CN113476459A - 一种高活性缓释止痛贴及其制备工艺 - Google Patents
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Abstract
本发明涉及一种高活性缓释止痛贴及其制备工艺,高活性缓释止痛贴包括依次叠加的背衬层、主体层和隔离层;其中,主体层包括以下组分:基质,包括骨架材料30~50wt%和助剂12~28wt%;活性成分,包括水杨酸甲酯6~12wt%、薄荷醇5~8wt%和樟脑1~4wt%;活性成分缓释包合料6~18wt%。本发明选用具有高活性、高挥发性药物,即水杨酸甲酯、薄荷醇和樟脑作为高活性缓释止痛贴的主体,主体中的活性成分采用缓释包合材料包合,使各活性成分的含量保留达到最大化并持续稳定释放,确保药物有效性;选用用低致敏亲水性的基质材料且制备工艺采用创新的无溶剂生产工艺技术,使透皮贴剂用于人体不易过敏,从而保证药物安全性。
Description
技术领域
本发明属于药物透皮贴剂制剂工艺技术领域,具体涉及一种高活性缓释止痛贴及其制备工艺。
背景技术
透皮贴剂在治疗疾病方面,尤其是风湿关节痛、肌肉痛、扭伤、颈椎腰腿痛等方面疗效显著,在临床使用中占有很大的比重。透皮给药是除口服、注射以外的第三大用药途径。而传统的镇痛透皮给药制剂,如黑膏药和橡胶膏具有较强的刺激性、致敏性,且载药量小而极大地限制了透皮给药制剂的进一步发展。
目前,国内透皮贴膏的传统生产方法是溶剂法,例如,公开号为CN107375891A的专利文献公开了一种用于祛风湿的外用贴膏的制备方法;由于溶剂法大量使用汽油作为溶剂,存在3大缺点:1、汽油易燃易爆,防爆防火措施要求严格,安全与环保成本极高;2、由于传统溶剂法生产工艺需要高温烘除溶剂,导致高活性易挥发药物有效成分随溶剂烘除而损失,严重影响药物有效性;3、汽油对中枢神经系统有麻醉作用,对皮肤有损害性,容易使皮肤过敏。
发明内容
基于现有技术中存在的上述不足,本发明的目的是提供一种创新的高活性缓释止痛贴及其制备工艺。
为了达到上述发明目的,本发明采用以下技术方案:
一种高活性缓释止痛贴,包括依次叠加的背衬层、主体层和隔离层;
其中,主体层包括以下组分:
基质,包括骨架材料30~50wt%和助剂12~28wt%;
活性成分,包括水杨酸甲酯6~12wt%、薄荷醇5~8wt%和樟脑1~4wt%;
活性成分缓释包合料6~18wt%。
作为优选方案,所述骨架材料包括天然橡胶、合成橡胶、热塑性橡胶中的至少一种。
作为优选方案,所述基质还包括聚异丁烯1~3wt%。
作为优选方案,所述活性成分缓释包合料包括尤特奇、环糊精、高岭土中的至少一种。
其中,尤特奇包括丙烯酸乙酯、甲基丙烯酸甲酯共聚物中的至少一种。
作为优选方案,所述助剂包括填充剂1~10wt%、增塑剂2~4wt%、软化剂3~4wt%和增粘剂6~10wt%。
作为优选方案,所述填充剂包括立德粉、氧化锌、硅酸铝中的至少一种。
作为优选方案,所述增塑剂包括液状石蜡、固体石蜡中的至少一种。
作为优选方案,所述软化剂包括羊毛脂、凡士林中的至少一种。
作为优选方案,所述增粘剂包括松香甘油酯、羧甲基纤维素钠中的至少一种。
本发明还提供如上任一方案所述的高活性缓释止痛贴的制备工艺,包括以下步骤:
(1)将基质包含的各组分进行捏合,得到基质;
(2)将活性成分以及缓释包合成分先进行包合,得到缓释包合料;
(3)将包合料加入基质中进行混合,混合完成对膏浆进行过滤,得到膏体;
(4)将膏体加热涂布于背衬层上,之后盖隔离层并经冷却通道收卷切片,得到高活性缓释止痛贴。
本发明与现有技术相比,有益效果是:
本发明选用具有高活性、高挥发性药物,即水杨酸甲酯、薄荷醇和樟脑作为高活性缓释止痛贴的主体,主体中的活性成分采用活性成分缓释包合料包合,使各活性成分的含量保留达到最大化并持续稳定释放,可以确保药物的有效性。
本发明采用无溶剂清洁生产工艺技术,无需使用溶剂,生产成本大幅度降低,无安全隐患,对环境不产生污染,减少了致敏因素,降低人体的过敏反应,可以明显改善生产安全性和和药物安全性,是对传统生产工艺的一次变革。
具体实施方式
以下通过具体实施例对本发明的技术方案作进一步解释说明。
实施例1:
本实施例的高活性缓释止痛贴的制备工艺,包括以下步骤:
(1)将骨架材料天然橡胶30wt%、热塑性橡胶SIS 16wt%、PB2400聚异丁烯2wt%加入混合分散机中充分混合分散,再加入羊毛脂2wt%、凡士林1wt%、液状石蜡2wt%、松香甘油酯10wt%、氧化锌7wt%捏合分散均匀,得到基质;
(2)将水杨酸甲酯10wt%、薄荷醇6.5wt%、樟脑3.5wt%、环糊精10wt%搅拌均匀后加入上述基质中进行捏合,再通过过滤机对膏浆进行过滤精炼使各成分充分混匀出料;
(3)经涂布机将膏体加热至80度涂布在背衬层上,盖隔离层经冷却隧道冷却至5度,然后收卷切片,制成每100cm2含膏量为1.6~1.9g的高活性缓释止痛贴。
其中,高活性缓释止痛贴包括依次叠加的背衬层、主体层和隔离层。
实施例2:
本实施例的高活性缓释止痛贴的制备工艺,包括以下步骤:
(1)将骨架材料天然橡胶15wt%、合成橡胶10wt%、热塑性橡胶SIS 15wt%、PB2400聚异丁烯2wt%加入混合分散机中充分混合分散,再加入羊毛脂2wt%、凡士林1wt%、液状石蜡5wt%、松香甘油酯10wt%、立德粉3wt%、氧化锌6wt%捏合分散均匀,得到基质;
(2)将水杨酸甲酯10wt%、薄荷醇6.5wt%、樟脑3.5wt%、高岭土11wt%搅拌均匀后加入上述基质中进行混合,再通过过滤机对膏浆进行过滤精炼使各成分充分混匀出料;
(3)经涂布机将膏体加热至80度涂布在背衬层上,盖隔离层经冷却隧道冷却至5度,然后收卷切片,制成每100cm2含膏量为1.6~1.9g的高活性缓释止痛贴。
其中,高活性缓释止痛贴包括依次叠加的背衬层、主体层和隔离层。
实施例3:
本实施例的高活性缓释止痛贴的制备工艺,包括以下步骤:
(1)将骨架材料天然橡胶15wt%、合成橡胶10wt%、热塑性橡胶SIS 15wt%、聚异丁烯B50 5wt%加入混合分散机中充分混合分散,再加入羊毛脂2wt%、凡士林1wt%、液状石蜡5wt%、羧甲基纤维素钠10wt%、硅酸铝1wt%、氧化锌6wt%捏合分散均匀,得到基质;
(2)将水杨酸甲酯10wt%、薄荷醇6.5wt%、樟脑3.5wt%、尤特奇(丙烯酸乙酯、甲基丙烯酸甲酯共聚物)10wt%搅拌均匀后加入上述基质中进行捏合,再通过过滤机对膏浆进行过滤精炼使各成分充分混匀出料;
(3)经涂布机将膏体加热至80度,然后涂布在背衬层上,盖隔离层经冷却隧道冷却至5度,然后收卷切片,制成每100cm2含膏量为1.6~1.9g的高活性缓释止痛贴。
其中,高活性缓释止痛贴包括依次叠加的背衬层、主体层和隔离层。
对比例1:
本对比例的止痛贴的制备工艺,包括以下步骤:
(1)将天然橡胶25wt%和合成橡胶10wt%用汽油浸泡24小时使充分溶胀后放入双轴搅拌机充分搅拌,再加入羊毛脂2wt%、凡士林2wt%、氧化锌20wt%、松香20wt%、液状石蜡1wt%充分搅拌混合,得到基质;
(2)将水杨酸甲酯10wt%、薄荷醇6.5wt%、樟脑3.5wt%加入基质中搅拌均匀后过滤出料;
(3)最后将膏体涂布在背衬层,加温120度烘除溶剂汽油,盖隔离层切片,制成每100cm2含膏量为1.6~1.9g的止痛贴。
其中,止痛贴包括依次叠加的背衬层、主体层和隔离层。
一、对上述实施例1-3以及对比例1得到的止痛贴的主体层的活性成分含量进行检测,具体操作如下:
将止痛贴剥离隔离层后放入装有100mL纯化水的烧瓶加热回流提取3小时,提取液为甲苯,稀释液为乙酸乙酯,内标为萘溶液,进气相色谱仪进行检测,检测结果如表1所示。
表1实施例1-3及对比例1的止痛贴的主体层的活性成分含量结果
水杨酸甲酯10% | 薄荷醇6.5% | 樟脑3.5% | |
实施例1 | 9.12% | 6.04% | 3.07% |
实施例2 | 9.30% | 6.25% | 3.21% |
实施例3 | 9.82% | 6.32% | 3.42% |
对比例1 | 7.65% | 4.87% | 2.50% |
二、对上述实施例1-3以及对比例1得到的止痛贴进行耐热测试,具体操作如下:
对于实施例1-3及对比例1,各取止痛贴2片,除去盖衬,置120℃烘箱中加热30分钟,放冷后观察。
测试结果如下:
(1)实施例1-3的止痛贴的膏背面均无泛黄及渗油现象,用手指触试膏面均仍有粘性;其中,实施例1的粘性比实施例2和3的粘性稍差。
(2)对比例1的止痛贴的膏背面有稍许泛黄现象。
另外,还对水杨酸甲酯6~12wt%、薄荷醇5~8wt%、樟脑1~4wt%的含量进行了测试对比,各活性成分的含量小于上述下限时,药效发挥不佳;含量高于上述上限时,活性成分保留较差,挥发较多。
在上述实施例及其替代方案中,骨架材料30~50wt%、助剂12~28wt%水杨酸甲酯6~12wt%、薄荷醇5~8wt%、樟脑1~4wt%、活性成分缓释包合料6~18wt%、填充剂1~10wt%、增塑剂2~4wt%、软化剂3~4wt%、增粘剂6~10wt%,上述各组分的含量均可在相应的范围内根据实际需要进行确定。
在上述实施例及其替代方案中,填充剂还可以任意选择立德粉、氧化锌、硅酸铝中的至少一种,增塑剂还可以选择液状石蜡、固体石蜡中的至少一种,软化剂还可以选择羊毛脂、凡士林中的至少一种,具体根据实际应用需求进行确定。
以上所述仅是对本发明的优选实施例及原理进行了详细说明,对本领域的普通技术人员而言,依据本发明提供的思想,在具体实施方式上会有改变之处,而这些改变也应视为本发明的保护范围。
Claims (10)
1.一种高活性缓释止痛贴,其特征在于,包括依次叠加的背衬层、主体层和隔离层;
其中,主体层包括以下组分:
基质,包括骨架材料30~50wt%和助剂12~28wt%;
活性成分,包括水杨酸甲酯6~12wt%、薄荷醇5~8wt%和樟脑1~4wt%;
活性成分缓释包合料6~18wt%。
2.根据权利要求1所述的一种高活性缓释止痛贴,其特征在于,所述骨架材料包括天然橡胶、合成橡胶、热塑性橡胶中的至少一种。
3.根据权利要求1所述的一种高活性缓释止痛贴,其特征在于,所述基质还包括聚异丁烯1~3wt%。
4.根据权利要求1所述的一种高活性缓释止痛贴,其特征在于,所述活性成分缓释包合料包括尤特奇、环糊精、高岭土中的至少一种。
5.根据权利要求1-4任一项所述的一种高活性缓释止痛贴,其特征在于,所述助剂包括填充剂1~10wt%、增塑剂2~4wt%、软化剂3~4wt%和增粘剂6~10wt%。
6.根据权利要求5所述的一种高活性缓释止痛贴,其特征在于,所述填充剂包括立德粉、氧化锌、硅酸铝中的至少一种。
7.根据权利要求5所述的一种高活性缓释止痛贴,其特征在于,所述增塑剂包括液状石蜡、固体石蜡中的至少一种。
8.根据权利要求5所述的一种高活性缓释止痛贴,其特征在于,所述软化剂包括羊毛脂、凡士林中的至少一种。
9.根据权利要求5所述的一种高活性缓释止痛贴,其特征在于,所述增粘剂包括松香甘油酯、羧甲基纤维素钠中的至少一种。
10.如权利要求1-9任一项所述的高活性缓释止痛贴的制备工艺,其特征在于,包括以下步骤:
(1)将基质包含的各组分进行捏合,得到基质;
(2)将活性成分以及活性成分缓释包合料混合,得到包合料;
(3)将包合料加入基质中进行混合,得到膏浆;之后对膏浆进行过滤,得到膏体;
(4)将膏体加热涂布于背衬层上,之后盖隔离层并经冷却通道收卷切片,得到高活性缓释止痛贴。
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