CN1451385A - Oral compound hypoglycemic medicine - Google Patents
Oral compound hypoglycemic medicine Download PDFInfo
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- CN1451385A CN1451385A CN 02108983 CN02108983A CN1451385A CN 1451385 A CN1451385 A CN 1451385A CN 02108983 CN02108983 CN 02108983 CN 02108983 A CN02108983 A CN 02108983A CN 1451385 A CN1451385 A CN 1451385A
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- metformin
- hypoglycemic medicine
- oral compound
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- compound hypoglycemic
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Abstract
An orally hypoglycemic medicine in the form of capsule, tablet, or slow-releasing tablet is prepared from biguanide component (dimethyl biguanide), sulfourea component chosen from glibenclamide, glibornuride, gliclazide, glipized and gliquidone, and supplementary product (zinc sulfate). Its advantages are high curative effect and no untoward reaction.
Description
Technical field
The present invention relates to a kind of oral compound hypoglycemic medicine.
Technical background
Diabetes are global common diseases of metabolism of a kind of serious harm human health, are its common outstanding feature with long-term hyperglycemia.Its Pathophysiology is the caused metabolism disorder of the relative or absolute hyposecretion of insulin, comprises sugar, protein, fat, water and electrolyte etc.It is unusual to it is characterized by hyperglycemia, glycosuria, glucose tolerance attenuating, insulin release test.Asymptomatic in early days clinically, to the symptom phase polyphagia, polydipsia, polyuria, excessive thirst, polyphagia just arranged, become thin, disease group such as fatigue and weak, the course of disease is very long, be one and secularly develop into the pathological process in badly damaged stage of pathological anatomy, reflecting that the beta Cell of islet reserve function is low gradually, hypoinsulinism and the insensitive evolution process of Insulin receptor INSR from pathological biochemistry and Pathophysiology.The various chronic complication of the normal appearance of long-term diabetic duration become the main cause that disables or die of illness.Severe complication persons such as coronary heart disease, myocardial infarction, ischemic or hemorrhagic apoplexy, blind, acromelic gangrene are taken place in diabetic population, than many 2~3 times or more of non-diabetic people.If can in time prevent and treat, patient's life-span can obviously prolong, and the labour force can be near normal.
More clinically what see is the constitutional type ii diabetes, and it is characterized in that: (1) onset is slower; (2) be more common in person in middle and old age; (3) plasma insulin level is pressed only relative property reduction of weighing machine, is after sugar stimulates and postpones to discharge and be higher than the normal person; (4) Insulin receptor INSR is often insensitive.
The oral drugs of treatment diabetes mainly contain biguanides and sulphanylureas at present.The indication of biguanides is: (1) is mainly used in treatment II type above middle age light medium-sized diabetes, every day insulin requirement amount<20 persons of unit; (2), can use instead or add and obtain good effect with this group medicine when sulphanylureas on probation loser; (3) islets of langerhans is have Drug resistance person and can reduce insulin dosage; (4) can prevent and treat subclinical phase diabetes, prevent that it is developed to the symptom phase.Its blood sugar reducing function mechanism of generally acknowledging may for: (1) is strengthened surrounding tissue sugar and is utilized; (2) suppress the glycogen heteroplasia; (3) suppressing intestinal sugar absorbs.Therefore, this medicine may have the effect that strengthens insulin sensitivity, and from alleviating the burden of beta Cell of islet, this medical instrument has positive effect.
The blood sugar reducing function mechanism that sulfonylurea drugs is generally acknowledged can be divided into outer two parts of pancreas in the pancreas: (1) pancreas internal stimulus β cell uelralante; (2) pancreas is strengthened insulin and the utilization of its receptors bind reinforcement sugar outward.The I type or the fragility diabetes mellitus type of all children's and morbidity in the past in 40 years old are generally all invalid, also should not use.Through clinical practice over 30 years, its indication is clear and definite.Mainly to as if elderly type ii diabetes patient with slight symptoms, every day the insulin requirement amount below 40 units, as it is more effective to be less than 20 persons of unit.
Zinc participates in the biosynthesis and the degraded of insulin, beta Cell of islet at first in endoplasmic reticulum insulin synthesis former, proinsulin is transported in the Golgi body again and is combined into six aggressiveness with zinc, leave behind the Golgi body under the effect of trypsin, carboxypeptidase, be hydrolyzed into insulin and C peptide, insulin further concentrates and forms the particulate core of β, and to be stored in the β granule with the bonded form of zinc.In case be subjected to stimulations such as glucose, the β granule is close to the β cell membrane, and membrana granulosa and cell membrane merge, uelralante.In the synthetic storage process of insulin, zinc plays an important role.If free available zinc is abundant in the blood, and zinc abundance in the β cell, then insulin secretion reduces; If blood zinc reduces, the obtainable zinc of β cell reduces, the alternative zinc of insulin and secrete increase then, and this is to cause hyperinsulinemia, produces one of reason of insulin resistant.
Because diabetes have symptoms such as polyphagia, polydipsia, polyuria, fatigue and weak, its blood potassium blood magnesium level all reduces.From protection beta Cell of islet function and rising urine osmotic pressure and improve symptom such as fatigue and weak, it is necessary as basic medication that diabetics replenishes the potassium magnesium ion: (1) is near the release of normal polarized state in order to insulin beta Cell of islet; (2) surrounding tissue is near normal polarized state to strengthen sugar utilization.
The oral drugs of treatment diabetes mainly contain biguanides and second filial generation sulfonylurea drugs at present.
Biguanides has metformin and phenformin, and first-selection is a metformin, and this medicine side effect is less relatively.
Second filial generation sulfonylurea drugs has glibenclamide, gliclazide, glipizide, gliquidone and glibornuride etc.
The zinc supplement preparation has the sulphuric acid zinc metal sheet.
Replenish the potassium magnesium ion potassium magnesium controlled-release tablet is arranged.
Clinical research shows; under the additional situation of potassium magnesium ion as basic medication; biguanides is in the same place with second filial generation sulfonylurea drugs and zinc sulfate compound recipe; can reduce the consumption of biguanides and sulfonylurea drugs respectively; but abirritate β cell uelralante; and the sensitivity of enhancing insulin, the protection beta Cell of islet.Owing in adjuvant, increased zinc sulfate, β cell uelralante is more become rationally, and reduced the insulin substitution zinc that zinc deficiency causes and secrete the probability of increase, further strengthened the sensitivity of insulin.
Summary of the invention
The object of the present invention is to provide a kind of for oral compound hypoglycemic medicine; it is in the same place by biguanides and second filial generation sulfonylurea drugs and zinc sulfate compound recipe; reach the consumption that reduces biguanides and sulfonylurea drugs; alleviate the stimulation of β cell and the sensitivity of enhancing insulin, thereby protect beta Cell of islet as much as possible.Owing in adjuvant, increased zinc sulfate, make β cell uelralante more become reasonable, and reduced the insulin substitution zinc that zinc deficiency causes and secreted the probability of increase, further strengthen the sensitivity of insulin, improved curative effect, avoided untoward reaction separately, reduced adverse effect to energy metabolism, make things convenient for patient's medication, under the situation of oral potassium magnesium controlled-release tablet as basic medication, the present invention makes the control of diabetes more become reasonable.
Technical scheme of the present invention realizes in the following manner:
The present invention is made up of biguanides, second filial generation sulfonylurea drugs and adjuvant etc.
The biguanides first-selection is a metformin, is phenformin secondly.
Second filial generation sulfonylurea drugs can be in the medicines such as glibenclamide, gliclazide, glipizide, gliquidone and glibornuride a kind of.
Adjuvant can be zinc sulfate, zinc oxide, magnesium stearate, Pulvis Talci, starch, mannitol, Polyethylene Glycol, polyvinylpyrrolidone, hydroxypropyl methylcellulose, III medical acrylic acid enteric resin, IV medical acrylic acid gastric solubleness resin etc.
The component of biguanides and second filial generation sulfonylurea drugs and percentage by weight are:
The percentage by weight of metformin and glibenclamide is between 500: 1~50: 1;
The percentage by weight of metformin and glipizide is between 250: 1~25: 1;
The percentage by weight of metformin and gliclazide is between 16: 1~2: 1;
The percentage by weight of metformin and gliquidone is between 80: 1~15: 1;
The percentage by weight of metformin and glibornuride is between 500: 1~50: 1.
A kind of oral compound hypoglycemic medicine includes biguanides and second filial generation sulfonylurea drugs and adjuvant and forms, and it can be produced and be capsule, tablet or slow releasing tablet.
Advantage of the present invention is as follows:
1, biguanides mainly is to suppress carbohydrate metabolism, glucolytic key enzyme; Generation, glycogen output, gluconeogenesis and the reduction small intestinal that suppresses ATP is to the absorption of glucose etc.Untoward reaction often has anorexia, nausea,vomiting,diarrhea and lactic acidosis etc., even dead.Be in the same place with second filial generation sulfonylurea drugs compound recipe, can reduce the consumption of biguanides, avoided untoward reaction, reduced adverse effect energy metabolism.
2, second filial generation sulfonylurea drugs mainly is to stimulate the beta Cell of islet uelralante; promote endogenous insulin secretion etc.; that untoward reaction often has is nauseating, upper abdomen distension and headache etc.; be in the same place with the biguanides compound recipe; can reduce the consumption of second filial generation sulfonylurea drugs; avoid untoward reaction, alleviated the burden of beta Cell of islet, thereby protected beta Cell of islet.
3, owing in adjuvant, increased zinc, β cell uelralante is more become rationally, and reduced the insulin substitution zinc that zinc deficiency causes and secrete the probability of increase, further strengthened the sensitivity of insulin.
4, the present invention has adopted capsule or the outer technology that is surrounded by thin film, has covered the disagreeable taste of medicine, can moistureproofly, anti-go mouldy.
5, thin film of the present invention is nontoxic polymer substance, and is simple to operate in the production process, do not have environmental pollution.
6, the present invention is for oral multicomponent hypoglycemic drug, and the patient takes medicine conveniently, and under the situation of oral potassium magnesium controlled-release tablet as basic medication, the present invention makes the control of diabetes more become reasonable.
The specific embodiment
For feature of the present invention is carried out clearer explanation, some concrete schemes now will be described, in conjunction with the embodiments, the invention will be further described:
Embodiment 1
A kind of oral compound hypoglycemic medicine, every component and content are:
Metformin 200mg
Glibenclamide 1.0mg
Right amount of auxiliary materials
Adjuvant can be zinc sulfate, zinc oxide, magnesium stearate, Pulvis Talci, starch, mannitol, Polyethylene Glycol, polyvinylpyrrolidone, hydroxypropyl methylcellulose, III medical acrylic acid enteric resin, IV medical acrylic acid gastric solubleness resin etc.
The percentage by weight of metformin and glibenclamide is between 500: 1~50: 1; In it is incapsulated, be finished product.
Embodiment 2
A kind of oral compound hypoglycemic medicine, every component and content are:
Metformin 200mg
Glipizide 2.0mg
Right amount of auxiliary materials
Adjuvant can be zinc sulfate, zinc oxide, magnesium stearate, Pulvis Talci, starch, mannitol, Polyethylene Glycol, polyvinylpyrrolidone, hydroxypropyl methylcellulose, III medical acrylic acid enteric resin, IV medical acrylic acid gastric solubleness resin etc.
The percentage by weight of metformin and glipizide is between 250: 1~25: 1; In it is incapsulated, be finished product.
Embodiment 3
A kind of oral compound hypoglycemic medicine, every component and content are:
Metformin 200mg
Gliclazide 25mg
Right amount of auxiliary materials
Adjuvant can be zinc sulfate, zinc oxide, magnesium stearate, Pulvis Talci, starch, mannitol, Polyethylene Glycol, polyvinylpyrrolidone, hydroxypropyl methylcellulose, III medical acrylic acid enteric resin, IV medical acrylic acid gastric solubleness resin etc.
The percentage by weight of metformin and gliclazide is between 16: 1~2: 1; In it is incapsulated, be finished product.
Embodiment 4
A kind of oral compound hypoglycemic medicine, every component and content are:
Metformin 200mg
Gliquidone 5.0mg
Right amount of auxiliary materials
Adjuvant can be zinc sulfate, zinc oxide, magnesium stearate, Pulvis Talci, starch, mannitol, Polyethylene Glycol, polyvinylpyrrolidone, hydroxypropyl methylcellulose, III medical acrylic acid enteric resin, IV medical acrylic acid gastric solubleness resin etc.
The percentage by weight of metformin and gliquidone is between 80: 1~15: 1; In it is incapsulated, be finished product.
Embodiment 5
A kind of oral compound hypoglycemic medicine, every component and content are:
Metformin 200mg
Glibornuride 1.0mg
Right amount of auxiliary materials
Adjuvant can be zinc sulfate, zinc oxide, magnesium stearate, Pulvis Talci, starch, mannitol, Polyethylene Glycol, polyvinylpyrrolidone, hydroxypropyl methylcellulose, III medical acrylic acid enteric resin, IV medical acrylic acid gastric solubleness resin etc.
The percentage by weight of metformin and glibornuride is between 500: 1~50: 1; In it is incapsulated, be finished product.
Embodiment 6
A kind of oral compound hypoglycemic medicine, every component and content are:
Metformin 200mg
Glibenclamide 1.0mg
Right amount of auxiliary materials
Adjuvant can be zinc sulfate, zinc oxide, magnesium stearate, Pulvis Talci, starch, mannitol, Polyethylene Glycol, polyvinylpyrrolidone, hydroxypropyl methylcellulose, III medical acrylic acid enteric resin, IV medical acrylic acid gastric solubleness resin etc.
The percentage by weight of metformin and glibenclamide is between 500: 1~50: 1; Tabletting on tablet machine is put into the coating pan blowing hot-air of rotation routinely, sprays thin film, and the component of thin film and percentage by weight are:
Medical IV acrylic acid gastric solubleness resin 1~30%
Polyethylene Glycol 0.1~3.0%
Hydroxypropyl methylcellulose 0.1~3.0%
Deionized water 0.1~3.0%
Magnesium stearate 0.1~2.5%
Pulvis Talci 0.1~2.5%
Ethanol 60~96%
Embodiment 7
A kind of oral compound hypoglycemic medicine, every component and content are:
Metformin 200mg
Glipizide 2.0mg
Right amount of auxiliary materials
Adjuvant can be zinc sulfate, zinc oxide, magnesium stearate, Pulvis Talci, starch, mannitol, Polyethylene Glycol, polyvinylpyrrolidone, hydroxypropyl methylcellulose, III medical acrylic acid enteric resin, IV medical acrylic acid gastric solubleness resin etc.
The percentage by weight of metformin and glipizide is between 250: 1~25: 1; Tabletting on tablet machine is put into the coating pan blowing hot-air of rotation routinely, sprays thin film, and the component of thin film and percentage by weight are:
Medical IV acrylic acid gastric solubleness resin 1~30%
Polyethylene Glycol 0.1~3.0%
Hydroxypropyl methylcellulose 0.1~3.0%
Deionized water 0.1~3.0%
Magnesium stearate 0.1~2.5%
Pulvis Talci 0.1~2.5%
Ethanol 60~96%
Embodiment 8
A kind of oral compound hypoglycemic medicine, every component and content are:
Metformin 200mg
Gliclazide 25mg
Right amount of auxiliary materials
Adjuvant can be zinc sulfate, zinc oxide, magnesium stearate, Pulvis Talci, starch, mannitol, Polyethylene Glycol, polyvinylpyrrolidone, hydroxypropyl methylcellulose, III medical acrylic acid enteric resin, IV medical acrylic acid gastric solubleness resin etc.
The percentage by weight of metformin and gliclazide is between 16: 1~2: 1; Tabletting on tablet machine is put into the coating pan blowing hot-air of rotation routinely, sprays thin film, and the component of thin film and percentage by weight are:
Medical IV acrylic acid gastric solubleness resin 1~30%
Polyethylene Glycol 0.1~3.0%
Hydroxypropyl methylcellulose 0.1~3.0%
Deionized water 0.1~3.0%
Magnesium stearate 0.1~2.5%
Pulvis Talci 0.1~2.5%
Ethanol 60~96%
Embodiment 9
A kind of oral compound hypoglycemic medicine, every component and content are:
Metformin 200mg
Gliquidone 5.0mg
Right amount of auxiliary materials
Adjuvant can be zinc sulfate, zinc oxide, magnesium stearate, Pulvis Talci, starch, mannitol, Polyethylene Glycol, polyvinylpyrrolidone, hydroxypropyl methylcellulose, III medical acrylic acid enteric resin, IV medical acrylic acid gastric solubleness resin etc.
The percentage by weight of metformin and gliquidone is between 80: 1~15: 1; Tabletting on tablet machine is put into the coating pan blowing hot-air of rotation routinely, sprays thin film, and the component of thin film and percentage by weight are:
Medical IV acrylic acid gastric solubleness resin 1~30%
Polyethylene Glycol 0.1~3.0%
Hydroxypropyl methylcellulose 0.1~3.0%
Deionized water 0.1~3.0%
Magnesium stearate 0.1~2.5%
Pulvis Talci 0.1~2.5%
Ethanol 60~96%
Embodiment 10
A kind of oral compound hypoglycemic medicine, every component and content are:
Metformin 200mg
Glibornuride 1.0mg
Right amount of auxiliary materials
Adjuvant can be zinc sulfate, zinc oxide, magnesium stearate, Pulvis Talci, starch, mannitol, Polyethylene Glycol, polyvinylpyrrolidone, hydroxypropyl methylcellulose, III medical acrylic acid enteric resin, IV medical acrylic acid gastric solubleness resin etc.
The percentage by weight of metformin and glibornuride is between 500: 1~50: 1; Tabletting on tablet machine is put into the coating pan blowing hot-air of rotation routinely, sprays thin film, and the component of thin film and percentage by weight are:
Medical IV acrylic acid gastric solubleness resin 1~30%
Polyethylene Glycol 0.1~3.0%
Hydroxypropyl methylcellulose 0.1~3.0%
Deionized water 0.1~3.0%
Magnesium stearate 0.1~2.5%
Pulvis Talci 0.1~2.5%
Ethanol 60~96%
Another object of the present invention is to provide a kind of production method of oral compound hypoglycemic medicine slow releasing tablet, the dual-sustained-release technical scheme that adopts skeleton slow release and film slow release and form capsule on the basis of embodiment 6~10 makes slow releasing tablet, now describes some concrete schemes.
Embodiment 11
The present invention is made up of label, basilar cloth film and release membranes.
The component of every label and content are:
Metformin 200mg
Glibenclamide 1.0mg
Right amount of auxiliary materials
Adjuvant can be zinc sulfate, zinc oxide, magnesium stearate, Pulvis Talci, starch, mannitol, Polyethylene Glycol, polyvinylpyrrolidone, hydroxypropyl methylcellulose, III medical acrylic acid enteric resin, IV medical acrylic acid gastric solubleness resin etc.
The component of basilar cloth film and percentage by weight are:
Medical IV acrylic acid gastric solubleness resin 1~30%
Polyethylene Glycol 0.1~3.0%
Hydroxypropyl methylcellulose 0.1~3.0%
Deionized water 0.1~3.0%
Magnesium stearate 0.1~2.5%
Pulvis Talci 0.1~2.5%
Ethanol 60~96%
The component of release membranes and percentage by weight are:
Acrylic resin latex 1~40%
Polyethylene Glycol 0.1~3.0%
Pulvis Talci 0.1~16%
Magnesium stearate 0.1~10%
Mannitol 0.1~5.0%
Tween 80 0~1.0%
Tris 0~1.0%
Deionized water 50~90%
Its production method is: ratio drying and adjuvant in above-mentioned label mix the back pelletizing press sheet, put into the coating pan blowing hot-air of rotation, make basilar cloth liquid by the component and the percentage by weight of above-mentioned basilar cloth film, and it is sprayed on the label; Make release membranes liquid by the component and the percentage by weight of above-mentioned release membranes again, it is sprayed on the label that is surrounded by basilar cloth film; Become finished product after drying, at last packing.
Embodiment 12
The present invention is made up of label, basilar cloth film and release membranes.
The component of every label and content are:
Metformin 200mg
Glipizide 2.0mg
Right amount of auxiliary materials
Adjuvant can be zinc sulfate, zinc oxide, magnesium stearate, Pulvis Talci, starch, mannitol, Polyethylene Glycol, polyvinylpyrrolidone, hydroxypropyl methylcellulose, III medical acrylic acid enteric resin, IV medical acrylic acid gastric solubleness resin etc.
The component of basilar cloth film and percentage by weight are:
Medical IV acrylic acid gastric solubleness resin 1~30%
Polyethylene Glycol 0.1~3.0%
Hydroxypropyl methylcellulose 0.1~3.0%
Deionized water 0.1~3.0%
Magnesium stearate 0.1~2.5%
Pulvis Talci 0.1~2.5%
Ethanol 60~96%
The component of release membranes and percentage by weight are:
Acrylic resin latex 1~40%
Polyethylene Glycol 0.1~3.0%
Pulvis Talci 0.1~16%
Magnesium stearate 0.1~10%
Mannitol 0.1~5.0%
Tween 80 0~1.0%
Tris 0~1.0%
Deionized water 50~90%
Its production method is: ratio drying and adjuvant in above-mentioned label mix the back pelletizing press sheet, put into the coating pan blowing hot-air of rotation, make basilar cloth liquid by the component and the percentage by weight of above-mentioned basilar cloth film, and it is sprayed on the label; Make release membranes liquid by the component and the percentage by weight of above-mentioned release membranes again, it is sprayed on the label that is surrounded by basilar cloth film; Become finished product after drying, at last packing.
Embodiment 13
The present invention is made up of label, basilar cloth film and release membranes.
The component of every label and content are:
Metformin 200mg
Gliclazide 25mg
Right amount of auxiliary materials
Adjuvant can be zinc sulfate, zinc oxide, magnesium stearate, Pulvis Talci, starch, mannitol, Polyethylene Glycol, polyvinylpyrrolidone, hydroxypropyl methylcellulose, III medical acrylic acid enteric resin, IV medical acrylic acid gastric solubleness resin etc.
The component of basilar cloth film and percentage by weight are:
Medical IV acrylic acid gastric solubleness resin 1~30%
Polyethylene Glycol 0.1~3.0%
Hydroxypropyl methylcellulose 0.1~3.0%
Deionized water 0.1~3.0%
Magnesium stearate 0.1~2.5%
Pulvis Talci 0.1~2.5%
Ethanol 60~96%
The component of release membranes and percentage by weight are:
Acrylic resin latex 1~40%
Polyethylene Glycol 0.1~3.0%
Pulvis Talci 0.1~16%
Magnesium stearate 0.1~10%
Mannitol 0.1~5.0%
Tween 80 0~1.0%
Tris 0~1.0%
Deionized water 50~90%
Its production method is: ratio drying and adjuvant in above-mentioned label mix the back pelletizing press sheet, put into the coating pan blowing hot-air of rotation, make basilar cloth liquid by the component and the percentage by weight of above-mentioned basilar cloth film, and it is sprayed on the label; Make release membranes liquid by the component and the percentage by weight of above-mentioned release membranes again, it is sprayed on the label that is surrounded by basilar cloth film; Become finished product after drying, at last packing.
Embodiment 14
The present invention is made up of label, basilar cloth film and release membranes.
The component of every label and content are:
Metformin 200mg
Gliquidone 5.0mg
Right amount of auxiliary materials
Adjuvant can be zinc sulfate, zinc oxide, magnesium stearate, Pulvis Talci, starch, mannitol, Polyethylene Glycol, polyvinylpyrrolidone, hydroxypropyl methylcellulose, III medical acrylic acid enteric resin, IV medical acrylic acid gastric solubleness resin etc.
The component of basilar cloth film and percentage by weight are:
Medical IV acrylic acid gastric solubleness resin 1~30%
Polyethylene Glycol 0.1~3.0%
Hydroxypropyl methylcellulose 0.1~3.0%
Deionized water 0.1~3.0%
Magnesium stearate 0.1~2.5%
Pulvis Talci 0.1~2.5%
Ethanol 60~96%
The component of release membranes and percentage by weight are:
Acrylic resin latex 1~40%
Polyethylene Glycol 0.1~3.0%
Pulvis Talci 0.1~16%
Magnesium stearate 0.1~10%
Mannitol 0.1~5.0%
Tween 80 0~1.0%
Tris 0~1.0%
Deionized water 50~90%
Its production method is: ratio drying and adjuvant in above-mentioned label mix the back pelletizing press sheet, put into the coating pan blowing hot-air of rotation, make basilar cloth liquid by the component and the percentage by weight of above-mentioned basilar cloth film, and it is sprayed on the label; Make release membranes liquid by the component and the percentage by weight of above-mentioned release membranes again, it is sprayed on the label that is surrounded by basilar cloth film; Become finished product after drying, at last packing.
Embodiment 15
The present invention is made up of label, basilar cloth film and release membranes.
The component of every label and content are:
Metformin 200mg
Glibornuride 1.0mg
Right amount of auxiliary materials
Adjuvant can be zinc sulfate, zinc oxide, magnesium stearate, Pulvis Talci, starch, mannitol, Polyethylene Glycol, polyvinylpyrrolidone, hydroxypropyl methylcellulose, III medical acrylic acid enteric resin, IV medical acrylic acid gastric solubleness resin etc.
The component of basilar cloth film and percentage by weight are:
Medical IV acrylic acid gastric solubleness resin 1~30%
Polyethylene Glycol 0.1~3.0%
Hydroxypropyl methylcellulose 0.1~3.0%
Deionized water 0.1~3.0%
Magnesium stearate 0.1~2.5%
Pulvis Talci 0.1~2.5%
Ethanol 60~96%
The component of release membranes and percentage by weight are:
Acrylic resin latex 1~40%
Polyethylene Glycol 0.1~3.0%
Pulvis Talci 0.1~16%
Magnesium stearate 0.1~10%
Mannitol 0.1~5.0%
Tween 80 0~1.0%
Tris 0~1.0%
Deionized water 50~90%
Its production method is: ratio drying and adjuvant in above-mentioned label mix the back pelletizing press sheet, put into the coating pan blowing hot-air of rotation, make basilar cloth liquid by the component and the percentage by weight of above-mentioned basilar cloth film, and it is sprayed on the label; Make release membranes liquid by the component and the percentage by weight of above-mentioned release membranes again, it is sprayed on the label that is surrounded by basilar cloth film; Become finished product after drying, at last packing.
Clinical efficacy of the present invention:
A kind of oral compound hypoglycemic medicine, every contains metformin 200mg, glibenclamide 1.0mg.
Case (1): open * *, the man, 56 years old, suffered from diabetes 3 years, oral always " glyburide ", i.e. glibenclamide sheet, every day 10mg, blood glucose can be reduced to normal range.But spirit is poor, and sense is dizzy, limbs fatigue.After this change 2 of clothes " compound hypoglycemic medicine " every day, add " potassium magnesium controlled-release tablet " 6.The back spirit improvement of 1 week, no giddy and limbs fatigue, blood glucose is normal.Over nearly 2 years, the patient is in high spirits, has rosy cheeks, and blood glucose is normal always, the not normal generation of the no rhythm of the heart.
Case (2): 5 * *, the woman, 42 years old, suffer from surplus the diabetes 10 year, oral always " glipizide ", i.e. glipizide tablet, every day, 15mg needed intravenous drip insulin 25u sometimes, and blood glucose just can be reduced to normal range.Spirit is poor, shallow complexion, and sense is dizzy, and left limb is weak.Change 3 of clothes " compound hypoglycemic medicine " every day before 1 year, adds " potassium magnesium controlled-release tablet " 6, the back spirit improvement of 1 week, the dizzy and weak disappearance of left limb.Existing oral " compound hypoglycemic medicine " reduced to 1~2 of every day, and still oral " potassium magnesium controlled-release tablet " 6 do not need the intravenous drip insulin, and be in high spirits, have rosy cheeks, and no giddy and limbs fatigue, blood glucose is normal.
Claims (10)
1, a kind of oral compound hypoglycemic medicine is made up of biguanides and second filial generation sulfonylurea drugs and adjuvant.
2, oral compound hypoglycemic medicine according to claim 1 can be produced and is capsule, tablet or slow releasing tablet.
3, oral compound hypoglycemic medicine according to claim 1, biguanides can be metformin or phenformin, first-selected metformin.
4, oral compound hypoglycemic medicine according to claim 1, second filial generation sulfonylurea drugs can be in the medicines such as glibenclamide, gliclazide, glipizide, gliquidone and glibornuride a kind of.
5, oral compound hypoglycemic medicine according to claim 1, adjuvant can be zinc sulfate, zinc oxide, magnesium stearate, Pulvis Talci, starch, mannitol, Polyethylene Glycol, polyvinylpyrrolidone, hydroxypropyl methylcellulose, III medical acrylic acid enteric resin, IV medical acrylic acid gastric solubleness resin etc.
6, oral compound hypoglycemic medicine according to claim 1, the ratio of metformin and glibenclamide are 500: 1~100: 1.
7, oral compound hypoglycemic medicine according to claim 1, the ratio of metformin and gliclazide are 3: 1~15: 1.
8, oral compound hypoglycemic medicine according to claim 1, the ratio of metformin and glipizide are 250: 1~50: 1.
9, oral compound hypoglycemic medicine according to claim 1, the ratio of metformin and gliquidone are 83: 1~16: 1.
10, oral compound hypoglycemic medicine according to claim 1, the ratio of metformin and glibornuride are 500: 1~100: 1.
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CN 02108983 CN1451385A (en) | 2002-04-18 | 2002-04-18 | Oral compound hypoglycemic medicine |
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CN 02108983 CN1451385A (en) | 2002-04-18 | 2002-04-18 | Oral compound hypoglycemic medicine |
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Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1682737B (en) * | 2005-03-01 | 2010-12-29 | 沈阳药科大学 | Compound dimethylbiguanide/glipizide control release tablet and preparing method |
CN104906115A (en) * | 2015-06-18 | 2015-09-16 | 青岛海之星生物科技有限公司 | Melbine and gliquidone compound sustained-release tablet and preparation method thereof |
CN104906114A (en) * | 2015-06-18 | 2015-09-16 | 青岛海之星生物科技有限公司 | Metformin-gliquidone compound sustained-release capsule and preparation method thereof |
CN105030793A (en) * | 2015-08-25 | 2015-11-11 | 瑞阳制药有限公司 | Metformin hydrochloride and glibenclamide capsule and preparation method thereof |
CN105832708A (en) * | 2016-05-26 | 2016-08-10 | 江西京通美联药业有限公司 | Sustained-release preparation for treating diabetes and preparation method thereof |
-
2002
- 2002-04-18 CN CN 02108983 patent/CN1451385A/en active Pending
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1682737B (en) * | 2005-03-01 | 2010-12-29 | 沈阳药科大学 | Compound dimethylbiguanide/glipizide control release tablet and preparing method |
CN104906115A (en) * | 2015-06-18 | 2015-09-16 | 青岛海之星生物科技有限公司 | Melbine and gliquidone compound sustained-release tablet and preparation method thereof |
CN104906114A (en) * | 2015-06-18 | 2015-09-16 | 青岛海之星生物科技有限公司 | Metformin-gliquidone compound sustained-release capsule and preparation method thereof |
CN105030793A (en) * | 2015-08-25 | 2015-11-11 | 瑞阳制药有限公司 | Metformin hydrochloride and glibenclamide capsule and preparation method thereof |
CN105832708A (en) * | 2016-05-26 | 2016-08-10 | 江西京通美联药业有限公司 | Sustained-release preparation for treating diabetes and preparation method thereof |
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