CN105797100B - 活血止痛压敏胶贴及其制备方法 - Google Patents
活血止痛压敏胶贴及其制备方法 Download PDFInfo
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Abstract
本发明公开了一种活血止痛压敏胶贴,其制备步骤如下:a)、称取干姜、山柰和苍术等二十三味原料,粉碎后得到混合粗粉,向混合粗粉中加入质量分数为90%的乙醇,浸渍2‑4天,渗漉,收集渗漉液,回收乙醇并浓缩至相对密度为1.05‑1.28的清膏,向清膏中加入水杨酸甲酯、颠茄流浸膏和促渗剂,搅拌混合均匀,得药物浸膏备用;b)、将薄荷脑、冰片和樟脑添加到压敏胶基质中,搅拌溶解,得含药基质备用;c)、将药物浸膏加到含药基质中,搅拌混合均匀,得胶液备用;d)、将胶液涂布于隔离纸上,在40~60℃条件下干燥,然后复合背衬,切割,即得活血止痛压敏胶贴,该活血止痛压敏胶贴对皮肤刺激性小、疗效好、且生产安全。
Description
技术领域
本发明涉及医药领域,具体涉及一种用于活血止痛的中药及其制备方法。
背景技术
活血止痛膏是一种收载于2015年版《中国药典》的中成药,其制备原料主要包括干姜、白芷、甘松、山奈等二十八味中药材,具有活血止痛、舒筋通络的功能,主治筋骨疼痛、肌肉麻痹、痰核流注、关节酸痛,临床上活血止痛膏主要用于治疗风湿痹症和伤筋等病症,疗效显著。但是,该制剂为橡胶膏剂,其采用天然橡胶为骨架材料、松香为增粘剂等作为橡胶膏基质,将中药提取浸膏、冰片、薄荷脑、樟脑、颠茄流浸膏、水杨酸甲酯与橡胶膏基质混合涂布而制成。其中天然橡胶和松香等不仅对皮肤有较强的刺激性和过敏性,且黏附性过大,透气性差,使患者依从性差,极大地阻碍了临床应用,不仅如此,天然橡胶采用汽油为溶剂,生产时存在极大的安全隐患,而且对环境会造成污染。
基于上述技术缺陷,本申请的申请人已研究开发了用于活血止痛的活血止痛凝胶(申请号为201310631458.2)和活血止痛巴布膏(申请号为201310653159.9),这两种药贴对皮肤刺激性小、疗效好且生产安全。但是,研究开发多种克服传统活血止痛膏的新药贴,一方面可以让消费者有多种选择,另一方面也可以应对巨大的市场需求,增加企业的市场竞争力。
发明目的
本发明的首要目的是提供一种对皮肤刺激性小、疗效好且生产安全的活血止痛压敏胶贴。
为了实现上述目的,本发明采用了以下技术方案:一种活血止痛压敏胶贴,是由以下重量份数的原料制备得到:干姜16~32、山柰9~18、白芷9~18、甘松8~16、大黄8~16、生天南星5~10、生半夏8~16、没药2~4、乳香2~4、冰片4~8、薄荷脑4~8、樟脑4~8、陈皮9~18、当归5~10、丁香5~10、胡椒5~10、香加皮4~8、细辛4~8、荆芥4~8、桂枝4~8、辛夷3~6、川芎3~6、独活3~6、牡丹皮2~4、辣椒2~4、苍术2~4、颠茄流浸膏6~12、水杨酸甲酯6~12,压敏胶基质40~200,促渗剂5~25,各原料组分总计以1000份计。
具体的方案为,各原料的重量份数为:干姜28、山柰16、白芷16、甘松14、大黄14、生天南星9、生半夏14、没药4、乳香4、冰片7、薄荷脑7、樟脑7、陈皮16、当归9、丁香9、胡椒9、香加皮7、细辛7、荆芥7、桂枝7、辛夷5、川芎5、独活5、牡丹皮4、辣椒4、苍术4、颠茄流浸膏11、水杨酸甲酯11,压敏胶基质80~100,促渗剂14-16。
本发明所述的干姜、山柰、白芷、甘松、大黄、生天南星、生半夏、没药、乳香、冰片、薄荷脑、樟脑、陈皮、当归、丁香、胡椒、香加皮、细辛、荆芥、桂枝、辛夷、川芎、独活、牡丹皮、辣椒和苍术、颠茄流浸膏和水杨酸甲酯是现有技术用于制备活血止痛膏的常用的二十八味原料,其记载于2015年版《中国药典》中,在该现有技术的基础上,本发明采用了丙烯酸酯类压敏胶的至少两种进行复配作为药贴基质,同时添加有促渗剂,这样制备得到的活血止痛压敏胶贴对皮肤刺激性小、生产安全,且疗效好。
本发明的处方设计依据是:丙烯酸酯类压敏胶是丙烯酸酯、丙烯酸和其它功能性单体的自由基引发聚合的产物,采用不同单体进行共聚能获得不同结构的酯基悬挂在主链上,这些悬挂的酯基可以调节聚合物的粘性、溶解性和渗透性。在常温下,丙烯酸酯类压敏胶具有优良的压敏性和粘接性,同时又具体优良的耐老化性、耐光性、耐水性、耐油性,以及可剥离性等特点。实际上,压敏胶总体上可分为橡胶型类、热塑性弹性体类、有机硅类、聚氨酯类和丙烯酸酯类共五类,除了丙烯酸酯类压敏胶外,申请人也尝试过采用其它四类压敏胶材料进行活血止痛压敏胶贴的研究开发,但是都存在着无法推广应用的技术缺陷,这是因为中药的活性成分性质复杂,对压敏胶基质的粘附性等会产生不同程度的影响,基质的粘附性、老化性和释药性又直接关系到制剂的疗效与稳定性。而与单种聚丙烯酸压敏胶相比,相对而言,申请人发现在促渗剂的辅助作用下,采用多种丙烯酸酯类压敏胶复配构成的基质材料不仅与活血止痛的药物活性成分具有很好的相容性,而且透皮释放性能也较好,制备得到的活血止痛压敏胶贴的生物利用度高。
作为进一步的优选方案:所述的促渗剂是氮酮和丙二醇按照1:0.5-1.5的体积比混合配制得到。氮酮是目前常用的化学促渗剂之一,其可破坏角质层脂质,增加角质层间细胞的流动性,降低药物的扩散阻力,且氮酮可作用于细胞内脂质,使扩散阻力减少;丙二醇属于脂肪醇类促渗剂,可增加药物的溶解度,在此背景知识条件下,申请人尝试采用丙二醇与氮酮构成的混合物应用于本发明的活血止痛压敏胶贴的制备,结果发现可有效延长氮酮在角质层中的滞留时间,从而延长活血止痛压敏胶贴的促渗时间。
具体的,所述的压敏胶基质是由Duro-Tak87-2510、Duro-Tak87-2287、Duro-Tak87-2296、Duro-Tak87-2888、Eudragit L100、Eudragit E100中的两种或两种以上复配得到。进一步的,申请人经过大量的实验研究,优选得到以下几种压敏胶基质的复配方式:所述的压敏胶基质是由Duro-Tak87-2888和Eudragit E100按照1:0.1的质量比混合配制得到;所述的压敏胶基质是由Duro-Tak87-2510、Duro-Tak87-2287和Eudragit L100按照1:1:0.3的质量比混合配制得到;所述的压敏胶基质是由Duro-Tak87-2287、Eudragit L100和Eudragit E100按照2:0.2:0.1的质量比混合配制得到。采用上述型号的压敏胶基质复配得到的基质应用于活血止痛药膏中与药效成分的相容性好,贴揭方便,对皮肤刺激性小。
本发明的另外一个发明目的是公开了上述活血止痛压敏胶贴的制备方法,包括以下步骤:
a)、称取干姜、山柰、白芷、甘松、大黄、生天南星、生半夏、没药、乳香、陈皮、当归、丁香、胡椒、香加皮、细辛、荆芥、桂枝、辛夷、川芎、独活、牡丹皮、辣椒和苍术共二十三味原料,粉碎后得到混合粗粉,向混合粗粉中加入质量分数为90%的乙醇,浸渍2-4天,渗漉,收集渗漉液,回收乙醇并浓缩至相对密度为1.05-1.28的清膏,向清膏中加入水杨酸甲酯、颠茄流浸膏和促渗剂,搅拌混合均匀,得药物浸膏备用,所述乙醇的添加量为混合粗粉总质量的6-10倍;
b)、将薄荷脑、冰片和樟脑添加到压敏胶基质中,搅拌溶解,得含药基质备用;
c)、将药物浸膏加到含药基质中,搅拌混合均匀,得胶液备用;
d)、将胶液涂布于隔离纸上,在40~60℃条件下干燥,然后复合背衬,切割,即得活血止痛压敏胶贴。
采用上述方法制备得到的活血止痛压敏胶贴具备以下几个方面的优点:
(1)对皮肤的刺激性与过敏性小:天然橡胶中含有多种杂质,如蛋白等,易引起过敏,而本发明的活血止痛压敏胶贴选用压敏胶为骨架材料,纯度高,有效降低了贴剂对皮肤的刺激性与过敏性,提高患者的依从性。
(2)药效更显著:传统工艺采用汽油作为溶剂制备活血止痛膏,混合与回收溶剂时的工艺温度较高,导致挥发性成分的损失,影响药效;而本发明采用乙酸乙酯作为溶剂,回收时的所需工艺温度明显低于汽油,这样不仅降低药物有效成分的挥发或损失,提高贴膏的药效,而且可以节约热能。
(3)安全生产:本发明采用乙酸乙酯取代现有技术的汽油,可以大大提高生产的安全性。
(4)降低环境污染:传统工艺采用大量的汽油作溶剂,回收时对大气污染较大;而本发明采用乙酸乙酯作溶剂,用量大大减少。
(5)生物利用度高:本发明选择促渗剂,改善了药物有效成分的透皮释放性能,提高了贴剂生物利用度。
需要说明的是,因乙醇的作用只是作为溶剂,其制备过程中又进行了回收,因此可以理解乙醇只是制备该压敏胶的过程原料,故不作为制备该压敏胶的原料,具体的,步骤a)中的搅拌时间为15~30分钟;步骤b)中的搅拌时间为5~10分钟;步骤c)中的搅拌时间为20~40分钟;所述的步骤d)中的干燥时间为0.5~1.5小时。
具体实施方式
为了进一步说明本发明公开的技术方案,以下通过7个实施例来说明:
实施例1:活血止痛压敏胶贴的制备
1)分别称取以下重量份数的原料:干姜28、山柰16、白芷16、甘松14、大黄14、生天南星9、生半夏14、没药4、乳香4、冰片7、薄荷脑7、樟脑7、陈皮16、当归9、丁香9、胡椒9、香加皮7、细辛7、荆芥7、桂枝7、辛夷5、川芎5、独活5、牡丹皮4、辣椒4、苍术4、颠茄流浸膏11、水杨酸甲酯11,Duro-Tak87-2888为50,Eudragit E100为5,氮酮7,丙二醇9;
2)将干姜、山柰、白芷、甘松、大黄、生天南星、生半夏、没药、乳香、陈皮、当归、丁香、胡椒、香加皮、细辛、荆芥、桂枝、辛夷、川芎、独活、牡丹皮、辣椒和苍术共二十三味原料粉碎混合得混合粗粉,向混合粗粉中加入质量分数为90%的乙醇,浸渍3天,渗漉,收集渗漉液,回收乙醇并浓缩至相对密度为1.20的清膏,向清膏中加入水杨酸甲酯、颠茄流浸膏、氮酮和丙二醇促渗剂,搅拌混合均匀,得药物浸膏,所述乙醇的添加量为混合粗粉总质量的8倍;
3)将Duro-Tak87-2888、Eudragit E100混合,加入薄荷脑、冰片和樟脑,搅拌溶解,得含药基质;
4)将药物浸膏加到含药基质中,搅拌混合均匀,得胶液,将胶液涂布于隔离纸上,在50℃条件下干燥1h,然后复合背衬,切割,即得活血止痛压敏胶贴。
实施例2:活血止痛压敏胶贴的制备
1)分别称取以下重量份数的原料:干姜16、山柰9、白芷9、甘松8、大黄8、生天南星5、生半夏8、没药2、乳香2、冰片4、薄荷脑4、樟脑4、陈皮9、当归5、丁香5、胡椒5、香加皮4、细辛4、荆芥4、桂枝4、辛夷3、川芎3、独活3、牡丹皮2、辣椒2、苍术2、颠茄流浸膏6、水杨酸甲酯6,Duro-Tak87-2510为50、Duro-Tak87-2287为50和Eudragit L100为15,氮酮9,丙二醇7;
2)将干姜、山柰、白芷、甘松、大黄、生天南星、生半夏、没药、乳香、陈皮、当归、丁香、胡椒、香加皮、细辛、荆芥、桂枝、辛夷、川芎、独活、牡丹皮、辣椒和苍术共二十三味原料粉碎混合得混合粗粉,向混合粗粉中加入质量分数为90%的乙醇,浸渍4天,渗漉,收集渗漉液,回收乙醇并浓缩至相对密度为1.05的清膏,向清膏中加入水杨酸甲酯、颠茄流浸膏、氮酮和丙二醇,搅拌混合均匀,得药物浸膏,所述乙醇的添加量为混合粗粉总质量的10倍;
3)将Duro-Tak87-2510、Duro-Tak87-2287和Eudragit L100混合,加入薄荷脑、冰片和樟脑,搅拌溶解,得含药基质;
4)将药物浸膏加到含药基质中,搅拌混合均匀,得胶液,将胶液涂布于隔离纸上,在40℃条件下干燥1.5h,然后复合背衬,切割,即得活血止痛压敏胶贴。
实施例3:活血止痛压敏胶贴的制备
1)分别称取以下重量份数的原料::干姜32、山柰18、白芷18、甘松16、大黄16、生天南星10、生半夏16、没药4、乳香4、冰片8、薄荷脑8、樟脑8、陈皮18、当归10、丁香10、胡椒10、香加皮8、细辛8、荆芥8、桂枝8、辛夷6、川芎6、独活6、牡丹皮4、辣椒4、苍术4、颠茄流浸膏12、水杨酸甲酯12,Duro-Tak87-2287为50、Eudragit L100为5和Eudragit E100为2.5,氮酮8,丙二醇15;
2)将干姜、山柰、白芷、甘松、大黄、生天南星、生半夏、没药、乳香、陈皮、当归、丁香、胡椒、香加皮、细辛、荆芥、桂枝、辛夷、川芎、独活、牡丹皮、辣椒和苍术共二十三味原料粉碎混合得混合粗粉,向混合粗粉中加入质量分数为90%的乙醇,浸渍2天,渗漉,收集渗漉液,回收乙醇并浓缩至相对密度为1.28的清膏,向清膏中加入水杨酸甲酯、颠茄流浸膏、氮酮和丙二醇,搅拌混合均匀,得药物浸膏,所述乙醇的添加量为混合粗粉总质量的6倍;
3)将Duro-Tak87-2287、Eudragit L100和Eudragit E100混合,加入薄荷脑、冰片和樟脑,搅拌溶解,得含药基质;
4)将药物浸膏加到含药基质中,搅拌混合均匀,得胶液,将胶液涂布于隔离纸上,在60℃条件下干燥0.5h,然后复合背衬,切割,即得活血止痛压敏胶贴。
实施例4:本发明的活血止痛压敏胶贴对小鼠二甲苯致炎的影响
选取雄性健康小鼠36只,随机分为3组,分别为对照组、活血止痛膏组(即2015版药典公开的活血止痛膏)、活血止痛压敏胶贴组,每组12只,各实验组小鼠每日在右耳贴敷药膏给药1次,连续3次,末次给药后1h,除去贴膏,右耳涂二甲苯0.05mL/只,左耳作对照,15min后处死小鼠,用直径7mm的打孔器将双耳同部位等面积切下,分别称重,计算右耳肿胀度。结果显示,本发明的活血止痛压敏胶贴与现有技术的活血止痛膏之间差异有显著性意义,相比而言,本发明的活血止痛压敏胶贴的抗炎作用明显优于现有技术的活血止痛膏,详见表1所示。
表1对小鼠二甲苯致炎耳重量的影响(n=12,)
与对照组比较:*p<0.05;与现有技术的活血止痛膏组比较:#p<0.05。
实施例5:本发明的活血止痛压敏胶贴对小鼠热板致痛的影响
调节超级恒温水浴的温度在55℃±0.5℃,将热板预热10min,取雌性健康小鼠,每次1只放在热板上,小鼠自放在热板上至出现舔后足所需时间(s)作为该鼠的痛阈值,凡舔后足时间小于5s或大于30s或跳跃者,弃之不用,将合格的36只小鼠随机分为对照组、活血止痛膏组、活血止痛压敏胶贴组,每组12只,各实验组小鼠每日在后腿贴敷药膏1次,连续3次,末次给药后1h,测定小鼠痛阈值。结果显示,本发明的活血止痛压敏胶贴与现有技术的活血止痛膏组之间差异有显著性意义,相比而言,本发明的活血止痛压敏胶贴的镇痛作用明显优于现有技术的活血止痛膏,详见表2所示。
表2对小鼠热板致痛痛阈时间的影响(n=12,)
与对照组比较:*p<0.05,与现有技术的活血止痛膏组比较:#p<0.05。
实施例6:本发明的活血止痛压敏胶贴对醋酸致小鼠扭体的影响
选取雄性健康小鼠36只,随机分为3组,分别为对照组、活血止痛膏组、活血止痛压敏胶贴组,每组12只,实验前剃去小鼠腹部毛,在小鼠腹部给药,1小时后分别重复给药一次,然后立即腹腔注射0.6%醋酸溶液0.1mL/10g,观察小鼠的扭体反应,以典型的后肢伸展,腹部扭曲,腹肌收缩为标准,记录15min内各组动物的扭体次数。结果显示,本发明的活血止痛压敏胶贴与现有技术的活血止痛膏组之间差异有显著性意义,相比而言,本发明的活血止痛压敏胶贴的镇痛作用明显优于现有技术的活血止痛膏,详见表3所示。
表3对小鼠醋酸致痛扭体次数的影响(n=12,)
与对照组比较:**p<0.01,与现有技术的活血止痛膏组比较:#p<0.05。
结论:本发明的活血止痛压敏胶贴与现有技术的活血止痛膏均有明显的抗炎镇痛作用,但是本发明的活血止痛压敏胶贴的抗炎镇痛作用明显优于现有技术的活血止痛膏。
实施例7:本发明的活血止痛压敏胶贴多次给药皮肤刺激性实验
取健康家兔(2.3±0.2kg)12只,雌雄各半,随机分为完整皮肤组和破损皮肤组,在给药前48小时,用6%硫化钠溶液将动物背部脊椎两侧脱毛,每侧面积约为50cm2,去毛后24小时检查去毛皮肤是否有因去毛而受伤,家兔的破损皮肤的制作如下:用手术刀将去毛消毒皮肤划破,以出现小渗血点为度,控制左右两侧皮肤的破损程度基本保持一致。
试验采用同体左右自身对照法:左侧去毛区分别给予本发明的活血止痛压敏胶贴或现有技术的活血止痛膏组,右侧去毛区分别给予基质对照,每天涂抹一次,连续给药7天;分别在停止给药后1、24、48、72小时观察给药部位有无红斑及水肿等情况,同时注意观察给药部位是否有色素沉着、出血点、皮肤粗糙等情况,按照标准(见表4)进行评分,评价多次给药后皮肤的刺激性强度。结果表明,本发明的活血止痛压敏胶贴连续给药7天后,在72小时内观察,家兔完整皮肤组未见红斑、水肿等刺激性反应;破损皮肤组有勉强可见的红斑形成,红斑可在48小时后逐渐消退,属于轻度刺激。现有技术的活血止痛膏组连续给药7天后,在72小时内观察,家兔完整皮肤组可见明显红斑、水肿等轻度刺激性反应;破损皮肤组有中度红斑、水肿,红斑可在72小时后逐渐减轻,属于中度刺激性。故本发明的活血止痛压敏胶贴比现有技术的活血止痛膏组刺激性小,临床使用更安全。
表4皮肤刺激反应评分及强度评价标准
备注:刺激性强度评价的评分标准:0~0.49,无刺激性;0.5~2.99;轻度刺激性;3.0~5.99,中度刺激性;6.0~8.0,重度刺激性。
Claims (8)
1.一种活血止痛压敏胶贴,是由以下重量份数的原料制备得到:干姜16~32、山柰9~18、白芷9~18、甘松8~16、大黄8~16、生天南星5~10、生半夏8~16、没药2~4、乳香2~4、冰片4~8、薄荷脑4~8、樟脑4~8、陈皮9~18、当归5~10、丁香5~10、胡椒5~10、香加皮4~8、细辛4~8、荆芥4~8、桂枝4~8、辛夷3~6、川芎3~6、独活3~6、牡丹皮2~4、辣椒2~4、苍术2~4、颠茄流浸膏6~12、水杨酸甲酯6~12,压敏胶基质40~200,促渗剂5~25,各原料组分总计以1000份计;
所述的压敏胶基质是由Duro-Tak87-2510、Duro-Tak87-2287、Duro-Tak87-2296、Duro-Tak87-2888、Eudragit L100和Eudragit E100这些丙烯酸酯类压敏胶中的两种以上复配得到;
所述活血止痛压敏胶贴的制备方法包括如下步骤:
a)、称取干姜、山柰、白芷、甘松、大黄、生天南星、生半夏、没药、乳香、陈皮、当归、丁香、胡椒、香加皮、细辛、荆芥、桂枝、辛夷、川芎、独活、牡丹皮、辣椒和苍术共二十三味原料,粉碎后得到混合粗粉,向混合粗粉中加入质量分数为90%的乙醇,浸渍2-4天,渗漉,收集渗漉液,回收乙醇并浓缩至相对密度为1.05-1.28的清膏,向清膏中加入水杨酸甲酯、颠茄流浸膏和促渗剂,搅拌混合均匀,得药物浸膏备用,所述乙醇的添加量为混合粗粉总质量的6-10倍;
b)、将薄荷脑、冰片和樟脑添加到压敏胶基质中,搅拌溶解,得含药基质备用;
c)、将药物浸膏加到含药基质中,搅拌混合均匀,得胶液备用;
d)、将胶液涂布于隔离纸上,在40~60℃条件下干燥,然后复合背衬,切割,即得活血止痛压敏胶贴。
2.根据权利要求1所述的活血止痛压敏胶贴,其特征在于:各原料的重量份数为:干姜28、山柰16、白芷16、甘松14、大黄14、生天南星9、生半夏14、没药4、乳香4、冰片7、薄荷脑7、樟脑7、陈皮16、当归9、丁香9、胡椒9、香加皮7、细辛7、荆芥7、桂枝7、辛夷5、川芎5、独活5、牡丹皮4、辣椒4、苍术4、颠茄流浸膏11、水杨酸甲酯11,压敏胶基质80~100,促渗剂14-16。
3.根据权利要求2所述的活血止痛压敏胶贴,其特征在于:所述的促渗剂是氮酮和丙二醇按照1:0.5-1.5的体积比混合配制得到。
4.根据权利要求1所述的活血止痛压敏胶贴,其特征在于:所述的压敏胶基质是由Duro-Tak87-2888和Eudragit E100按照1:0.1的质量比混合配制得到。
5.根据权利要求1所述的活血止痛压敏胶贴,其特征在于:所述的压敏胶基质是由Duro-Tak87-2510、Duro-Tak87-2287和Eudragit L100按照1:1:0.3的质量比混合配制得到。
6.根据权利要求1所述的活血止痛压敏胶贴,其特征在于:所述的压敏胶基质是由Duro-Tak87-2287、Eudragit L100和Eudragit E100按照2:0.2:0.1的质量比混合配制得到。
7.根据权利要求1所述的活血止痛压敏胶贴,其特征在于:步骤a)中的搅拌时间为15~30分钟;步骤b)中的搅拌时间为5~10分钟;步骤c)中的搅拌时间为20~40分钟。
8.根据权利要求1所述的活血止痛压敏胶贴,其特征在于:所述的步骤d)中的干燥时间为0.5~1.5小时。
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