CN111714461A - 一种草果挥发油包合物内服片及其制备方法 - Google Patents
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Abstract
本申请公开了一种草果挥发油包合物内服片及其制备方法,其中草果挥发油包合物内服片按照质量份数,包括3‑5份草果挥发油,36‑60份β‑环糊精,36‑60份稀释剂,2‑5份黏合剂,3‑7份润滑剂。本申请的一个技术效果在于,本申请能够增强挥发油稳定性、减少挥发、掩盖其不良气味、且利于患者服用及携带。
Description
技术领域
本申请属于保健产品技术领域,具体地说,涉及一种草果挥发油包合物内服片及其制备方法。
背景技术
草果,姜科植物草果Amomum tsao-ko Crevost et Lemaire的干燥成熟果实,主要分布于我国广西、云南、四川和贵州等地,其味辛,性温,入脾、胃二经,功能燥湿温中,除痰截疟。宋《桂海虞衡志》中“红盐草果,邕州取新生草果,入梅汁盐渍,令色红,暴干荐酒,芬味甚高,世珍之”的记载,就药食同源的药物发展历程来看,本品作为食品使用的历史可能更早。
现在,草果90%以上用于食品添加,只有不到5%应用于中成药的配置和其他领域,我国对草果有效成分进行过大量研究工作,其主要活性成分为草果挥发油,具有镇痛、抗胃溃疡及抗乙肝病毒等主要药理作用,及抗氧化性、抗诱变及防霉等作用,可用于回肠痉挛、乙型肝炎、急性结膜炎、多种类型的癫痫、妊高征伴腹水引起的腹胀等。但挥发油极易挥发、对光和热不稳定,具有不良气味,不便于携带和服用,难以有效的进行药用,因此,有必要提供一种草果挥发油包合物内服片。
发明内容
本申请的一个目的是提供一种草果挥发油包合物内服片的技术方案。
根据本申请的一个方面,本申请提供一种草果挥发油包合物内服片,按照质量份数,包括3-5份草果挥发油,36-60份β-环糊精,36-60份稀释剂,2-5份黏合剂,3-7份润滑剂。
可选地,按照质量份数,包括4份草果挥发油,48份β-环糊精,48份稀释剂,3份黏合剂,5份润滑剂。
可选地,所述稀释剂包括淀粉和微晶纤维素。
可选地,所述淀粉和微晶纤维素的质量比为1:1。
可选地,所述黏合剂为聚维酮K30。
可选地,所述润滑剂为滑石粉。
根据本申请的另一个方面,本申请还提供一种上述的草果挥发油包合物内服片的制备方法,包括以下步骤:
提供草果挥发油,β-环糊精,份稀释剂,黏合剂,润滑剂;
将草果挥发油溶解于无水乙醇,加入β-环糊精制备的饱和水溶液搅拌至混合均匀,超声40-50min,冷藏16-20h,抽滤后用乙酸乙酯洗脱,干燥得到草果挥发油包合物;
将草果挥发油包合物与稀释剂混合均匀,加入黏合剂和润湿剂制粒,干燥后过筛,在加入润滑剂混合均匀,进行压片制得草果挥发油包合物内服片。
可选地,所述草果挥发油通过以下方法制备得到:
称取草果粗粉,加入8倍量水浸泡1h,使用水蒸气蒸馏法进行提取,冷藏后油水分离后即得草果挥发油。
可选地,所述超声的功率为500w,频率40KHz。
可选地,所述润湿剂为75%乙醇溶液。
本申请的一个技术效果在于,本申请能够增强挥发油稳定性、减少挥发、掩盖其不良气味、且利于患者服用及携带。
附图说明
此处所说明的附图用来提供对本申请的进一步理解,构成本申请的一部分,本申请的示意性实施例及其说明用于解释本申请,并不构成对本申请的不当限定。在附图中:
图1是本申请实施例1中制备得到的草果挥发油;
图2是本申请实施例1中制备得到的草果挥发油包合物;
图3是本申请实施例1中制备得到的草果挥发油内服片。
具体实施方式
以下将配合附图及实施例来详细说明本申请的实施方式,借此对本申请如何应用技术手段来解决技术问题并达成技术功效的实现过程能充分理解并据以实施。
实施例1
称取草果粗粉,加入8倍量水浸泡1h,使用水蒸气蒸馏法进行提取,冷藏后油水分离后即得草果挥发油。
称取4份草果挥发油,48份β-环糊精,48份稀释剂,3份黏合剂,5份润滑剂;其中稀释剂为质量比1:1的淀粉和微晶纤维素,黏合剂为聚维酮K30,聚维酮K30制成4%聚维酮K30乙醇溶液备用,润滑剂为滑石粉。
将草果挥发油溶解于2份无水乙醇中,加入β-环糊精制备的饱和水溶液搅拌至混合均匀,超声45min(功率500w,频率40KHz),冷藏18h,抽滤后用乙酸乙酯洗脱三次,干燥得到草果挥发油包合物;
采用湿法制粒压片法制备草果挥发油包合物内服片,润湿剂为75%乙醇溶液。将草果挥发油包合物与稀释剂混合均匀,加入黏合剂和润湿剂制粒,45℃以下干燥,24目筛整粒,在加入润滑剂混合均匀,进行压片制得草果挥发油包合物内服片。
本申请将草果挥发油嵌入环糊精筒状结构内,以形成超微粒分散物,不仅可以保证药物原有的性质和作用,而且转化成的碳水化合物,能够有效地被人体所吸收,并直接参与人体的机体代谢过程中。包合物极少受到外界的影响,以一种平衡状态而存在,具有良好的稳定性,同时,这也在一定程度上增加药物的稳定性。将草果挥发油包合于β-环糊精中,能够增强挥发油稳定性、减少挥发、掩盖其不良气味、且利于患者服用及携带。此外,将草果挥发油制成固体制剂在方便运输、储存、服用的同时也对草果挥发油中的有效成分进行了富集。
基于实施例1制备的草果挥发油的抑菌活性实验
4.1培养基和菌株
试药:抗真菌活性检测阳性对照药物氟康唑溶于DMSO,离心取上清液,贮存浓度为50mg/mL,4℃密封避光保存。
4.1.1培养基
(1)沙氏液体培养基:蛋白胨10.0g、葡萄糖40.0g溶解于1000ml蒸馏水中,115℃高压灭菌30分钟,备用。
(2)沙氏固体培养基:蛋白胨10.0g、葡萄糖40.0g、琼脂20g溶解于1000ml蒸馏水中,115℃高压灭菌30分钟,备用。
(3)亚甲蓝M-H琼脂培养基:M-H琼脂+2%葡萄糖+0.5ug/ml亚甲蓝,121℃高压灭菌15min,备用。
(4)LB液体培养基:精密称取胰蛋白胨10g、酵母提取物5g、氯化钠10g,置于1000mL蓝盖试剂瓶中,并用蒸馏水定容到1000mL,121℃高压灭菌15min,备用。
(5)LB固体培养基:精密称取胰蛋白胨10g、酵母提取物5g、氯化钠10g,琼脂15g,置于1000mL蓝盖试剂瓶中,并用蒸馏水定容到1000mL,121℃高压灭菌15min,备用。
4.1.2菌株
白色念珠菌标准株SC5314、白色念珠菌临床分离耐药株23#、金黄色葡萄球菌、大肠杆菌。
4.2抑菌试验实验方法K-B法(标准滤纸片法)
4.2.1取培养基上37℃培养16~18h的纯菌落,制备菌悬液,调整浓度为1×107CFU/mL,每个平板各加载菌液500uL,立即用棉拭子均匀涂板,放置10分钟左右,待菌液完全被平板吸收,用镊子加载直径为6mm的无菌滤纸片。
4.2.2加载纸片后,取一定量的待测样品加载在滤纸片的正中心,防止抑菌圈畸形,待样品均匀、完全的吸收后,放入恒温恒湿箱或CO2培养箱中,一般情况下,孵育18-24h(真菌)或12-16h(细菌)后,检查每一块平板,若接种平板满意,抑菌圈应为正圆形,菌落应相互融合生长。测量抑菌环的直径边缘为80%被抑制即可,如果菌落生长较弱,应该继续培养20~24h。
4.2.3在不反光的黑色背景下读取抑菌圈的直径,抑菌圈的直径包括纸片的直径。抑菌圈的界限应该是以肉眼观察没有明显可见真菌生长的区域,在抑菌圈边缘微弱生长的、仅能在放大镜下观察到的细小菌落应忽略。
4.3抑菌试验实验结果
实施例1制备的草果挥发油对白色念珠菌标准株SC5314、白色念珠菌临床耐药株23#、金黄色葡萄球菌和大肠杆菌均具有活性。
实施例2
称取草果粗粉,加入8倍量水浸泡1h,使用水蒸气蒸馏法进行提取,冷藏后油水分离后即得草果挥发油。
称取3份草果挥发油,36份β-环糊精,36份稀释剂,2份黏合剂,3份润滑剂;其中稀释剂为质量比1:1的淀粉和微晶纤维素,黏合剂为聚维酮K30,聚维酮K30制成4%聚维酮K30乙醇溶液备用,润滑剂为滑石粉。
将草果挥发油溶解于2份无水乙醇中,加入β-环糊精制备的饱和水溶液搅拌至混合均匀,超声45min(功率500w,频率40KHz),冷藏18h,抽滤后用乙酸乙酯洗脱三次,干燥得到草果挥发油包合物;
采用湿法制粒压片法制备草果挥发油包合物内服片,润湿剂为75%乙醇溶液。将草果挥发油包合物与稀释剂混合均匀,加入黏合剂和润湿剂制粒,45℃以下干燥,24目筛整粒,在加入润滑剂混合均匀,进行压片制得草果挥发油包合物内服片。
实施例3
称取草果粗粉,加入8倍量水浸泡1h,使用水蒸气蒸馏法进行提取,冷藏后油水分离后即得草果挥发油。
称取5份草果挥发油,60份β-环糊精,60份稀释剂,5份黏合剂,7份润滑剂;其中稀释剂为质量比1:1的淀粉和微晶纤维素,黏合剂为聚维酮K30,聚维酮K30制成4%聚维酮K30乙醇溶液备用,润滑剂为滑石粉。
将草果挥发油溶解于2份无水乙醇中,加入β-环糊精制备的饱和水溶液搅拌至混合均匀,超声45min(功率500w,频率40KHz),冷藏18h,抽滤后用乙酸乙酯洗脱三次,干燥得到草果挥发油包合物;
采用湿法制粒压片法制备草果挥发油包合物内服片,润湿剂为75%乙醇溶液。将草果挥发油包合物与稀释剂混合均匀,加入黏合剂和润湿剂制粒,45℃以下干燥,24目筛整粒,在加入润滑剂混合均匀,进行压片制得草果挥发油包合物内服片。
如在说明书及权利要求当中使用了某些词汇来指称特定成分或方法。本领域技术人员应可理解,不同地区可能会用不同名词来称呼同一个成分。本说明书及权利要求并不以名称的差异来作为区分成分的方式。如在通篇说明书及权利要求当中所提及的“包含”为一开放式用语,故应解释成“包含但不限定于”。“大致”是指在可接收的误差范围内,本领域技术人员能够在一定误差范围内解决所述技术问题,基本达到所述技术效果。说明书后续描述为实施本申请的较佳实施方式,然所述描述乃以说明本申请的一般原则为目的,并非用以限定本申请的范围。本申请的保护范围当视所附权利要求所界定者为准。
还需要说明的是,术语“包括”、“包含”或者其任何其他变体意在涵盖非排他性的包含,从而使得包括一系列要素的商品或者系统不仅包括那些要素,而且还包括没有明确列出的其他要素,或者是还包括为这种商品或者系统所固有的要素。在没有更多限制的情况下,由语句“包括一个……”限定的要素,并不排除在包括所述要素的商品或者系统中还存在另外的相同要素。
上述说明示出并描述了发明的若干优选实施例,但如前所述,应当理解发明并非局限于本文所披露的形式,不应看作是对其他实施例的排除,而可用于各种其他组合、修改和环境,并能够在本文所述发明构想范围内,通过上述教导或相关领域的技术或知识进行改动。而本领域人员所进行的改动和变化不脱离发明的精神和范围,则都应在发明所附权利要求的保护范围内。
Claims (10)
1.一种草果挥发油包合物内服片,其特征在于,按照质量份数,包括3-5份草果挥发油,36-60份β-环糊精,36-60份稀释剂,2-5份黏合剂,3-7份润滑剂。
2.根据权利要求1所述的草果挥发油包合物内服片,其特征在于,按照质量份数,包括4份草果挥发油,48份β-环糊精,48份稀释剂,3份黏合剂,5份润滑剂。
3.根据权利要求1所述的草果挥发油包合物内服片,其特征在于,所述稀释剂包括淀粉和微晶纤维素。
4.根据权利要求3所述的草果挥发油包合物内服片,其特征在于,所述淀粉和微晶纤维素的质量比为1:1。
5.根据权利要求1所述的草果挥发油包合物内服片,其特征在于,所述黏合剂为聚维酮K30。
6.根据权利要求1所述的草果挥发油包合物内服片,其特征在于,所述润滑剂为滑石粉。
7.一种权利要求1-6任一所述的草果挥发油包合物内服片的制备方法,其特征在于,包括以下步骤:
提供草果挥发油,β-环糊精,份稀释剂,黏合剂,润滑剂;
将草果挥发油溶解于无水乙醇,加入β-环糊精制备的饱和水溶液搅拌至混合均匀,超声40-50min,冷藏16-20h,抽滤后用乙酸乙酯洗脱,干燥得到草果挥发油包合物;
将草果挥发油包合物与稀释剂混合均匀,加入黏合剂和润湿剂制粒,干燥后过筛,在加入润滑剂混合均匀,进行压片制得草果挥发油包合物内服片。
8.根据权利要求7所述的制备方法,其特征在于,所述草果挥发油通过以下方法制备得到:
称取草果粗粉,加入8倍量水浸泡1h,使用水蒸气蒸馏法进行提取,冷藏后油水分离后即得草果挥发油。
9.根据权利要求7所述的制备方法,其特征在于,所述超声的功率为500w,频率40KHz。
10.根据权利要求7所述的制备方法,其特征在于,所述润湿剂为75%乙醇溶液。
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