CN105481844A - Pharmaceutical composition for the treatment of hypertension - Google Patents
Pharmaceutical composition for the treatment of hypertension Download PDFInfo
- Publication number
- CN105481844A CN105481844A CN201510893564.7A CN201510893564A CN105481844A CN 105481844 A CN105481844 A CN 105481844A CN 201510893564 A CN201510893564 A CN 201510893564A CN 105481844 A CN105481844 A CN 105481844A
- Authority
- CN
- China
- Prior art keywords
- pharmaceutical composition
- compound
- treatment
- hypertensive
- hypertension
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 206010020772 Hypertension Diseases 0.000 title claims abstract description 21
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 19
- 150000001875 compounds Chemical class 0.000 claims abstract description 19
- 239000003937 drug carrier Substances 0.000 claims abstract description 6
- 230000001631 hypertensive effect Effects 0.000 claims description 14
- 239000003795 chemical substances by application Substances 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 5
- 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
- -1 microgranules Substances 0.000 claims description 4
- 239000003826 tablet Substances 0.000 claims description 4
- 239000000314 lubricant 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
- 239000005555 hypertensive agent Substances 0.000 claims description 2
- 239000008101 lactose Substances 0.000 claims description 2
- 235000019426 modified starch Nutrition 0.000 claims description 2
- 239000000843 powder Substances 0.000 claims description 2
- 238000002360 preparation method Methods 0.000 claims description 2
- 230000002892 effect on hypertension Effects 0.000 abstract 1
- 241000700159 Rattus Species 0.000 description 16
- 230000036772 blood pressure Effects 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- 210000002254 renal artery Anatomy 0.000 description 4
- 206010002091 Anaesthesia Diseases 0.000 description 3
- 238000001467 acupuncture Methods 0.000 description 3
- 230000037005 anaesthesia Effects 0.000 description 3
- FAKRSMQSSFJEIM-RQJHMYQMSA-N captopril Chemical compound SC[C@@H](C)C(=O)N1CCC[C@H]1C(O)=O FAKRSMQSSFJEIM-RQJHMYQMSA-N 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- 241000189617 Chorda Species 0.000 description 2
- 241001398042 Serica Species 0.000 description 2
- 210000001015 abdomen Anatomy 0.000 description 2
- 229960000830 captopril Drugs 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000007928 intraperitoneal injection Substances 0.000 description 2
- 206010008190 Cerebrovascular accident Diseases 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 206010020802 Hypertensive crisis Diseases 0.000 description 1
- 241001465754 Metazoa Species 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
- 208000006011 Stroke Diseases 0.000 description 1
- 206010042434 Sudden death Diseases 0.000 description 1
- 210000000683 abdominal cavity Anatomy 0.000 description 1
- 230000003187 abdominal effect Effects 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 239000003429 antifungal agent Substances 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
- 210000001367 artery Anatomy 0.000 description 1
- 230000004071 biological effect Effects 0.000 description 1
- 230000031018 biological processes and functions Effects 0.000 description 1
- 230000002490 cerebral effect Effects 0.000 description 1
- 208000026106 cerebrovascular disease Diseases 0.000 description 1
- RNFNDJAIBTYOQL-UHFFFAOYSA-N chloral hydrate Chemical compound OC(O)C(Cl)(Cl)Cl RNFNDJAIBTYOQL-UHFFFAOYSA-N 0.000 description 1
- 229960002327 chloral hydrate Drugs 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
- 208000029078 coronary artery disease Diseases 0.000 description 1
- 230000035487 diastolic blood pressure Effects 0.000 description 1
- 239000002612 dispersion medium Substances 0.000 description 1
- 239000012153 distilled water Substances 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 238000003304 gavage Methods 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 description 1
- 239000007951 isotonicity adjuster Substances 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 229940049954 penicillin Drugs 0.000 description 1
- 230000002980 postoperative effect Effects 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000035488 systolic blood pressure Effects 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention relates to a pharmaceutical composition for the treatment of hypertension. The pharmaceutical composition comprises an effective amount of a compound and a pharmaceutically acceptable carrier. The compound has a structure as below. The compound of the present invention has significant effect on hypertension, and can be developed into a clinically effective novel pharmaceutical composition.
Description
Technical field
The present invention relates to field of medicaments, specifically, the present invention relates to one and treat hypertensive pharmaceutical composition.
Background technology
Hypertension is a kind of common disease, frequently-occurring disease.Along with the raising of people's living standard, hyperpietic is increasing, and particularly hypertensive crisis, severe hypertension patient numbers are in continuous growth, and for this kind of illness, not only injectable drug is little safely but also effectively clinically.Hypertension affects work and life, and hypertension is again coronary heart disease, the most important Hazard Factor of cerebro-vascular diseases.In infraction, 50% is hyperpietic, and the people of cerebral apoplexy patient 76% has hypertension history.Therefore hypertensive danger is sudden death or disables.Hyperpietic will learn life and take good care of and early treatment, with the development of symptom management.
Summary of the invention
One is the object of the present invention is to provide to treat hypertensive pharmaceutical composition.
In order to realize object of the present invention, the invention provides one and treat hypertensive compound, this compound has having structure:
The present invention also provides one to treat hypertensive pharmaceutical composition, and described pharmaceutical composition includes the compound of effective amount and pharmaceutically acceptable carrier, and described compound has having structure:
Preferably, described pharmaceutically acceptable carrier is thinner, disintegrating agent, tackiness agent, lubricant, stablizer or corrigent.
Preferably, described thinner is sugar derivatives, starch derivative or derivatived cellulose.
Preferably, described thinner is lactose.
Preferably, described pharmaceutical composition is powder, microgranules, granule, capsule or tablet.
The present invention also provides the purposes of compound in the hypertensive medicine of preparation treatment, and this compound has having structure:
Term used herein " pharmaceutically acceptable " refers to not eliminate the biologic activity of compound as herein described or the material of character, as carrier or thinner.This kind of material is applied to and individual does not cause undesirable biological action or not with harmful way and any component interaction comprised in its composition.
" pharmaceutically acceptable carrier " comprises any and all solvents as the term is employed herein, dispersion medium, coating material, tensio-active agent, antioxidant, sanitas (such as antiseptic-germicide, anti-mycotic agent), isotonic agent, absorption delay agent, salt, sanitas, drug stabilizing agent, tackiness agent, vehicle, disintegrating agent, lubricant, sweeting agent, correctives, dyestuff etc. and its combination, this is well-known to those skilled in the art (for example, see Remington'sPharmaceuticalSciences, 18thEd.MackPrintingCompany, 1990, pp.1289-1329).Except with except the inconsistent carrier of activeconstituents, consider to use any conventional carrier in treatment or pharmaceutical composition.
Compound of the present invention, for hypertensive Be very effective, can be developed to pharmaceutical composition effectively new clinically.
Embodiment
Below by way of the description of embodiment, the invention will be further described, but this is not limitation of the present invention, those skilled in the art are according to basic thought of the present invention, various amendment or improvement can be made, but only otherwise depart from basic thought of the present invention, all within the scope of the present invention.
Experimental example
The structural formula of target compound is:
Get SPF level SD rat 40, male and female half and half, leave and take 10 rats (male and female half and half) at random as Normal group, all the other 30 rats are as modeling group.Modeling group rat lies on the back with the rat after Chloral Hydrate (0.4ml/100g) intraperitoneal injection of anesthesia of 10% and is fixed on operating table, and cut off belly chaeta, 5% iodophor disinfection, 75% alcohol takes off iodine, covers hole towel.Abdominal cavity is opened along the abdomen median line otch that operates, by aseptic technique, careful blunt separation goes out left renal artery, penetrate chorda serica chirurgicalis sterilis, be that the acupuncture needle of 0.25mm is close to parallel placement with Renal artery blood vessel major axis diameter, extract acupuncture needle out after tightening the Renal artery and acupuncture needle with chorda serica chirurgicalis sterilis, result causes unilateral renal artery stenosis, and offside kidney and artery do not touch.Rats in normal control group is except the not ligation Renal artery, and all the other operation techniques are all the same, as sham operated rats.Postoperative continuous 3d abdominal injection penicillin (3 × 10
4u/d) preventing infection.Each treated animal is all normally raised.
Modeling rat 30 is got, Etomidate100mgkg after modeling 10w
-1intraperitoneal injection of anesthesia, BP-100A full-automatic rat non-invasive blood pressure measuring system tail cover method measures each modeling rat blood pressure, as Hypertensive Rats blood pressure values before administration.Be divided into 3 groups by blood pressure values, be respectively model control group, Captopril tablets group, target compound group, often organize 10, male and female half and half.Its blood pressure is measured, as normal rat blood pressure values before administration with method anesthesia Normal group (sham operated rats) rat tail cover method.
Each administration group according to dosage gastric infusion after grouping, Captopril tablets 0.009gkg
-1, target compound 0.002gkg
-1.Sham operated rats, model control group give equal-volume distilled water with method gavage.Every day 1 time, continuous 4w.The results are shown in following table.
| Group | Systolic pressure (mmHg) | Diastolic pressure (mmHg) |
| Sham operated rats | 125.7±5.62 | 78.56±5.21 |
| Model group | 165.45±7.51 | 118.62±6.39 |
| Captopril group | 132.71±6.03 | 92.34±10.28 |
| Target compound group | 142.8±6.73 | 97.39±9.79 |
Claims (7)
1. treat a hypertensive compound, it is characterized in that, this compound has having structure:
2. treat a hypertensive pharmaceutical composition, it is characterized in that, described pharmaceutical composition includes the compound of effective amount and pharmaceutically acceptable carrier, and described compound has having structure:
3. the hypertensive pharmaceutical composition for the treatment of according to claim 2, is characterized in that, described pharmaceutically acceptable carrier is thinner, disintegrating agent, tackiness agent, lubricant, stablizer or corrigent.
4. the hypertensive pharmaceutical composition for the treatment of according to claim 3, is characterized in that, described thinner is sugar derivatives, starch derivative or derivatived cellulose.
5. the hypertensive pharmaceutical composition for the treatment of according to claim 4, is characterized in that, described thinner is lactose.
6. the hypertensive pharmaceutical composition for the treatment of according to claim 3, is characterized in that, described pharmaceutical composition is powder, microgranules, granule, capsule or tablet.
7. the purposes of compound in the hypertensive medicine of preparation treatment, it is characterized in that, this compound has having structure:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510893564.7A CN105481844A (en) | 2015-12-08 | 2015-12-08 | Pharmaceutical composition for the treatment of hypertension |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510893564.7A CN105481844A (en) | 2015-12-08 | 2015-12-08 | Pharmaceutical composition for the treatment of hypertension |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105481844A true CN105481844A (en) | 2016-04-13 |
Family
ID=55669163
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510893564.7A Pending CN105481844A (en) | 2015-12-08 | 2015-12-08 | Pharmaceutical composition for the treatment of hypertension |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105481844A (en) |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1308536A (en) * | 1998-07-06 | 2001-08-15 | 布里斯托尔-迈尔斯斯奎布公司 | Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists |
| WO2008156601A1 (en) * | 2007-06-14 | 2008-12-24 | Amgen Inc. | Tricyclic inhibitors of hydroxysteroid dehydrogenases |
| CN101619057A (en) * | 2002-06-24 | 2010-01-06 | 阿卡蒂亚药品公司 | N-substituted piperidine derivatives as serotonin receptor agents |
| US20100094000A1 (en) * | 2008-09-03 | 2010-04-15 | Takeda Pharmaceutical Company Limited | Pyrazole compounds |
| WO2011141848A1 (en) * | 2010-05-11 | 2011-11-17 | Pfizer Inc. | Morpholine compounds as mineralocorticoid receptor antagonists |
-
2015
- 2015-12-08 CN CN201510893564.7A patent/CN105481844A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1308536A (en) * | 1998-07-06 | 2001-08-15 | 布里斯托尔-迈尔斯斯奎布公司 | Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists |
| CN101619057A (en) * | 2002-06-24 | 2010-01-06 | 阿卡蒂亚药品公司 | N-substituted piperidine derivatives as serotonin receptor agents |
| WO2008156601A1 (en) * | 2007-06-14 | 2008-12-24 | Amgen Inc. | Tricyclic inhibitors of hydroxysteroid dehydrogenases |
| US20100094000A1 (en) * | 2008-09-03 | 2010-04-15 | Takeda Pharmaceutical Company Limited | Pyrazole compounds |
| WO2011141848A1 (en) * | 2010-05-11 | 2011-11-17 | Pfizer Inc. | Morpholine compounds as mineralocorticoid receptor antagonists |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20160413 |
|
| RJ01 | Rejection of invention patent application after publication |