CN116440248B - 含肽和羟丙基四氢吡喃三醇外用制剂组合物及其制备方法 - Google Patents
含肽和羟丙基四氢吡喃三醇外用制剂组合物及其制备方法 Download PDFInfo
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- CN116440248B CN116440248B CN202310334281.3A CN202310334281A CN116440248B CN 116440248 B CN116440248 B CN 116440248B CN 202310334281 A CN202310334281 A CN 202310334281A CN 116440248 B CN116440248 B CN 116440248B
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Abstract
本发明提供了含肽和羟丙基四氢吡喃三醇外用制剂组合物及其制备方法,涉及含肽的医药配制品领域,该外用制剂的原料包括:组分A、组分B、组分C和组分D;其中,组分A包括:羟丙基四氢吡喃三醇;组分B包括:四氢甲基嘧啶羧酸;组分C包括:乙酰基六肽‑8、乙酰基八肽‑3、乙酰基七肽‑4、棕榈酰三肽‑5、乙酰基四肽‑2、甘油、1,2‑己二醇、PPG‑5‑鲸蜡醇聚醚‑20、乙基己基甘油;组分D包括:丁二醇、芍药根提取物、1,2‑己二醇。该外用制剂组合物能够有效修复皮肤损伤,能够安全实现良好的抗皱抗衰、修复效果。
Description
技术领域
本发明涉及含肽的医药配制品领域,具体涉及含肽和羟丙基四氢吡喃三醇外用制剂组合物及其制备方法。
背景技术
衰老由内源性因素和外源性因素共同作用的结果,其中,氧化自由基损伤以及NAD+水平下降是导致衰老问题发生的两大因素,此外,皮肤屏障的受损也是衰老的关键影响因素,皮肤屏障受损后,通常会造成皮肤大量流失水分、营养,进而加速老化过程,但目前皮肤屏障临床修复产品,如过氧化苯甲酰或维A酸类等,通常会存在表皮屏障损伤、经表皮失水等问题。
在现有的不同种类具有抗衰老功效的原料中,有两种功效性组分被重点关注,羟丙基四氢吡喃三醇是一种具有抗衰老活性物的木糖衍生物,能够促进胶原蛋白合成,预防衰老。肽,例如乙酰基六肽-8,它可以参与竞争SNAP-25在融泡复合体的位点,进而影响复合体的形成。当融泡复合体稍有不稳定时,囊泡不能有效释放神经递质,从而致使肌肉收缩减弱,有助于防止皱纹的形成。现有的研究,如专利CN113117051A公开了一种抗衰老透皮多肽制剂及其制备方法,该透皮制剂包括以下按重量百分比计的组分:羟丙基四氢吡喃三醇1%-50%、胶原蛋白肽0.1%-5%、腺苷0.1%-1.0%、肌肽0.1%-0.5%、透皮肽0.5%-5.0%、对羟基苯乙酮0.4%-0.8%与余量的水。该多肽制剂具有促进吸收率提高、胶原蛋白合成,防止糖基化,抑制脂质氧化等功效。但该发明更侧重于提高透皮多肽制剂的皮肤吸收率问题,对皮肤修复等未做重点关注。
再如专利CN115317416A公开了一种补水抗衰修复组合物及其制备工艺和应用,该组合物包括A、B、C、D四种组分,其中,A组分包括Gly-Gly和/或Ala-Gln,以及乙酰基六肽-37;B组分包括GHK、GHK.Cu、乙酰基四肽-22、乙酰基六肽-8、六肽-9、六肽-10、七肽、乙酰基十肽-3、十肽-4或十五肽中的一种或多种;C组分包括高纯竹荪提取物,以及羟丙基四氢吡喃三醇和/或高纯积雪草提取物;D组分包括海藻糖和/或甘露糖。该组合物在保证抗衰修复的前提下,补水保湿效果优良。但该发明中的组合物更侧重于化妆品层面,其功效更偏向于护肤,抗衰等效果通常微弱或短暂,需要持久使用才能达到相应功效。
针对现有技术中含肽和羟丙基四氢吡喃三醇产品所存在的抗衰效果弱或短暂,且难以起到修复作用的问题,寻找一种功效优异的抗衰修复含肽和羟丙基四氢吡喃三醇外用制剂组合物及其制备方法十分必要。
发明内容
本发明针对现有技术存在的问题,提供了含肽和羟丙基四氢吡喃三醇外用制剂组合物及其制备方法,该外用制剂组合物能够有效修复皮肤损伤,能够安全实现良好的抗衰效果。
为实现上述目的,本发明采用的技术方案如下:
本发明提供了一种外用制剂,原料包括:组分A、组分B、组分C和组分D;所述组分A包括:羟丙基四氢吡喃三醇;
所述组分B包括:四氢甲基嘧啶羧酸;
所述组分C包括:乙酰基六肽-8、乙酰基八肽-3、乙酰基七肽-4、棕榈酰三肽-5、乙酰基四肽-2、甘油、1,2-己二醇、PPG-5-鲸蜡醇聚醚-20、乙基己基甘油;所述组分D包括:丁二醇、芍药根提取物、1,2-己二醇。
进一步地,按重量份数计,所述组分C包括:0.01-0.03份乙酰基六肽-8、0.01-0.03份乙酰基八肽-3、0.005-0.01份乙酰基七肽-4、0.001份棕榈酰三肽-5、0.001份乙酰基四肽-2、24-27份甘油、2-4份1,2-己二醇、0.8-1.5份PPG-5-鲸蜡醇聚醚-20、0.1-0.3份乙基己基甘油。
优选地,按重量份数计,所述组分C包括:0.02份乙酰基六肽-8、0.02份乙酰基八肽-3、0.008份乙酰基七肽-4、0.001份棕榈酰三肽-5、0.001份乙酰基四肽-2、25份甘油、3份1,2-己二醇、1份PPG-5-鲸蜡醇聚醚-20、0.2份乙基己基甘油。
进一步地,按重量份数计,所述组分D包括:30-35份丁二醇、6-9份芍药根提取物、0.8-1.5份1,2-己二醇。
优选地,按重量份数计,所述组分D包括:32份丁二醇、8份芍药根提取物、1份1,2-己二醇。
进一步地,所述C组分和D组分均还包括水。
进一步地,所述组分A、组分B、组分C和组分D的重量比为9-10:0.2-0.4:0.8-1.5:0.2-0.4。
优选地,所述组分A、组分B、组分C和组分D的重量比为9.5:0.3:1:0.3。
进一步地,所述羟丙基四氢吡喃三醇、四氢甲基嘧啶羧酸和乙酰基六肽-8的重量比为9-10:0.2-0.4:0.00008-0.00045。
进一步地,所述四氢甲基嘧啶羧酸、乙酰基八肽-3和芍药根提取物的重量比为0.2-0.4:0.00008-0.00045:0.012-0.036。
进一步地,所述外用制剂的剂型包括贴剂、液体剂或膏剂。
进一步地,本发明还提供了上述的外用制剂的制备方法,包括以下步骤:将组分A、组分B、组分C和组分D混合即得;所述组分C由乙酰基六肽-8、乙酰基八肽-3、乙酰基七肽-4、棕榈酰三肽-5、乙酰基四肽-2、甘油、1,2-己二醇、PPG-5-鲸蜡醇聚醚-20、乙基己基甘油混合即得,所述组分B由丁二醇、芍药根提取物、1,2-己二醇混合即得。
在一些具体的实施方式中,所述外用制剂的原料按重量份数计(实际用量占比的),包括:9-10份羟丙基四氢吡喃三醇、0.2-0.4份四氢甲基嘧啶羧酸、0.00008-0.00045份乙酰基六肽-8、0.00008-0.00045份乙酰基八肽-3、0.00004-0.00015份乙酰基七肽-4、0.000008-0.000015份棕榈酰三肽-5、0.000008-0.000015份乙酰基四肽-2、0.192-0.405份甘油、0.016-0.06份1,2-己二醇、0.0064-0.0225份PPG-5-鲸蜡醇聚醚-20、0.0008-0.0045份乙基己基甘油、0.06-0.14份丁二醇、0.012-0.036份芍药根提取物、0.0016-0.006份1,2-己二醇。
在一些优选的实施方式中,所述外用制剂的原料按重量份数计(实际用量占比的),包括:9.5份羟丙基四氢吡喃三醇、0.3份四氢甲基嘧啶羧酸、0.0002份乙酰基六肽-8、0.0002份乙酰基八肽-3、0.00008份乙酰基七肽-4、0.00001份棕榈酰三肽-5、0.00001份乙酰基四肽-2、0.25份甘油、0.03份1,2-己二醇、0.01份PPG-5-鲸蜡醇聚醚-20、0.002份乙基己基甘油、0.096份丁二醇、0.024份芍药根提取物、0.003份1,2-己二醇。
本发明所取得的技术效果是:
本发明组合物中,乙酰基六肽-8能够竞争性结合SNAP-25受体,抑制神经递质传导,从而减少面部肌肉收缩皱纹形成;四氢甲基嘧啶羧酸具有以下性能:①隔离:可以在细胞、酶、蛋白质和其他生物分子周围形成一个保护壳,从而降低炎症和损伤反应。②修复:能提升皮肤细胞的免疫防护能力,改善肌肤薄、粗糙、疤痕等不良状况,使肌肤恢复平滑。③保湿:是非常优秀的保湿剂。可以滋润补水,改善皮肤微循环,促进透明质酸合成和分泌。羟丙基四氢吡喃三醇通过促进细胞外基质的合成,从而起到恢复细胞外基质功能作用,诱导真皮层中糖胺聚糖(GAGS)的生成,促进真皮层细胞加速产生IV型、VII型胶原蛋白,增强真皮层和表皮层的连接性,使表皮和真皮贴合更紧密,提高真皮层和表皮层的结合能力。乙酰基八肽-3是基于人体皮肤生化机制而设计的抗皱多肽活性原料,其活性比母体肽六胜肽活性更强,具有抗皱的作用。芍药根提取物能够增强皮肤细胞的活力和性能,促进胶原蛋白纤维的合成,减少脂质过氧化物的产生,进而延缓机体组织的衰老。羟丙基四氢吡喃三醇、四氢甲基嘧啶羧酸和乙酰基六肽-8之间,以及四氢甲基嘧啶羧酸、乙酰基八肽-3和芍药根提取物之间均存在协同作用,三者相互协同应用至本发明的外用制剂组合物中,能够有效提高组合物的修复皮肤损伤功能,安全实现良好的抗皱抗衰效果。
具体实施方式
以下通过特定的具体实例说明本发明的实施方式,本领域技术人员可由本说明书所揭露的内容轻易地了解本发明的其他优点与功效。本发明还可以通过另外不同的具体实施方式加以实施或应用,本说明书中的各项细节也可以基于不同观点与应用,在没有背离本发明的精神下进行各种修饰或改变。
在进一步描述本发明具体实施方式之前,应理解,本发明的保护范围不局限于下述特定的具体实施方案;还应当理解,本发明实施例中使用的术语是为了描述特定的具体实施方案,而不是为了限制本发明的保护范围。
当实施例给出数值范围时,应理解,除非本发明另有说明,每个数值范围的两个端点以及两个端点之间任何一个数值均可选用。除非另外定义,本文中使用的所有技术和科学术语具有与本发明所属技术领域的普通技术人员通常理解的相同意义。
值得说明的是,本发明中使用的芍药提取物购自扶风斯诺特生物科技有限公司,其余原料均为普通市售产品,因此对其来源不做具体限定。
实施例1
本实施例的组方,详见下表:
表1实施例1的组方
实施例2
本实施例的组方,详见下表:
表2实施例2的组方
实施例3
本实施例的组方,详见下表:
表3实施例3的组方
对比例1
本对比例的组方(与实施例3的区别仅在于,将乙酰基八肽-3、芍药根提取物替换为等量四氢甲基嘧啶羧酸),详见下表:
表4对比例1的组方
对比例2
本对比例的组方(与实施例3的区别仅在于,将四氢甲基嘧啶羧酸、芍药根提取物替换为等量乙酰基八肽-3),详见下表:
表5对比例2的组方
对比例3
本对比例的组方(与实施例3的区别仅在于,将乙酰基八肽-3、四氢甲基嘧啶羧酸替换为等量芍药根提取物),详见下表:
表6对比例3的组方
对比例4
本对比例的组方(与实施例3的区别仅在于,羟丙基四氢吡喃三醇、四氢甲基嘧啶羧酸和乙酰基六肽-8的重量比不同),详见下表:
表7对比例4的组方
一、抗皱功效测试
(1)测试目的:通过测量健康男女性受试者在使用测试样品前和使用样品后皱纹特征计数的变化,来检测各实例样品的抗皱功效。
(2)受试者:选择符合试验要求的中国健康男性或女性;
年龄30-60周岁;
能很好配合试验者,在研究期间能保持生活的规律性;
每组10人,共计60人。
(3)排除标准:
凡具有下列任一条件的必须排除进入本项研究:
近一周使用抗组胺药或近一个月内使用免疫抑制剂者。
近两个月内受试部位应用任何抗炎药物者。
受试者患有炎症性皮肤临床未愈者。
胰岛素依赖性糖尿病患者。
正在接受治疗的哮喘或其他慢性呼吸系统疾病患者。
在近6个月内接受抗癌化疗者。
免疫缺陷或自身免疫性疾病患者。
哺乳期或妊娠妇女。
双侧乳房切除及双侧腋下淋巴结切除者。
在皮肤待试部位由于瘢痕、色素、萎缩、鲜红斑痣、肤色不均、毛囊炎或其他瑕疵而影响试验结果的判定者。
参加其他的临床试验研究者。
2个月内参加过其他的临床试验包括斑贴试验研究者。
体质高度敏感者。
非自愿参加或不能按实验要求完成规定内容者。
研究者认为不适于参加本研究者。
(4)待测样:
实施例1-3以及对比例1-4中产品(对比例2中产品肽含量较高,存在较强致敏作用,不进行后续抗皱试验)。
(5)测试方法:
测试参数:皱纹特征计数;
仪器:皮肤图像分析仪;
测试时间点:第0天(记为D0)、第28天(记为D28);
测试部位:脸部;
测试方式:用洁面产品清洁面部,并用干面巾纸擦干皮肤,在温度21±1℃,50±10% RH的实验室中静坐30min后,使用皮肤图像分析仪对面部皱纹特征进行采集并统计。
(6)使用方法:
使用部位:脸部;
使用频率:一天两次,早晚各一次;
使用周期:4周;
使用方法:全脸使用。
表8皱纹特征计数
实例 | D0 | D28 | 下降率(%) |
实施例1 | 121.78±24.25 | 97.64±26.36* | 19.82 |
实施例2 | 116.52±22.13 | 90.09±20.23** | 22.68 |
实施例3 | 124.33±30.26 | 95.42±27.58** | 23.25 |
对比例1 | 118.76±22.75 | 111.59±29.84 | 8.79 |
对比例3 | 112.68±31.60 | 105.32±31.32 | 6.53 |
对比例4 | 122.35±25.89 | 109.38±24.67 | 10.60 |
(注:与初始值D0相比,*:p<0.05,**:p<0.01。)
二、经皮失水及表皮厚度测试
(1)测试目的:通过测量小鼠在使用测试样品前和使用样品后的经皮失水率以及表皮厚度情况,来检测各实例样品的保湿功效以及抗角化情况,进而探究修复功效。
(2)受试动物:雌性裸鼠;
6-8周龄;
每组6只,共计54只。
(3)待测样:
实施例1-3以及对比例1-4中产品。
(4)测试方法:
测试参数:
仪器:失水率探头;
测试时间点:第0天(记为D0)、第21天(记为D21);
测试部位:背部;
测试方式:在裸鼠背部选择试验区皮肤(6cm×6cm),涂抹前测量含水率,涂抹各实例中产品2mg/只,空白组、模型组不涂抹产品,模型组和各实例组使用UVB紫外灯进行照射(紫外波长280-320nm,照射2h,灯管距离背部2h),每周照射5次,每天不超过1次,21天后再次测量含水率,统计失水率情况;处死裸鼠,将试验区皮肤组织切片,HE染色后,统计各组小鼠的表皮厚度。
表9经皮失水及表皮厚度测试结果
根据本申请的抗皱以及经皮失水及表皮厚度测试试验结果可知,本发明中各实施例的制剂具有良好的抗皱功效,同时具有较好的保湿性以及抑制表皮层紫外刺激增厚问题,进而可知其对皮肤屏障存在一定修复作用,主要通过前述两项方式进行,对于修复而言,是否由其他途径调控如减缓炎症细胞浸润等,还有待进一步研究。相比较之下,对比例1以及对比例3-4的相关抗皱效果较差,对比例2刺激性较强同时修复效果也并不佳,存在安全问题,不适于产品的生产与应用。
最后应当说明的是,以上内容仅用以说明本发明的技术方案,而非对本发明保护范围的限制,本领域的普通技术人员对本发明的技术方案进行的简单修改或者等同替换,均不脱离本发明技术方案的实质和范围。
Claims (5)
1.一种外用制剂,其特征在于:原料由以下成分组成:组分A、组分B、组分C和组分D;所述组分A由以下成分组成:羟丙基四氢吡喃三醇;
所述组分B由以下成分组成:四氢甲基嘧啶羧酸;
所述组分C由以下成分组成:0.02份乙酰基六肽-8、0.02份乙酰基八肽-3、0.008份乙酰基七肽-4、0.001份棕榈酰三肽-5、0.001份乙酰基四肽-2、25份甘油、3份1,2-己二醇、1份PPG-5-鲸蜡醇聚醚-20、0.2份乙基己基甘油和70.75份水;
所述组分D由以下成分组成:32份丁二醇、8份芍药根提取物、1份1,2-己二醇和59份水;
所述组分A、组分B、组分C和组分D的重量比为9.5:0.3:1:0.3。
2.一种外用制剂,其特征在于:原料由以下成分组成:组分A、组分B、组分C和组分D;所述组分A由以下成分组成:羟丙基四氢吡喃三醇;
所述组分B由以下成分组成:四氢甲基嘧啶羧酸;
所述组分C由以下成分组成:0.01份乙酰基六肽-8、0.01份乙酰基八肽-3、0.005份乙酰基七肽-4、0.001份棕榈酰三肽-5、0.001份乙酰基四肽-2、24份甘油、2份1,2-己二醇、0.8份PPG-5-鲸蜡醇聚醚-20、0.1份乙基己基甘油和73.1份水;
所述组分D由以下成分组成:30份丁二醇、6份芍药根提取物、0.8份1,2-己二醇和63.2份水;
所述组分A、组分B、组分C和组分D的重量比为9:0.2:0.8:0.2。
3.一种外用制剂,其特征在于:原料由以下成分组成:组分A、组分B、组分C和组分D;所述组分A由以下成分组成:羟丙基四氢吡喃三醇;
所述组分B由以下成分组成:四氢甲基嘧啶羧酸;
所述组分C由以下成分组成:0.03份乙酰基六肽-8、0.03份乙酰基八肽-3、0.01份乙酰基七肽-4、0.001份棕榈酰三肽-5、0.001份乙酰基四肽-2、27份甘油、4份1,2-己二醇、1.5份PPG-5-鲸蜡醇聚醚-20、0.3份乙基己基甘油和67.1份水;
所述组分D由以下成分组成:35份丁二醇、9份芍药根提取物、1.5份1,2-己二醇和54.5份水;
所述组分A、组分B、组分C和组分D的重量比为10:0.4:1.5:0.4。
4.根据权利要求1-3任一项所述的外用制剂,其特征在于:所述外用制剂的剂型包括贴剂、液体剂或膏剂。
5.如权利要求1-3任一项所述的外用制剂的制备方法,其特征在于:包括以下步骤:将组分A、组分B、组分C和组分D混合即得;所述组分C由乙酰基六肽-8、乙酰基八肽-3、乙酰基七肽-4、棕榈酰三肽-5、乙酰基四肽-2、甘油、1,2-己二醇、PPG-5-鲸蜡醇聚醚-20、乙基己基甘油混合即得,所述组分B由丁二醇、芍药根提取物、1,2-己二醇混合即得。
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