CN106619163A - 光甘草定纳米混悬剂及其制备方法 - Google Patents
光甘草定纳米混悬剂及其制备方法 Download PDFInfo
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Abstract
本发明涉及光甘草定纳米混悬剂及其制备方法。本发明制剂处方中以重量百分比计含有0.5～20％的光甘草定、0.1～20％的稳定剂及余量的水。本发明采用超声预分散结合高压均质法制备光甘草定纳米混悬剂。本发明的光甘草定纳米混悬剂大大改善光甘草定的溶解性，提高了使用效率，并且减少了其在化妆品中的用量，节约生产成本。
Description
技术领域
本发明涉及美容护肤化妆品技术领域，具体涉及一种光甘草定纳米混悬剂及其制备方法。
背景技术
光甘草定是光果甘草中的主要黄酮类成分之一，是目前国际上高档美白化妆品的主要功效成分。它能深入皮肤内部并保持高活性，美白并高效抗氧化。有效抑制黑色素生成过程中多种酶的活性，特别是抑制酪胺酸酵素活性。同时还具有防止皮肤粗糙和抗炎、抗菌的功效。光甘草定是目前疗效好、功能全面的美白成分。经实验室证明，光甘草定的美白功效，比常见美白成分维生素C高出232倍，也因此受到人们的大力追捧。此外，光甘草定尚有一定的降血脂和降血压的作用。
从一吨的新鲜光果甘草中，仅能提取到不足100g的光甘草定。超低的提取率，让光甘草定的成本，几近等同黄金。因此在世界化妆品界，被誉为“美白黄金”。然而光甘草定不溶于水，且在液态油脂中溶解度低，在实际应用时其透皮吸收效果不理想，因此效果的发挥往往被限制。
纳米混悬制剂仅由有效成分、稳定剂(表面活性剂或者高分子聚合物)及水组成。不同于其他的纳米体系，此技术体系不采用任何药物载体，因此具有载药量高、副作用小、起效快等优势。它是一种通过提高饱和溶解度及溶出速度并且提高皮肤吸附效果来改善难溶性有效成分成分的生物利用度的方法。制备光甘草定纳米混悬剂，预期可提高光甘草定的溶出速率、改善其生物利用度的同时节约用量，降低成本。
目前纳米混悬剂的制备方法主要有沉淀法和高压均质法两种。其中高压均质法无需使用有机溶剂，得到的颗粒粒径小、分布范围窄、污染小，且高压均质技术易于实现工业化生产，因此发展空间广阔。
发明内容
本发明的目的是提供一种提高光甘草定溶解速率的纳米混悬剂及其制备方法。
本发明的光甘草定纳米混悬制剂，其特征在于：按重量百分比计，其含有0.5～20％的光甘草定、0.1～20％的稳定剂及余量的水。
本发明的光甘草定纳米混悬制剂，其粒径范围在适宜皮肤吸收的100～800nm。
本发明的光甘草定纳米混悬剂制备方法，包括以下制备步骤：
(1)在搅拌下将光甘草定原料粉末直接加入到含有稳定剂的水溶液中，500W超声30秒，形成光甘草定粗混悬剂；
(2)将光甘草定粗混悬剂转移至0～5℃预冷的高压均质机中均质，先在500bar下循环5次，然后在1300bar～1500bar下循环10-20次，制成光甘草定纳米混悬剂。
本发明所述的稳定剂为吐温80、泊洛沙姆188、十二烷基硫酸钠、多库酯钠、胆酸钠、羟丙甲基纤维素、聚乙烯吡咯烷酮中的一种或多种。
本发明的优点在于：
(1)光甘草定难溶于水，且价格昂贵，制成纳米混悬剂后，光甘草定能够迅速溶解并且加强皮肤吸附。增强使用效果的同时，降低光甘草定在化妆品中的使用量，节约生产成本。
(2)本发明的光甘草定纳米混悬剂制备方法采用超声预分散结合高压均质。超声可防止后期高压均质过程的堵塞。工艺简单，剂量准确，适宜于规模化生产。
(3)本发明的纳米混悬剂处方中，经过大量的处方筛选，选择吐温80、泊洛沙姆188、十二烷基硫酸钠、多库酯钠、胆酸钠、羟丙甲基纤维素E5、聚乙烯吡咯烷酮K17中的一种或多种作为纳米混悬剂的稳定剂，得到的光甘草定纳米混悬剂可以稳定地存在6个月以上，有利于进一步加工。
附图说明
图1：光甘草定纳米混悬剂粒径分布图，横坐标：粒径(diameter)，纵坐标：百分率(％，intensity)。
下面实施例仅对本发明作进一步的详细说明，但应注意本发明的保护范围不应受这些实例的任何限制。
实施例1
将0.8g光甘草定在搅拌下加入到含有0.4g吐温80的80ml水溶液中，500W超声30秒，形成光甘草定粗混悬剂。将光甘草定粗混悬剂转移至0～5℃预冷的高压均质机中均质，先在500bar下循环5次，然后在1300bar下循环15次，即得光甘草定纳米混悬剂，测得纳米混悬剂的平均粒径为342nm。粒径分布如图1所示，表明其粒径分布范围均一。
实施例2
将1g光甘草定在搅拌下加入到含有0.5g泊洛沙姆188的100ml水溶液中，500W超声30秒，形成光甘草定粗混悬剂。将光甘草定粗混悬剂转移至0～5℃预冷的高压均质机中均质，先在500bar下循环5次，然后在1300bar下循环15次，即得光甘草定纳米混悬剂，测得纳米混悬剂的平均粒径为395nm。
实施例3
将2g光甘草定在搅拌下加入到含有0.1g十二烷基硫酸钠的50ml水溶液中，500W超声30秒，形成光甘草定粗混悬剂。将光甘草定粗混悬剂转移至0～5℃预冷的高压均质机中均质，先在500bar下循环5次，然后在1400bar下循环12次，即得光甘草定纳米混悬剂，测得纳米混悬剂的平均粒径为591nm。
实施例4
将3g光甘草定在搅拌下加入到含有0.5g羟丙甲基纤维素E5和0.2g胆酸钠的100ml水溶液中，500W超声30秒，形成光甘草定粗混悬剂。将光甘草定粗混悬剂转移至0～5℃预冷的高压均质机中均质，先在500bar下循环5次，然后在1300bar下循环20次，即得光甘草定纳米混悬剂，测得纳米混悬剂的平均粒径为433nm。
实施例5
将0.5g光甘草定在搅拌下加入到含有0.4g聚乙烯吡咯烷酮K17的50ml水溶液中，500W超声30秒，形成光甘草定粗混悬剂。将光甘草定粗混悬剂转移至0～5℃预冷的高压均质机中均质，先在500bar下循环5次，然后在1300bar下循环15次，即得光甘草定纳米混悬剂，测得纳米混悬剂的平均粒径为501nm。
实施例6
将0.5g光甘草定在搅拌下加入到含有0.3g多库酯钠的50ml水溶液中，500W超声30秒，形成光甘草定粗混悬剂。将光甘草定粗混悬剂转移至0～5℃预冷的高压均质机中均质，先在500bar下循环5次，然后在1500bar下循环15次，即得光甘草定纳米混悬剂，测得纳米混悬剂的平均粒径为776nm。
Claims (3)
1.一种光甘草定纳米混悬剂，其特征在于，按重量百分比计，其含有0.5～20％的光甘草定、0.1～20％的稳定剂及余量的水。
2.根据权利要求1所述的光甘草定纳米混悬剂，其特征在于包括以下制备步骤：
(1)在搅拌下将光甘草定原料粉末直接加入到含有稳定剂的水溶液中，500W超声30秒，形成光甘草定粗混悬剂；
(2)将光甘草定粗混悬剂转移至0～5℃预冷的高压均质机中均质，先在500bar下循环5次，然后在1300bar～1500bar下循环10-20次，制成光甘草定纳米混悬剂。
3.根据权利要求1或2所述的光甘草定纳米混悬剂，其特征在于所述稳定剂选自吐温80、泊洛沙姆188、十二烷基硫酸钠、多库酯钠、胆酸钠、羟丙甲基纤维素、聚乙烯吡咯烷酮中的一种或多种。
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| CN108904316A (zh) * | 2018-08-17 | 2018-11-30 | 江西中医药大学 | 天然美白抗氧化组合物及由其制备的纳米凝胶化妆品 |
| CN109316439A (zh) * | 2018-11-26 | 2019-02-12 | 华熙福瑞达生物医药有限公司 | 一种含有海茴香干细胞的混悬修护精华液 |
| CN109316439B (zh) * | 2018-11-26 | 2021-08-06 | 华熙生物科技股份有限公司 | 一种含有海茴香干细胞的混悬修护精华液 |
| CN111658615A (zh) * | 2020-07-31 | 2020-09-15 | 青岛科技大学 | 吲哚美辛纳米粒及其制备方法 |
| CN111686078A (zh) * | 2020-07-31 | 2020-09-22 | 青岛科技大学 | 槲皮素纳米粒及其制备方法 |
| CN113786369A (zh) * | 2021-11-05 | 2021-12-14 | 青岛科技大学 | 一种含人参总皂苷的天然抗氧化纳米组合物及其制备方法 |
| CN115120563A (zh) * | 2022-05-06 | 2022-09-30 | 青岛科技大学 | 一种姜黄素与青蒿素组合纳米粒及其制备方法 |
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