CN108524509A - 一种治疗高血压的药物组合物 - Google Patents
一种治疗高血压的药物组合物 Download PDFInfo
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- 206010020772 Hypertension Diseases 0.000 title claims abstract description 27
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 12
- 150000001875 compounds Chemical class 0.000 claims abstract description 11
- 239000003814 drug Substances 0.000 claims abstract description 8
- 229940079593 drug Drugs 0.000 claims abstract description 5
- 239000003937 drug carrier Substances 0.000 claims abstract description 3
- 150000003839 salts Chemical class 0.000 claims abstract description 3
- 239000002552 dosage form Substances 0.000 claims description 2
- 230000036772 blood pressure Effects 0.000 abstract description 8
- 239000008280 blood Substances 0.000 abstract description 5
- 210000004369 blood Anatomy 0.000 abstract description 5
- 230000001631 hypertensive effect Effects 0.000 abstract description 5
- 208000024891 symptom Diseases 0.000 abstract description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract description 3
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- IAZDPXIOMUYVGZ-WFGJKAKNSA-N Dimethyl sulfoxide Chemical compound [2H]C([2H])([2H])S(=O)C([2H])([2H])[2H] IAZDPXIOMUYVGZ-WFGJKAKNSA-N 0.000 description 2
- 241001398042 Serica Species 0.000 description 2
- 210000004204 blood vessel Anatomy 0.000 description 2
- FAKRSMQSSFJEIM-RQJHMYQMSA-N captopril Chemical compound SC[C@@H](C)C(=O)N1CCC[C@H]1C(O)=O FAKRSMQSSFJEIM-RQJHMYQMSA-N 0.000 description 2
- 229960000830 captopril Drugs 0.000 description 2
- 239000007928 intraperitoneal injection Substances 0.000 description 2
- 210000003734 kidney Anatomy 0.000 description 2
- 238000005160 1H NMR spectroscopy Methods 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 208000031481 Pathologic Constriction Diseases 0.000 description 1
- 229930182555 Penicillin Natural products 0.000 description 1
- JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 description 1
- 206010038378 Renal artery stenosis Diseases 0.000 description 1
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- 230000002924 anti-infective effect Effects 0.000 description 1
- 239000002220 antihypertensive agent Substances 0.000 description 1
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- 210000003017 ductus arteriosus Anatomy 0.000 description 1
- NPUKDXXFDDZOKR-LLVKDONJSA-N etomidate Chemical compound CCOC(=O)C1=CN=CN1[C@H](C)C1=CC=CC=C1 NPUKDXXFDDZOKR-LLVKDONJSA-N 0.000 description 1
- 229960001690 etomidate Drugs 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
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- 230000036541 health Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 229940049954 penicillin Drugs 0.000 description 1
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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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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Abstract
本发明涉及一种治疗高血压的药物组合物，所述药物组合物包含下式的化合物或其药学上可接受的盐、和药学上可以接受的载体：
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高血压的药物组合物。
背景技术
高血压人群已日益成为现代都市人的一大健康杀手，不能不引起我们重视。高血压病主要损害人体血。它能促使动脉管壁变硬，管腔变狭——即平时所说的“动脉硬化，高血压病若合并糖尿病则会加速、加重血管损，使病情迅速恶化，应该积极治疗。随着现代医学的不断发展，高血压治疗的理念也在不断的发展变化，对于高血压的治疗不仅仅局限在降压治疗上，有效的预防和治疗高血压引起的一系列并发症是高血压治疗更为重要的方面。现在对高血压的治疗，提高患者的长期生存率是更为重要的内容，否则的话，血压降低了，而高血压患者的生存率不能提高甚至会降低患者的生存率，这也就使得降压治疗失去了最根本的意义。可以说，在现有的降压药物中，还没有符合现在高血压治疗理念十分理想的药物问世。
发明内容
本发明的目的在于提供一种治疗高血压的药物组合物。
为了实现本发明的目的，本发明提供一种治疗高血压的药物组合物，所述药物组合物包含下式的化合物或其药学上可接受的盐、和药学上可以接受的载体：
优选地，所述药物组合物可以制成各种药学上可接受的剂型。
本发明还提供化合物在制备治疗高血压的药物中的用途，所述化合物具有下列结构：
本发明所述的药物可以用于治疗或者减轻高血压症状及相关症状、障碍和疾病，适用于多种类型的高血压患者，能够高效、安全的调节血压，缓慢释放维持较为平稳的血药浓度和更长的作用时间，具有毒副作用减小、服用更加方便的优点。
具体实施方式
本领域技术人员将理解的是，上述说明书中所公开的概念和具体实施方式可易于用作修改或设计实施本发明相同目的的其它实施方式的基础。本领域技术人员也将理解的是，这些等同的实施方式没有脱离所附权利要求书中阐明的本发明的精神和范围。
实验例1本发明化合物的表征
1H NMR(400MHz,DMSO-d6)δ1.82-2.10(7H,m),2.18(6H,s),2.35-2.50(2H,m),3.0-3.1(2H,m),3.31-3.39(2H,m),3.35(3H,s),3.61-3.74(2H,m),4.36(2H,t),6.99(1H,d),7.97(1H,d),8.01(1H,dt),8.39(1H,d),8.45(1H,d),8.97(1H,s)。
实验例2本发明化合物对于高血压的治疗效果
取SPF级SD大鼠40只，雌雄各半，随机留取10只大鼠(雌雄各半)作为正常对照组，其余30只大鼠作为造模组。造模组大鼠以10％的水合氯醛(0.4ml/100g)腹腔注射麻醉后的大鼠仰卧固定于手术台上，剪去腹部体毛，5％碘伏消毒，75％酒精脱碘，盖上孔巾。沿腹正中线作手术切口打开腹腔，按无菌操作，小心钝性分离出左肾动脉，穿入无菌丝线，把直径为0.25mm的针灸针与肾动脉血管长轴紧贴平行放置，用无菌丝线扎紧肾动脉和针灸针后抽出针灸针，结果造成单侧肾动脉狭窄，对侧肾脏和动脉不触及。正常对照组大鼠除不结扎肾动脉外，其余手术操作均同上，作为假手术组。术后连续3d腹腔注射青霉素(3×104U/d)预防感染。各组动物均正常饲养。
造模10w后取造模大鼠30只，Etomidate 100mg·kg-1腹腔注射麻醉，BP-100A全自动大鼠无创血压测量系统尾套法测量各造模大鼠血压，作为给药前高血压模型大鼠血压数值。按血压数值均分为3组，分别为模型对照组、卡托普利片组、目标化合物组，每组10只，雌雄各半。同法麻醉正常对照组(假手术组)大鼠尾套法测量其血压，作为给药前正常大鼠血压数值。
分组后各给药组按剂量灌胃给药，卡托普利片0.003g·kg-1，目标化合物0.003g·kg-1。假手术组、模型对照组同法灌胃给予等体积蒸馏水。每天1次，连续4w。结果见下表。
Claims (3)
1.一种治疗高血压的药物组合物，其特征在于，所述药物组合物包含下式的化合物或其药学上可接受的盐、和药学上可以接受的载体：
2.根据权利要求1所述的治疗高血压的药物组合物，其特征在于，所述药物组合物可以制成各种药学上可接受的剂型。
3.化合物在制备治疗高血压的药物中的用途，其特征在于，所述化合物具有下列结构：
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| CN201710125903.6A CN108524509A (zh) | 2017-03-05 | 2017-03-05 | 一种治疗高血压的药物组合物 |
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| CN108524509A true CN108524509A (zh) | 2018-09-14 |
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Application publication date: 20180914 |
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