CN104997780B - A kind of Rosuvastatin calcium composition and its application in reducing blood lipid hypoglycemic medicament is prepared - Google Patents
A kind of Rosuvastatin calcium composition and its application in reducing blood lipid hypoglycemic medicament is prepared Download PDFInfo
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- CN104997780B CN104997780B CN201510360617.9A CN201510360617A CN104997780B CN 104997780 B CN104997780 B CN 104997780B CN 201510360617 A CN201510360617 A CN 201510360617A CN 104997780 B CN104997780 B CN 104997780B
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Abstract
Application the invention discloses a kind of pharmaceutical composition of reducing blood lipid blood glucose and its in the medicine for preparing treatment diabetes B, by active component and pharmaceutically, available auxiliary material is prepared the pharmaceutical composition, and described active component includes following component：（1）Rosuvastatin or its officinal salt；（2）Ciclopirox or Ciclopirox Olamine.Have the function that to cooperate with reducing blood lipid hypoglycemic after rosuvastain calcium and Ciclopirox use in conjunction, the two is prepared into the treatment that can be used for diabetes B after pharmaceutical composition.
Description
Technical field
The present invention relates to a kind of cardiovascular drugs, more particularly to a kind of pharmaceutical composition containing rosuvastain calcium and its
Application in reducing blood lipid hypoglycemic medicament is prepared, belongs to pharmaceutical technology field.
Background technology
Diabetes B original name, more in the sequela of 35~40 years old, accounts for diabetic 90% Adult Onset's patients with type Ⅰ DM
More than.Diabetes B be from based on insulin resistance with insulin relative deficiency to based on hypoinsulinism with insulin
The pathologic process of resistance, its cause of disease not yet illustrate completely, and generally acknowledged diabetes are one kind in environmental factor (such as life style at present
Change) in the presence of complex inheritance by multiple genes respectively or caused by interacting it is sick.Increasing evidence in recent years
It is vital to prove that inflammation serves in the generating process that insulin resistance and beta Cell of islet damage.Cause diabetes B
Main inducing to include fat, physical exertion very few and stress.Stress include anxiety, fatigue, direct stimulation, wound, operation, divide
Childbirth, other major diseases, and use hormone for raising blood glucose etc..Due to above-mentioned inducement, the insulin secreting ability of patient
And body gradually reduces to the sensitiveness of insulin, blood glucose rise, causes diabetes.Clinical manifestation：Based on insulin resistance,
Because of insulin resistance, insulin sensitivity declines, and insulin increases to compensate its insulin resistance, but the height of relative patient in blood
For blood glucose, insulin secretion still relative deficiency.
At present, treating the medicine of diabetes B includes：1. OHA.（1）Biguanides（Such as melbine）, it is this kind of
Medicine has the ability for reducing liver output glucose, and muscle cell, adipocyte and liver can be helped to be absorbed from blood
More glucose, so as to reduce blood sugar level.（2）Sulfonylureas（Such as Glimepiride, glibenclamide, gliclazide and Ge Lie quinolines
Ketone）, the main function of this kind of OHA is to stimulate pancreas islet to discharge more insulin.（3）Thiazolidinediones（As Roger arranges
Ketone and Pioglitazone）, such medicine can strengthen insulin sensitivity, help muscle cell, adipocyte and liver to absorb more
Glucose in more blood.But Rosiglitazone may increase heart disease risk.（4）Benzoic acid derivative class（Such as Rui Gelie
How and Nateglinide）, the mechanism of action of this kind of medicine is similar to sulfonylurea drugs, and mainly stimulating pancreas produces more insulin
To reduce blood glucose.（5）Alpha-glucosidase restrainer（Such as acarbose and voglibose）, this kind of antidiabetic drug can suppress human body
Absorption of the alimentary canal to carbohydrate, main function are to reduce postprandial blood sugar.2. trypsin class medicine.If by changing lifestyles
Blood glucose still can not be controlled well with using OHA, or takes other drugs to bring harmful effect to you
When, doctor will may suggest using insulin.At present, insulin can not be oral, can only utilize syringe or novopen etc.
Device passes through hypodermic injection.The onset time of different insulin preparations and acting duration are also different.Patient is needed in doctor
Guidance under, from the insulin-type for being adapted to itself current state of an illness, and formulate the appropriate injection of insulin time.
At present, still without the hypoglycemic document report of Ciclopirox, more not by its with Hydroxymethylglutaryl list acyl coenzyme A also
The document report of reducing blood lipid blood glucose after reductase inhibitor combination.
The content of the invention
The cause of disease and later phase clinical Symptoms for diabetes B, modern treatment viewpoint is from simple control before
Blood glucose switchs to hypoglycemic, lipid-loweringing, improves the treatment of the too many levels such as insulin resistance.
The present inventor closelys follow newest clinical treatment theory, and a large amount of drug effects are carried out by cell assay in vitro and animal experiment
Experiment, obtain a kind of compound medicine especially suitable for diabetes B treatment.Therefore, it is an object of the invention to provide one
Kind pharmaceutical composition and its application in reducing blood lipid hypoglycemic medicament is prepared.
In order to realize the purpose of the present invention, inventor is studied and screened by a large amount of cells and animal experiment, finally
Obtain following technical scheme：
A kind of pharmaceutical composition of reducing blood lipid blood glucose, the pharmaceutical composition available auxiliary material system by active component and pharmaceutically
Standby to form, described active component includes following component：（1）Rosuvastatin or its officinal salt；（2）Ciclopirox or Ciclopirox
Amine.
It should be noted that Ciclopirox Olamine is Ciclopirox（Ciclopirox, 1- hydroxy-4-methyl -6- cyclohexyl -2
（1H）- pyridone）With the double salt of 2- ethylaminoethanols, the Multiple salts forms are designed to increase water-soluble, its medicine in vivo
It is basically identical to imitate effect.
Preferably, the pharmaceutical composition of reducing blood lipid blood glucose as described above, the officinal salt of Rosuvastatin therein is auspicious
Relax and cut down statin calcium.
It is further preferred that the pharmaceutical composition of reducing blood lipid blood glucose as described above, wherein described active component is by component
（1）And component（2）Composition.
It is further preferred that the pharmaceutical composition of reducing blood lipid blood glucose as described above, rosuvastain calcium and ring pyrrole therein
The quality amount ratio of ketone or Ciclopirox Olamine is（1-20）：1.
Still further preferably, the pharmaceutical composition of reducing blood lipid blood glucose as described above, rosuvastain calcium and ring therein
The quality amount ratio of pyrrone or Ciclopirox Olamine is（1-10）：1.
Still further preferably, the pharmaceutical composition of reducing blood lipid blood glucose as described above, rosuvastain calcium and ring therein
The quality amount ratio of pyrrone or Ciclopirox Olamine is（2-5）：1.
It should be noted that the pharmaceutical composition of reducing blood lipid blood glucose of the present invention is oral formulations, described oral system
Agent includes tablet, capsule, granule, dripping pill.These oral formulations can add medicine on the basis of above-mentioned active component
The upper available auxiliary material of agent, by the conventional formulation technique of this area, prepares piece agent, capsule, granule, dripping pill.
In the Some Animals experiment of the present invention, after we are once fed 8 weeks using high fat high-carbonhydrate diet, by 40mg/kg once
Property intraperitoneal injection Streptozotocin (STZ) be successfully, reproduced diabetes B rat model, then carrying out intervention by medicine controls
Treat, medication surveys blood fat and fasting blood-glucose after 4 weeks, as a result shows：After rosuvastain calcium and Ciclopirox therapeutic alliance, model is big
The fasting blood-glucose of mouse significantly reduces, and its 24h urine volume is also greatly reduced compared to model control group.In addition, dosage halve after it is auspicious
The effect of the easypro rosuvastain calcium reduction cholesterol and triglyceride for cutting down statin calcium-Ciclopirox drug combination group and high dose is big
Cause suitable.For diabetes B patient often with disorders of lipid metabolism, this is also that it merges the major reason of the big Vascular complication such as the heart, brain
One of, and the latter is that diabetes are lethal, the main reason for disabling.Therefore diabetic's disorders of lipid metabolism is corrected, is contributed to
Prevent and treat the generation and development of big Vascular complication.
Based on the studies above achievement and the ordinary technical knowledge of those skilled in the art is combined, the present invention also provides a kind of system
Medicinal way, i.e. described component（1）And component（2）The active ingredient compositions of composition are preparing treatment diabetes B or drop blood
Application in the hypoglycemic medicine of fat.Preferably, component（1）For rosuvastain calcium.
Compared with prior art, pharmaceutical composition of the present invention has the following advantages that and marked improvement：Rosuvastain
Have the function that to cooperate with reducing blood lipid hypoglycemic after spit of fland calcium and Ciclopirox use in conjunction, can be used after the two is prepared into pharmaceutical composition
In the treatment of diabetes B.Meanwhile the dosage of rosuvastain calcium and Ciclopirox or Ciclopirox Olamine is only the two of conventional amount used
/ mono-, therefore medical expense, side effect and adverse reaction rate necessarily reduce.
Embodiment
The present inventor have studied the bioactivity of rosuvastain calcium combination Ciclopirox reducing blood lipid blood glucose by animal experiment,
It is specific test example below, technical scheme and technique effect is done and further lays down a definition and illustrates, but this hair
Bright protection domain is not limited to the embodiment.
Embodiment 1
Male SD rat 50, body weight 180-220g.After adaptability is fed l weeks, taken out at random from 50 male SD rats
It is Normal group to take 8, and remaining 42 is only used as making duplication animal model, and method is：Give high glucose and high fat feed (lard
10%, sucrose 20%, cholesterol 2.5%, cholate 1%, conventional feed 66.5%) feed.Normal group gives normal rats
Forage feed.After 8 weeks, low dose of Streptozotocin (STZ) 40mg/kg is injected intraperitoneally for 12 hours in modeling rat limosis, normal right
The citrate buffer of same dose is only injected according to group as control.After 1 week, after Rat Fast 12h, blood is taken to survey blood glucose, mainly
It is judged to more than 7.0mmol/L replicating successful rat model with fasting blood-glucose.
The rat for choosing 32 Cheng Mo is randomly divided into model group, Rui Shu cuts down group, Ciclopirox group, auspicious-ring group, and each group is to medicament
Amount is as follows：Rui Shu cuts down a group gavage and gives rosuvastain calcium 5mg/kg；Ciclopirox group gavage gives Ciclopirox 2mg/kg；Auspicious-ring group fills
Stomach gives rosuvastain calcium 2.5mg/kg and Ciclopirox 1mg/kg；Normal group, model group such as gavage at the capacity physiology salt simultaneously
Water.5 groups of equal daily gavages 1 time, continuous 4 weeks.Administration records the 24h urine volume of rat after terminating；Blood glucose, blood are determined after putting to death rat
Fat.Blood sugar test：Tail point cuts tail after being sterilized with 75% medicinal alcohol and takes blood, and blood glucose is detected with JPS-5 types blood glucose meter is surmounted.Blood
Fat detects：Each group rat heart takes blood, puts 37% constant water bath box water-bath 5 minutes, and 3000 revs/min (desk centrifuge) centrifuges 3 points
Clock, supernatant is taken, TC, TG are detected by automatic clinical chemistry analyzer.
There is more drinks, more foods, diuresis, weight loss (three-many-one-little) symptom, essence in the diabetes B model that the present invention replicates
God is dispirited, and hair is matt, delay of response.After rosuvastain calcium and Ciclopirox treatment, the diabetes B three of rat
More one are obviously improved less, and fasting blood-glucose significantly reduces, and is shown in Table 1.
Each group rat urine volume and fasting blood-glucose compare after the pharmaceutical intervention of table 1
| Group | Sample size | Urine volume（Ml/ is only） | Fasting blood-glucose（mmol/L） |
| Normal group | 8 | 31.17±6.08** | 5.45±1.07** |
| Model group | 8 | 70.45±13.37 | 14.42±3.15 |
| Rui Shu cuts down group | 8 | 71.20±9.66 | 13.19±1.29 |
| Ciclopirox group | 8 | 58.26±10.72* | 11.05±2.10 |
| Auspicious-ring group | 8 | 42.75±9.30* $$# | 6.70±1.18* $$## |
Each group compared with model group,* P＜ 0.05,** P＜ 0.01；
Auspicious-ring group with it is auspicious relax cut down group compared with,$ P＜ 0.05,$$ P＜ 0.01；
Auspicious-ring group compared with Ciclopirox group,# P＜ 0.05,## P＜ 0.01.
In addition, model group rats, compared with Normal group, blood fat is significantly raised, difference have highly significant (P＜
0.01)；Rui Shu cuts down group compared with model group, and blood fat substantially reduces, difference have conspicuousness (P＜ 0.05)；Ciclopirox group and model
Group is compared, blood fat no significant difference (P＞ 0.05)；Compared with model group, blood fat substantially reduces auspicious-ring group, and difference has significantly
Property (P＜ 0.05), compared with each single medicine group, difference have conspicuousness (P＜ 0.05).It is shown in Table 2.
Each group rat blood serum T-CHOL and triglycerides compare after the pharmaceutical intervention of table 2
| Group | Sample size | T-CHOL（g） | Triglycerides（mmol/L） |
| Normal group | 8 | 1.60±0.19** | 0.89±0.15** |
| Model group | 8 | 2.62±0.33 | 1.53±0.19 |
| Rui Shu cuts down group | 8 | 1.91±0.37* | 1.25±0.24* |
| Ciclopirox group | 8 | 2.57±0.22 | 1.50±0.18 |
| Auspicious-ring group | 8 | 2.02±0.28*# | 1.28±0.20* |
Each group compared with model group,* P＜ 0.05,** P＜ 0.01；
Auspicious-ring group with it is auspicious relax cut down group compared with,$ P＜ 0.05,$$ P＜ 0.01；
Auspicious-ring group compared with Ciclopirox group,# P＜ 0.05,## P＜ 0.01.
Claims (7)
1. a kind of pharmaceutical composition of reducing blood lipid blood glucose, the pharmaceutical composition available auxiliary material group by active component and pharmaceutically
Into, it is characterised in that described active component is made up of following component：（1）Rosuvastatin or its officinal salt；（2）Ring pyrrole
Ketone or Ciclopirox Olamine, described component（1）And component（2）Quality amount ratio be（1-20）：1.
2. the pharmaceutical composition of reducing blood lipid blood glucose according to claim 1, it is characterised in that described Rosuvastatin can
Pharmaceutical salts are rosuvastain calcium.
3. the pharmaceutical composition of reducing blood lipid blood glucose according to claim 1, it is characterised in that described component（1）And component
（2）Quality amount ratio be（1-10）：1.
4. the pharmaceutical composition of reducing blood lipid blood glucose according to claim 3, it is characterised in that described component（1）And component
（2）Quality amount ratio be（2-5）：1.
5. according to the pharmaceutical composition of any one of the claim 1-4 reducing blood lipid blood glucose, it is characterised in that described medicine group
Compound is oral formulations, and described oral formulations include tablet, capsule, granule, dripping pill.
6. the component described in claim 1（1）And component（2）The active ingredient compositions of composition are preparing treatment diabetes B
Medicine in application.
7. the component described in claim 1（1）And component（2）The active ingredient compositions of composition are preparing the medicine of reducing blood lipid blood glucose
Application in thing.
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103127505A (en) * | 2011-11-24 | 2013-06-05 | 北京大学第三医院 | Uses of statin compound serving as partly used medicine for curing diabetes mellitus |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103127505A (en) * | 2011-11-24 | 2013-06-05 | 北京大学第三医院 | Uses of statin compound serving as partly used medicine for curing diabetes mellitus |
Non-Patent Citations (4)
| Title |
|---|
| AntimycoticCiclopiroxOlamine in the Diabetic Environment Promotes Angiogenesis and Enhances Wound Healing;SaeHeeKo等;《PLOS one》;20111118;第6卷(第11期);e27844（1-9） * |
| 瑞舒伐他汀与辛伐他汀治疗２型糖尿病伴高血脂患者的疗效比较;李蕊;《山西医药杂志》;20130131;第４２卷(第１期);55-56 * |
| 瑞舒伐他汀对2 型糖尿病患者的降脂疗效及血管内皮功能的影响;吴剑利，等;《中国现代医生》;20140228;第52 卷(第6 期);63-65 * |
| 血脂康联合瑞舒伐他汀钙治疗糖尿病高脂血症疗效观察;廖建辉;《亚太传统医药》;20130430;第9卷(第4期);162-163 * |
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Inventor after: Weng Jianping Inventor after: Guo Wenrong Inventor before: Bai Lingqiang |
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Effective date of registration: 20180212 Address after: 201206 Shanghai city Pudong New Area Jin Road No. 879 Applicant after: Xudong Haipu Pharmaceutical Co., Ltd., Shanghai Address before: 721001 Zhongshan West Road Baoji city Shaanxi province Jintai District No. 78 Chen Ji pharmaceutical Applicant before: Bai Lingqiang |
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