CN104138382A - 一种含盐酸左氧氟沙星的组合物 - Google Patents

一种含盐酸左氧氟沙星的组合物 Download PDF

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CN104138382A
CN104138382A CN201410400713.7A CN201410400713A CN104138382A CN 104138382 A CN104138382 A CN 104138382A CN 201410400713 A CN201410400713 A CN 201410400713A CN 104138382 A CN104138382 A CN 104138382A
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levofloxacin hydrochloride
levofloxacin
hydrochloride
telmisartan
parts
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CN104138382B (zh
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李捍雄
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Euphorbia Biological Medicine Co ltd
Guangdong Zerui Pharmaceutical Co ltd
Guangzhou Lianrui Pharmaceutical Co ltd
Guangzhou Runlin Pharmaceutical Technology Co ltd
GUANGZHOU YIPINHONG PHARMACEUTICAL CO Ltd
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Abstract

本发明公开了一种含盐酸左氧氟沙星的组合物,由如下重量份的组分组成:盐酸左氧氟沙星1-3,替米沙坦1-3。鉴于盐酸左氧氟沙星对厌氧菌的抑制效果不好,在某些场合的抗菌应用受到限制,本发明经过大量实验,在盐酸左氧氟沙星中按照限定比例添加替米沙坦与其混配,制得的药物组合物除了保持盐酸左氧氟沙星原有的广谱抗菌性之后,对厌氧菌也具有良好的抑制效果,从而拓宽了盐酸左氧氟沙星的应用范围。

Description

一种含盐酸左氧氟沙星的组合物
技术领域
本发明涉及一种含盐酸左氧氟沙星的组合物。
背景技术
盐酸左氧氟沙星,中文别名:左氧氟沙星盐酸盐;(3S)-(-)-9-氟-2,3-二氢-3-甲基-10-(4-甲基-1-哌嗪基)-7-氧-;7H-吡啶并[1,2,3-de]-[1,4]苯并恶嗪-6-羧酸盐酸盐;左氟沙星·盐酸盐;英文名称:LevofloxacinHydrochloride。盐酸左氧氟沙星适用于敏感菌引起的泌尿生殖系统感染,包括单纯性、复杂性尿路感染、细菌性前列腺炎、淋病奈瑟菌尿道炎或宫颈炎(包括产酶株所致者)。呼吸道感染,包括敏感革兰阴性杆菌所致支气管感染急性发作及肺部感染。胃肠道感染,由志贺菌属、沙门菌属、产肠毒素大肠杆菌、亲水气单胞菌、副溶血弧菌等所致。另可治疗伤寒,骨和关节感染,皮肤软组织感染和败血症等全身感染。
盐酸左氧氟沙星具有抗菌谱广、抗菌作用强的特点。对大多数肠杆菌科细菌,如大肠埃希菌、克雷白菌属、沙雷菌属、变形杆菌属、志贺菌属、沙门菌属、枸橼酸杆菌、不动杆菌属以及铜绿假单胞菌、流感嗜血杆菌、淋球菌等革兰阴性细菌有较强的抗菌活性。对部分甲氧西林敏感葡萄球菌、肺炎链球菌、化脓性链球菌、溶血性链球菌等革兰阳性菌和军团菌、支原体、衣原体也有良好的抗菌作用,但对厌氧菌和肠球菌的作用较差。
发明内容
本发明的目的是克服现有技术的不足,提供一种能抗厌氧菌的含盐酸左氧氟沙星的药物组合物。
为了实现上述目的,本发明采用如下技术方案:
一种含盐酸左氧氟沙星的组合物,由如下重量份的组分组成:
盐酸左氧氟沙星  1-3
替米沙坦        1-3。
其优选的重量份数为:
盐酸左氧氟沙星  2
替米沙坦        1。
与现有技术相比,本发明具有如下有益效果:鉴于盐酸左氧氟沙星对厌氧菌的抑制效果不好,在某些场合的抗菌应用受到限制,本发明经过大量实验,在盐酸左氧氟沙星中按照限定比例添加替米沙坦与其混配,制得的药物组合物除了保持盐酸左氧氟沙星原有的广谱抗菌性之后,对厌氧菌也具有良好的抑制效果,从而拓宽了盐酸左氧氟沙星的应用范围。
具体实施方式
实施例1:
将盐酸左氧氟沙星和替米沙坦按2:1的重量比混合,制得药物组合物。
实施例2:
将盐酸左氧氟沙星和替米沙坦按1:1的重量比混合,制得药物组合物。
实施例3:抗菌实验
测定方法如下:
1)受试药物用DMSO溶解后,配置成800μg/ml母液备用。
2)试验方法:采用MB培养基于96孔板用二倍稀释法测定药物对受试菌株的最低抑菌浓度(MIC)。梯度稀释使平行各孔浓度为:128、64、32、16、8、4、2、1、0.5、0.25、0.125、0.0625(μg/ml);置于37℃培养箱培养24小时,用(MULTISKAN EX)酶标仪扫描试验后的96孔板,在紫外吸收显示无菌生长的孔内,取其中药物浓度最低者为受试药品对受试细菌的最低抑菌浓度(MIC)。
3)阳性对照组为万古霉素。
4)实验菌株:E.coli为大肠埃希菌ATCC25922;SA为金黄色葡萄球菌(staphylococcus aureus)ATCC25923;MRSA1为耐甲氧苯青霉素金黄色葡萄球菌(methicillin-resistant staphylococcus aureus)临床分离亚种;SE为表皮葡萄球菌(staphylococcus epidermidis)ATCC12228;CP为产气荚膜梭菌(C.perfringens);BF为脆弱拟杆菌(b.fragilis)。
最低抑菌浓度(MIC)值见表1。
表1.目标化合物的最低抑菌浓度(MIC)(单位为μg/ml)
受试药物 E.coli SA MRSA1 CP SE BF
实施例1 4 8 8 4 16 4
实施例2 4 8 8 4 16 4
盐酸左氧氟沙星 2 8 8 128 16 128
万古霉素 >128 1 0.5 2 2 2
由表1数据可以得出盐酸左氧氟沙星对产气荚膜梭菌和脆弱拟杆菌这两个厌氧菌的抑制效果不好,而实施例1和2对产气荚膜梭菌和脆弱拟杆菌这两个厌氧菌的抑制效果不错,并且对其他菌种的抑制效果也不错。

Claims (2)

1.一种含盐酸左氧氟沙星的组合物,其特征在于由如下重量份的组分组成:
盐酸左氧氟沙星  1-3
替米沙坦        1-3。
2.如权利要求1所述的组合物,其特征在于,由如下重量份的组分组成:
盐酸左氧氟沙星  2
替米沙坦        1。
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Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1561200A (zh) * 2001-10-09 2005-01-05 布里斯托尔·迈尔斯斯奎布公司 快速熔融口服剂型
CN102961381A (zh) * 2012-12-13 2013-03-13 鼎正动物药业(天津)有限公司 一种左氧氟沙星复合制剂及其制备方法
CN103070862A (zh) * 2011-10-25 2013-05-01 新疆华世丹药物研究有限责任公司 去氢骆驼蓬碱衍生物在制备抗菌药物中的应用
CN103156826A (zh) * 2012-03-16 2013-06-19 成都华神集团股份有限公司 百秋李醇的新用途

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1561200A (zh) * 2001-10-09 2005-01-05 布里斯托尔·迈尔斯斯奎布公司 快速熔融口服剂型
CN103070862A (zh) * 2011-10-25 2013-05-01 新疆华世丹药物研究有限责任公司 去氢骆驼蓬碱衍生物在制备抗菌药物中的应用
CN103156826A (zh) * 2012-03-16 2013-06-19 成都华神集团股份有限公司 百秋李醇的新用途
CN102961381A (zh) * 2012-12-13 2013-03-13 鼎正动物药业(天津)有限公司 一种左氧氟沙星复合制剂及其制备方法

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