CN114869816A - 一种马齿苋提取物组合物 - Google Patents
一种马齿苋提取物组合物 Download PDFInfo
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Abstract
本发明涉及一种包含油性马齿苋提取物的组合物，该组成物应用于经皮吸收的药品或化妆品领域，通过添加芦笋提取物成分有效提高了油性马齿苋提取物的透皮递送性。
Description
技术领域
本发明涉及一种包含马齿苋提取物的组合物，该组成物应用于经皮吸收的药品或化妆品领域，有效成分具有较高的透皮递送性。
背景技术
马齿苋(Portulaca oleracea L)，为马齿苋科植物，是我国的传统中药，具有散血消肿、清热解毒之功效，是我国***规定的78种药食同源性野生植物之一。马齿苋的全草含有丰富的肾上腺素、黄酮、强心苷等物质，研究结果表明：马齿苋的种子、叶中含丰富的不饱和脂肪酸，例如ω-3、6脂肪酸，ω-3、6脂肪酸可以有效减少花生四烯酸的产生，在人体，尤其是皮肤中，不饱和脂肪酸是重要的抗炎成分。
近年来以天然成分、植物成分为主要配方的护肤品逐渐受到关注和喜爱，不断开发新的天然成分护肤品，使其达到更好的护肤效果，已成为本领域当前的重要研究课题。目前对护肤品的使用已不局限于单纯的护肤领域，还延伸至一些皮肤病的辅助治疗领域。
对于皮肤类保养品和药品，有效成分经皮吸收率是一个重要的产品指标，马齿苋所含的不饱和脂肪酸例如ω-3脂肪酸等均是脂溶性的油性物质，这类物质通常难以经皮输送，使用后残留在皮肤表面后，很容易被洗掉。因此，需要增强油性马齿苋提取物透皮递送的效果。
芦笋(Asparagus officinalis linn.)，学名石刁柏，又名龙须菜、文山竹、露笋等，是百合科天门冬属多年生宿根性草本植物。芦笋是一种质地优良、营养丰富的保健型蔬菜，含有人体不可缺少的氨基酸、矿物质和其它多种营养元素，也含有皂苷类化合物及黄酮类等多种活性成分。芦笋提取物具有溶血、降胆固醇、抗炎和对肿瘤的抑制作用等多方面的药理活性，研究发现芦笋提取物能具有抗癌、抗菌作用。
发明内容
本发明发现，芦笋提取物能显著提高含有不饱和脂肪酸有效成分的油性马齿苋提取物的透皮递送率，从而提高油性马齿苋提取物在经皮吸收化妆品和药物领域的应用前景和价值。
本发明提供一种提高油性马齿苋提取物透皮递送率的方法，其特征在于将所述油性马齿苋提取物与芦笋提取物或含有芦笋提取物的溶液混合。
本发明进一步提供一种含马齿苋提取物的组合物，其特征在于，所述组合物包括油性马齿苋提取物、芦笋提取物，所述组合物具有提高的油性马齿苋提取物透皮递送率。
所述油性马齿苋提取物通过亲脂性溶剂例如：***、乙酸乙酯、丙烷、丁烷流体以及超临界CO2流体萃取得到。
所述芦笋提取物为醇或水或醇/水提取物。
所述芦笋提取物以溶液的方式存在。
所述芦笋提取物溶液的浓度为10-20mg/ml。
本发明有利且令人惊讶地消除或减少了现有油性马齿苋提取物透皮递送的效果差的缺点。特别地，将芦笋的醇或水或醇/水提取物用作分散介质，以增强油性马齿苋提取物的透皮递送性并增强包括油性马齿苋提取物分散体的组合物的透皮递送性。本发明的分散介质由天然产物形成，甚至可以食用。
具体实施方式
下面通过实施例的方式进一步说明本发明，但并不因此将本发明限制在所述的实施例范围之中。下列实施例中未注明具体条件的实验方法，按照常规方法和条件，或按照商品说明书选择。
实施例1
含不饱和脂肪酸的油性马齿苋提取物的制备
以鲜马齿苋、生活饮用水为主要原料，鲜马齿苋经挑选、清洗、切碎，按重量比1:3比例加水浸泡12h，80℃下熬煮6h，过滤获得马齿苋渣。
亚临界异丁烷萃取技术萃取马齿苋渣，提取油性马齿苋提取物：亚临界流体萃取工艺设定条件为，萃取压力0.8MPa，萃取温度40℃，萃取150min，得到马齿苋油浸膏，萃取三次后合并每次得到的马齿苋油浸膏，经4000r/min离心15min、过滤后制备获得粗油性马齿苋提取物。
按照g/mL计，将粗油性马齿苋提取物与0.5mol/L KOH-乙醇溶液按1：20混合，然后放于75℃的水浴中搅拌、回流120min，得到皂化液；加入与0.5mol/L KOH-乙醇溶液等量的冰蒸馏水迅速冷却，然后用与0.5mol/L KOH-乙醇溶液等量的石油醚萃取皂化物，经萃取多次，取水层加一倍量水稀释，缓慢加入10％的HCl，调至pH＝2-3，此时可明显看到油层和水层，立即用与0.5mol/L KOH-乙醇溶液等量的石油醚萃取混合脂肪酸，萃取多次，通过分液漏斗得到石油醚层；石油醚层用5％的NaCl溶液水洗至中性，再用无水硫酸钠干燥、过滤后旋转蒸发，即得纯化的油性马齿苋提取物，该提取物呈淡黄色。
实施例2
芦笋提取物的制备
(1)将芦笋干燥、粉碎，过10-40目筛，按固/液比1∶5-1∶20(W/V)加入70％的乙醇，在超声功率20-800W/cm2，温度20-60℃条件下，提取40分钟，经液-固分离得到芦笋的提取液，提取液减压蒸馏回收乙醇；
(2)将步骤(1)得到的浓缩液按体积比为1∶0.5加入水饱和正丁醇进行萃取，按相同的方法再重复2-3次，合并萃取液，萃取剂减压回收，得到纯化的芦笋提取物；
(3)将步骤(2)得到的浸膏，分别按浓度10mg/ml、15mg/ml、20mg/ml配制成水溶液。
实施例3-6
马齿苋精油组合物的制备
按重量百分比计，按照表1所述比例混合各组分，加热至60-70℃，混合均匀后得到马齿苋精油组合物：
表1：不同组分的马齿苋精油组合物
| 组分 | 实施例3 | 实施例4 | 实施例5 | 实施例6 |
| 油性马齿苋提取物 | 7.0 | 7.0 | 7.0 | 7.0 |
| 水 | 93.0 | 0 | 0 | 0 |
| 10mg/ml芦笋提取物溶液 | 0 | 93.0 | 0 | 0 |
| 15mg/ml芦笋提取物溶液 | 0 | 0 | 93.0 | 0 |
| 20mg/ml芦笋提取物溶液 | 0 | 0 | 0 | 93.0 |
实施例7
透皮递送实验
计算不同油性马齿苋提取物溶液通过模仿人类皮肤的扩散池的扩散速率，具体步骤为：
以健康雄性Wistar大鼠背部皮肤为渗透屏障，在体外Franz扩散池中进行测试；
将皮肤固定于接收池和供给池之间(皮肤内层面向接收池)，保证皮肤与接收液之间无气泡；
扩散池参数：有效扩散面积约3.14cm2，接收池容积约8.5mL，磁力搅拌速度600rpm，接收液的温度为37.0±0.1℃。
在接收池内充满释放介质1％SDS-10％乙醇-生理盐水，排除气泡，开启搅拌，并恒温至(37.0±0.1)℃，向皮肤表面分别均匀涂布样品约1g，于1、2、4、6、8、10、12h吸取接收液0.5mL，取样后立即加入同等体积同等温度的释放介质。用HPLC测定经0.22μm滤膜过滤的接收液中马齿苋提取物的浓度。计算不同时间药物累积透过量。
按以下公式计算马齿苋提取物单位面积累积透皮量：
上述公式中：Q：累积透皮量；S：有效扩散面积；V：接收池中生理盐水体积；Ci：第1次至上次取样时接收液中药物浓度；Cn：该次取样时接收液中药物浓度；m0：样品理论称样量；m：样品实际称样量。
测试结果如表2所示。
表2：不同实施例的马齿苋提取物皮肤累积透过量(12h)
从表2的实验结果看，单独组分的实施例3马齿苋提取物精油经皮渗透量较小，实施例4-5中以芦笋提取物溶液作为分散剂，马齿苋提取物的经皮渗透量显著增加，且增加量与芦笋提取物溶液浓度呈正相关。
Claims (6)
1.一种马齿苋提取物的组合物，其特征在于，所述组合物包括油性马齿苋提取物和芦笋提取物。
2.如权利要求1所述的组合物，其特征在于，所述油性马齿苋提取物通过亲脂性溶剂萃取得到。
3.如权利要求1所述的组合物，其特征在于，所述芦笋提取物为醇或水或醇/水提取物。
4.如权利要求1所述的组合物，其特征在于，所述芦笋提取物以溶液的方式存在.
5.如权利要求4所述的组合物，其特征在于，所述芦笋提取物溶液的浓度为10-20mg/ml。
6.一种提高油性马齿苋提取物透皮递送率的方法，其特征在于将所述油性马齿苋提取物与芦笋提取物或含有芦笋提取物的溶液混合。
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