CN108524502A - A kind of pharmaceutical composition for treating diabetes B - Google Patents
A kind of pharmaceutical composition for treating diabetes B Download PDFInfo
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- CN108524502A CN108524502A CN201710125241.2A CN201710125241A CN108524502A CN 108524502 A CN108524502 A CN 108524502A CN 201710125241 A CN201710125241 A CN 201710125241A CN 108524502 A CN108524502 A CN 108524502A
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- diabetes
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
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- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
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- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
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Abstract
The invention discloses a kind of pharmaceutical compositions for treating diabetes B, establish diabetes rat model, drug is to the hypoglycemic of diabetic model rats through the invention, the experiment of blood fat, the result shows that, drug of the present invention is in protection islet cell function and adjusts diabetic supersession disease side and plays the role of fairly obvious, it can delay blood glucose rise speed, adjust the disorder of blood lipid metabolism, and then postpone the progress of diabetic duration, the islet function of diabetes rat can obviously be protected, especially there is stronger bioactivity in the insulin resistance side of improvement diabetes rat.In structure, the pharmaceutical composition of the treatment diabetes B includes the compound or its pharmaceutically acceptable salt and pharmaceutically acceptable carrier of following formula：
Description
Technical field
The present invention relates to field of medicaments, and specifically, the present invention relates to a kind of pharmaceutical compositions for treating diabetes B.
Background technology
Diabetes are a kind of non-contagious chronic diseases for endangering human health and life.The morbidity of China's diabetes at present
Rate and the death rate rise rapidly, oneself rises one of faster country through becoming the whole world, and are more than many developed countries.Diabetes are
Cause one of the risk factor of cardiovascular danger event incidence and case fatality rate, long term hyperglycemia that will induce body that oxidation occurs and answer
Swashing causes vascular endothelial cell damage, leads to histiocytic chronic apoptosis, can also cause disorders of lipid metabolism, further adds
The process of weight diabetic condition.Therefore, the drug of research and development treatment diabetes B prevents diabetes simultaneously for hypoglycemic and further
Hair disease such as vascular diseases etc. are all of great significance.
Invention content
The purpose of the present invention is to provide a kind of pharmaceutical compositions for treating diabetes B.
In order to achieve the object of the present invention, the present invention provides a kind of pharmaceutical composition for treating diabetes B, the drug
Compound of the composition comprising following formula or its pharmaceutically acceptable salt and pharmaceutically acceptable carrier：
Preferably, solubility of the described pharmaceutical composition in physiological saline or serum is not less than 10 μM.
It is highly preferred that described pharmaceutical composition can be the pharmaceutical formulation of liquid form and tablet form.
It is highly preferred that the pharmaceutical formulation of the tablet form has enteric coating.
The present invention also provides purposes of the compound in the drug for preparing treatment diabetes B, under the compound has
Array structure：
Drug of the present invention is in protection islet cell function and adjusts diabetic supersession disease side and has fairly obvious work
With can delay blood glucose rise speed, adjust the disorder of blood lipid metabolism, and then postpone the progress of diabetic duration, can obviously protect
The islet function of diabetes rat is protected, it is especially living with stronger biology in the insulin resistance side of improvement diabetes rat
Property, there are the potentiality for being developed into new drug clinically.
Description of the drawings
Fig. 1 is each group pancreas HE dyeing cross-sectional views (× 200).
Fig. 2 is each group pancreas immunohistochemistry cross-sectional view (× 200).
A. normal group；B. model group；C. drug low dose group of the present invention；D. drug middle dose group of the present invention；E. of the invention
Drug high dose group.
Specific implementation mode
For the effect of clear drug therapy diabetes B of the present invention, it is described in detail in following embodiment.Pass through
Compare each group rat blood sugar blood lipid level, and to being observed after pancreatic tissue dyeing and immunohistochemistry, multi-angle shows medicine of the present invention
Object is the effect for the treatment of in terms of diabetes B.
Therapeutic effect of 1 drug of the present invention of experimental example for diabetes B
Drug of the present invention has following structural：
The foundation of diabetes B rat model
It is overnight to be deprived of food but not water 12h or more after rat conventinal breeding is up to standard, wherein 10 are only used as normally organizing progress abdominal cavity note
Penetrate 60mgkg-160mgkg is subcutaneously injected in citrate buffer, remaining rat disposable celiac-1Streptozotocin
(STZ).After 72h, fast blood glucose meter detects rat tail vein blood glucose, with fasting blood-glucose>11.1mmol·L-1As diabetes mould
Type Success criteria.
Experiment packet and administration
The successful rat of modeling is randomly divided into 4 groups：Model group, the high, medium and low dosage group of drug of the present invention.Normal group and
Model group rats carry out gavage with normal saline daily；Medicine group (high, medium and low) rat of the present invention daily respectively press 120,
90、60mg·kg-1Gavage is given, experimental period is 4 weeks.
Blood parameters detect
It is overnight that Rat Fast be can't help into water 12h after drug study, after weighing blood is measured with fast blood glucose meter tail vein
Sugar gives 50mgkg later-1Phenobarbital intraperitoneal anesthesia cuts off skin in the centripetal end of rat aorta crotch from abdomen
It is punctured at 1~3mm and takes blood, detection serum TG, CHO, HDL, LDL are horizontal.
Make pancreas and pancreas immunohistochemistry slice
Pancreas, the aorta for winning rat are placed in room temperature in 10% buffered formalin fixer and preserve, to do common disease
Reason HE dyeing and immunohistochemistry are prepared.
Statistical analysis
It is counted using statistical package SPSS 11.5, all experimental datasIt indicates, two samples compare using t
It examines, each comparison among groups one-way analysis of variance, P≤0.05 is that difference is statistically significant.
Influences of the STZ to diabetes B rat model fasting blood-glucose
STZ is injected after conventinal breeding is up to standard, after 3d rat occurs drink, more foods, diuresis symptom, model group rats and just
Normal group compares, the former fasting blood-glucose is significantly raised (P ＜ 0.01), tail vein blood measure fasting blood glucose level all greater than>
11.1mmol·L-1, illustrate modeling success, reach diabetes B standard.
Influence of the drug of the present invention to diabetic model rats blood glucose
Upper limit 27.9mmolL of the model group rats fasting blood glucose level all greater than blood glucose meter-1, shown compared with normal group
It writes and increases (P ＜ 0.01).After gavage, low, middle dose group rat fasting blood-glucose level is not significantly different compared with model group, and
High dose drug of the present invention is after 4 weeks, and rat blood sugar is on a declining curve in group, compared with model group, statistically significant (P ＜
0.05, P ＜ 0.01), though show that drug high dose of the present invention cannot effectively control blood glucose rise in the short time, it can be in certain journey
Delay the occurrence and development process of rat model diabetic duration on degree, as a result following table.
Note：Compared with the control group,aP ＜ 0.01；Compared with model group,bP ＜ 0.05,cP ＜ 0.01.
Influence result of the drug of the present invention to diabetes rat blood fat see the table below
Note：Compared with the control group,aP ＜ 0.01；Compared with model group,bP ＜ 0.05,cP ＜ 0.01.
It can be seen from the table, compared with normal group, model group rats TG, TC, LDL serum levels, which have, significantly increases (P ＜
0.01), HDL serum levels decline apparent (P ＜ 0.01)；Compared with model group, low dosage each index of medicine group rat of the present invention
Without significant difference, middle and high dosage medicine group rat TG, TC, LDL level of the present invention is on a declining curve, and HDL levels become in rising
Gesture has significant difference (P ＜ 0.05, P ＜ 0.01), is shown in Table 2.
Each group pancreas HE dyeing cross-sectional view is shown in Fig. 1 after giving drug of the present invention.
Normal rats pancreas islet entirety structure is complete, and form rule is full, sharpness of border, and pancreas islet quantity is more and island inner cell
Number arrangement is very close.Model group rats pancreas islet form shrinkage, volume become smaller, and form is irregular, pancreas islet quantity and island endocrine
Cell number significantly reduces, disorganized.Compared with model group, low, middle dose group rat pancreas islet quantity and island endocrine cell
Number is slightly increased, but still less；High dose group pancreas islet volume increases, and island inner cell density increases, and cell arrangement is more equal
Even regular, pancreas islet form, structure tend to be normal substantially.Illustrate that drug of the present invention has preferable protection, repair to pancreas islet.
Drug of the present invention is shown in Fig. 2 to the influence result of each group pancreatic tissue immunohistochemistry insulin antigen presentation.
Control rats pancreas islet volume, form are normal, and rounded or oval, boundary is apparent from, island inner cell number also compared with
It is more, and cell arrangement is orderly neat, cytoplasm is full, abundant.Model group rats islet cells atrophy degree is serious, small volume,
Form is highly irregular, and pancreas islet quantity is obviously less, and islet cells is disorganized, sparse, obscurity boundary is unclear.With model group
Compare, low, middle dosage medicine group rat Langerhans islet quantity of the present invention and island endocrine cell quantity are slightly increased, but quantity still compared with
Few, pancreas islet volume is slightly increased relative to model group；High dose medicine group pancreas islet quantity of the present invention significantly increases, island endocrine
Cell density obviously increases, and arrangement is relatively uniform, and Pancreas Islet Structure is normal, form primitive rule.
Claims (5)
1. a kind of pharmaceutical composition for treating diabetes B, which is characterized in that described pharmaceutical composition includes the compound of following formula
Or its pharmaceutically acceptable salt and pharmaceutically acceptable carrier：
2. the pharmaceutical composition for the treatment of diabetes B according to claim 1, which is characterized in that described pharmaceutical composition
Solubility in physiological saline or serum can be not less than 10 μM.
3. the pharmaceutical composition for the treatment of diabetes B according to claim 2, which is characterized in that described pharmaceutical composition
It can be the pharmaceutical formulation of liquid form and tablet form.
4. the pharmaceutical composition for the treatment of diabetes B according to claim 3, which is characterized in that the tablet form
Pharmaceutical formulation can have enteric coating.
5. purposes of the compound in the drug for preparing treatment diabetes B, which is characterized in that the compound has following knot
Structure：
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710125241.2A CN108524502A (en) | 2017-03-03 | 2017-03-03 | A kind of pharmaceutical composition for treating diabetes B |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710125241.2A CN108524502A (en) | 2017-03-03 | 2017-03-03 | A kind of pharmaceutical composition for treating diabetes B |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN108524502A true CN108524502A (en) | 2018-09-14 |
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ID=63488529
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710125241.2A Withdrawn CN108524502A (en) | 2017-03-03 | 2017-03-03 | A kind of pharmaceutical composition for treating diabetes B |
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| Country | Link |
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| CN (1) | CN108524502A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110749579A (en) * | 2019-08-29 | 2020-02-04 | 西安医学院 | Method for detecting influence of drug on pancreatic islet cell lipid uptake through immunofluorescence |
-
2017
- 2017-03-03 CN CN201710125241.2A patent/CN108524502A/en not_active Withdrawn
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110749579A (en) * | 2019-08-29 | 2020-02-04 | 西安医学院 | Method for detecting influence of drug on pancreatic islet cell lipid uptake through immunofluorescence |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| WW01 | Invention patent application withdrawn after publication |
Application publication date: 20180914 |
|
| WW01 | Invention patent application withdrawn after publication |