CN105943687A - 一种治疗心绞痛的中药自微乳速释滴丸及制备方法 - Google Patents
一种治疗心绞痛的中药自微乳速释滴丸及制备方法 Download PDFInfo
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Abstract
本发明公开了一种治疗心绞痛的中药自微乳速释滴丸及制备方法，该速释滴丸是通过提取败酱草，皂矾，闹羊花，山豆根，青礞石，马宝，卷柏，五味子中的有效药物成分，制得中药提取物；然后将中药提取物与二乙二醇单乙基醚、单亚油酸甘油酯和聚氧乙烯蓖麻油EL混合搅拌均匀后与调配液混合制得自微乳液，最后均质而成，本发明具有便于携带、易于保存、使用方便、载药量高、快速释药、生物利用度高的显著优势。
Description
技术领域
本发明涉及一种药物及其制备方法，尤其涉及一种治疗心绞痛的中药自微乳速释滴丸及制备方法，属医药技术领域。
背景技术
心绞痛是指由于冠状动脉粥样硬化狭窄导致冠状动脉供血不足，心肌暂时缺血与缺氧所引起的以心前区疼痛为主要临床表现的一组综合征。其特点为阵发性的前胸压榨性疼痛感觉，可伴有其他症状，疼痛主要位于胸骨后部，可放射至心前区与左上肢。常在体力劳累、情绪激动(发怒、焦急、过度兴奋)、受寒、饱食、吸烟时发生贫血、心动过速等为常见的诱因，持续数分钟，休息或用硝酸酯制剂后消失。心绞痛目前在我国的发病率呈逐年上升趋势，严重危害着人民群众的健康和生活。目前西医治疗应用硝酸甘油类扩张冠状血管，但会产生毒副作用，容易使患者出现博动性剧烈头痛、头昏、眩晕等症状，且容易复发，见效慢，价格昂贵，而中药制剂学作为我国的传统医学，具有作用强、见效快、药效持久等优点，且没有依赖性、耐药性以及毒副作用，因此选择一种中药制剂治疗心绞痛，对于治疗心绞痛具有十分重要的临床意义。
药物的自微乳化，是利用油相、表面活性剂和助乳化剂等，将药物成分(特别是难溶性药物成分)制成均一的液体，在胃肠道环境中可自发形成粒径在微米级以下的微乳，能够提高药物的吸收速度和生物利用度。但是，自微乳药物通常为液体，稳定性差，在临床使用时会带来不便。将自微乳药物固体化，是现今制药领域的研究热点。滴丸是一类临床常用的药物剂型，常以固体或液体药物与一定成分的基质熔融混匀后，滴入相反极性的液体中冷凝成丸。由于滴丸的制备过程，其本质是利用固体分散体原理将药物制成小丸的形式，因此，滴丸充分发挥了固体分散体增溶、速释的特点，常作为急救药物制剂的剂型选择之一。同时，滴丸具有承载药物含量高、便于携带、简单易用等特点，常被用作家庭急救药物的首选制剂，如复方丹参滴丸、银杏酮酯滴丸等。本发明具有便于携带、易于保存、使用方便、载药量高、快速释药、生物利用度高的显著优势。
发明内容
本发明的目的在于克服现有技术的不足，提供了一种治疗心绞痛的中药自微乳速释滴丸及制备方法，以解决现有技术中，药物携带不便、载药量不足、药效不明显等技术问题而提出的。本发明是通过以下技术方案实现的：
本发明公开了一种治疗心绞痛的中药自微乳速释滴丸及制备方法，包括以下制备步骤：
1、中药提取物的制备：
1)、称取中药败酱草80～120g，皂矾70～100g，闹羊花50～80g，山豆根50～70g，青礞石30～50g，马宝30～40g，卷柏40～60g和五味子30～50g，混合粉碎后，加入质量为中药质量3～5倍的浓度为65～80％的乙醇溶液，在常温浸泡3～5天，过滤去渣得提取液Ⅰ；
2)、将过滤饼放入容器中，加入重量为滤饼重量2～4倍的水，加热煮沸2～3小时，冷却后过滤去渣，得提取液Ⅱ；
3)、将提取液Ⅰ与提取液Ⅱ合并，减压旋转加热蒸发，浓缩至含水量在5～10％粘稠膏状物，得中药提取物；
2、中药自微乳制备：
1)、将制得的中药提取物加入二乙二醇单乙基醚50～200ml，超声分散溶解。
2)、取单亚油酸甘油酯20～25g、聚氧乙烯蓖麻油EL15～20g与上述含中药有效成分的二乙二醇单乙基醚溶液混合，超声分散后，以500～1000rpm的转速搅拌25～30min，得中药自微乳液。
3、中药自微乳滴丸制备：
以2～3倍质量(400～600g)的聚乙二醇-6000/聚乙二醇-4000(质量比1：1)与上述中药自微乳液混合，搅拌均匀并水浴加热至60～80℃保温，使用滴丸锅以每分钟30～60滴的速度，于10～20cm高度滴入2～8℃的液体石蜡中，收集冷凝筒底部的成型固体滴丸，整粒后即得治疗心绞痛的中药自微乳速释滴丸。
将上述配方以现代工艺提取并制得自微乳速释滴丸，本发明所要解决的技术问题，是将复方中药提取有效成分，并将其制成自微乳，提高了单位药物的载药量和难溶性成分的含量，再通过滴丸的形式将中药自微乳固化，制成自微乳速释滴丸，本发明具有载药量高、快速释药优势，为治疗心绞痛提供了一种新中药剂型，即可口服，亦可通过舌下含服。与现有丸剂、片剂相比，具有体积小、载药量高、快速释药特点，是治疗心绞痛疾病的理想药物剂型。
具体实施方式
下面对本发明的实施例作详细说明，本实施例在以本发明技术方案为前提下进行实施，给出了详细的实施方式和具体的操作过程，但本发明的保护范围不限于下述的实施例。
实施例1
本发明公开了一种治疗心绞痛的中药自微乳速释滴丸及制备方法，制备方法如下：
1)称取中药败酱草80g，皂矾70g，闹羊花80g，山豆根70g，青礞石50g，马宝40g，卷柏60g，五味子50g，混合粉碎后，加入1500g浓度为65％的乙醇溶液，在常温下浸泡3天，过滤去渣得提取液Ⅰ；
2)将步骤1)过滤中得到的滤饼加入500g的水，100℃下加热煮沸2h，冷却后，过滤，收集滤液得到提取液Ⅱ；
3)将提取液Ⅰ和提取液Ⅱ合并，减压旋转加热蒸发后得到中药提取物A；
4)将中药提取物A加入到50ml的二乙二醇单乙基醚中，进行超声分散溶解，得到溶解液B；
5)将单亚油酸甘油酯20g、聚氧乙烯蓖麻油EL15g和溶解液B三者混合后，进行超声分散溶解，搅拌均匀后得到中药自微乳液C；
6)将聚乙二醇-6000和聚乙二醇-4000按质量比1:1混合后形成的调配液D与上述中药自微乳液C混合，调配液D的重量为400g是中药自微乳液C重量的2倍，搅拌均匀并水浴加热至60℃保温，得到目标混合药剂E；
7)将目标混合药剂E滴加到2℃的液体石蜡中，收集冷凝成型的固体滴丸，整粒后即得到治疗心绞痛的中药自微乳速释滴丸。
实施例2
1)称取中药败酱草120g，皂矾100g，闹羊花80g，山豆根70g，青礞石30g，马宝30g，卷柏40g，五味子30g，混合粉碎后，加入2500g浓度为80％的乙醇在常温浸泡5天，过滤去渣得提取液Ⅰ；
2)将步骤1)过滤中得到的滤饼加入2倍重量的水，100℃下加热煮沸3h，冷却后，过滤，收集滤液得到提取液Ⅱ；
3)将提取液Ⅰ和提取液Ⅱ合并，减压旋转加热蒸发后得到中药提取物A；
4)将中药提取物A加入到200ml的二乙二醇单乙基醚中，进行超声分散溶解，得到溶解液B；
5)将单亚油酸甘油酯25g、聚氧乙烯蓖麻油EL20g和溶解液B三者混合后，进行超声分散溶解，搅拌均匀后得到中药自微乳液C；
6)将聚乙二醇-6000和聚乙二醇-4000按质量比1:1混合后形成的调配液D与上述中药自微乳液C混合，调配液D的重量为600g是中药自微乳液C的3倍，搅拌均匀并水浴加热至80℃保温，得到目标混合药剂E；
7)将目标混合药剂E滴加到8℃的液体石蜡中，收集冷凝成型的固体滴丸，整粒后即得到治疗心绞痛的中药自微乳速释滴丸。
步骤7)中用到的设备为滴丸锅，滴加的速度为30滴/分钟。
实施例3
与实施例2中的各步骤相同，取样比例相同，区别在于实施例3中步骤7)中滴液滴加的速度为60滴/分钟；步骤5)中各组分用量为：二乙二醇单乙基醚200ml，单亚油酸甘油酯20g，聚氧乙烯蓖麻油EL20g；步骤1)中的有机溶剂是浓度为75％的乙醇溶液，室温下浸泡3天。
实施例4
本实施例中，制备步骤为：
1、中药提取物的制备：
1)、称取中药败酱草100g，皂矾90g，闹羊花70g，山豆根60g，青礞石40g，马宝35g，卷柏50g，五味子40，混合粉碎后，加入5倍浓度为70％的乙醇在常温浸泡3天，过滤去渣得醇提液；
2)、将过滤饼放入容器中，加入3倍的水，温度控制在100℃，加热煮沸2～3小时，冷却后过滤去渣得水提液；
3)、将醇提液、水提液合并减压旋转蒸发，浓缩至含水量在5～10％粘稠膏状物，得中药提取物；
2、中药自微乳制备：
1)、将制得的中药提取物加入二乙二醇单乙基醚100ml，超声分散溶解。
2)、取单亚油酸甘油酯20g、聚氧乙烯蓖麻油EL20g与上述含药的二乙二醇单乙基醚溶液混合，超声分散后，以1000rpm的转速搅拌25～30min，得中药自微乳液。
3、中药自微乳滴丸制备：
将600g的聚乙二醇-6000/聚乙二醇-4000(质量比1：1)混合液与上述中药自微乳液混合，搅拌均匀并水浴加热至60～80℃保温，使用滴丸锅以每分钟30～60滴的速度，在10～20cm高度滴入5℃的液体石蜡中，收集冷凝筒底部的成型固体滴丸，整粒后即得治疗心绞痛的中药自微乳速释滴丸。
Claims (7)
1.一种治疗心绞痛的中药自微乳速释滴丸的制备方法，其特征在于，包括以下制备步骤：
1)称取败酱草、皂矾、闹羊花、山豆根、青礞石、马宝、卷柏和五味子，粉碎混合后，加入到有机溶剂中浸泡，过滤，收集滤液得到提取液Ⅰ；
2)将步骤1)中过滤后得到的滤饼与纯净水混合，加热煮沸2～3h，冷却后，过滤，收集滤液得到提取液Ⅱ；
3)将所述提取液Ⅰ和所述提取液Ⅱ合并，蒸发溶剂后，得到中药提取物A；
4)将所述中药提取物A加入到二乙二醇单乙基醚中，进行超声分散溶解，得到溶解液B；
5)将单亚油酸甘油酯、聚氧乙烯蓖麻油EL和所述溶解液B三者混合后，进行超声分散溶解，搅拌均匀后得到中药自微乳液C；
6)将聚乙二醇-6000和聚乙二醇-4000混合后形成的调配液D与上述中药自微乳液C混合，搅拌均匀并水浴加热至60～80℃保温，得到目标混合药剂E；
7)将目标混合药剂E滴加到2～8℃的液体石蜡中，收集冷凝成型的固体滴丸，整粒后即得到治疗心绞痛的中药自微乳速释滴丸。
2.如权利要求1所述的一种治疗心绞痛的中药自微乳速释滴丸的制备方法，其特征在于，所述败酱草、皂矾、闹羊花、山豆根、青礞石、马宝、卷柏、五味子、二乙二醇单乙基醚、单亚油酸甘油酯、聚氧乙烯蓖麻油EL、聚乙二醇-6000和聚乙二醇-4000的组份含量为：
败酱草 80～120g
皂矾 70～100g
闹羊花 50～80g
山豆根 50～70g
青礞石 30～50g
马宝 30～40g
卷柏 40～60g
五味子 30～50g
二乙二醇单乙基醚 50～200ml
单亚油酸甘油酯 20～25g
聚氧乙烯蓖麻油 EL15～20g
聚乙二醇-6000 200～300g
聚乙二醇-4000 200～300g。
3.如权利要求1所述的一种治疗心绞痛的中药自微乳速释滴丸的制备方法，其特征在于，所述败酱草、皂矾、闹羊花、山豆根、青礞石、马宝、卷柏、五味子、二乙二醇单乙基醚、单亚油酸甘油酯、聚氧乙烯蓖麻油EL、聚乙二醇-6000和聚乙二醇-4000的组份含量为：
败酱草 80g
皂矾 70g
闹羊花 50g
山豆根 50g
青礞石 30g
马宝 30g
卷柏 40g
五味子 30g
二乙二醇单乙基醚 100ml
单亚油酸甘油酯 25g
聚氧乙烯蓖麻油 EL20g
聚乙二醇-6000 300g
聚乙二醇-4000 300g。
4.如权利要求1所述的一种治疗心绞痛的中药自微乳速释滴丸的制备方法，其特征在于，步骤1)中所述有机溶剂是浓度为65～80％的乙醇溶液，所述浸泡的时间为3～5天。
5.如权利要求1所述的一种治疗心绞痛的中药自微乳速释滴丸的制备方法，其特征在于，步骤3)中所述中药提取物A中的含水量为5～10％。
6.如权利要求1所述的一种治疗心绞痛的中药自微乳速释滴丸的制备方法，其特征在于，步骤6)中所述调配液D是由聚乙二醇-6000和聚乙二醇-4000按质量比1:1进行调配的，所述目标混合药剂E中的调配液D的质量是中药自微乳液C质量的2～3倍。
7.一种治疗心绞痛的中药自微乳速释滴丸，其特征在于，所述治疗心绞痛的中药自微乳速释滴丸是通过权利要求1～6所述的一种治疗心绞痛的中药自微乳速释滴丸的制备方法中任一方法制得的。
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