CN1212135C - 复方活化血竭 - Google Patents

复方活化血竭 Download PDF

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CN1212135C
CN1212135C CN02142360.1A CN02142360A CN1212135C CN 1212135 C CN1212135 C CN 1212135C CN 02142360 A CN02142360 A CN 02142360A CN 1212135 C CN1212135 C CN 1212135C
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compound
blood
sanguis draxonis
daemonorops draco
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CN1483433A (zh
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周家礽
汪伯良
陈植和
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Yunnan Shengke Pharmaceutical Co ltd
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Kunming Dihon Pharmaceutical Co Ltd
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Abstract

本发明涉及到一种治疗心脑血管疾病的药物，尤其是由天然植物中的提取物制成的复方制剂，本发明所述的复方活化血竭，其特征在于其有效药用成份由血竭包合物和三七总皂甙组成，血竭包合物的重量百分比为占复方中的20-80%，三七总皂甙的重量百分比为占复方中的80-20%，本发明有活血化瘀，通络止痛功能。主要用于胸痹心痛(冠心病心绞痛)，能够有效治疗和预防冠心病、高血压病、高血脂症等心脑血管疾病。

Description

复方活化血竭
技术领域
本发明涉及到一种治疗心脑血管疾病的药物，尤其是由天然植物中的提取物制成的复方制剂。
技术背景
三七总皂甙本身在临床已成为一种著名的抗心脑缺血药物，在治疗心血管疾病方面进行了较多的基础和临床研究，表明具有抗心肌缺血、抗休克、抗心律失常作用和抑制血管平滑肌细胞增殖等药理作用，能治疗冠心病、高血压病、高血脂症等，是治疗和预防心血管疾病的良药。血竭除具有相似于三七皂甙的药理、药效及临床疗效外，血竭中所含数十种黄酮成分，显示出抗氧自由基，降低高脂血症，抗菌消炎、促进创面和骨折愈合等效用，更有其突出之处。
目前有较多文献报道采用三七总皂甙、血竭与其它成份配伍制成的多种治疗心脑血管疾病的药物，配伍所成的药物当中，未发现三七总皂甙及血竭的显著的增效作用。
发明内容
本发明的目的旨在提供一种具有显著增效作用的复方活化血竭。
本发明所述的复方活化血竭，其有效药用成份由血竭包合物和三七总皂甙组成，血竭包合物的重量百分比为占复方中的20-80％，三七总皂甙的重量百分比为占复方中的80-20％。
本发明所述的血竭包合物为血竭的β-环糊精包合物，三七总皂甙为已有的。本发明的剂型主要为口服剂型，也可制成其他剂型。在本发明的组成中，还可以含有药用辅料，药用辅料的用量视剂型而定。
本发明所述的复方制剂，显著的疗效来源于血竭的包合及二组份的协同增效。
本发明的药效学试验采用ADP静注所致小鼠肺栓塞残废模型；电刺激所致大鼠颈动脉血栓形成模型；以及体内外AA、ADP、PAF诱导兔血小板聚集方法，证实复方活化血竭的保护作用。拆方分析显示β-环糊精包合血竭疗效较不包合血竭明显提高，复方活化血竭疗效最优，且呈量效关系，明显优于等剂量的不包合血竭或三七皂甙。提示血竭经包合并与三七皂甙配伍，可能提高生物利用度从而呈协同增效效应。
复方活化血竭显著抑制实验性高脂血症动物血清TC、LDL-C及TG水平升高，并显著增加HDL-C/TC比值，其降脂作用与阳性对照血脂康疗效相似，表明本发明有显著降脂和改善脂蛋白分布的良好作用，同时兼有升高SOD活性和降低血中MDA的作用。
本实验总的证实包合血竭与三七皂甙复方配伍，不仅较未包合血竭药效提高，亦较二者单一使用的效应更为提高，说明复方活化血竭的组方是合理的，两种传统活血化瘀通脉药物经现代制剂构成复方作为心脑血管缺血性疾病的防治新药具有药效学试验依据。
复方活化血竭胶囊小鼠经口MTD(最大而受量)为20g/kg体重，为临床推荐用量(约为0.054g/kg)的370倍；大鼠进行灌胃给药90天，停药恢复30天的长期毒性试验。分成空白对照，高、中、低四个组。结果显示：给药期及恢复期试验动物一般状况良好，脏器重量及脏器系数，血液学及血液生化学指标，病理组织学检查均未见与药物有关的异常改变。此外试验中期和末期凝血系统指标均未发生异常，显示本发明安全性好。
本发明有活血化瘀，通络止痛功能。主要用于胸痹心痛(冠心病心绞痛)，能够有效治疗和预防冠心病、高血压病、高血脂症等心脑血管疾病。
复方活化血竭进行拆方药效学研究证明较等剂量的包合血竭或等剂量三七皂甙效价大为提高，产生协同增效作用。急毒和长毒研究显示本发明安全，且无出血的危险性。本发明可能成为防治心脑缺血性疾病的一种高效、低毒新药；亦可能在妇科炎症肿块、消化道出血、溃疡、皮肤口腔疮疡，抑或糖尿病并发症和脉管炎等方面得到扩展应用。
具体实施方式
实施例1：
取血竭β-环糊精包合物1500克，三七总皂甙1500克，加适量赋形剂混匀，填装制成胶囊10000粒。
实施例2：
取血竭β-环糊精包合物2000克，三七总皂甙1000克，赋形剂适量，混匀制成软质颗粒，干燥，压片，制成10000片口服药片。

Claims (1)

1、一种复方活化血竭制剂，其特征在于其有效药用成份由血竭β-环糊精包合物和三七总皂甙组成，血竭β-环糊精包合物的重量百分比为占制剂中的20-80％，三七总皂甙的重量百分比为占制剂中的80-20％。
CN02142360.1A 2002-09-19 2002-09-19 复方活化血竭 Expired - Lifetime CN1212135C (zh)

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CN1212135C true CN1212135C (zh) 2005-07-27

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