CN1602873A - Sustained release preparation of glipizide/metformin hydrochloride and its preparation method - Google Patents
Sustained release preparation of glipizide/metformin hydrochloride and its preparation method Download PDFInfo
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- CN1602873A CN1602873A CN 200410055411 CN200410055411A CN1602873A CN 1602873 A CN1602873 A CN 1602873A CN 200410055411 CN200410055411 CN 200410055411 CN 200410055411 A CN200410055411 A CN 200410055411A CN 1602873 A CN1602873 A CN 1602873A
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- glipizide
- metformin hydrochloride
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Abstract
The invention relates to a compound sustained-release preparation composed of glipizide and metformin hydrochloride, and its preparing method. The weight ratio of glipizide to metformin hydrochloride is 1 : 100-200, the best ratio is 1:100 and it adds a proper amount of medicinal auxiliary to the preparation. The compound sustained-release tablet can not only make advantages complementation on glipizide and metformin hydrochloride, promote and increase secretion of beta-cell insulin, and raise the utilization of glucose in tissues, such as muscle, etc, but also reduce the stimulus of metformin hydrochloride to stomach intestine, and largely strengthen curative effect and drug application safety.
Description
[technical field]
The present invention relates to a kind of antihypelipidemic preparation and be glipizide diabecron sustained-release preparation with and preparation method thereof.
[background technology]
The glipizide metformin hydrochloride tablet is a kind of glipizide and these two kinds compound preparations that are used for the treatment of the oral hyperglycemia medicine of type 2 diabetes mellitus of metformin hydrochloride of containing that Bristol-Myers Squibb company develops, first get permission listing in the U.S. in October, 2002, commodity are called Metaglip , the listing dosage form is an oral tablet, and specification has three kinds of (glipizide/metformin hydrochloride) 2.5mg/250mg, 2.5mg/500mg, 5mg/500mg.At present, domestic Glipizide sustained-release sheet, capsule and the diabecron sustained-release tablet that had gone on the market already and be used for the treatment of diabetes, the compound preparation of glipizide metformin hydrochloride is not still gone public.Slow releasing tablet has protective effect to stomach; Active component in the compound preparation can play synergism.Also not having at present to have protective effect and active component can play synergistic preparation to stomach.
[summary of the invention]
The object of the present invention is to provide a kind of determined curative effect, safe, the compliance of taking medicine is good can protective effect be arranged and active component can play synergistic hypoglycemic compound slow releasing preparation and preparation method thereof to stomach.
On the basis of Glipizide sustained-release sheet, capsule and the diabecron sustained-release tablet of Shang Shi glipizide metformin hydrochloride tablet and domestic listing, it is the slow releasing preparation of principal agent that my company has developed with glipizide and metformin hydrochloride through great deal of experimental abroad.
Scheme provided by the invention is: a kind of blood sugar lowering slow releasing preparation, contain glipizide and metformin hydrochloride, and its weight ratio is 1: 100-200.Pharmaceutic adjuvant has: a kind of in hydroxyethyl-cellulose, hydroxypropyl emthylcellulose, starch, pregelatinized Starch, dextrin, sucrose, sodium carboxymethyl cellulose, microcrystalline Cellulose, ethanol, magnesium stearate, carboxymethylstach sodium, the cross-linked carboxymethyl cellulose or several.Pharmaceutic adjuvant is as filler commonly used in framework material and the preparation process, lubricant, wetting agent, binding agent etc.This blood sugar lowering slow releasing preparation can be slow releasing tablet or slow releasing capsule.
The preparation method of the compound antihypelipidemic slow releasing preparation of mentioning among the present invention is as follows:
Take by weighing glipizide, the metformin hydrochloride of recipe quantity, pulverize, sieve,, make soft material, granulate with an amount of pharmaceutic adjuvant mix homogeneously, drying, granulate, tabletting or filling detect, packing.
The compound slow-release tablet of glipizide and metformin hydrochloride, not only make glipizide and metformin hydrochloride to have complementary advantages, promote to increase the beta cell secretion of insulin, increase the utilization of glucose at tissues such as muscle, suppress the decomposition of hepatic glycogen and the heteroplasia effect of glycogen, reduce the opposing of insulin, but also can reduce metformin hydrochloride, improve the curative effect and the drug safety of medicine greatly the gastrointestinal zest.
[specific embodiment]
The invention will be further described below in conjunction with embodiment.
Sustained-release tablet recipe one:
Glipizide 2.5g, metformin hydrochloride 250.0g, right amount of auxiliary materials is made 1000 altogether.
Sustained-release tablet recipe two:
Glipizide 2.5g, metformin hydrochloride 500.0g, right amount of auxiliary materials is made 1000 altogether.
Sustained-release tablet recipe three:
Glipizide 5.0g, metformin hydrochloride 500.0g, right amount of auxiliary materials is made 1000 altogether.
Slow releasing capsule prescription one:
Glipizide 2.5g, metformin hydrochloride 250.0g, right amount of auxiliary materials is made 1000 altogether.
Slow releasing capsule prescription two:
Glipizide 2.5g, metformin hydrochloride 500.0g, right amount of auxiliary materials is made 1000 altogether.
Glipizide 5.0g, metformin hydrochloride 500.0g, right amount of auxiliary materials is made 1000 altogether.Slow releasing capsule prescription three:
What be prepared from according to above prescription is the compound antihypelipidemic slow releasing tablet of principal agent or the first-line treatment that slow releasing capsule is applicable to type 2 diabetes mellitus with glipizide and metformin hydrochloride, ancillary drug as diet and motion, can be not among the type 2 diabetes mellitus patient because of diet and motion Satisfactory Control in the hyperglycemia symptom, effective glucose level control; As diet, motion, and the previous tretament of sulfonylureas or biguanides fails to control fully type 2 diabetes mellitus patient's blood sugar level, and the blood sugar lowering slow releasing preparation among the present invention is applicable to second line treatment.
The usage and dosage of compound antihypelipidemic slow releasing preparation when first-line treatment of mentioning among the present invention is:
Oral, 30min takes before dinner, and single dose is 5mg glipizide/500mg metformin hydrochloride, and a day maximal dose is no more than 10mg glipizide/1000mg metformin hydrochloride.
The usage and dosage of compound antihypelipidemic slow releasing preparation when second line treatment of mentioning among the present invention is:
Fail the patient of complete blood sugar control for single glipizide (or other sulfonylureas) or metformin hydrochloride, the suggestion initial dose of the compound antihypelipidemic slow releasing preparation among the present invention is 2.5mg/250mg, single dose is 5mg glipizide/500mg metformin hydrochloride afterwards, and 30min takes before dinner.
Be preparation method embodiment below
Embodiment 1:
According to sustained-release tablet recipe 1, take by weighing the glipizide (pulverizing 100 mesh sieves) and an amount of carmethose mix homogeneously of recipe quantity, add by recipe quantity then and pulverized the metformin hydrochloride powder of 100 mesh sieves and an amount of hypromellose mix homogeneously, add again and be no more than 5% hypromellose aqueous solution and make soft material in right amount, crossing 20 mesh sieves granulates, dry 4h under 60 ℃, cross 16 mesh sieve granulate, add an amount of magnesium stearate always be mixed even, detection level, it is heavy to calculate sheet, select corresponding punch die tabletting, after the assay was approved, aluminum-plastic packaged then, the dress box, vanning, packing, warehouse-in after the assay was approved.
Embodiment 2:
According to sustained-release tablet recipe 2, take by weighing the glipizide (pulverizing 100 mesh sieves) and an amount of carmethose mix homogeneously of recipe quantity, add by recipe quantity then and pulverized the metformin hydrochloride powder of 100 mesh sieves and an amount of hypromellose mix homogeneously, add again and be no more than 5% hypromellose aqueous solution and make soft material in right amount, crossing 20 mesh sieves granulates, dry 4h under 60 ℃, cross 16 mesh sieve granulate, add an amount of magnesium stearate always be mixed even, detection level, it is heavy to calculate sheet, select corresponding punch die tabletting, after the assay was approved, aluminum-plastic packaged then, the dress box, vanning, packing, warehouse-in after the assay was approved.
Embodiment 3:
According to sustained-release tablet recipe 3, take by weighing the glipizide (pulverizing 100 mesh sieves) and an amount of carmethose mix homogeneously of recipe quantity, add by recipe quantity then and pulverized the metformin hydrochloride powder of 100 mesh sieves and an amount of hypromellose mix homogeneously, add again and be no more than 5% hypromellose aqueous solution and make soft material in right amount, crossing 20 mesh sieves granulates, dry 4h under 60 ℃, cross 16 mesh sieve granulate, add an amount of magnesium stearate always be mixed even, detection level, it is heavy to calculate sheet, select corresponding punch die tabletting, after the assay was approved, aluminum-plastic packaged then, the dress box, vanning, packing, warehouse-in after the assay was approved.
Embodiment 4:
According to slow releasing capsule prescription 4, take by weighing the glipizide (pulverizing 100 mesh sieves) of recipe quantity and the carmethose mix homogeneously of recipe quantity, add by recipe quantity then and pulverized the metformin hydrochloride powder of 100 mesh sieves and the hypromellose mix homogeneously of recipe quantity, add 2% hypromellose aqueous solution again and make soft material in right amount, crossing 20 mesh sieves granulates, dry 4h under 60 ℃, cross 16 mesh sieve granulate, add a spot of magnesium stearate and always be mixed evenly, detect drug content, determine to be filled into capsule after the loading amount, then the polishing, detect qualified after, carry out aluminum-plastic packaged, the dress box, vanning, packing, warehouse-in after the assay was approved.
Embodiment 5:
According to slow releasing capsule prescription 5, take by weighing the glipizide (pulverizing 100 mesh sieves) of recipe quantity and the carmethose mix homogeneously of recipe quantity, add by recipe quantity then and pulverized the metformin hydrochloride powder of 100 mesh sieves and the hypromellose mix homogeneously of recipe quantity, add 2% hypromellose aqueous solution again and make soft material in right amount, crossing 20 mesh sieves granulates, dry 4h under 60 ℃, cross 16 mesh sieve granulate, add a spot of magnesium stearate and always be mixed evenly, detect drug content, determine to be filled into capsule after the loading amount, then the polishing, detect qualified after, carry out aluminum-plastic packaged, the dress box, vanning, packing, warehouse-in after the assay was approved.
Embodiment 6:
According to slow releasing capsule prescription 6, take by weighing the glipizide (pulverizing 100 mesh sieves) of recipe quantity and the carmethose mix homogeneously of recipe quantity, add by recipe quantity then and pulverized the metformin hydrochloride powder of 100 mesh sieves and the hypromellose mix homogeneously of recipe quantity, add 2% hypromellose aqueous solution again and make soft material in right amount, crossing 20 mesh sieves granulates, dry 4h under 60 ℃, cross 16 mesh sieve granulate, add a spot of magnesium stearate and always be mixed evenly, detect drug content, determine to be filled into capsule after the loading amount, then the polishing, detect qualified after, carry out aluminum-plastic packaged, the dress box, vanning, packing, warehouse-in after the assay was approved.
Compare the slow releasing preparation that is prepared from according to the difference prescription, some slow releasing tablet or slow releasing capsule, excessive being not suitable for of profile swallowed, and we think that best prescription should be
Glipizide 2.5g, metformin hydrochloride 250.0g, right amount of auxiliary materials is made 1000 altogether.
Claims (6)
1, a kind of blood sugar lowering slow releasing preparation,, it is characterized in that containing glipizide and metformin hydrochloride.
2, blood sugar lowering slow releasing preparation according to claim 1 is characterized in that described blood sugar lowering slow releasing preparation is slow releasing tablet or slow releasing capsule.
3, profit requires 1 described blood sugar lowering slow releasing preparation, it is characterized in that described glipizide and metformin hydrochloride weight ratio are 1: 100-200.
4,, it is characterized in that described glipizide and metformin hydrochloride weight ratio are 1: 100 according to the described blood sugar lowering slow releasing preparation of claim 1.
5, a kind of preparation method as claim 1,2,3 or 4 described blood sugar lowering slow releasing preparation is characterized in that lattice take by weighing row pyrazine and metformin hydrochloride in proportion,, granulates granulate, total mixing, tabletting, packing with an amount of pharmaceutic adjuvant mixing.
6, the preparation method of blood sugar lowering slow releasing preparation according to claim 5 is characterized in that the pharmaceutic adjuvant that adds has: a kind of in hydroxyethyl-cellulose, hydroxypropyl emthylcellulose, starch, pregelatinized Starch, dextrin, sucrose, sodium carboxymethyl cellulose, microcrystalline Cellulose, ethanol, magnesium stearate, carboxymethylstach sodium, the cross-linked carboxymethyl cellulose or several.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410055411 CN1602873A (en) | 2004-07-23 | 2004-07-23 | Sustained release preparation of glipizide/metformin hydrochloride and its preparation method |
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| Application Number | Priority Date | Filing Date | Title |
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| CN 200410055411 CN1602873A (en) | 2004-07-23 | 2004-07-23 | Sustained release preparation of glipizide/metformin hydrochloride and its preparation method |
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| CN1602873A true CN1602873A (en) | 2005-04-06 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1331470C (en) * | 2005-09-29 | 2007-08-15 | 周卓和 | Method for preparing high stripping-degree hautriwaic glipizide capsule |
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2004
- 2004-07-23 CN CN 200410055411 patent/CN1602873A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1331470C (en) * | 2005-09-29 | 2007-08-15 | 周卓和 | Method for preparing high stripping-degree hautriwaic glipizide capsule |
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