CN111888371A - 一种糖基化橙皮素化合物在制备缓解痛经制品中的应用 - Google Patents
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Abstract
本发明属于医疗卫生技术领域，公开了一种糖基化橙皮素化合物在制备缓解痛经制品中的应用。该化合物具有如下式(Ⅰ)所示的结构，其中R1为H、CH3、OCH3或OCH2CH3；R2为H、CH3、OCH3或OCH2CH3；R3为Glu、Rha、Xyl或Gal；n为1‑9之间的整数。该化合物具有非常好的缓解痛经的效果，可以很好的应用于制备缓解痛经制品。
Description
技术领域
本发明属于医疗卫生技术领域，特别涉及一种糖基化橙皮素化合物在制备缓解痛经制品中的应用。
背景技术
痛经为最常见的妇科症状之一，指行经前后或月经期出现下腹部疼痛、坠胀，伴有腰酸，伴有恶心、呕吐、腹泻、头晕、乏力等症状，严重时面色发白、出冷汗，症状严重者影响生活质量。痛经分为原发性痛经和继发性两类，原发性痛经指生殖器官无器质性病变的痛经；继发性痛经指由盆腔器质性疾病，如子宫内膜异位症、子宫腺肌病等引起的痛经。痛经在女性中是常见的症状，原发性痛经的治疗，主要是对症治疗，以止痛，镇静为主。
一项针对14-25岁年轻女性所作的调查显示，该年龄阶段的女性中有高达88％的人有痛经、经期不准、腹胀、腰痛等困扰，其中最常见的为痛经。调查中还发现，很多女性在每次痛经时服用止痛药。然而服用止痛药虽然能短时间内缓解痛经症状，但是药效不能持久，必须长期服药，长期服用止痛药会加重患者身体的肝脏负担，严重者会造成神经系统功能紊乱，记忆力降低、失眠等不良后果。也有部分患者采用针灸法或使用止痛装置，这些方式存在的问题是使用起来不方便，卫生方面也难以保障。因此，如何能有效缓解和治疗痛经，同时不给身体带来各种不良反应和毒副作用，并具备使用方便的特点，是值得研究的问题。
痛经多数是由气血不畅或受寒引起的，因此促进子宫血液循环能起到暖宫活血的作用，有助于缓解痛经。
发明内容
为了克服现有技术的缺点与不足，本发明的目的在于提供一种糖基化橙皮素化合物在制备缓解痛经制品中的应用。
本发明的目的通过下述技术方案实现：
一种糖基化橙皮素化合物在制备缓解痛经制品中的应用，该化合物具有如下式(Ⅰ)所示的结构：
其中R1为H、CH3、OCH3或OCH2CH3；R2为H、CH3、OCH3或OCH2CH3；R3为Glu、Rha、Xyl或Gal；n为1-9之间的整数。
所述缓解痛经制品为缓解痛经的缓释透皮贴剂，该缓释透皮贴剂由背衬层、含药储库层、防粘保护层构成，所述含药储库层是将糖基化橙皮素溶于溶剂，再压敏胶均匀混合，涂于背衬层上，加热烘干，制成含药储库层；每平方厘米含药储库层含糖基化橙皮素的量为0.3-3.0mg。
所述溶剂为乙酸乙酯；所述压敏胶为水溶性丙烯酸压敏胶、脂溶性丙烯酸压敏胶、有机硅类压敏胶或聚异丁烯压敏胶；每平方厘米含药储库层含压敏胶的量为1.0-30.0mg，压敏胶占缓释透皮贴剂重量的70.0-95.0％。
所述含药储库层中还含有透皮促进剂，透皮促进剂包括氮酮、油酸、三乙酸甘油酯、肉豆蔻酸异丙酯，每平方厘米含药储库层含透皮促进剂的量为0-1.0mg，透皮促进剂占缓释透皮贴剂重量的0-10.0％；所述含药储库层中还含有结晶抑制剂十八醇，每平方厘米含药储库层含结晶抑制剂的量为0.05-0.4mg，结晶抑制剂占缓释透皮贴剂重量的0.3-5.0％；每平方厘米含糖基化橙皮素的量为0.3-3.0mg。
所述缓解痛经制品为缓解痛经的贴膏剂、膜剂、涂膜剂、膏药以及其他药学上可接受的剂型。
所述所述R3为Glu或Rha；n为1-5之间的整数。
本发明相对于现有技术具有如下的优点及有益效果：
本发明创造性地发现这类化合物能够促进人体血液循环，将其制成缓释透皮贴剂、软膏剂、贴膏剂、膜剂、涂膜剂、膏药以及其他药学上可接受的剂型用于女性“气海穴”上皮肤，可以达到暖宫止痛的效用；药物缓慢释放，可以达到作用时间长、药物反应温和的效果；同时具有原料来源广泛、成本低的生产优势以及对人体无毒副作用的应用前提。
附图说明
图1为本发明实施例1所述使用含有1％糖基化橙皮素的洗剂与对照洗剂后的血流量比例图。
图2为本发明实施例2处理前后皮肤温度图，其中(a)为处理前皮肤图像，(b)为使用精制水处理后皮肤温度图像，(c)为使用含1％糖基化橙皮素溶液处理后皮肤温度图像。
具体实施方式
下面结合实施例及附图对本发明作进一步详细的描述，但本发明的实施方式不限于此。
以下实施例使用的糖基化橙皮素化合物有如下式(Ⅰ)所示的结构，其制备方法参照申请号为201910433199.X的专利申请：
其中R1为H、CH3、OCH3或OCH2CH3；R2为H、CH3、OCH3或OCH2CH3；R3为Glu、Rha、Xyl或Gal；n为1-9之间的整数。
实施例1
在室温下接触糖基化橙皮素霜30分钟后的测量血流量
将左手在室温下使用含有质量分数1％的糖基化橙皮素的洗剂涂抹，该洗剂由甘油、水、糖基化橙皮素按一定比例混合均匀制成，30分钟后进行检测；右手使用同样剂量对照洗剂涂抹，30分钟后进行检测。对照洗剂包括保湿剂、乙醇&对羟基苯甲酸酯。使用激光血流量检测仪FL0-N1对左右手相同部位进行检测，结果显示如图1所示，使用含质量分数1％的糖基化橙皮素的洗剂的左手血流量明显高于使用对照洗剂的右手。
实施例2
在室温下接触糖基化橙皮素喷雾30分钟后的测量血流量
使用含有质量分数1％的糖基化橙皮素的喷雾溶液对皮肤进行喷射，该喷雾由水与糖基化橙皮素按一定比例制成，接触30分钟后使用激光多普勒血流成像仪进行检测，结果显示如图2所示，使用含有1％糖基化橙皮素的喷雾溶液的皮肤血流量图2-(c)明显高于使用前皮肤血流量图2-(a)，也明显高于使用精制水作为对照后的血流量图2-(b)。
实施例3
缓解痛经缓释透皮贴剂的制备方法如下：
将糖基化橙皮素、氮酮、十八醇溶解于乙酸乙酯中，加入脂溶性丙烯酸酯压敏胶混合均匀，将混匀的胶浆涂于背衬材料，面积10000cm2，加热烘干，再覆盖上保护层，按需要尺寸切割，包装，即制成含糖基化橙皮素的缓释透皮贴剂。
上述实施例为本发明较佳的实施方式，但本发明的实施方式并不受上述实施例的限制，其他的任何未背离本发明的精神实质与原理下所作的改变、修饰、替代、组合、简化，均应为等效的置换方式，都包含在本发明的保护范围之内。
Claims (6)
1.一种糖基化橙皮素化合物在制备缓解痛经制品中的应用，该化合物具有如下式(Ⅰ)所示的结构：
其中R1为H、CH3、OCH3或OCH2CH3；R2为H、CH3、OCH3或OCH2CH3；R3为Glu、Rha、Xyl或Gal；n为1-9之间的整数。
2.根据权利要求1所述的应用，其特征在于：所述缓解痛经制品为缓解痛经的缓释透皮贴剂，该缓释透皮贴剂由背衬层、含药储库层、防粘保护层构成，所述含药储库层是将糖基化橙皮素溶于溶剂，再压敏胶均匀混合，涂于背衬层上，加热烘干，制成含药储库层；每平方厘米含药储库层含糖基化橙皮素的量为0.3-3.0mg。
3.根据权利要求2所述的应用，其特征在于：所述溶剂为乙酸乙酯；所述压敏胶为水溶性丙烯酸压敏胶、脂溶性丙烯酸压敏胶、有机硅类压敏胶或聚异丁烯压敏胶；每平方厘米含药储库层含压敏胶的量为1.0-30.0mg，压敏胶占缓释透皮贴剂重量的70.0-95.0％。
4.根据权利要求2所述的应用，其特征在于：所述含药储库层中还含有透皮促进剂，透皮促进剂包括氮酮、油酸、三乙酸甘油酯、肉豆蔻酸异丙酯，每平方厘米含药储库层含透皮促进剂的量为0-1.0mg，透皮促进剂占缓释透皮贴剂重量的0-10.0％；所述含药储库层中还含有结晶抑制剂十八醇，每平方厘米含药储库层含结晶抑制剂的量为0.05-0.4mg，结晶抑制剂占缓释透皮贴剂重量的0.3-5.0％；每平方厘米含糖基化橙皮素的量为0.3-3.0mg。
5.根据权利要求1所述的应用，其特征在于：所述缓解痛经制品为缓解痛经的贴膏剂、膜剂、涂膜剂、膏药以及其他药学上可接受的剂型。
6.根据权利要求1所述的应用，其特征在于：所述所述R3为Glu或Rha；n为1-5之间的整数。
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