CN102119931B - Novel metformin hydrochloride slow-releasing tablet and preparation method thereof - Google Patents
Novel metformin hydrochloride slow-releasing tablet and preparation method thereof Download PDFInfo
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- CN102119931B CN102119931B CN 201110041177 CN201110041177A CN102119931B CN 102119931 B CN102119931 B CN 102119931B CN 201110041177 CN201110041177 CN 201110041177 CN 201110041177 A CN201110041177 A CN 201110041177A CN 102119931 B CN102119931 B CN 102119931B
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Abstract
The invention provides a novel metformin hydrochloride slow-releasing tablet and a preparation method thereof. The slow-releasing tablet comprises the following components by weight percent: 66.6%-73.5% of metformin hydrochloride, 30.9%-21.5% chitosan, 2.0%-4.0% of copolymerization and 0.5%-1.0% of superfine silica powder. The dry granulating technique is adopted in the preparation method and the preparation method comprises the following steps: uniformly mixing the metformin hydrochloride, chitosan, copolymerization and superfine silica powder in proportion according to the prescription, granulating by using a dry granulating machine, adding superfine silica powder and uniformly mixing, and then pressing the mixture into tablet, thereby acquiring the novel metformin hydrochloride slow-releasing tablet.
Description
Technical field
The present invention relates to a kind of slow releasing agent for the treatment of the hyperglycemia medicine and preparation method thereof, is a kind of diabecron sustained-release tablet and preparation method thereof specifically.
Background technology
Metformin hydrochloride is biguanides.Biguanides is the effective oral hypoglycemic thing of generally recognized as safe in the world, routine administration for the type ii diabetes of growing up at present, its blood sugar lowering mechanism is main by strengthening surrounding tissue to picked-up and the utilization of glucose, the anaerobic glycolysis of muscular tissue is increased, and aerobic metabolism is constant, and it concentrates on intestinal wall, suppress glucose in the absorption of intestinal, suppress glyconeogenesis, suppress the release of glucagon or the effect of inhibition insulin anta gonists, and increase the sensitivity of insulin.Metformin hydrochloride to islet function normally or the diabetes of having lost hypoglycemic activity is arranged per capita, without hypoglycemic activity, irrelevant with normal pancreatic function and beta Cell of islet to the normal person.
The metformin hydrochloride common dose is large, be 500mg/ time, because its half-life in human body is shorter, for keeping effective blood drug concentration, clinical oral administration ordinary tablet every day 2-3 time, each 1-2 sheet has brought inconvenience to the patient, also causes adverse reaction rate high because blood drug level just rises and falls simultaneously, be necessary its slow releasing preparation is studied for this reason, improved, purpose is to reduce to take number of times, makes blood drug level gently to reduce the untoward reaction of medicine.
Because metformin hydrochloride is the very large medicine of a kind of water solublity, and dosage is larger, therefore, make slow releasing tablet great difficulty is arranged, adopt at present common slow-release material hydroxypropyl emthylcellulose, sodium carboxymethyl cellulose etc., the slow-release material use amount is excessive, cause sheet great, the slow release index does not reach quality index requirement in the American Pharmacopeia USP32 standard yet, needs particularly to control in 24 hours that steadily to discharge, keep therapeutic effect that blood drug level stably makes it to reach good with certain speed be difficulty.
Said diabecron sustained-release tablet is the macromolecular material of pharmaceutically commonly using that adopts hydroxypropyl emthylcellulose, ethyl cellulose, sodium carboxymethyl cellulose etc. common among the patent CN1391890A, to form the slow releasing agent of gel-type, and adopt organic carboxyl acid or alcohol under 50-60 ℃ of molten condition, to granulate, technological operation is extremely inconvenient, and said preparation also is difficult to reach the purpose that the control medicine steadily discharges with certain speed.
Said diabecron sustained-release tablet is to have adopted hydroxypropyl emthylcellulose and micropowder ethyl cellulose to do slow-release material among the patent CN1543937C, this slow-release material consumption is less, and along with after the metformin dissolving, produce " scoring " in the hydrated gel layer that slow-release material forms thus affected slow release effect, the purpose of the steady release that is difficult to reach desirable.Quality index does not reach the requirement of American Pharmacopeia USP32 version drug standard.And the wet granulation technique of process using routine, technique is loaded down with trivial details.
The diabecron sustained-release tablet of the product commodity of Mei during the U.S. hundred-Shi Guibao company (BMS) " Glucophage XR " by name, it is to use hydroxypropyl emthylcellulose, sodium carboxymethyl cellulose, microcrystalline Cellulose, what magnesium stearate etc. were made is a kind of gel Barrier hydrophilic skeleton slow releasing agent, after oral tablets is met water, hydroxypropyl emthylcellulose, these macromolecular materials that form skeleton of sodium carboxymethyl cellulose form rapidly the layer of gel barrier layer on the surface of tablet, and the release of medicine is controlled by two kinds of mechanism of diffusion of gel layer by corrosion and the medicine of gel layer.Adopt the slow releasing tablet of this mechanism preparation, the large usage quantity of skeleton macromolecular material causes the heavy sheet type of sheet excessive.The sheet of " Glucophage XR " product heavily is 1g, and wherein active drug is 0.5g, needs granulate to swallow when taking, and can not bite into pieces, and the heavy too large tablet of the sheet of must swallowing like this is very inconvenient, especially to Chinese, to the old people.
Therefore be necessary the improvement technology, development slice type is less, work simplification, cost are lower, only take diabecron sustained-release tablet once every day.
Summary of the invention
The purpose of this invention is to provide a kind of diabecron sustained-release tablet and preparation method thereof, this slow releasing tablet sheet type less (sheet is heavy is down to the 0.7g/ sheet by original 1.2g/ sheet), every day only take once, and employing dry granulation technology, allow preparation technology simplify, cost, cheap selling is served the common people.
For implementing the technical scheme that purpose of the present invention adopts be: formed by metformin hydrochloride 66.6%-73.5%, chitosan 30.9%-21.5%, copolyvidone 2.0%-4.0%, micropowder silica gel 0.5%-1.0%; its preparation method is to adopt dry granulation technology; behind the metformin hydrochloride of supplementary material recipe quantity, chitosan, copolyvidone mix homogeneously, granulate, add behind the micropowder silica gel mixing tabletting and get final product with dry granulating machine.
The metformin hydrochloride crude drug fineness 80-100 order that the present invention adopts, the specification of chitosan are that high density 120 orders, copolyvidone are KollidonVA 64.
The key technology point is in the supplementary material prescription of the present invention, adoption of innovation marine organisms natural material-chitosan do slow-release material, chitosan is a kind of natural polycation alkaline polysaccharide, it is the main component of the crustacean shells such as shrimp, Eriocheir sinensis, extensively be present in nature, chitosan has good biocompatibility and biodegradability, and its catabolite is harmless to health.
Chitosan is in being applied to Metformin Extended-release Tablets, we find in the test, this slow-release material forms the gel barrier layer retardance release except showing, also can and medicine between form to a certain degree adsorption by hydrogen bond, its slow release efficient significantly increases like this, has therefore realized the heavy requirement of decrease sheet.Experiment shows, the sheet of the diabecron sustained-release tablet of pastille 500mg heavily is reduced to the 0.7g/ sheet from the 1.2g/ sheet, and importantly according to the check of USP standard USP32 version, product index is all up to specification, so this product quality has reached international standard.
Second key problem in technology point of the present invention is; owing to adopting this special adjuvant of copolyvidone; and adopted dry granulation technology to replace traditional wet granulation technique; the equipment that uses is the dry granulating machine that German Alexandria produces; direct pressing becomes dried granule, after carry out tabletting, avoided like this process of preparation wet granular and oven dry; thereby reduced production cost, greatly reduced the market price of slow releasing tablet.Table 1 is the gap of diabecron sustained-release tablet Sino-U.S. standards of pharmacopoeia; Table 2 is that the commercially available 0.5 several Metformin Extended-release Tablets that restrain specification are carried out sheet weight, price, mass ratio, with USP standard commercially available domestic metformin HCI extended release is tested, and major part does not meet standard-required.
The gap of table 1 diabecron sustained-release tablet Sino-U.S. standards of pharmacopoeia
The commercially available 0.5 gram specification Metformin Extended-release Tablets of table 2, sheet weight, price, mass ratio are
(annotate: product reaches standard-required and beats " √ " otherwise " * ")
Advantage of the present invention is, owing to having adopted natural biological skeleton slow-release material chitosan, itself is useful to health, and because it can also form adsorption by hydrogen bond with medicine, the consumption of slow-release material is greatly reduced, only need sheet heavy 21% just can reach the steadily purpose of release of control medicine, sheet heavily is down to 0.7 g/piece from 1.2 g/pieces, swallow conveniently, adopt USP standard USP32 check, product quality is fully up to specification.
The specific embodiment
Embodiment 1
Take by weighing metformin hydrochloride 50.0kg (fineness 80-100 order); chitosan 17.2kg (specification: high density 120 orders); copolyvidone (being KollidonVA 64) 2.45Kg; three-dimensional hybrid 2 hours is to evenly; the vertical dry-process granulator that produces with German Alexandria makes dried granule; after adding micropowder silica gel 0.35Kg mixing, tabletting obtains 100,000.Every hydrochloric metformin 500mg, sheet heavily are 698mg.
Claims (2)
1. diabecron sustained-release tablet is characterized in that being comprised of the supplementary material of following percentage by weight:
The specification of metformin hydrochloride crude drug fineness 80～100 orders, chitosan is that high density 120 orders, copolyvidone are KollidonVA 64, adopts the dry granulation technology preparation.
2. the preparation method of a diabecron sustained-release tablet claimed in claim 1 is characterized in that the metformin hydrochloride of supplementary material recipe quantity, chitosan, copolyvidone mix homogeneously, carries out dry granulation, obtains adding behind the granule behind the micropowder silica gel mix homogeneously tabletting and get final product with dry granulating machine.
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| CN 201110041177 CN102119931B (en) | 2011-02-21 | 2011-02-21 | Novel metformin hydrochloride slow-releasing tablet and preparation method thereof |
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| CN 201110041177 CN102119931B (en) | 2011-02-21 | 2011-02-21 | Novel metformin hydrochloride slow-releasing tablet and preparation method thereof |
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| CN102119931B true CN102119931B (en) | 2013-02-13 |
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| CN106176652B (en) * | 2016-09-28 | 2020-03-13 | 重庆科瑞南海制药有限责任公司 | Metformin hydrochloride sustained release tablet and preparation method thereof |
| CN106860416A (en) * | 2017-03-01 | 2017-06-20 | 华益药业科技(安徽)有限公司 | Metformin hydrochloride tablet and preparation method thereof |
| CN106963740A (en) * | 2017-03-27 | 2017-07-21 | 华益药业科技(安徽)有限公司 | A kind of diabecron sustained-release tablet and preparation method thereof |
| CN111388438A (en) * | 2020-05-08 | 2020-07-10 | 福建东瑞制药有限公司 | Metformin hydrochloride sustained release tablet and preparation method thereof |
| CN113598345A (en) * | 2021-08-06 | 2021-11-05 | 武汉英纽林生物科技有限公司 | Functional food containing linseed powder and capable of interfering with hyperglycemia by combining with metformin |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003002151A1 (en) * | 2001-06-26 | 2003-01-09 | Farmatron Ltd. | Oral pharmaceutical compositions with modified release of the active ingredient |
| CN101057849A (en) * | 2007-02-27 | 2007-10-24 | 齐齐哈尔医学院 | Slow-releasing preparation containing metformin hydrochloride and glipizide and its preparation method |
| CN101658501A (en) * | 2008-08-26 | 2010-03-03 | 北京科信必成医药科技发展有限公司 | Minocycline hydroehloride sustained- release tablets and preparation method thereof |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003002151A1 (en) * | 2001-06-26 | 2003-01-09 | Farmatron Ltd. | Oral pharmaceutical compositions with modified release of the active ingredient |
| CN101057849A (en) * | 2007-02-27 | 2007-10-24 | 齐齐哈尔医学院 | Slow-releasing preparation containing metformin hydrochloride and glipizide and its preparation method |
| CN101658501A (en) * | 2008-08-26 | 2010-03-03 | 北京科信必成医药科技发展有限公司 | Minocycline hydroehloride sustained- release tablets and preparation method thereof |
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Denomination of invention: Metformin hydrochloride sustained release tablets and its preparation method Effective date of registration: 20220630 Granted publication date: 20130213 Pledgee: Shandong Shouguang Rural Commercial Bank Co.,Ltd. Pledgor: SHOUGUANG FUKANG PHARMACEUTICAL Co.,Ltd. Registration number: Y2022980009599 |