CN102908349A - Metformin hydrochloride compound medicament - Google Patents
Metformin hydrochloride compound medicament Download PDFInfo
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- CN102908349A CN102908349A CN2012104349915A CN201210434991A CN102908349A CN 102908349 A CN102908349 A CN 102908349A CN 2012104349915 A CN2012104349915 A CN 2012104349915A CN 201210434991 A CN201210434991 A CN 201210434991A CN 102908349 A CN102908349 A CN 102908349A
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Abstract
The invention provides a metformin hydrochloride compound medicament, which relates to the technical fields of medicaments and medicament preparation. A compound preparation contains 0.1-99.9 percent (by weight) of metformin hydrochloride, 99.9-0.1 percent (by weight) of L-carnitine and 99.9-0.1 percent (by weight) of vitamin B1. The compound preparation has a good treatment effect on diabetes mellitus, and can be used for lowering the untoward effect occurrence rate of metformin hydrochloride, enhancing the metabolic capabilities of organisms, effectively lowering the risk of lactic acidosis, enhancing fat metabolism, enhancing oxygen uptake capability and resisting fatigue.
Description
Technical field:
The present invention relates to medicine and medicine manufacture technology field, relate in particular to a kind of metformin hydrochloride combination drug.
Background technology:
Type 2 diabetes mellitus also is adult's morbidity type diabetes, how to fall ill after 35～40 years old, accounts for diabetics more than 90%.The ability that produces insulin in the type 2 diabetes mellitus patient body is not to completely lose, insulin even produce too much in some patient bodies, but the action effect of insulin has a greatly reduced quality, so the insulin in the patient body may be in a kind of state of relative shortage.Can stimulate by some oral drugs the secretion of insulin in the body.In a word, the short-term goal of type 2 diabetes mellitus treatment is control blood glucose, and long term object is generation and the development of prevention related complication.
2007, China mainland area (not comprising Hong Kong, Macao, Taiwan) became diabetes the second big country that is only second to India (4,085 ten thousand people), patient 3,981 ten thousand people, prevalence 4.3%; Estimate to reach 5,927 ten thousand people in 2025, prevalence reaches 5.6%.
Biguanides is used to treat diabetes from the 50's of 20th century, metformin hydrochloride is widely used in the treatment of type 2 diabetes mellitus both at home and abroad.This is because metformin hydrochloride is a kind of blood sugar lowering, has the blood glucose toleration that improves the type 2 diabetes mellitus patient, reduces the effect of basis and post-prandial glycemia.The mechanism of action of metformin hydrochloride is different from the oral anti-blood glucose medicine of other type, it can reduce the generation of glycogen, reduce intestinal to the absorption of sugar, and the sensitivity that can improve insulin by picked-up and the utilization of increase periphery sugar, different from sulfonylureas is that metformin hydrochloride can not produce hypoglycemia to the patient of type 2 diabetes mellitus patient or euglycemia.After the metformin hydrochloride treatment, the secretion of insulin remains unchanged, and reduce the fasting insulin level and every day plasma insulin level.Lactic acid can cause that to conversion of glucose the lactic acid accumulation causes lactic acidosis in the mitochondrion but biguanides is by suppressing.
Lactic acidosis (lactic acidosis, LA) is a kind of more rare and serious Diabetic Acute complication, in case occur, case fatality rate can be up to more than 50%, especially blood lactic acid〉25mmol/L, case fatality rate is up to 80%.LA is that diabetics glucose oxygenate process is blocked, and the glucose zymolysis increases, and produces a large amount of lactic acid, makes the synthetic a kind of diabetic supersession complication that causes greater than lactic acid gathering in degraded and the drainage body of lactic acid.Lactic acid is the end-product of glucose anerobic glycolysis, is formed by the acetone acid reduction.Under oxygen free condition, glucose carries out zymolysis in cytosol, and product acetone acid is hydroconverted into lactic acid through DPNH (NADH) in the middle of it under the effect of lactic acid dehydrogenase, and NADH then changes nadide (NAD+) into.Lactic acid also can be under the lactic acid dehydrogenase effect, oxidation when NAD+ is converted into NADH again and become acetone acid, and this is the reversible reaction by the lactic dehydrogenase enzyme catalysis.And acetone acid can enter the further oxidation of mitochondrion under aerobic conditions, under the catalysis of pyruvate carboxylase, generates S-acetyl-coenzyme-A, is decomposed into H through tricarboxylic acid cycle oxidation production capacity again
2O and CO
2Acetone acid can be glucose through the pyruvate carboxylation shunt heteroplasia also in addition.When mitochondrion because organizing relative or absolute anoxia during dysfunction, acetone acid easily accumulates in the endochylema and changes lactic acid into, piles up gradually, thereby LA occurs.
Summary of the invention:
The object of the invention is to overcome the defective of prior art, and a kind of metformin hydrochloride combination drug is provided, and this combination drug synergism is strong, effectively reduces adverse reaction rate.
This combination drug contains metformin hydrochloride, L-BETAIN and vitamin B
1
For realizing the object of the invention, technical scheme realizes in the following way:
A kind of metformin hydrochloride combination drug is characterized in that: this compound preparation contains the 0.1%-99.9%(weight ratio) metformin hydrochloride, 99.9%-0.1%(weight ratio) L-BETAIN and 99.9%-0.1%(weight ratio) vitamin B
1
Described combination drug is prepared into oral formulations.
Described oral formulations is tablet or capsule.
Metformin hydrochloride is widely used in the treatment of type 2 diabetes mellitus both at home and abroad.This is because metformin hydrochloride is a kind of blood sugar lowering, has the blood glucose toleration that improves the type 2 diabetes mellitus patient, reduces the effect of basis and post-prandial glycemia.The mechanism of action of metformin hydrochloride is different from the oral anti-blood glucose medicine of other type, it can reduce the generation of glycogen, reduce intestinal to the absorption of sugar, and the sensitivity that can improve insulin by picked-up and the utilization of increase periphery sugar, different from sulfonylureas is that metformin hydrochloride can not produce hypoglycemia to the patient of type 2 diabetes mellitus patient or euglycemia.After the metformin hydrochloride treatment, the secretion of insulin remains unchanged, and reduce the fasting insulin level and every day plasma insulin level.
Levocarnitine is the natural composition with bioactive human body cell, is a kind of water solublity quaternary ammonium compound, and its major function is long-chain fatty acid to be transported to mitochondrion carry out beta oxidation and produce power.Because the betaoxidation of fatty acid carries out in mitochondrial substrate, coenzyme A is the coenzyme of acetylization reaction in the body, and the metabolism of sugar, fat and protein is played an important role, and can be used as acidosic auxiliary treatment.And the long-chain acyl coenzyme A (CoA) that forms in Cell sap can not pass through mitochondrial inner membrane, needs the carrier carnitine on the inner membrance to carry, and crosses over inner membrance and enters substrate with the form of fatty acyl group.
Vitamin B1 is one of vitamin B group, and the coenzyme form is diphosphothiamine (TPP).Vitamin B1 can be kept the function of normal glucose metabolism and nerve conduction, participates in the oxidative decarboxylation of acetone acid and α-ketoglutaric acid, relates to glycometabolic some physiological function in the body more active, and body is just larger to the demand of vitamin B1.Vitamin B1 has the heat in the sugar is decomposed out, and then once is decomposed into the effect of water and carbon dioxide, plays an important role in participating in carbohydate metabolism.
Lactic acid diabetes are had good therapeutic effect, and L-BETAIN and vitamin B1 participates in Intramitochondrial lactic acid metabolism to biguanides to conversion of glucose in the mitochondrion by suppressing, and can not cause the lactic acidosis that causes because of the lactic acid accumulation.
So the compositions of metformin hydrochloride, L-BETAIN and vitamin B1 not only has good therapeutic effect to diabetes, and can reduce the adverse reaction rate of metformin hydrochloride, improve the metabolic capacity of body.
Beneficial effect of the present invention is: 1) diabetics is had good therapeutic effect; 2) metabolic capacity of enhancing human body, the risk of reduction lactic acidosis; 3) improve lipid metabolism, improve oxygen uptake capacity, resisting fatigue.
The specific embodiment:
For technological means, creation characteristic that the present invention is realized, reach purpose and effect is easy to understand, below in conjunction with specific embodiment, further set forth the present invention.
Embodiment one
Take by weighing metformin hydrochloride 100g, L-BETAIN 100g, vitamin B
14g, carbomer 200g, HPMC10g, octadecanol 20g, NaHCO
3All cross 80 mesh sieves, fully behind the mixing, add an amount of magnesium stearate as lubricant, behind the mix homogeneously, the dry method direct compression, Hardness Control is at 3～4kg.
Embodiment two
Get
RS (a kind of material of making coating) 100g is dissolved in the 1000mL acetone, adds successively Pulvis Talci 20g, triethyl citrate 20g, and dimethicone is an amount of, and stirring spends the night obtains coating solution.With metformin hydrochloride 250g, L-BETAIN 250g, vitamin B
1The 10g crude drug is crushed to 100 orders, with the lactose mix homogeneously, puts into fluid bed, regulates inlet temperature to 35 ℃, preheating 5 min.Then regulating the boiling air quantity makes material be in best fluidized state.Regulating inlet temperature is 40 ℃, and atomisation pressure is 150 kPa, and spray rate is 5 mLmin
-1, adopting the side spray mode to spray into mass concentration is 1 gL
-1The pre-pelletize of ethyl cellulose alcoholic solution 200mL, until sprayed, stop hydrojet and continue dry 10min, take out the particle screening, get 80～120 purpose particles and put into again fluid bed preheating 5min, press that coating increases weight 100%, the antitackiness agent Pulvis Talci and
The ratio 20% of RS, spray rate 5 mLmin
-1, atomisation pressure 150KPa prepares microcapsule, the coating powder that obtains add mass fraction be behind 1% the Pulvis Talci mixing at 40 ℃ of aging 10 min, obtain acid hydrochloride salt metformin slow-releasing microcapsule, load capsule.
Embodiment three
With metformin hydrochloride 250g, L-BETAIN 250g, vitamin B
110g crude drug and MCC(microcrystalline Cellulose) 250g pulverizes respectively, crosses 100 mesh sieves.With progressively increase method mix homogeneously and cross 80 mesh sieves of equivalent, add an amount of 2%HPMC solution and make soft material, extrude round as a ball.Take out micropill, in 50 ℃ of dry 3h, sieve to get micropill between 18～24 orders.The hole diameter of sieve (perforated) plate is 0.9mm, and extruding rotating speed is 30rmin
-1, with 50rmin
-1High speed shear 1min, 40rmin
-1Round as a ball 4min.Get an amount of Aquacoat, it is 12. 5% coating solution that thin up is mixed with solid content concentration, mixes, and 30 ℃ of insulations are for subsequent use.18～24 order micropills are placed fluidisation preheating in the miniature fluidized bed prilling lagging cover drier, carry out coating with the coating solution that prepared, fluidized drying and get final product.40 ℃ of coating temperature, hydrojet speed 1.1mLmin
-1, atomizing pressure 0.05MPa.Load capsule, and get final product.
Above demonstration and described ultimate principle of the present invention, principal character and advantage of the present invention.The technical staff of the industry should understand; the present invention is not restricted to the described embodiments; what describe in above-described embodiment and the description only is preference of the present invention; be not used for limiting the present invention; without departing from the spirit and scope of the present invention; the present invention also has various changes and modifications, and these changes and improvements all fall in the claimed scope of the invention.The claimed scope of the present invention is defined by appending claims and equivalent thereof.
Claims (3)
1. metformin hydrochloride combination drug, it is characterized in that: this compound preparation contains the 0.1%-99.9%(weight ratio) metformin hydrochloride, 99.9%-0.1%(weight ratio) L-BETAIN and 99.9%-0.1%(weight ratio) vitamin B
1
2. metformin hydrochloride combination drug according to claim 1, it is characterized in that: described combination drug is prepared into oral formulations.
3. metformin hydrochloride combination drug according to claim 2, it is characterized in that: described oral formulations is tablet or capsule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012104349915A CN102908349A (en) | 2012-11-05 | 2012-11-05 | Metformin hydrochloride compound medicament |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012104349915A CN102908349A (en) | 2012-11-05 | 2012-11-05 | Metformin hydrochloride compound medicament |
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| CN102908349A true CN102908349A (en) | 2013-02-06 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108289899A (en) * | 2015-09-22 | 2018-07-17 | 维京治疗公司 | Using the conjoint therapy of the glycogenetic inhibitor of grape |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1891229A (en) * | 2005-07-07 | 2007-01-10 | 北京华安佛医药研究中心有限公司 | Medicinal composition for preventing or treating metabolic syndrome |
-
2012
- 2012-11-05 CN CN2012104349915A patent/CN102908349A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1891229A (en) * | 2005-07-07 | 2007-01-10 | 北京华安佛医药研究中心有限公司 | Medicinal composition for preventing or treating metabolic syndrome |
Non-Patent Citations (1)
| Title |
|---|
| 张敬东 等: "盐酸二甲双胍联合左卡尼汀治疗28 例非酒精性脂肪肝病的临床疗效", 《华西药学杂志》 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108289899A (en) * | 2015-09-22 | 2018-07-17 | 维京治疗公司 | Using the conjoint therapy of the glycogenetic inhibitor of grape |
| JP2018528254A (en) * | 2015-09-22 | 2018-09-27 | バイキング セラピューティクス，インコーポレーテッド | Combination therapy with glucose production inhibitors |
| EP3352762A4 (en) * | 2015-09-22 | 2019-06-05 | Viking Therapeutics, Inc. | Conjoint therapies with inhibitors of glucose production |
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Application publication date: 20130206 |