CN114831968A - 一种促进白色脂肪棕色化的山奈酚减肥贴剂及其制备工艺 - Google Patents
一种促进白色脂肪棕色化的山奈酚减肥贴剂及其制备工艺 Download PDFInfo
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Abstract
本发明公开了一种促进白色脂肪棕色化的山奈酚减肥贴剂及其制备工艺，配方包括：尤特奇E100、丁二酸、柠檬酸三乙酯、甘油、山奈酚和山奈挥发油，制备工艺包括：步骤一，准备原料；步骤二，提取挥发油；步骤三，制备贴剂；步骤四，冷却裁剪；所述步骤二中，挥发提取器的回流提取的时间为5h，本发明通过添加山奈酚和山奈挥发油，以及局部透皮给药的方式，促进白色脂肪棕色化产热，所述步骤四中，烘箱的干燥温度为45℃，烘干时间为3h，使白色脂肪组织中UCP1、PGC‑1α表达水平升高，产生抗肥胖的作用，并通过调整尤特奇E100、丁二酸、柠檬酸三乙酯、甘油、山奈酚和山奈挥发油的比例，实现了贴剂的最佳黏附性、最高渗透率和最优减肥效果。
Description
技术领域
本发明涉及医药技术领域，具体为一种促进白色脂肪棕色化的山奈酚减肥贴剂及其制备工艺。
背景技术
体内能量消耗与摄入的不平衡是肥胖发生的主要诱因，脂肪组织主要分为白色脂肪组织(White adipose tissue，WAT)和棕色脂肪组织(Brown adipose tissue，BAT)，WAT占成年人体内脂肪组织的绝大部分，它的过度沉积是形成肥胖的主要原因，BAT富含线粒体，是机体重要的产热组织，随着研究的深入，发现当机体暴露于寒冷或药物的刺激时，WAT中出现一些UCP1表达阳性的脂肪细胞，细胞内线粒体数量增加，耗氧量增加，产热增加，其功能与棕色脂肪细胞相似，这一过程称为白色脂肪棕色化，众多研究证实，白色脂肪棕色化能提高机体能量代谢，改善机体胰岛素抵抗，达到降低体脂，减轻体重的效果，白色脂肪棕色化是防治肥胖和相关代谢性疾病最有希望的策略之一。
发明内容
本发明的目的在于提供一种促进白色脂肪棕色化的山奈酚减肥贴剂及其制备工艺，以解决上述背景技术中提出的问题。
为实现上述目的，本发明提供如下技术方案：一种促进白色脂肪棕色化的山奈酚减肥贴剂，配方包括：尤特奇E100、丁二酸、柠檬酸三乙酯、甘油、山奈酚和山奈挥发油，各组分的质量份数分别是：1.2g的尤特奇E100、0.06g的丁二酸、0.4g的柠檬酸三乙酯、0.3g的甘油和0.05g的山奈酚，山奈挥发油质量百分比含量为5％。
一种促进白色脂肪棕色化的山奈酚减肥贴剂的其制备工艺，包括步骤一，准备原料；步骤二，提取挥发油；步骤三，制备贴剂；步骤四，冷却裁剪；
其中上述步骤一中，按照各组分的质量百分含量分别是：1.2g的尤特奇E100、0.06g的丁二酸、0.4g的柠檬酸三乙酯、0.3g的甘油、0.05g的山奈酚和5％的山奈挥发油进行选取，并按照质量百分比之和为1进行称取；
其中上述步骤二中，精准称取山奈粉末，加入适量蒸馏水，浸泡后于挥发提取器中回流提取，收集山奈挥发油，以备后续使用；
其中上述步骤三中，将尤特奇E100、丁二酸、柠檬酸三乙酯、甘油投入烧杯中，然后加入适量乙醇，不断进行搅拌直至其完全溶解，再加入精密称取的山奈酚、山奈挥发油，然后不断搅拌混匀，最后均匀涂布成大小合适的膜剂；
其中上述步骤四中，取步骤三中得到的膜剂，放入烘箱中干燥，然后待其冷却后剪切成适宜大小，再向膜剂上贴上保护模成分，得到所需的山奈酚透皮贴剂。
优选的，所述步骤二中，称取山奈粉末时需要过40目筛，所称取重量为100g。
优选的，所述步骤二中，蒸馏水需按照料液比1：10进行添加，浸泡时间为1h。
优选的，所述步骤二中，挥发提取器的回流提取的时间为5h。
优选的，所述步骤三中，烧杯中加入的乙醇浓度为75％，加入乙醇后的搅拌溶解的温度为45℃，涂布成功的膜剂大小尺寸为10cm×10cm。
优选的，所述步骤四中，烘箱的干燥温度为45℃，烘干时间为3h。
与现有技术相比，本发明的有益效果是：本发明通过添加山奈酚和山奈挥发油，以及局部透皮给药的方式，促进白色脂肪棕色化产热，使白色脂肪组织中UCP1、PGC-1α表达水平升高，产生抗肥胖的作用，并通过调整尤特奇E100、丁二酸、柠檬酸三乙酯、甘油、山奈酚和山奈挥发油的比例，实现了贴剂的最佳黏附性、最高渗透率和最优减肥效果。
附图说明
图1为本发明的工艺流程图；
图2为丁二酸单因素实验图；
图3为尤特奇E100单因素实验图；
图4为柠檬酸三乙酯单因素实验图；
图5为甘油单因素实验图；
图6为山奈酚标准品图谱图；
图7为山奈酚透皮贴剂渗透效果图；
图8为山奈挥发油单因素实验图；
图9为HFD-C与HFD-KPF50小鼠体态对比图；
图10为HFD-C与HFD-KPF50小鼠体重对比图；
图11为ND-C与HFD-KPF25、50、100各组小鼠体重对比图；
图12为HFD-C与HFD-KPF50小鼠棕色脂肪标记基因蛋白表达对比图；
图13为HFD-C与HFD-KPF50小鼠棕色脂肪标记基因UCP1表达灰度值对比图；
图14为HFD-C与HFD-KPF50小鼠棕色脂肪标记基因PGC-1α表达灰度值对比图。
具体实施方式
下面将结合本发明实施例中的附图，对本发明实施例中的技术方案进行清楚、完整地描述，显然，所描述的实施例仅仅是本发明一部分实施例，而不是全部的实施例。基于本发明中的实施例，本领域普通技术人员在没有做出创造性劳动前提下所获得的所有其他实施例，都属于本发明保护的范围。
请参阅图1-14，本发明提供的一种技术方案：
实施例：
一种促进白色脂肪棕色化的山奈酚减肥贴剂，配方包括：尤特奇E100、丁二酸、柠檬酸三乙酯、甘油、山奈酚和山奈挥发油，各组分的质量份数分别是：1.2g的尤特奇E100、0.06g的丁二酸、0.4g的柠檬酸三乙酯、0.3g的甘油和0.05g的山奈酚，山奈挥发油质量百分比含量为5％。
一种促进白色脂肪棕色化的山奈酚减肥贴剂的其制备工艺，包括步骤一，准备原料；步骤二，提取挥发油；步骤三，制备贴剂；步骤四，冷却裁剪；
其中上述步骤一中，按照各组分的质量百分含量分别是：1.2g的尤特奇E100、0.06g的丁二酸、0.4g的柠檬酸三乙酯、0.3g的甘油、0.05g的山奈酚和5％的山奈挥发油进行选取，并按照质量百分比之和为1进行称取；
其中上述步骤二中，使用40目筛筛选并精准称取山奈粉末100g，按照料液比1：10加入蒸馏水，浸泡1h后于挥发提取器中回流提取5h，收集山奈挥发油，以备后续使用；
其中上述步骤三中，将尤特奇E100、丁二酸、柠檬酸三乙酯、甘油投入烧杯中，然后加入适量浓度为75％的乙醇，在45℃下不断进行搅拌直至其完全溶解，再加入精密称取的山奈酚、山奈挥发油，搅拌混匀，最后均匀涂布成10cm×10cm膜剂；
其中上述步骤四中，取步骤三中得到的膜剂，放入烘箱中45℃干燥3h，然后待其冷却后剪切成适宜大小，再向膜剂上贴上保护模成分，得到所需的山奈酚透皮贴剂。
对比例1：
在确保配方中其余组分不变的情况下，改变丁二酸的添加量，以初黏力和持黏力为评价标准进行单因素考察，其制备工艺参照实施例。对比例2：
在确保配方中其余组分不变的情况下，改变尤特奇E100的添加量，以初黏力和持黏力为评价标准进行单因素考察，其制备工艺参照实施例。
对比例3：
在确保配方中其余组分不变的情况下，改变柠檬酸三乙酯的添加量，以初黏力和持黏力为评价标准进行单因素考察，其制备工艺参照实施例。
对比例4：
在确保配方中其余组分不变的情况下，改变甘油的添加量，以初黏力和持黏力为评价标准进行单因素考察，其制备工艺参照实施例。对比例5：
在确保配方中其余组分不变的情况下，改变山奈挥发油的浓度，以促进贴剂渗透能力的促进作用为评价标准进行单因素考察，其制备工艺参照实施例，并使用该贴剂进行体外经皮渗透实验，实验步骤如下：剥取SD大鼠腹部皮肤，去除皮下脂肪及黏连物，生理盐水冲洗干净后使用，将鼠皮固定于扩散仪的接收室上，皮肤角质层向上，将剪切好的山奈酚贴剂贴于角质层一侧，于接收室中注入接收液，盖上封口膜，分别于1、2、4、8、16、24、48、72h吸取透皮接收液，并及时补充等量同温新鲜介质，接收液通过HPLC测定山奈酚含量，色谱条件如下：采用Agilent ZORBAX Eclipse XDB-C18色谱柱(250mm×4.6mm,5μm)，流动相为甲醇-0.4％磷酸(67：33)，流速为1mL/min，柱温25℃，检测波长为360nm，进样量20μL，测定渗透的山奈酚含量，筛选对山奈酚具有较好促渗作用的山奈挥发油浓度。对比例6：
在确保配方中其余组分不变的情况下，通过改变山奈酚(KPF)的含量，来探究KPF对高脂饮食小鼠体重及体态的影响，选取50只雄性C57小鼠，随机分为5组，每组10只，分别为正常饮食对照组(ND-C)、高脂饮食对照组(HFD-C)、高脂饮食山奈酚低剂量组(HFD-KPF25)、高脂饮食山奈酚中剂量组(HFD-KPF50)、高脂饮食山奈酚高剂量组(HFD-KPF100)，对照组给予不含山奈酚的透皮贴剂敷贴，山奈酚低剂量给药组给予山奈酚含量为25mg的透皮贴剂敷贴，山奈酚中剂量给药组山奈酚含量为50mg的透皮贴剂敷贴，山奈酚高剂量给药组给予山奈酚含量为100mg的透皮贴剂敷贴，小鼠腹股沟除毛后敷贴1cm*1cm贴剂，每天更换，实验结束后，称重、拍照、分离腹股沟皮下白色脂肪组织(iWAT)，进行组织切片及HE染色与免疫组化实验，剩余样本进行Western-blotting实验，Western blotting结果显示山奈酚作用后棕色脂肪标记基因UCP1与PGC-1α表达显著升高，表达结果参考图12-14。
基于上述，本发明采用尤特奇E100、丁二酸、柠檬酸三乙酯、甘油、山奈酚、山奈挥发油制备具有减肥作用的山奈酚透皮贴剂，用于促进白色脂肪棕色化，为达到最佳药效，处方配比为1.2g的尤特奇E100、0.06g的丁二酸、0.4g的柠檬酸三乙酯、0.3g的甘油、0.05g的山奈酚和5％的山奈挥发油，该处方条件下具有最佳黏附性，最高渗透率及最优减肥效果。
对于本领域技术人员而言，显然本发明不限于上述示范性实施例的细节，而且在不背离本发明的精神或基本特征的情况下，能够以其他的具体形式实现本发明。因此，无论从哪一点来看，均应将实施例看作是示范性的，而且是非限制性的，本发明的范围由所附权利要求而不是上述说明限定，因此旨在将落在权利要求的等同要件的含义和范围内的所有变化囊括在本发明内。不应将权利要求中的任何附图标记视为限制所涉及的权利要求。
Claims (7)
1.一种促进白色脂肪棕色化的山奈酚减肥贴剂，配方包括：尤特奇E100、丁二酸、柠檬酸三乙酯、甘油、山奈酚和山奈挥发油，其特征在于：各组分的质量份数分别是：1.2g的尤特奇E100、0.06g的丁二酸、0.4g的柠檬酸三乙酯、0.3g的甘油和0.05g的山奈酚，山奈挥发油质量百分比含量为5％。
2.一种促进白色脂肪棕色化的山奈酚减肥贴剂的其制备工艺，包括步骤一，准备原料；步骤二，提取挥发油；步骤三，制备贴剂；步骤四，冷却裁剪；其特征在于：
其中上述步骤一中，按照各组分的质量百分含量分别是：1.2g的尤特奇E100、0.06g的丁二酸、0.4g的柠檬酸三乙酯、0.3g的甘油、0.05g的山奈酚和5％的山奈挥发油进行选取，并按照质量百分比之和为1进行称取；
其中上述步骤二中，精准称取山奈粉末，加入适量蒸馏水，浸泡于挥发提取器中回流提取，收集山奈挥发油，以备后续使用；
其中上述步骤三中，将尤特奇E100、丁二酸、柠檬酸三乙酯、甘油投入烧杯中，然后加入适量乙醇，不断进行搅拌直至其完全溶解，再加入精密称取的山奈酚、山奈挥发油，然后不断搅拌混匀，最后均匀涂布成大小合适的膜剂；
其中上述步骤四中，取步骤三中得到的膜剂，放入烘箱中干燥，然后待其冷却后剪切成适宜大小，再向膜剂上贴上保护模成分，得到所需的山奈酚透皮贴剂。
3.根据权利要求2所述的一种促进白色脂肪棕色化的山奈酚减肥贴剂的其制备工艺，其特征在于：所述步骤二中，称取山奈粉末时需要过40目筛，所称取重量为100g。
4.根据权利要求2所述的一种促进白色脂肪棕色化的山奈酚减肥贴剂的其制备工艺，其特征在于：所述步骤二中，蒸馏水需按照料液比1：10进行添加，浸泡时间为1h。
5.根据权利要求2所述的一种促进白色脂肪棕色化的山奈酚减肥贴剂的其制备工艺，其特征在于：所述步骤二中，挥发提取器的回流提取的时间为5h。
6.根据权利要求2所述的一种促进白色脂肪棕色化的山奈酚减肥贴剂的其制备工艺，其特征在于：所述步骤三中，烧杯中加入的乙醇浓度为75％，加入乙醇后的搅拌溶解的温度为45℃，涂布成功的膜剂大小尺寸为10cm×10cm。
7.根据权利要求2所述的一种促进白色脂肪棕色化的山奈酚减肥贴剂的其制备工艺，其特征在于：所述步骤四中，烘箱的干燥温度为45℃，烘干时间为3h。
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