各组分:
以上述各组分的总和为100wt%计。
在一些实施方案中,上述任一所述的组合物中,所述工业***提取物或***二酚的质量百分含量可以例如为5wt%、6wt%、7wt%、8wt%。
在一些实施方案中,上述任一所述的组合物中,所述维生素E的质量百分含量可以例如为1wt%、2wt%、3wt%、4wt%。
在一些实施方案中,上述任一所述的组合物中,所述视黄醇的质量百分含量可以例如为1wt%、2wt%、3wt%。
在一些实施方案中,上述任一所述的组合物中,所述大豆卵磷脂的质量百分含量可以例如为2wt%、3wt%、4wt%。
在一些实施方案中,上述任一所述的组合物中,所述辅酶Q10的质量百分含量可以例如为2wt%、3wt%、4wt%。
在一些实施方案中,上述任一所述的组合物中,所述组合物包含以下质量百分含量的各组分:
以上述各组分的总和为100wt%计。
在一些实施方案中,上述任一所述的组合物中,所述组合物还包括牡丹籽油、柠檬果皮油、沙棘果油、葡萄籽油中的一种或几种。
在一些实施方案中,上述组合物中,根据效用和成本,所述组合物包含以下质量百分含量的各组分:
以上述各组分的总和为100wt%计。
在一些实施方案中,上述任一所述的组合物中,所述牡丹籽油的质量百分含量可以例如为1wt%、2wt%、3wt%、4wt%。
在一些实施方案中,上述任一所述的组合物中,所述柠檬果皮油的质量百分含量可以例如为1wt%、2wt%、3wt%、4wt%。
在一些实施方案中,上述任一所述的组合物中,所述沙棘果油的质量百分含量可以例如为1wt%、2wt%、3wt%、4wt%。
在一些实施方案中,上述任一所述的组合物中,所述葡萄籽油的质量百分含量可以例如为1wt%、2wt%、3wt%、4wt%。
在一些实施方案中,上述任一所述的组合物中,所述组合物包含以下质量百分含量的各组分:
上述各组分的总和为100wt%计。
在一些实施方案中,上述任一所述的组合物中,所述组合物包含以下质量百分含量的各组分:
上述各组分的总和为100wt%计。
在一些实施方案中,上述任一所述的组合物中,所述组合物包含以下质量百分含量的各组分:
以所述组合物的总质量为100wt%计。
在一些实施方案中,上述任一所述的组合物中,所述组合物包含以下质量百分含量的各组分:
以所述组合物的总质量为100wt%计。
在一些实施方案中,上述任一所述的组合物中,所述组合物包含以下质量百分含量的各组分:
以所述组合物的总质量为100wt%计。
在另一个方面,本发明还提供上述任一所述的组合物的制备方法,包括将所述植物油之外的组分加入所述植物油中,55-60℃加热搅拌溶解至澄清的步骤。
在另一个方面,本发明还提供一种软胶囊,其由囊壳和填充在囊壳中的内容物构成,所述内容物包括治疗有效量的上述任一所述的组合物。
在一些实施方案中,上述软胶囊中,所述囊壳为明胶软胶囊壳。
在另一个方面,本发明还提供上述任一所述的软胶囊的制备方法,包括将除所述植物油之外的组分加入所述植物油中,55-60℃加热搅拌溶解至澄清,装入所述囊壳内的步骤。
在另一个方面,本发明还提供上述任一所述的组合物和/或上述任一所述的软胶囊在制备如下任一所示的产品中的应用:
1)抗氧化的产品;
2)修复皮肤光照损伤的产品;
3)预防或治疗皮肤炎症的产品;
4)抗衰老的产品;
5)改善睡眠的产品;
6)调节内分泌的产品;
7)提高机体免疫力的产品。
本发明的调理剂组合物中主要成分配伍后具有协同增效作用,生物利用度高,其抗氧化性能显著提高,具有很好的抗衰老功效,并能有效缓解皮肤炎症,修复肌肤光损伤,还可调节内分泌,改善睡眠,稳定性好,其安全无毒副作用,可长期使用,外用可滋养皮肤、延缓皮肤衰老、有效缓解皮肤炎症、减轻皮肤光损,内服可促进睡眠、调节内分泌、提高机体免疫力,同时可以抑制与清除体内自由基。本发明的组合物可以作为调理剂长期使用。
具体实施方式
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。
以下结合具体实施例,对本发明作进一步说明。应理解,以下实施例仅用于说明本发明而非用于限定本发明的范围。
广谱系***油和***二酚均为云南汉盟制药有限公司实验室自制样品。
实施例1
称量8g广谱系***油、1g维生素E、2g视黄醇、2g大豆卵磷脂、2g辅酶Q10和85g火麻仁油,将称量好的广谱系***油、维生素E、视黄醇、大豆卵磷脂、辅酶Q10依次加入到火麻仁油中,55-60℃加热3h,搅拌溶解至澄清,装入明胶软胶囊壳内,0.58g/粒。
实施例2
称量5g广谱系***油、4g维生素E、0.1g视黄醇、0.1g大豆卵磷脂、4g辅酶Q10、3g牡丹籽油和83.8g火麻仁油,将称量好的广谱系***油、维生素E、视黄醇、大豆卵磷脂、辅酶Q10、牡丹籽油依次加入到火麻仁油中,55-60℃加热3h,搅拌溶解至澄清,装入明胶软胶囊壳内,0.58g/粒。
实施例3
称量10g***二酚、0.1g维生素E、5g视黄醇、5g大豆卵磷脂、0.1g辅酶Q10、4.8g柠檬果皮油和75g火麻仁油,将称量好的***二酚、维生素E、视黄醇、大豆卵磷脂、辅酶Q10、柠檬果皮油依次加入到火麻仁油中,55-60℃加热3h,搅拌溶解至澄清,装入明胶软胶囊壳内,0.58g/粒。
实施例4
称量10g广谱系***油、5g维生素E、5g视黄醇、5g大豆卵磷脂、5g辅酶Q10、5g柠檬果皮油和65g火麻仁油,将称量好的广谱系***油、维生素E、视黄醇、大豆卵磷脂、辅酶Q10、柠檬果皮油依次加入到火麻仁油中,55-60℃加热3h,搅拌溶解至澄清,装入明胶软胶囊壳内,0.58g/粒。
实施例5
称量5g***二酚、1g维生素E、1g视黄醇、1g大豆卵磷脂、1g辅酶Q10、1g牡丹籽油和90g火麻仁油,将称量好的***二酚、维生素E、视黄醇、大豆卵磷脂、辅酶Q10、牡丹籽油依次加入到火麻仁油中,55-60℃加热3h,搅拌溶解至澄清,装入明胶软胶囊壳内,0.58g/粒。
实施例6
称量8g***二酚、1g维生素E、2g视黄醇、4g大豆卵磷脂、0.1g辅酶Q10、3g沙棘果油和81.9g火麻仁油,将称量好的***二酚、维生素E、视黄醇、大豆卵磷脂、辅酶Q10、沙棘果油依次加入到火麻仁油中,55-60℃加热3h,搅拌溶解至澄清,装入明胶软胶囊壳内,0.58g/粒。
对比例1
称量7g维生素E、7g视黄醇、7g大豆卵磷脂、7g辅酶Q10、7g柠檬果皮油和65g火麻仁油,将称量好的维生素E、视黄醇、大豆卵磷脂、辅酶Q10、柠檬果皮油依次加入到火麻仁油中,55-60℃加热3h,搅拌溶解至澄清,装入明胶软胶囊壳内,0.58g/粒。
对比例2
称量11g广谱系***油、6g视黄醇、6g大豆卵磷脂、6g辅酶Q10、6g柠檬果皮油和65g火麻仁油,将称量好的广谱系***油、视黄醇、大豆卵磷脂、辅酶Q10、柠檬果皮油依次加入到火麻仁油中,55-60℃加热3h,搅拌溶解至澄清,装入明胶软胶囊壳内,0.58g/粒。
对比例3
称量15g广谱系***油,加入65g火麻仁油中,55-60℃加热3h,搅拌溶解至澄清,装入明胶软胶囊壳内,0.58g/粒。
对比例4
称量35g维生素E,加入65g火麻仁油中,55-60℃加热3h,搅拌溶解至澄清,装入明胶软胶囊壳内,0.58g/粒。
对比例5
称量12g广谱系***油、15g维生素E,加入65g火麻仁油中,55-60℃加热3h,搅拌溶解至澄清,装入明胶软胶囊壳内,0.58g/粒。
测试例1抗氧化性能评价
分别取实施例1-6及对比例1-5制备的软胶囊内容物配制成不同浓度的乙醇溶液(每一个样品都分别配制为6、10、15、20、25、50μg/mL的浓度),分别取上述配制好的待测样品2.0mL加入具塞试管中,加入2.0mL 0.2mmol/L的DPPH溶液,摇匀后避光反应30min,用无水乙醇作参比,在517nm下测定其吸光度A1;同时测定2.0mL 0.2mmol/L的DPPH溶液与2.0mL的无水乙醇混合液的吸光度A0,以及2.0mL待测样品与2.0mL的无水乙醇混合液的吸光度A2。测定结果以清除率(E)表示,计算公式为:E=[1-(A1-A2)]/A0×100%。以待测样品的浓度为横坐标,清除率值为纵坐标绘制待测样品清除DPPH·的曲线,根据曲线的线性回归方程,计算得到DPPH·清除率为50%时的待测样品浓度,定义为半抑制浓度(IC50)。用清除率为50%的样品浓度IC50值来衡量样品对DPPH·的清除能力,结果见表1。
表1各样品清除DPPH的能力比较
从表1可以看出,实施例1-6的组合物均具有很好的自由基清除效果,对比例1-5的组合物虽有一定的清除自由基作用,但是效果明显不如实施例1-6的组合物。特别是对比例3和4,与其他实施例和对比例相比,自由基清除作用显著下降,说明***二酚与维生素E组合后其抗氧化活性增强,特别是再与本发明组合物中其它成分配伍后抗氧化活性更强,说明组合物的各个组分组合后具有协同增效作用。
测试例2修复光损伤的动物实验
剔除小鼠(ICR小鼠,购自浙江中医药大学动物实验中心,体重量为20±5g)背部毛发,充分暴露其背部皮肤后进行UVB(300mJ/cm2)辐照小鼠,每天一次,连续3天,造模结束,造模成功的小鼠背部皮肤出现明显红斑鳞屑改变。
建模成功的小鼠共100只,随机分成10组,每组10只,各组小鼠分别给以实施例1-6及对比例1-5制备的软胶囊内容物,每日早晚分别涂抹1ml胶囊内容物于小鼠背部损伤皮肤,共给药两周。
对小鼠背部UVB照射区域进行皮肤损伤状况评分(评分细则见表2),结果如表3所示。
表2小鼠背部UVB照射区域皮肤损伤状况评分标准
表3小鼠背部皮肤损伤状况评分
从表3的结果可以看出,与对比例的组合物相比,本发明实施例1-6的组合物具有较好的光修复作用,说明***二酚或广谱系***油与其它成分配伍后光损伤修复作用增强,具有协同增效作用。
Claims (10)
1.一种组合物,其包含工业***提取物或***二酚、维生素E、视黄醇、大豆卵磷脂、辅酶Q10和植物油。
4.根据权利要求1-3任一项所述的组合物,其特征在于:所述植物油为火麻仁油、向日葵籽油、橄榄油、山茶油、小麦胚芽油、甜杏仁油中的一种或多种;
优选地,所述植物油为火麻仁油。
5.根据权利要求1-4任一项所述的组合物,其特征在于:所述工业***提取物中按质量百分比含有30%-99%的***二酚;
优选地,所述工业***提取物中按质量百分比含有50%-99%的***二酚;
优选地,所述工业***提取物为广谱系***油。
6.根据权利要求1所述的组合物,其特征在于:所述组合物还包含牡丹籽油、柠檬果皮油、沙棘果油、葡萄籽油中的一种或多种。
8.一种软胶囊,其由囊壳和填充在囊壳中的内容物构成,所述内容物包括治疗有效量的权利要求1-7任一项所述的组合物。
9.根据权利要求8所述的软胶囊,其特征在于:所述囊壳为明胶软胶囊壳。
10.权利要求1-7任一项所述的组合物和/或权利要求8或9所述的软胶囊在制备如下任一所示的产品中的应用:
1)抗氧化的产品;
2)修复皮肤光照损伤的产品;
3)预防或治疗皮肤炎症的产品;
4)抗衰老的产品;
5)改善睡眠的产品;
6)调节内分泌的产品;
7)提高机体免疫力的产品。
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