CN110025615A - 一种治疗炎症性皮肤病的药物、乳膏及其制备方法 - Google Patents
一种治疗炎症性皮肤病的药物、乳膏及其制备方法 Download PDFInfo
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Abstract
本发明属于大环内酯类免疫抑制剂技术领域,公开了一种治疗炎症性皮肤病的药物、乳膏及其制备方法,所述治疗炎症性皮肤病的药物为雷帕霉素;所述治疗炎症性皮肤病的药物的乳膏为载药量为0.4%的O/W型雷帕霉素乳膏;按照100g计由雷帕霉素0.4g、硬脂酸6g、单硬脂酸甘油酯2.7g、凡士林3.3g、月桂氮卓酮2g、液体石蜡10.7g、三乙醇胺2g、尼泊金乙酯0.2g、甘油10g和纯化水65g组成。本发明利用雷帕霉素的抗炎作用来治疗炎症性皮肤病可能是玫瑰痤疮等炎症性皮肤病的一种新的治疗手段。
Description
技术领域
本发明属于大环内酯类免疫抑制剂技术领域,尤其涉及一种治疗炎症性皮肤病的药物、乳膏及其制备方法。
背景技术
炎症性皮肤病主要包括玫瑰痤疮,痤疮,银屑病等。玫瑰痤疮(Rosacea)是一种常见的好发于面部皮肤血管和毛囊皮脂腺的慢性炎症性皮肤病,其发病机制目前还不明确,治疗方法也缺乏针对性。痤疮是好发于青少年面部的,是毛囊皮脂腺单位的慢病炎症性皮肤病,临床表现以面部的粉刺,丘疹,脓疱,结节等多形性皮损为特点。对青少年的社交和心理造成很大的影响。银屑病俗称牛皮鲜,全身均可发病,以四肢,头皮较常见,临床表现为红斑,鳞屑,是一种病程较长,易复发甚至难以治愈的慢性炎症皮肤病,因其发病原因复杂,目前也没有明确的发病机制和治疗方案。
雷帕霉素是科学家于1975年首次从智利复活节岛的土壤中发现的一种由土壤链霉菌分泌的次生代谢物,发现其具有很好的抗炎作用,其化学结构属于“三烯大环内酯类”化合物。起初被作为低毒性的抗真菌药物,1977年发现具有免疫抑制作用,1989年开始把雷帕霉素作为治疗器官移植的排斥反应的新药进行试用,从动物实验及临床应用的效果看,是一种疗效好,低毒,无肾毒性的新型免疫抑制剂。目前临床上仍用于器官移植的抗排斥反应和自身免疫性疾病的治疗,但其用于炎症性皮肤病治疗还未见报道。
综上所述,现有技术存在的问题是:目前的慢性炎症皮肤病易复发甚至难以治愈的,目前也没有明确的发病机制和治疗方案。雷帕霉素用于炎症性皮肤病治疗还未见报道。
解决上述技术问题的难度:
因玫瑰痤疮等炎症性皮肤病发病机制不明确,目前的治疗方案也不明确,需要研究其具体的分子机制,然后在基础研究的基础上将雷帕霉素制成乳膏,用在志愿者身上,需要大量的临床观察才能最终确定疗效,因此存在一定的难度。
解决上述技术问题的意义:
因为目前没有明确的关于雷帕霉素治疗炎症性皮肤病的报道,因此研究雷帕霉素治疗玫瑰痤疮等炎症性皮肤病对于临床上炎症性皮肤病的治疗具有重要意义。
发明内容
针对现有技术存在的问题,本发明提供了一种治疗炎症性皮肤病的药物、乳膏及其制备方法。
本发明是这样实现的,一种治疗炎症性皮肤病的药物,所述治疗炎症性皮肤病的药物为雷帕霉素,局部涂抹,一天三次。
进一步,所述治疗炎症性皮肤病的药物是大环内酯类免疫抑制剂,化学结构式:
分子式:C51H79NO13;分子量:914.172。
本发明的另一目的在于提供一种包含所述治疗炎症性皮肤病的药物的乳膏,所述治疗炎症性皮肤病的药物的乳膏为载药量为0.4%的O/W型雷帕霉素乳膏;
按照100g计由雷帕霉素0.4g、硬脂酸6g、单硬脂酸甘油酯2.7g、凡士林3.3g、月桂氮卓酮2g、液体石蜡10.7g、三乙醇胺2g、尼泊金乙酯0.2g、甘油10g和纯化水65g组成。
本发明的另一目的在于提供一种所述治疗炎症性皮肤病的药物的乳膏的制备方法,所述治疗炎症性皮肤病的乳膏的制备方法包括以下步骤:
第一步,称取处方量的油相成分硬脂酸、单硬脂酸甘油酯、凡士林、月桂氮卓酮、液体石蜡,将其置于250mL的烧杯中加热至80℃,使其成油溶液;
第二步,再称取处方量的水相成分甘油、三乙醇胺、蒸馏水,将其置于250mL的烧杯中加热至80℃,使其成水溶液;
第三步,然后边搅拌边缓慢将油溶液加入到水溶液中,加完后,搅拌至室温即成空白基质;将雷帕霉素均匀分散在空白基质中即成雷帕霉素乳膏。
本发明的另一目的在于提供一种包含所述治疗炎症性皮肤病的药物的治疗玫瑰痤疮的药物。
本发明的另一目的在于提供一种包含所述治疗炎症性皮肤病的药物的治疗痤疮的药物。
本发明的另一目的在于提供一种包含所述治疗炎症性皮肤病的药物的治疗银屑病的药物。
综上所述,本发明的优点及积极效果为:利用雷帕霉素的抗炎作用来治疗炎症性皮肤病可能是玫瑰痤疮等炎症性皮肤病的一种新的治疗手段。
附图说明
图1是本发明实施例提供的治疗炎症性皮肤病的乳膏的制备方法流程图。
图2和图3是本发明实施例提供的雷帕霉素治疗玫瑰痤疮志愿者的疗效图。
具体实施方式
为了使本发明的目的、技术方案及优点更加清楚明白,以下结合实施例,对本发明进行进一步详细说明。应当理解,此处所描述的具体实施例仅仅用以解释本发明,并不用于限定本发明。
针对目前慢性炎症皮肤病易复发甚至难以治愈,目前也没有明确的发病机制和治疗方案,雷帕霉素用于炎症性皮肤病治疗还未见报道的问题,本发明的目的在于提出雷帕霉素的新用途,即通过雷帕霉素治疗玫瑰痤疮,银屑病,痤疮等皮肤病,实现炎症性皮肤病在临床治疗中的一种新的方法。
下面结合附图对本发明的应用原理作详细的描述。
本发明实施例提供的治疗炎症性皮肤病的药物为雷帕霉素。
雷帕霉素是一种新型大环内酯类免疫抑制剂。物理性质:为白色固体结晶,熔点为183-185℃,亲脂性,溶解于甲醇、乙醇、丙酮、氯仿等有机溶剂,极微溶于水,几乎不溶于乙醚。化学性质:由七单位的乙酸盐和七单位的丙酸盐通过聚酮途径合成
雷帕霉素的化学结构式:
分子式:C51H79NO13;分子量:914.172。
本发明实施例提供的治疗炎症性皮肤病的乳膏为载药量为0.4%的O/W型雷帕霉素乳膏。按照100g计由雷帕霉素0.4g、硬脂酸6g、单硬脂酸甘油酯2.7g、凡士林3.3g、月桂氮卓酮2g、液体石蜡10.7g、三乙醇胺2g、尼泊金乙酯0.2g、甘油10g和纯化水65g组成。
如图1所示,本发明实施例提供的治疗炎症性皮肤病的乳膏的制备方法包括以下步骤:
S101:称取处方量的油相成分硬脂酸、单硬脂酸甘油酯、凡士林、月桂氮卓酮、液体石蜡,将其置于250mL的烧杯中加热至80℃,使其成油溶液;
S102:再称取处方量的水相成分甘油、三乙醇胺、蒸馏水,将其置于250mL的烧杯中加热至80℃,使其成水溶液;
S103:然后边搅拌边缓慢将油溶液加入到水溶液中,加完后,搅拌至室温即成空白基质;将雷帕霉素均匀分散在空白基质中即成雷帕霉素乳膏。
本发明实施例提供的治疗炎症性皮肤病的乳膏的处方见表1。
表1雷帕霉素乳膏处方的组成
本发明实施例提供的治疗炎症性皮肤病的乳膏的评价
1外观性状
得到的雷帕霉素乳膏为白色半固体,涂布均匀细腻,延展性好。
2乳滴大小
得到的雷帕霉素乳膏,乳滴大小较均一,大部分在1μm左右。
3稳定性
称取10g左右基质,4000rpm离心20min,均未出现分层现象。
4pH值测定
取3批制备的乳膏0.5g,用水稀释10倍溶解,测定其pH值,得空白基质的pH值均为7.0左右。
5加速试验
取3批制备的雷帕霉素乳膏,将其分别置于4℃、40℃及室温下,30天、60天及90天后,考察其色泽、均匀性、稠度、pH及是否有药物析出。
下面结合临床实施例对本发明的应用效果作详细的描述。
如图2所示,典型病例:曹某某,女,78岁,2018年5月因面部持续性红斑出现近三个月就诊,初发于鼻部皮损,就诊时鼻面部,口周均有皮损,面部持续性红斑,伴有毛细血管扩张。中南大学湘雅医院皮肤科门诊确诊为“玫瑰痤疮”,采用本发明治疗,治疗2个月后,毛细血管扩张明显减轻,皮损效果有所好转,面部红斑症状减轻。
如图3所示,典型病例:邹丹,女,43岁,2018年2月因面部持续性红斑出现4年而就诊,初发于面颊皮损,就诊时面颊和口周均有皮损,面部持续性红斑,有大量散在分布的丘疹,伴有毛细血管扩张。中南大学湘雅医院皮肤科门诊确诊为“玫瑰痤疮”,采用本发明治疗,治疗2个月后,毛细血管扩张明显减轻,皮损效果有所好转,面部红斑症状减轻。
以上所述仅为本发明的较佳实施例而已,并不用以限制本发明,凡在本发明的精神和原则之内所作的任何修改、等同替换和改进等,均应包含在本发明的保护范围之内。
Claims (7)
1.一种治疗炎症性皮肤病的药物,其特征在于,所述治疗炎症性皮肤病的药物为雷帕霉素。
2.如权利要求1所述的治疗炎症性皮肤病的药物,其特征在于,所述治疗炎症性皮肤病的药物是大环内酯类免疫抑制剂,化学结构式:
分子式:C51H79NO13;分子量:914.172。
3.一种包含权利要求1所述治疗炎症性皮肤病的药物的乳膏,其特征在于,所述治疗炎症性皮肤病的药物的乳膏为载药量为0.4%的O/W型雷帕霉素乳膏;
按照100g计由雷帕霉素0.4g、硬脂酸6g、单硬脂酸甘油酯2.7g、凡士林3.3g、月桂氮卓酮2g、液体石蜡10.7g、三乙醇胺2g、尼泊金乙酯0.2g、甘油10g和纯化水65g组成。
4.一种如权利要求3所述治疗炎症性皮肤病的药物的乳膏的制备方法,其特征在于,所述治疗炎症性皮肤病的乳膏的制备方法包括以下步骤:
第一步,称取处方量的油相成分硬脂酸、单硬脂酸甘油酯、凡士林、月桂氮卓酮、液体石蜡,将其置于250mL的烧杯中加热至80℃,使其成油溶液;
第二步,再称取处方量的水相成分甘油、三乙醇胺、蒸馏水,将其置于250mL的烧杯中加热至80℃,使其成水溶液;
第三步,然后边搅拌边缓慢将油溶液加入到水溶液中,加完后,搅拌至室温即成空白基质;将雷帕霉素均匀分散在空白基质中即成雷帕霉素乳膏。
5.一种包含权利要求1~2任意一项所述治疗炎症性皮肤病的药物的治疗玫瑰痤疮的药物。
6.一种包含权利要求1~2任意一项所述治疗炎症性皮肤病的药物的治疗痤疮的药物。
7.一种包含权利要求1~2任意一项所述治疗炎症性皮肤病的药物的治疗银屑病的药物。
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