CN116270900A - 一种包含金钗石斛提取物的外用组合物及其制备方法和应用 - Google Patents
一种包含金钗石斛提取物的外用组合物及其制备方法和应用 Download PDFInfo
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Abstract
本发明涉及植物提取物技术领域,尤其涉及一种包含金钗石斛提取物的外用组合物及其制备方法和应用,所述外用组合物包括以下重量份组分制备而成:金钗石斛50~70份、黄芩30~50份、土茯苓0.5~1份、杏仁5~10份、水薄荷8~12份、石榴皮多酚15~25份、水杨酸20~50份。本发明所述外用组合物用于有效抑制痤疮病程发展,缓解痤疮皮肤病变。
Description
技术领域
本发明涉及植物提取物技术领域,尤其涉及一种包含金钗石斛提取物的外用组合物及其制备方法和应用。
背景技术
寻常痤疮(acne vulgaris)又名青年痤疮(acnejuvenilis),是一种毛囊、皮脂腺的慢性炎症,主要发生在颜面及胸背等多脂区,有自限性,皮损多形;如粉刺、丘疹、脓疱、结节,常伴有皮脂溢出,青春期后,大多痊愈或减轻。以往痤疮被认为是皮脂腺疾病,实质上损害包括毛囊、皮脂腺及表皮,属于中医“肺风粉刺”范畴。
痤疮是一种多因素的疾病,主要与皮脂产生增多,毛囊口上皮角化亢进及毛囊内丙酸痤疮杆菌增殖有关,也有一定的遗传因素。皮脂腺的发育及皮脂腺的产生受雄激素的支配,而雄激素的增加受年龄、内分泌、遗传等因素影响。痤疮患者的皮脂腺较大,皮脂腺分泌产物较正常人多,由于皮脂腺分泌增加,皮脂中亚油酸水平相对减少,(两者为负相关性)影响脂肪的合成,导致滤泡上皮缺乏脂肪酸,从而诱导滤泡过度角化,使上皮细胞不能正常脱落,导致毛囊口过度变小,皮脂不能顺畅排出,淤积在毛囊口,形成粉刺。
毛囊内正常寄生痤疮丙酸痤疮杆菌(PA),糠秕孢子菌及表皮葡萄球菌等,当游离的脂肪酸增多,丙酸痤疮杆菌不能产生足量的酶分解皮脂,淤滞的脂肪酸使毛囊周围产生非特异性炎症反应。丙酸痤疮杆菌还可分泌低分子多肽,吸引中性粒细胞进入毛囊,导致其水解酶释放,使毛囊上皮渗漏破裂,导致毛囊内容物进入周围真皮组织,造成了从单纯炎症到丘疹、脓肿、结节、囊肿的一系列临床表现。
痤疮患者皮肤中5α-还原酶比正常人高,5α-还原酶可引起皮脂增多。有严重痤疮的女性,发病突然,月经不调,雄激素升高,提示有潜在性卵巢功能不良。同时雄激素过高,还可致多毛、声音变粗,性欲增加,男性可出现脱发、黑棘皮症等。
精神压力可使肾上腺皮质分泌增加,许多痤疮病人可受精神因素影响而加重。
除上述原因外,饮食也可影响痤疮,如脂肪、糖、辛辣、可可、乳酪、花生等均可增加皮脂产生和使炎症加剧。
痤疮病程波动很大,因此治疗上变化也大。治疗痤疮目的:①纠正改变毛囊角化模式;②降低皮脂腺的活性;③减少毛囊菌群,尤其是PA;④减轻炎症反应。因此,提供一种外用非激素类高效治疗药物有待解决。
发明内容
本发明的目的在于提供一种包含金钗石斛提取物的外用组合物及其制备方法和应用,用于有效抑制痤疮病程发展,缓解痤疮皮肤病变。
为了实现上述发明目的,本发明提供以下技术方案:
本发明提供了一种包含金钗石斛提取物的外用组合物,包括以下重量份组分制备而成:金钗石斛50~70份、黄芩30~50份、土茯苓0.5~1份、杏仁5~10份、水薄荷8~12份、石榴皮多酚15~25份、水杨酸20~50份。
本发明还提供了所述包含金钗石斛提取物的外用组合物的制备方法,包括以下步骤:
金钗石斛、黄芩、土茯苓、杏仁混合,得原料混合物;原料混合物与水混合,煎煮提取2~6次,合并提取液,减压浓缩得到原料混合提取浓缩液;水薄荷进行超临界CO2萃取,得到水薄荷提取物;原料混合提取浓缩液、水薄荷提取物、石榴皮多酚和水杨酸,搅拌,得到组合物。
优选的,所述原料混合物与水的混合比例为1g:15~25mL。
优选的,所述煎煮提取的温度为130~150℃,所述每次煎煮提取的时间为50~70min。
优选的,所述减压浓缩至提取液原体积的1/10~1/12。
优选的,所述超临界CO2萃取的压力为8~12MPa,所述超临界CO2萃取的温度为45~55℃,所述超临界CO2萃取的CO2流量为15~25L/h,所述超临界CO2萃取的时间为1~2h。
优选的,所述搅拌的转速为550~600r/min,所述搅拌的温度为30~40℃。
本发明还提供了所述包含金钗石斛提取物的外用组合物或制备方法制备所得组合物在制备缓解痤疮产品中的应用。
本发明提供了一种包含金钗石斛提取物的外用组合物及其制备方法和应用,本发明以金钗石斛作为主要功效药物,进行联合配伍,得到一种具有缓解痤疮功效的配方,通过调整各原料的用量配比,结合适宜金钗石斛提取的提取方法,制备得到组合物,有效抑制痤疮病程,缓解痤疮带来的颜面部以及皮肤病变情况。
具体实施方式
本发明提供了一种包含金钗石斛提取物的外用组合物,包括以下重量份组分制备而成:金钗石斛50~70份、黄芩30~50份、土茯苓0.5~1份、杏仁5~10份、水薄荷8~12份、石榴皮多酚15~25份、水杨酸20~50份。
在本发明中,所述金钗石斛的重量份为50~70份,进一步优选为55~65份,再进一步优选为58~62份;金钗石斛:作为神经保护作用,抗炎、抗病毒因子。
在本发明中,所述黄芩的重量份为30~50份,进一步优选为35~45份,再进一步优选为38~42份;黄芩:具有抗炎、抗过敏等功效与作用;黄芩中所含的黄芩甙、黄芩甙元等成分能够损害肥大细胞的酶激活系统,抑制过敏性介体的释放,可以有效抑制组织胺所导致的皮肤过敏反应。
在本发明中,所述土茯苓的重量份为0.5~1份,进一步优选为0.6~0.9份,再进一步优选为0.7~0.8份;土茯苓:土茯苓粉外敷具有抗菌消炎、促进免疫力的功效与作用。
在本发明中,所述杏仁的重量份为5~10份,进一步优选为6~9份,再进一步优选为7~8份;杏仁:具有滋润皮肤和美白去黄等作用与功效;杏仁中所含的脂肪油可以软化皮肤角质层,滋润皮肤。
在本发明中,所述水薄荷的重量份为8~12份,进一步优选为9~11份,再进一步优选为9.5~10.5份;水薄荷:能够引起皮肤超微结构的改变,有促透作用。
在本发明中,所述石榴皮多酚的重量份为15~25份,进一步优选为16~24份,再进一步优选为18~22份;石榴皮多酚:体外有效抗炎,具有抗疤痕以及调脂功效。
在本发明中,所述水杨酸的重量份为20~50份,进一步优选为25~45份,再进一步优选为30~40份;水杨酸:可以去除聚积过厚的角质层,促进新陈代谢,还能促进表皮细胞快速更新。
本发明还提供了所述包含金钗石斛提取物的外用组合物的制备方法,包括以下步骤:
金钗石斛、黄芩、土茯苓、杏仁混合,得原料混合物;原料混合物与水混合,煎煮提取2~6次,合并提取液,减压浓缩得到原料混合提取浓缩液;水薄荷进行超临界CO2萃取,得到水薄荷提取物;原料混合提取浓缩液、水薄荷提取物、石榴皮多酚和水杨酸,搅拌,得到组合物。
在本发明中,金钗石斛、黄芩、土茯苓、杏仁混合,得原料混合物;原料混合物与水混合,煎煮提取2~6次,合并提取液,减压浓缩得到原料混合提取浓缩液;所述原料混合物与水的混合比例优选为1g:15~25mL,进一步优选为1g:16~24mL,再进一步优选为1g:18~22mL,所述煎煮提取的次数为2~6次,进一步优选为3~5次,再进一步优选为4次,所述煎煮提取的温度优选为130~150℃,进一步优选为135~145℃,再进一步优选为136~144℃,所述每次煎煮提取的时间优选为50~70min,进一步优选为55~65min,再进一步优选为58~62min,所述减压浓缩优选为至提取液原体积的1/10~1/12,进一步优选为1/11。
在本发明中,水薄荷进行超临界CO2萃取,得到水薄荷提取物;所述超临界CO2萃取的压力优选为8~12MPa,进一步优选为9~11MPa,再进一步优选为9.5~10.5MPa,所述超临界CO2萃取的温度优选为45~55℃,进一步优选为46~54℃,再进一步优选为48~52℃,所述超临界CO2萃取的CO2流量优选为15~25L/h,进一步优选为16~24L/h,再进一步优选为18~22L/h,所述超临界CO2萃取的时间优选为1~2h,进一步优选为1.2~1.8h,再进一步优选为1.4~1.6h。
在本发明中,原料混合提取浓缩液、水薄荷提取物、石榴皮多酚和水杨酸,搅拌,得到组合物;所述搅拌的转速优选为550~600r/min,进一步优选为560~590r/min,再进一步优选为570~580r/min,所述搅拌的温度优选为30~40℃,进一步优选为32~38℃,再进一步优选为34~36℃。
下面结合实施例对本发明进行详细的说明,但是不能把它们理解为对本发明保护范围的限定。
实施例1
金钗石斛60份、黄芩40份、土茯苓0.75份、杏仁7.5份、水薄荷10份、石榴皮多酚20份、水杨酸35份。
金钗石斛、黄芩、土茯苓、杏仁混合,得原料混合物;原料混合物与水按照1g:20mL混合,煎煮提取4次,提取的温度为140℃,每次提取的时间为60min,合并提取液,减压浓缩至提取液原体积的1/11,得到原料混合提取浓缩液;
水薄荷进行超临界CO2萃取,萃取的压力为10MPa,萃取的温度为50℃,萃取的CO2流量为20L/h,萃取时间为1.5h,得到水薄荷提取物;
原料混合提取浓缩液、水薄荷提取物、石榴皮多酚(浓度为60%,购自西安瑞盈生物科技有限公司)和水杨酸(市售购买即可),580r/min搅拌混合,搅拌温度为35℃,得到组合物。
实施例2
金钗石斛50份、黄芩30份、土茯苓0.5份、杏仁5份、水薄荷8份、石榴皮多酚15份、水杨酸20份。
金钗石斛、黄芩、土茯苓、杏仁混合,得原料混合物;原料混合物与水按照1g:15mL混合,煎煮提取2次,提取的温度为130℃,每次提取的时间为50min,合并提取液,减压浓缩至提取液原体积的1/10,得到原料混合提取浓缩液;
水薄荷进行超临界CO2萃取,萃取的压力为8MPa,萃取的温度为45℃,萃取的CO2流量为15L/h,萃取时间为1h,得到水薄荷提取物;
原料混合提取浓缩液、水薄荷提取物、石榴皮多酚(浓度为60%,购自西安瑞盈生物科技有限公司)和水杨酸(市售购买即可),550r/min搅拌混合,搅拌温度为30℃,得到组合物。
实施例3
金钗石斛70份、黄芩50份、土茯苓1份、杏仁10份、水薄荷12份、石榴皮多酚25份、水杨酸50份。
金钗石斛、黄芩、土茯苓、杏仁混合,得原料混合物;原料混合物与水按照1g:25mL混合,煎煮提取6次,提取的温度为150℃,每次提取的时间为70min,合并提取液,减压浓缩至提取液原体积的1/12,得到原料混合提取浓缩液;
水薄荷进行超临界CO2萃取,萃取的压力为12MPa,萃取的温度为55℃,萃取的CO2流量为25L/h,萃取时间为2h,得到水薄荷提取物;
原料混合提取浓缩液、水薄荷提取物、石榴皮多酚(浓度为60%,购自西安瑞盈生物科技有限公司)和水杨酸(市售购买即可),600r/min搅拌混合,搅拌温度为40℃,得到组合物。
实施例4
金钗石斛55份、黄芩35份、土茯苓0.6份、杏仁6份、水薄荷9份、石榴皮多酚18份、水杨酸30份。
金钗石斛、黄芩、土茯苓、杏仁混合,得原料混合物;原料混合物与水按照1g:16mL混合,煎煮提取3次,提取的温度为135℃,每次提取的时间为55min,合并提取液,减压浓缩至提取液原体积的1/10,得到原料混合提取浓缩液;
水薄荷进行超临界CO2萃取,萃取的压力为9MPa,萃取的温度为48℃,萃取的CO2流量为18L/h,萃取时间为1h,得到水薄荷提取物;
原料混合提取浓缩液、水薄荷提取物、石榴皮多酚(浓度为60%,购自西安瑞盈生物科技有限公司)和水杨酸(市售购买即可),560r/min搅拌混合,搅拌温度为32℃,得到组合物。
实施例5
金钗石斛65份、黄芩45份、土茯苓0.8份、杏仁8份、水薄荷11份、石榴皮多酚22份、水杨酸40份。
金钗石斛、黄芩、土茯苓、杏仁混合,得原料混合物;原料混合物与水按照1g:22mL混合,煎煮提取4次,提取的温度为145℃,每次提取的时间为65min,合并提取液,减压浓缩至提取液原体积的1/12,得到原料混合提取浓缩液;
水薄荷进行超临界CO2萃取,萃取的压力为11MPa,萃取的温度为52℃,萃取的CO2流量为23L/h,萃取时间为2h,得到水薄荷提取物;
原料混合提取浓缩液、水薄荷提取物、石榴皮多酚(浓度为60%,购自西安瑞盈生物科技有限公司)和水杨酸(市售购买即可),580r/min搅拌混合,搅拌温度为38℃,得到组合物。
实验例
实施例1~5制备所得组合物以下称为实施例1外用药膏、实施例2外用药膏、实施例3外用药膏、实施例4外用药膏、实施例5外用药膏。
体重2~2.5kg的大耳白兔60只,适应性饲养一周后,造模,在家兔左耳内侧每日涂抹煤焦油0.5mL一次,连续14天,在此过程中每日揭除前日形成的痂,表皮活检证实第14天造模成功,每组10只,分为实施例1外用药膏组、实施例2外用药膏组、实施例3外用药膏组、实施例4外用药膏组、实施例5外用药膏组和模型组。同批次体重2~2.5kg的大耳白兔10只,正常饲喂,作为对照组。
造模成功后,实施例1外用药膏组、实施例2外用药膏组、实施例3外用药膏组、实施例4外用药膏组、实施例5外用药膏组的白兔,分别涂抹实施例1外用药膏、实施例2外用药膏、实施例3外用药膏、实施例4外用药膏、实施例5外用药膏,早晚各涂抹一次于患处,治疗6周,模型组与对照组采用生理盐水对患处相应位置进行擦拭。
治疗第42天,采用常规实验方式测定兔耳血中睾酮和雌二醇的含量,各组取10只白兔的平均值,观察兔耳组织病理;分为无症状、轻症状(角化物质增厚轻度、表皮增厚细胞4~5层、毛囊角化物质多,不致密,未充满毛囊)、中症状(角化物质增厚中度、表皮增厚细胞6~7层、毛囊角化物质多,致密,未充满毛囊);重症状(角化物质增厚重度、表皮增厚细胞8~9层、毛囊角化物质多,致密,充满毛囊),四个等级,满足每个等级中3个相应病理表现的及被认定为相应等级。
表1治疗第42天兔耳血中睾酮含量
表2治疗第42天兔耳血中雌二醇含量
表3治疗第42天兔耳组织病理学变化情况
由表1记载,可得本发明制备所得组合物对于兔耳血中睾酮的水平作用为降低,从而促进兔耳患处痊愈,然而,根据表2记载可知,本发明制备所得组合物对于雌二醇的含量并无明显影响;表3记载了本发明制备所得组合物治疗42天后,白兔耳组织病理情况,根据表3记载可知本发明制备所得组合物可有效治愈白兔耳组织病变,其中实施例1组合物在原料用量中等的情况下,达到了良好的治疗效果,实施例3组合物为原料用量大剂量组,治疗效果最佳,治疗后白兔状况为痊愈或者轻症。
以上所述仅是本发明的优选实施方式,应当指出,对于本技术领域的普通技术人员来说,在不脱离本发明原理的前提下,还可以做出若干改进和润饰,这些改进和润饰也应视为本发明的保护范围。
Claims (8)
1.一种包含金钗石斛提取物的外用组合物,其特征在于,包括以下重量份组分制备而成:金钗石斛50~70份、黄芩30~50份、土茯苓0.5~1份、杏仁5~10份、水薄荷8~12份、石榴皮多酚15~25份、水杨酸20~50份。
2.权利要求1所述包含金钗石斛提取物的外用组合物的制备方法,其特征在于,包括以下步骤:
金钗石斛、黄芩、土茯苓、杏仁混合,得原料混合物;原料混合物与水混合,煎煮提取2~6次,合并提取液,减压浓缩得到原料混合提取浓缩液;水薄荷进行超临界CO2萃取,得到水薄荷提取物;原料混合提取浓缩液、水薄荷提取物、石榴皮多酚和水杨酸,搅拌,得到组合物。
3.如权利要求2所述包含金钗石斛提取物的外用组合物的制备方法,其特征在于,所述原料混合物与水的混合比例为1g:15~25mL。
4.如权利要求2所述包含金钗石斛提取物的外用组合物的制备方法,其特征在于,所述煎煮提取的温度为130~150℃,所述每次煎煮提取的时间为50~70min。
5.如权利要求2所述包含金钗石斛提取物的外用组合物的制备方法,其特征在于,所述减压浓缩至提取液原体积的1/10~1/12。
6.如权利要求2所述包含金钗石斛提取物的外用组合物的制备方法,其特征在于,所述超临界CO2萃取的压力为8~12MPa,所述超临界CO2萃取的温度为45~55℃,所述超临界CO2萃取的CO2流量为15~25L/h,所述超临界CO2萃取的时间为1~2h。
7.如权利要求2所述包含金钗石斛提取物的外用组合物的制备方法,其特征在于,所述搅拌的转速为550~600r/min,所述搅拌的温度为30~40℃。
8.权利要求1所述包含金钗石斛提取物的外用组合物或权利要求2~7任一项制备方法制备所得组合物在制备缓解痤疮产品中的应用。
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