CN106474124B - 一种抑制菌丝和杀灭白念珠菌的药物 - Google Patents
一种抑制菌丝和杀灭白念珠菌的药物 Download PDFInfo
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Abstract
本发明提供了一种含有氧化苦参碱的药物组合物在抑制菌丝和杀灭白念珠菌方面的用途。本发明还提供了一种药物组合物，其中包括氧化苦参碱和赖氨酸，二者的质量比例为12:1。
Description
技术领域
本发明涉及医药化学领域，具体地，涉及含有氧化苦参碱的药物组合物在抑制菌丝和杀灭白念珠菌方面的用途。
背景技术
氧化苦参碱是从从豆科属植物苦参(Sophora flavescens Ait.)或平科植物广豆根(Sophora subprostrata Chun et T.Chen)中分离出来的生物碱，也可以通过化学合成法制得，分子式为C15H24N2O2。氧化苦参碱是苦参的主要药理活性成分之一，具有清热解毒、利尿祛风的功效。有研究发现氧化苦参碱对肺癌、胃癌细胞诱导的血管内皮细胞增殖具有抑制作用。截至申请日为止，还未有氧化苦参碱用于抑制菌丝和杀灭白念珠菌方面的报道。
赖氨酸是人体必需氨基酸之一，能促进人体发育、增强免疫功能，并有提高中枢神经组织功能的作用。
本申请发明人意外发现氧化苦参碱具有很好的抑制菌丝和杀灭白念珠菌的活性，特别是以特定比例和赖氨酸组合使用时具有协同抗白念珠菌活性。
发明概述
本发明的一个方面，提供了一种药物，其中包括氧化苦参碱。
本发明的另一个方面，提供了一种药物组合物，其中包括氧化苦参碱和赖氨酸。
更进一步地，本发明提供了一种药物组合物，其中包括氧化苦参碱和赖氨酸，二者的质量比例为12:1。
本发明的另一个方面，提供了氧化苦参碱在制备抗菌药物中的用途。
本发明的另一个方面，提供了氧化苦参碱和赖氨酸的药物组合物在制备抗菌药物中的用途。
本发明的另一个方面，提供了氧化苦参碱和赖氨酸的药物组合物在制备抗菌药物中的用途，二者的质量比例为12:1。
本发明的另一个方面，所述细菌包括大肠埃希菌、金黄色葡萄球菌和白念珠菌。
本发明的另一个方面，所述细菌是白念珠菌。
本发明的另一个方面，接受治疗的患者包括哺乳动物和鸟类。优选地，是哺乳动物。更优选地，是人。
本发明所述药物可以是本领域已知的任何药剂形式，包括但不限于片剂、胶囊、滴丸、注射液、冻干粉针、汤剂、缓释制剂、散剂、颗粒剂、栓剂、气雾剂等。
本发明制备药物制剂采用本领域已知的药物辅料，包括粘合剂、填充剂、润滑剂、稀释剂、溶剂、缓释材料等。包括但不限于淀粉、糊精、乳糖、甘露醇、微晶纤维素、羟丙甲纤维素、聚维酮、交联羧甲基纤维素钠、滑石粉、硬脂酸、泊洛沙姆、乙基纤维素、丙烯酸树脂等。
本发明的药物可以通过局部给药和系统性给药进行施用。局限性给药包括局部给药。系统性给药包括口服，胃肠外的(例如静脉内的，肌肉内的，皮下的或直肠的)，以及其他系统性给药途径。在系统性给药中，该活性化合物首先到达血浆，然后分布入靶组织中。局部给药和口服给药是优选的用于本发明的给药途径。
以下实施例进一步阐述本发明。这些实施例仅仅意在说明本发明，而不应被理解为限制性。
具体实施方式
实施例1：
取氧化苦参碱120g，加入淀粉细粉150g，用等量递增法混匀，用80％的乙醇，制成颗粒，干燥，整粒，混匀，加入滑石粉5g，硬脂酸镁3g，压片即得(1000片)。
实施例2：
取氧化苦参碱120g，赖氨酸10g，加入淀粉细粉150g，用等量递增法混匀，用80％的乙醇，制成颗粒，干燥，整粒，混匀，加入滑石粉5g，硬脂酸镁3g，压片即得(1000片)。
实施例3：
取氧化苦参碱150g，加入淀粉细粉200g，滑石粉10g，硬脂酸镁5g，制成颗粒，干燥，装入胶囊(1000粒)。
实施例4：
取氧化苦参碱120g，赖氨酸10g，微晶纤维素200g，交联聚乙烯吡咯烷酮60g，混匀，加入适量乙醇制粒，干燥，整粒，在加入羧甲基淀粉钠8g，硬脂酸镁4g，混匀，压片(1000片)。
实施例5：抗菌效果试验
以大肠埃希菌、金黄色葡萄球菌、白念珠菌为试验菌，采用浊度法，考察活性剂的抑菌效果。
菌悬液的制备：大肠埃希菌、金黄色葡萄球菌分别在无菌条件下接种至10ml营养肉汤培养基中，35℃，培养24h。菌悬液用无菌生理盐水稀释，使菌液浓度达106cfu/ml。白念珠菌在无菌条件下接种至10ml改良马丁液体培养基中，25℃，培养48h。菌悬液用无菌生理盐水稀释，使菌液浓度达106cfu/ml。
供试液的配制：分别称取对羟基苯甲酸酯0.2g和称(量)取对羟基苯甲酸酯0.2g、苯乙醇5ml，溶于100ml营养肉汤培养基中，供大肠埃希菌、金黄色葡萄球菌测试用。分别称取对羟基苯甲酸酯0.2g和称(量)取对羟基苯甲酸酯0.2g、苯乙醇5ml，溶于100ml改良马丁液体培养基中，供白念珠菌试用。取10ml供试液至试管中，高压灭菌。每个测试菌设3管供试液(氧化苦参碱组、赖氨酸组、氧化苦参碱和赖氨酸的组合物组(12:1质量比))，并设3组对照管(空白药物，氧化苦参碱和赖氨酸的组合物组(5:1质量比)，氧化苦参碱和赖氨酸的组合物组(1:12质量比))。无菌条件下，每支试管添加菌悬液0.2ml。大肠埃希菌、金黄色葡萄球菌35℃，培养24h，白念珠菌25℃，培养48h。
按照《中国药典2010年版二部》附录规定的抑菌剂效力检查法指导原则，对本发明供试液进行抑菌效力验证试验。
实验结果如下：
表1大肠埃希菌组抑菌效力试验菌数下降lg值
表2金黄色葡萄球菌组抑菌效力试验菌数下降lg值
表3白念珠菌组抑菌效力试验菌数下降lg值
表1-3数据表明，(1)氧化苦参碱对于大肠埃希菌、金黄色葡萄球菌和白念珠菌均具有抑制作用，特别是对于白念珠菌的抑制作用很强。
(2)赖氨酸单独使用时，并没有表现出抗菌活性。
(3)当氧化苦参碱和赖氨酸以12:1的质量比组合时，表现出协同抗菌活性，特别是对于白念珠菌的抑制作用很强。
(4)当氧化苦参碱和赖氨酸以5:1和1:12的质量比组合时，虽然具有抗菌作用，但抗菌活性还不如单独使用氧化苦参碱。
数据分析：对以上数据进行分析可以得出如下结论：氧化苦参碱具有抗大肠埃希菌、金黄色葡萄球菌和白念珠菌活性，特别是具有很强的抗白念珠菌活性。当氧化苦参碱和赖氨酸以特定比例(12:1的质量比)组合时，表现出协同抗菌活性，但其他重量比例的氧化苦参碱和赖氨酸的组合物则会降低氧化苦参碱的抗菌活性。
Claims (3)
1.一种药物组合物，其中包括氧化苦参碱和赖氨酸，氧化苦参碱和赖氨酸的质量比例为12:1，所述药物组合物是片剂、胶囊、滴丸或注射液。
2.如权利要求1所述的药物组合物在制备抗菌药物中的用途。
3.如权利要求2所述的用途，其中所述菌包括白念珠菌、大肠埃希菌和金黄色葡萄球菌。
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