CN105748668A - 陈皮和广藿香组合物在制备抗化疗呕吐药物中的用途 - Google Patents
陈皮和广藿香组合物在制备抗化疗呕吐药物中的用途 Download PDFInfo
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Abstract
本发明涉及一种陈皮和广藿香组合物在制备抗化疗呕吐药物中的用途,该组合物由陈皮广藿香水煎浓缩提取物、陈皮多糖、广藿香挥发油按6:2:3的比例组成,该组合物对由癌症化疗引起的呕吐有很好的疗效。
Description
技术领域
本发明涉及一种药物组合物,更具体地涉及一种由陈皮广藿香水煎浓缩提取物、陈皮多糖、广藿香挥发油组成的天然药物组合物,以及该天然药物组合物在用于制备减少癌症化疗引起的呕吐药物中的用途。
背景技术
癌症目前已成为人类面临的一大杀手,死亡率仅次于心血管疾病,而且呈逐年上升的趋势。我国每年有180万恶性肿瘤患者,其中2/3的病人接受化疗,虽然有一定的疗效,但化疗后大部分患者会出现不同程度的副作用,其中最常见的副作用是恶心、呕吐等胃肠道反应。频繁的呕吐可导致消化液大量丢失,水、电解质、酸碱平衡紊乱,使病人痛苦不堪,严重影响病人的生存质量,不仅会影响到疗效,甚至使病人难以忍受而中断治疗。
目前,临床常用的止吐药主要有组胺(H2)、乙酰胆碱(M)及多巴胺(DA)受体拮抗药和大麻类药物等,但这些药物对化疗后呕吐的疗效差,而且毒副作用强,应用上受到很大限制。新型止吐药,如NK1受体拮抗剂和5-HT3受体拮抗类药物,虽然对化疗后呕吐止吐效果好,但价格昂贵,使用范围窄,而且毒副反应大,临床多需联合用药。
中医药对于癌症化疗减毒的研究,令人瞩目。因此,研发一种高效低毒、价格低廉,易于推广的可用于减轻癌症化疗呕吐副作用的天然中药成为临床亟待解决的问题。
陈皮,为芸香科植物橘(CitrusreticulataBlanco)及其栽培变种的成熟果皮,又名橘皮,具有健脾理气,燥湿化痰的功效,能和中,可治胃失和降、恶心呕吐。广藿香为唇形科植物PogostemoncablinB/ante)Benth的全草。入肺、脾、胃经,有快气,和中,辟秽,祛湿功效,主治感冒暑湿,寒热,头痛,胸脘痞闷,呕吐泄泻,疟疾,痢疾,口臭。本发明人对二者的有效成分进行提取分离,经过大量的各配方比例的研究和实验,最后获得了本发明的最佳药物比例组合物,是与多受体靶点比例相契合的创新性的组合物,并证明了其对癌症化疗引起的呕吐有极好的疗效,由此完成了本发明。
发明内容
本发明第一个目的在于提供一种天然药物组合物,该组合物低毒高效,疗效确切、便于应用及推广,可以对抗化疗后呕吐副作用。
本发明第二个目的在于提供上述天然药物组合物在制备减少癌症化疗副作用的药物中的用途。
本发明提供的一种天然药物组合物,由陈皮广藿香水煎浓缩提取物、陈皮多糖、广藿香挥发油以重量计按6:2:3的比例组成。
其中,陈皮广藿香水煎浓缩提取物、陈皮多糖、广藿香挥发油可通过本领域技术人员公知的常规方法进行提纯获得,陈皮多糖甚至可以商业购得,采用常规方法获得的这些成分或采用商业购得的成分组成的本发明的天然药物均能获得相同的疗效。以下列出的方法仅仅是发明人认为更优选的方法,并不意在对该天然药物组合物中各成分的提取方法作出特别的限制。
优选地,上述天然药物组合物中陈皮广藿香水煎浓缩提取物的制备方法是:
按照配伍比例为1:1取陈皮、广藿香,蒸馏水浸泡,加热煎煮,过滤,保存滤液,药渣再加蒸馏水,同法浸泡、煎煮、过滤,将两次滤液混合,加热浓缩至小体积,超滤膜过滤,减压干燥,即得。
上述天然药物组合物中陈皮多糖的制备方法是:
陈皮粉碎过筛,80%的乙醇回流30min,脱去表面脂肪、抽滤、风干,脱脂后的样品,用索氏提取器提取2次,每次30min,将两次浸提液减压过滤,去除滤渣,合并两次滤液减压浓缩至小体积,即得。
上述天然药物组合物中广藿香挥发油制备方法是:
广藿香干燥,粉碎,过筛,水浸泡,水蒸气蒸馏法提取,乙醚萃取,挥干乙醚,即得。
本发明天然药物组合物在抗呕吐方面的有益效果如下:
1、本发明天然药物组合物具有良好的抗呕吐作用,现已完成临床前在大鼠异嗜高岭土模型的药理学研究。研究表明:该天然药物组合物对于顺铂所致大鼠异嗜高岭土行为有明显的对抗作用,其作用优于单独应用陈皮广藿香水煎浓缩提取物、陈皮多糖及广藿香挥发油。
2、本发明人独创地将陈皮广藿香水煎浓缩提取物、陈皮多糖、广藿香挥发油进行组合,并通过大量实验确定这些组分之间的用量配比,使该组合物发挥了很好的协同作用,获得意外的效果。经过我们反复实验研究,各组分的用量比例是6:2:3时增效明显,这是本发明人付出大量创造性劳动而获得的,本领域普通技术人员仅仅通过公开的内容无法简单获得这种配比范围以及最佳用量比例。
3、该天然药物组合物陈皮广藿香水煎浓缩提取物、陈皮多糖、广藿香挥发油各组分均可通过常规手段获得,其中一些组分例如陈皮多糖还可通过商业购得,这样的组合物本身具有获得方便、成本较低的效果。这也是发明人通过大量创造性劳动方获得的兼具极佳疗效和较高工业实用性的产品。
具体实施方式
下面通过实施例和试验例进一步阐述本发明天然药物组合物的制备,以及其在抗呕吐应用的有益效果。
实施方案
第一步:各种提取物的制备
(1)陈皮广藿香水煎浓缩提取物的制备
按照配伍比例为1:1取陈皮、广藿香,蒸馏水浸泡,加热煎煮,过滤,保存滤液,药渣再加蒸馏水,同法浸泡、煎煮、过滤,将两次滤液混合,加热浓缩至小体积,超滤膜过滤,减压干燥,即得。
(2)陈皮多糖的制备
陈皮粉碎过筛,80%的乙醇回流30min,脱去表面脂肪、抽滤、风干,脱脂后的样品,用索氏提取器提取2次,每次30min,将两次浸提液减压过滤,去除滤渣,合并两次滤液减压浓缩至小体积,即得。
(3)广藿香挥发油的制备
广藿香干燥,粉碎,过筛,水浸泡,水蒸气蒸馏法提取,乙醚萃取,挥干乙醚,即得。
药效及药理学资料:
在下述试验例子中组合物为:陈皮广藿香水煎浓缩提取物、陈皮多糖、广藿香挥发油的用量比例为6:2:3,由常规手段制得的或商业购得的上述四种成分组成的组合物具有与上述方法制得的组合物相同的效果,其实验资料这里不再列举,本领域技术人员对此能够认可。以下是优选的实施方式获得的药效及药理学资料:
试验例1:天然药物组合物治疗呕吐作用的药效学研究
1、试验材料
(1)高岭土
(2)顺铂(cisplatin)
(3)盐酸昂丹司琼注射液
(4)大鼠,雄性,实验前自由进食饮水。
2、试验方法:
将大鼠随机分为7组,每组6只,A组为空白组,B组为模型对照组,C组为昂丹司琼组,D组为陈皮广藿香水煎浓缩提取物,E组为陈皮多糖组,F组为广藿香挥发油组,G组为本发明的天然药物组合物(陈皮广藿香水煎浓缩提取物、陈皮多糖、广藿香挥发油按6:2:3比例混合)。A、B组先以给以生理盐水5ml·kg-1ig;C组给予给与恩丹西酮4mg·kg-1ip预处理;D-G组给相应的药物10g.kg-1(相当于含生药量)ig预处理,连续给药物三天,第二天给药后禁食。第三天给药30min后除A组外,均给予顺铂3mg·kg-1ip,观察各组在给药后6h内大鼠的异嗜高岭土行为,记录大鼠进食高岭土量。
3、实验结果
与对照组比较,模型组大鼠进食高岭土量明显增加(P<0.01)。昂丹司琼组及本发明的组合物能够显著减少大鼠进食高岭土量。结果见表1.
表1在顺铂(3mg·kg?1,ip)诱导的大鼠异嗜模型的作用观察(n=6,mg)
组别 | 剂量(g/kg) | 高岭土量(mg) |
A | 48.0±10.7 | |
B | 1850.9±155.6 a | |
C | 0.004 | 421.9±85.7b |
D | 10a | 1547.5±98.7 |
E | 10a | 1752.4±198.0 |
F | 10a | 1747.1±217.5 |
G | 10a | 910.6±85.3b |
注:a相当于含生药量,与对照组比较a P<0.01,与模型组相比b P<0.01。
Claims (2)
1.一种抗化疗呕吐的陈皮广藿香组合物,其特征在于该组合物由陈皮广藿香水煎浓缩提取物、陈皮多糖、广藿香挥发油以重量计按6:2:3的比例组成,
其中陈皮广藿香水煎浓缩提取物的制备方法是:
按照配伍比例为1:1取陈皮、广藿香,蒸馏水浸泡,加热煎煮,过滤,保存滤液,药渣再加蒸馏水,同法浸泡、煎煮、过滤,将两次滤液混合,加热浓缩至小体积,超滤膜过滤,减压干燥,即得;
其中陈皮多糖的制备方法是:
陈皮粉碎过筛,80%的乙醇回流30min,脱去表面脂肪、抽滤、风干,脱脂后的样品,用索氏提取器提取2次,每次30min,将两次浸提液减压过滤,去除滤渣,合并两次滤液减压浓缩至小体积,即得;
其中广藿香挥发油的制备方法是:
广藿香干燥,粉碎,过筛,水浸泡,水蒸气蒸馏法提取,乙醚萃取,挥干乙醚,即得。
2.如权利要求1所述的陈皮广藿香组合物在制备减少化疗呕吐药物中的用途。
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