CN105616420A - Pharmaceutical composition for reducing blood fat - Google Patents
Pharmaceutical composition for reducing blood fat Download PDFInfo
- Publication number
- CN105616420A CN105616420A CN201610028583.8A CN201610028583A CN105616420A CN 105616420 A CN105616420 A CN 105616420A CN 201610028583 A CN201610028583 A CN 201610028583A CN 105616420 A CN105616420 A CN 105616420A
- Authority
- CN
- China
- Prior art keywords
- pharmaceutical composition
- blood fat
- compound
- fat reducing
- group
- 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
- 239000008280 blood Substances 0.000 title claims 8
- 210000004369 blood Anatomy 0.000 title claims 8
- 239000008194 pharmaceutical composition Substances 0.000 title claims 8
- 150000001875 compounds Chemical class 0.000 claims 6
- 239000003085 diluting agent Substances 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 2
- 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 2
- 229920000881 Modified starch Polymers 0.000 claims 1
- 239000011230 binding agent Substances 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 239000001913 cellulose Substances 0.000 claims 1
- 229920002678 cellulose Polymers 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000008187 granular material Substances 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- 239000000314 lubricant Substances 0.000 claims 1
- 239000004531 microgranule Substances 0.000 claims 1
- 235000019426 modified starch Nutrition 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 239000003381 stabilizer Substances 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
Classifications
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention relates to a pharmaceutical composition for reducing blood fat. The pharmaceutical composition contains an effective dose of compound and a pharmaceutically acceptable carrier, wherein the structure of the compound is as shown in the specification. The compound provided by the invention has an obvious effect on reducing blood fat and can be developed into a new pharmaceutical composition which is effective clinically.
Description
Technical field
The present invention relates to field of medicaments, specifically, the present invention relates to the pharmaceutical composition of a kind of blood fat reducing.
Background technology
Owing to lipid metabolism or operating make one or more lipids of blood plasma extremely higher than being just frequently referred to hyperlipemia. Lipid is insoluble or poorly soluble in water must be existed with lipoprotein form with protein bound, and therefore, hyperlipemia is often hyperlipoproteinemia. Show as hypercholesterolemia, hypertriglyceridemia or both have concurrently.
The clinical manifestation of hyperlipemia is mainly lipid and deposits caused arteriosclerosis in the xanthoma caused by intradermal deposition and lipid at blood vessel endothelium. Although hyperlipemia can cause xanthoma, but its incidence rate is not significantly high; And atherosclerotic generation and development are a kind of slowly progressive processes. Therefore under normal conditions, most of patients non-evident sympton and abnormal sign. Many people are owing to just finding have blood plasma lipoprotein level to raise when other reasons carries out blood biochemical inspection.
Summary of the invention
It is an object of the invention to provide the pharmaceutical composition of a kind of blood fat reducing.
In order to realize the purpose of the present invention, the present invention provides the compound of a kind of blood fat reducing, and this compound has having structure:
The present invention also provides for the pharmaceutical composition of a kind of blood fat reducing, and described pharmaceutical composition comprises the compound of effective dose and pharmaceutically acceptable carrier, and described compound has having structure:
Preferably, described pharmaceutically acceptable carrier is diluent, disintegrating agent, binding agent, lubricant, stabilizer or corrigent.
Preferably, described diluent is sugar derivatives, starch derivatives or cellulose derivative.
Preferably, described diluent is lactose.
Preferably, described pharmaceutical composition is powder, microgranule, granule, capsule or tablet.
The present invention also provides for compound purposes in the medicine of preparation blood fat reducing, and this compound has having structure:
Term used herein " pharmaceutically acceptable " refers to the material of biologic activity or the character not eliminating compound as herein described, such as carrier or diluent. This kind of material is applied to individuality and is not resulted in undesirable biological action or not with harmful way and any component interaction in the compositions comprising it.
" pharmaceutically acceptable carrier " includes any and all of solvent as the term is employed herein, disperse medium, coating material, surfactant, antioxidant, preservative (such as antibacterial, antifungal), isotonic agent, absorption delay agent, salt, preservative, drug stabilizing agent, binding agent, excipient, 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 the inconsistent carrier of active component, consider to use any conventional carrier in treatment or pharmaceutical composition.
The compound of the present invention is notable for lipid-lowering effect, it is possible to develop into pharmaceutical composition effectively new clinically.
Detailed description of the invention
Below by way of the description of detailed description of the invention, the invention will be further described, but this is not limitation of the present invention, those skilled in the art's basic thought according to the present invention, various modifications may be made or improves, but without departing from the basic thought of the present invention, all within the scope of the present invention.
Experimental example
The structural formula of target compound is:
Choose cleaning grade SD rat 120, body weight 180-220g, male and female half and half, after rat adaptability is fed 7 days, tail venous blood sampling, detects blood lipid level, get rid of the impact on experimental result of the non-health laboratory animal, and sub-cage rearing after rat being randomly divided into 4 groups according to body weight, sex, respectively normal group, model group, positive drug group, administration group, often group 30. Except normal group gives normal diet nursing, all the other are respectively organized rat and first give vitamin D3700000 IU/kg, gavage in the 3 days normal saline of equal volume (normal group give), then raise with high lipid food (weight %): cholesterol 1%, propylthiouracil 0.61%, natrii tauroglycocholas 0.35%, Adeps Sus domestica 5%, normal feedstuff 93.04%, raises 8 weeks, to cause hyperlipidemia exception animal model.
Within after modeling the 3rd day, starting administration, each group dosage is as follows: normal group and model group, gives normal saline gavage 1mL/100g body weight; Positive drug group, atorvastatin solution 0.09mg/ml, give gavage 1mL/100g body weight; Administration group, the target compound of 0.01g adds 9000mL normal saline and becomes suspension, gives gavage 1mL/100g body weight. 1 times/day, successive administration 20d.
The rat of each group, with 25% urethane 3ml/kg intraperitoneal injection of anesthesia, after 30 minutes, by each group of rat back fixation respectively, cuts abdominal cavity open, and abdominal aortic blood 5m1 does blood lipids index. Abdominal aortic blood 5m1,5000 turns/min of centrifuge are centrifuged 10min, prepare serum. Aspartate transaminase (AST) activity detection kit (Sigma-Aldrich) is adopted to detect AST.
Result is shown in following table.
| Group | AST(U/L) |
| Normal group | 81.19��9.46 |
| Model group | 251.36��12.72 |
| Positive drug group | 171.19��7.29 |
| Administration group | 173.36��6.86 |
As seen from the above table, the effect of positive drug group and administration group there was no significant difference.
Claims (7)
1. the compound of a blood fat reducing, it is characterised in that this compound has having structure:
2. the pharmaceutical composition of a blood fat reducing, it is characterised in that described pharmaceutical composition comprises the compound of effective dose and pharmaceutically acceptable carrier, and described compound has having structure:
3. the pharmaceutical composition of blood fat reducing according to claim 2, it is characterised in that described pharmaceutically acceptable carrier is diluent, disintegrating agent, binding agent, lubricant, stabilizer or corrigent.
4. the pharmaceutical composition of blood fat reducing according to claim 3, it is characterised in that described diluent is sugar derivatives, starch derivatives or cellulose derivative.
5. the pharmaceutical composition of blood fat reducing according to claim 4, it is characterised in that described diluent is lactose.
6. the pharmaceutical composition of blood fat reducing according to claim 3, it is characterised in that described pharmaceutical composition is powder, microgranule, granule, capsule or tablet.
7. compound purposes in the medicine of preparation blood fat reducing, it is characterised in that this compound has having structure:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610028583.8A CN105616420A (en) | 2016-01-16 | 2016-01-16 | Pharmaceutical composition for reducing blood fat |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610028583.8A CN105616420A (en) | 2016-01-16 | 2016-01-16 | Pharmaceutical composition for reducing blood fat |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105616420A true CN105616420A (en) | 2016-06-01 |
Family
ID=56032042
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610028583.8A Pending CN105616420A (en) | 2016-01-16 | 2016-01-16 | Pharmaceutical composition for reducing blood fat |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105616420A (en) |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1711260A (en) * | 2002-11-05 | 2005-12-21 | 瑟维尔实验室 | Pyridopyrimidinone compounds, processes for their preparation and medicaments containing them |
| CN101641358A (en) * | 2007-03-23 | 2010-02-03 | 霍夫曼-拉罗奇有限公司 | Aza-pyridopyrimidinone derivatives |
| CN103694255A (en) * | 2014-01-09 | 2014-04-02 | 华中师范大学 | Pyridinooxazone-pyridinopyrimidone compounds and preparation method and application thereof |
-
2016
- 2016-01-16 CN CN201610028583.8A patent/CN105616420A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1711260A (en) * | 2002-11-05 | 2005-12-21 | 瑟维尔实验室 | Pyridopyrimidinone compounds, processes for their preparation and medicaments containing them |
| CN101641358A (en) * | 2007-03-23 | 2010-02-03 | 霍夫曼-拉罗奇有限公司 | Aza-pyridopyrimidinone derivatives |
| CN103694255A (en) * | 2014-01-09 | 2014-04-02 | 华中师范大学 | Pyridinooxazone-pyridinopyrimidone compounds and preparation method and application thereof |
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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 | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160601 |