CN105748477A - 一种治疗小儿肠炎的药物 - Google Patents
一种治疗小儿肠炎的药物 Download PDFInfo
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- CN105748477A CN105748477A CN201610216624.6A CN201610216624A CN105748477A CN 105748477 A CN105748477 A CN 105748477A CN 201610216624 A CN201610216624 A CN 201610216624A CN 105748477 A CN105748477 A CN 105748477A
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- 208000004232 Enteritis Diseases 0.000 title claims abstract description 20
- 239000003814 drug Substances 0.000 title claims description 8
- 229940079593 drug Drugs 0.000 title description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 18
- 150000001875 compounds Chemical class 0.000 claims abstract description 16
- 239000003937 drug carrier Substances 0.000 claims abstract description 6
- 241000588724 Escherichia coli Species 0.000 claims description 9
- 239000003085 diluting agent Substances 0.000 claims description 7
- 239000003795 chemical substances by application Substances 0.000 claims description 5
- 230000005764 inhibitory process Effects 0.000 claims description 4
- GUBGYTABKSRVRQ-QKKXKWKRSA-N lactose group Chemical group OC1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O)[C@H](O2)CO)[C@H](O1)CO GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 4
- 239000011230 binding agent Substances 0.000 claims description 3
- 239000000314 lubricant Substances 0.000 claims description 3
- 238000002360 preparation method Methods 0.000 claims description 3
- 239000003381 stabilizer Substances 0.000 claims description 3
- 229920000881 Modified starch Polymers 0.000 claims description 2
- 239000002775 capsule Substances 0.000 claims description 2
- 239000001913 cellulose Substances 0.000 claims description 2
- 229920002678 cellulose Polymers 0.000 claims description 2
- 239000008187 granular material Substances 0.000 claims description 2
- 239000008101 lactose Substances 0.000 claims description 2
- 239000004531 microgranule Substances 0.000 claims description 2
- 235000019426 modified starch Nutrition 0.000 claims description 2
- 239000000843 powder Substances 0.000 claims description 2
- 239000003826 tablet Substances 0.000 claims description 2
- 244000052616 bacterial pathogen Species 0.000 abstract description 3
- 230000000694 effects Effects 0.000 abstract description 3
- 230000000844 anti-bacterial effect Effects 0.000 description 4
- 229920001817 Agar Polymers 0.000 description 3
- 241000894006 Bacteria Species 0.000 description 3
- 239000008272 agar Substances 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- 230000003385 bacteriostatic effect Effects 0.000 description 2
- 235000016709 nutrition Nutrition 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- 230000002335 preservative effect Effects 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 208000035143 Bacterial infection Diseases 0.000 description 1
- NQRYJNQNLNOLGT-UHFFFAOYSA-N C1CCNCC1 Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 1
- 241000589875 Campylobacter jejuni Species 0.000 description 1
- 206010010071 Coma Diseases 0.000 description 1
- 241000709687 Coxsackievirus Species 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 241000702670 Rotavirus Species 0.000 description 1
- 241000607142 Salmonella Species 0.000 description 1
- 241000191967 Staphylococcus aureus Species 0.000 description 1
- 241000700605 Viruses Species 0.000 description 1
- 206010048222 Xerosis Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000000843 anti-fungal effect Effects 0.000 description 1
- 229940121375 antifungal agent Drugs 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- 230000004071 biological effect Effects 0.000 description 1
- 230000031018 biological processes and functions Effects 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 239000012050 conventional carrier Substances 0.000 description 1
- -1 correctives Substances 0.000 description 1
- 239000012531 culture fluid Substances 0.000 description 1
- 230000013872 defecation Effects 0.000 description 1
- 230000018044 dehydration Effects 0.000 description 1
- 238000006297 dehydration reaction Methods 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 208000001848 dysentery Diseases 0.000 description 1
- 201000006549 dyspepsia Diseases 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 206010016766 flatulence Diseases 0.000 description 1
- 238000011534 incubation Methods 0.000 description 1
- 238000011081 inoculation Methods 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
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- 239000002609 medium Substances 0.000 description 1
- 239000012982 microporous membrane Substances 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
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- 241000701161 unidentified adenovirus Species 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 239000003643 water by type Substances 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4453—Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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Abstract
本发明涉及一种治疗小儿肠炎的药物组合物，所述药物组合物包含有效量的化合物和药学上可接受的载体，所述化合物具有下列结构：
Description
技术领域
本发明涉及医药领域，具体的说，本发明涉及一种治疗小儿肠炎的药物。
背景技术
小儿肠炎大部分是由于感染细菌或病毒而引起的，如轮状病毒、腺病毒、柯萨奇病毒等，不过，病毒性肠炎的症状一般比较轻微。由细菌引发的肠炎则症状较重，其中，常见细菌有空肠弯曲菌、沙门氏菌、痢疾杆菌、致病性大肠杆菌、金黄色葡萄球菌等；也可因外感风寒或湿热引起，轻度小儿肠炎表现为大便次数增多，中度小儿肠炎表现为每天大便超过10次，呈蛋花羹样或水样，有脱水现象，消化不良，胃胀，重度小儿肠炎表现为大便喷射而出，重度脱水，皮肤干燥，呼吸不适，虚脱，营养元素缺乏，甚至昏迷。小儿肠炎多由各种致病菌引起，近期发现大肠埃希菌ATCC35218是其中重要的致病菌之一。
发明内容
本发明的目的在于提供一种治疗小儿肠炎的药物组合物。
为了实现本发明的目的，本发明提供一种治疗小儿肠炎的药物组合物，所述药物组合物包含有效量的化合物和药学上可接受的载体，所述化合物具有下列结构：
优选地，所述药学上可接受的载体为稀释剂、崩解剂、粘合剂、润滑剂、稳定剂或矫正剂。
优选地，所述稀释剂为糖衍生物、淀粉衍生物或纤维素衍生物。
优选地，所述稀释剂为乳糖。
优选地，所述药物组合物为散剂、微粒剂、颗粒剂、胶囊剂或片剂。
本发明还提供化合物在制备体外抑制大肠埃希菌ATCC35218的药物中的用途，该化合物具有下列结构：
本文所用的术语“药学上可接受的”指不消除本文所述的化合物的生物学活性或性质的物质，如载体或稀释剂。这类物质被施用于个体不导致不希望的生物学作用或者不以有害方式与包含它的组合物中的任何组分相互作用。
如本文所用的术语“药学上可接受的载体”包括任何和所有的溶剂、分散介质、包衣材料、表面活性剂、抗氧化剂、防腐剂(例如抗菌剂、抗真菌剂)、等渗剂、吸收延迟剂、盐、防腐剂、药物稳定剂、粘合剂、赋形剂、崩解剂、润滑剂、甜味剂、矫味剂、染料等和其组合，这是本领域技术人员所熟知的(例如参见Remington'sPharmaceuticalSciences,18thEd.MackPrintingCompany,1990,pp.1289-1329)。除了与活性成分不相容的载体外，在治疗或药物组合物中考虑使用任何常规载体。
本发明的药物组合物对于引起小儿肠炎的病原菌效果显著，可以开发成临床上有效的新的药物组合物。
具体实施方式
以下通过具体实施方式的描述对本发明作进一步说明，但这并非是对本发明的限制，本领域技术人员根据本发明的基本思想，可以做出各种修改或改进，但是只要不脱离本发明的基本思想，均在本发明的范围之内。
实验例本发明化合物在制备体外抑制大肠埃希菌ATCC35218的药物中的用途的研究
抑菌试验
使用下列化合物，采用本领域中经典的滤纸片法来进行抑菌试验，其中：
目标化合物的结构式为：
供试菌种大肠埃希菌ATCC35218购自上海坤肯生物化工有限公司。
培养液
营养琼脂和营养肉汤，购自北京中科晨宇实验设备有限公司。
试验方法
将大肠埃希菌ATCC35218接种于琼脂平板营养液平面上，接种时均匀密布。
称取目标化合物0.01克，加入20000毫升无菌水，超声30分钟，然后0.22μm的微孔滤膜过滤，得到溶液。镊取无菌圆形滤纸片，喷洒上述溶液至完全润湿，贴在已接种细菌的琼脂平板营养液平面上。将琼脂平板置于37℃的培养箱内，温育18小时。测量抑菌环的直径。测定3次取平均值。
1.4结果
大肠埃希菌ATCC35218的抑菌环的平均直径为13.88mm，这表明目标化合物具有极强的体外抑制大肠埃希菌ATCC35218的效果。
Claims (6)
1.一种治疗小儿肠炎的药物组合物，其特征在于，所述药物组合物包含有效量的化合物和药学上可接受的载体，所述化合物具有下列结构：
2.根据权利要求1所述的治疗小儿肠炎的药物组合物，其特征在于，所述药学上可接受的载体为稀释剂、崩解剂、粘合剂、润滑剂、稳定剂或矫正剂。
3.根据权利要求2所述的治疗小儿肠炎的药物组合物，其特征在于，所述稀释剂为糖衍生物、淀粉衍生物或纤维素衍生物。
4.根据权利要求3所述的治疗小儿肠炎的药物组合物，其特征在于，所述稀释剂为乳糖。
5.根据权利要求2所述的治疗小儿肠炎的药物组合物，其特征在于，所述药物组合物为散剂、微粒剂、颗粒剂、胶囊剂或片剂。
6.化合物在制备体外抑制大肠埃希菌ATCC35218的药物中的用途，其特征在于，该化合物具有下列结构：
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2016
- 2016-04-08 CN CN201610216624.6A patent/CN105748477B/zh active Active
Non-Patent Citations (1)
| Title |
|---|
| MU,LI-HUA: "synthesis and inhitibory effect of piperine derivates on monoamine oxidase,bioorganic and medicinal chemistry letters", 《BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS》 * |
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