CN104622822A - Metformin hydrochloridetablet composition and preparation method thereof - Google Patents
Metformin hydrochloridetablet composition and preparation method thereof Download PDFInfo
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- CN104622822A CN104622822A CN201410813845.2A CN201410813845A CN104622822A CN 104622822 A CN104622822 A CN 104622822A CN 201410813845 A CN201410813845 A CN 201410813845A CN 104622822 A CN104622822 A CN 104622822A
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- metformin hydrochloride
- hyprolose
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- magnesium stearate
- hypromellose
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Abstract
The invention belongs to the technical field of medicine preparations, and particularly relates to a metformin hydrochloridetablet composition. The metformin hydrochloridetablet composition is characterized by being prepared from metformin hydrochloride, dextrin, hydroxypropylcellulose, a hydroxypropyl methylcellulosealcohol solution, magnesium stearate and talcum powder. The composition is highly consistent with an original trituration in dissolution curve, and has good stability.
Description
Technical field
The invention belongs to technical field of pharmaceuticals, be specifically related to a kind of metformin hydrochloride tablet agent compositions.
Background technology
Metformin hydrochloride tablet is biguanides.Not the concentration by stimulating beta Cell of islet to increase insulin; but directly act on the metabolic process of sugar; promote the anerobic glycolysis of sugar; increase the peripheral tissues such as muscle, fat to the picked-up of glucose and utilization; thus protect islet beta cell function in damaged condition from further infringement, be conducive to the long-term control of diabetes.It suppresses intestinal absorption glucose, and suppresses hepatic gluconeogenesis, reduces glycogen and exports, and blood sugar in diabetic patients and glycolated hemoglobin can be made to reduce, without the effect impelling lipogenesis, to normal person without obvious hypoglycemic activity.Compare with sulfonylurea hypoglycemic agent, owing to not stimulating insulin secretion, seldom cause hypoglycemia, and synergism when both share, can be played, to improve hypoglycemic curative effect.Clinical indication is mainly: the type 2 diabetes mellitus that diet alone and sports can not effectively control, particularly fat type 2 diabetes mellitus; For 1 type or type 2 diabetes mellitus, this product and insulin share, and can increase the hypoglycemic activity of insulin, reduce insulin dosage, prevent hypoglycemia from occurring; Also can share with sulphanylureas oral hypoglycemic, tool synergism.
The former product that grinds of metformin hydrochloride tablet is researched and developed by Shi Guibao company, domestic at present have a lot of imitated metformin hydrochloride tablet manufacturer, because metformin hydrochloride tablet unitary tablet drug dose is large, addible adjuvant is relatively less, therefore how on the basis ensureing medicine molding, the stripping of medicine controlled well is key factor, there is research (" comparison of Greasy Wool diformin tablet dissolution ", " medical Leader ", the 24th volume the 6th phase) show that the stripping of import diformin tablet is soon more domestic, bibliographical information (" quality evaluation of commercially available metformin hydrochloride tablet " in addition, " Chinese Journal of New Drugs ", 20th volume the 3rd phase) although the sample that different manufacturers is produced compares related substance and content is suitable with the former product that grinds, but stripping curve there are differences, therefore with former, whether its bioavailability and clinical effectiveness grind that product is consistent exists query, and for domestic imitation medicine, how to filter out and can ensure to grind product bioavailability and the more consistent product of stripping also its quality key that can ensure with former, and actual feedback clinical at present often domestic kind be difficult to reach former curative effect of grinding product, this is because will realize the dissolution overall with original product, to indicate limit value relatively easy, but it is very large to pass through the selection combination of multi-medicament supplementary product kind and the selection realization of consumption and the basically identical difficulty often of original product dissolution rate, also the comparative test being routine is unapproachable.
Summary of the invention
The object of this invention is to provide and a kind of and formerly grind the consistent metformin hydrochloride tablet of product dissolving out capability height, to ensure that the curative effect of preparation and bioavailability can with former to grind product more consistent.
Metformin hydrochloride tablet agent compositions of the present invention, it is characterized in that being made up of the component of following weight portion: metformin hydrochloride 200-300 part, DEXTRIN-60 parts, hyprolose (inside adding) 2-4 part, 15% alcoholic solution of 4% hypromellose is appropriate, hyprolose (additional) 2-4 part, magnesium stearate 1.2-1.8 part, Pulvis Talci 2-4 part.
Metformin hydrochloride tablet agent compositions of the present invention, it is characterized in that being made up of following component: metformin hydrochloride 200-300g, DEXTRIN-60g, hyprolose (inside adding) 2-4g, 15% alcoholic solution 180-200g of 4% hypromellose, hyprolose (additional) 2-4g, magnesium stearate 1.2-1.8g, Pulvis Talci 2-4g, makes 1000 altogether.Be preferably: metformin hydrochloride 250g, dextrin 50g, hyprolose (inside adding) 3g, 15% alcoholic solution of 4% hypromellose is appropriate, hyprolose (additional) 3g, magnesium stearate 1.5g, Pulvis Talci 3g.
Above-mentioned metformin hydrochloride tablet agent compositions, preferably also comprises coatings further.
The present invention also provides the preparation method of above-mentioned metformin hydrochloride tablet agent compositions, and it comprises following steps:
1) 15% alcoholic solution of 4% hypromellose is prepared;
2) get metformin hydrochloride, dextrin, in add hyprolose, mixing, 15% alcoholic solution adding 4% hypromellose makes wet granular;
3) dry, granulate;
4) to cross 30 mesh sieves for subsequent use for magnesium stearate;
5) granule after granulate, additional hyprolose, magnesium stearate, Pulvis Talci, mixing, tabletting.
Above-mentioned preparation method, preferably comprises the step of coating further.
The application is by a large amount of prescription screening, the metformin hydrochloride tablet stripping curve that the metformin hydrochloride tablet prepared and Shi Guibao company of Yuan Yan producer produce is basically identical, and current a lot of metformin hydrochloride tablet stripping curves and the former obvious difference that grinds, the concordance of bioavailability can not be ensured.
Dissolution determination method: sample thief 6, with 1000mL purified water for dissolution medium, turns basket rotating speed 100r/min, temperature 37 ± DEG C, after dispensing, respectively 5,10,15,30,45min samples 10mL (simultaneously supplementing equality of temperature medium 10mL), filter, precision measures subsequent filtrate 2mL, be placed in 100mL measuring bottle, be diluted with water to scale, as need testing solution, measure medicament contg with HPLC method, calculate the accumulation dissolution of every sheet.
The former reference preparation that grinds is the metformin hydrochloride tablet that Shi Guibao company produces.
Preparation embodiment
Embodiment 1
Preparation method:
1) 15% alcoholic solution of 4% hypromellose is prepared;
2) get metformin hydrochloride, dextrin, in add hyprolose, mixing, 15% alcoholic solution adding 4% hypromellose makes wet granular;
3) dry, granulate;
4) to cross 30 mesh sieves for subsequent use for magnesium stearate;
5) granule after granulate, additional hyprolose, magnesium stearate, Pulvis Talci, mixing, tabletting.
6) coating.
Comparing embodiment 1
Tablet with reference to the embodiment of the present application 1 forms, and binding agent is 5%PVP solution.
Preparation method is with reference to embodiment 1.
Comparing embodiment 2
Tablet with reference to the embodiment of the present application 1 forms, and binding agent is 10% starch slurry.
Preparation method is with reference to embodiment 1.
Comparing embodiment 3
Tablet with reference to the embodiment of the present application 1 forms, and disintegrating agent is carboxymethyl starch sodium.
Preparation method is with reference to embodiment 1.
Comparing embodiment 4
Tablet with reference to the embodiment of the present application 1 forms, and disintegrating agent is cross-linking sodium carboxymethyl cellulose.
Preparation method is with reference to embodiment 1.
Measure the dissolution of above-mentioned sample and reference preparation respectively, the results are shown in following table.
Stripping curve result (%):
Result of the test shows the application's preparation and former to grind reference preparation stripping curve basically identical, there is good In Vitro Dissolution performance, drug bioavailability can be made to keep basically identical, and when changing the adjuvant composition of the application's preparation, no matter be disintegrating agent or binding agent, its stripping curve obviously with former to grind product inconsistent, cannot reach the technique effect of the application, show that the entirety composition of the application can ensure medicine and the former dissolution rate grinding product, this effect cannot be predicted according to adjuvant itself.
In addition, by comparing the relative standard deviation of dissolution, find that the application's preparation and the former RSD numerical value grinding 5 sample times of product are all less than 2.3%.The application's RSD scope different sample time is at 1.2-2.2%, preparation process has good stability, and other samples different sample times RSD numerical value all relatively large, if the RSD scope of comparative example 1-4 is respectively at 3.4-5.2%, 2.9-4.5%, 1.2-4.2%, 2.1-5.5%, in RSD change to show greatly between comparative example each sample batch, relatively poor, the difference of stripping concordance greatly.Illustrate that the tablet uniformity of the application's formula preparation is good, relative to comparative example preparation Be very effective.
Long-time stability comparative experiments result
Above-described embodiment sample is stored at normal temperatures, measures the related substance in long-term put procedure and active component content, its stripping curve of Simultaneously test:
Long-time stability measuring result (%)
Long-time stability stripping curve measurement result
Result shows that invention formulation long-time stability were tested after 12 months and still stablizes, related substance and content remain stable, stripping curve also keeps stable, this result shows that the application's preparation is significant with application to actual production, can at utmost keep and former concordance of grinding the bioavailability of product.
Claims (6)
1. a metformin hydrochloride tablet agent compositions, it is characterized in that being made up of the component of following weight portion: metformin hydrochloride 200-300 part, DEXTRIN-60 parts, hyprolose (inside adding) 2-4 part, 15% alcoholic solution of 4% hypromellose is appropriate, hyprolose (additional) 2-4 part, magnesium stearate 1.2-1.8 part, Pulvis Talci 2-4 part.
2. metformin hydrochloride tablet agent compositions according to claim 1, it is characterized in that being made up of following component: metformin hydrochloride 200-300g, DEXTRIN-60g, hyprolose (inside adding) 2-4g, 15% alcoholic solution of 4% hypromellose is appropriate, hyprolose (additional) 2-4g, magnesium stearate 1.2-1.8g, Pulvis Talci 2-4g, makes 1000 altogether.
3. metformin hydrochloride tablet agent compositions according to claim 2, it is characterized in that being made up of following component: metformin hydrochloride 250g, dextrin 50g, hyprolose (inside adding) 3g, 15% alcoholic solution of 4% hypromellose is appropriate, hyprolose (additional) 3g, magnesium stearate 1.5g, Pulvis Talci 3g.
4., according to the metformin hydrochloride tablet agent compositions of any one of claim 1-3, also comprise coatings further.
5., according to the preparation method of the metformin hydrochloride tablet agent compositions of any one of claim 1-3, comprise following steps:
1) 15% alcoholic solution of 4% hypromellose is prepared;
2) get metformin hydrochloride, dextrin, in add hyprolose, mixing, 15% alcoholic solution adding 4% hypromellose makes wet granular;
3) dry, granulate;
4) to cross 30 mesh sieves for subsequent use for magnesium stearate;
5) granule after granulate, additional hyprolose, magnesium stearate, Pulvis Talci, mixing, tabletting.
6. the preparation method of metformin hydrochloride tablet agent compositions according to claim 5, comprises coating steps further.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410813845.2A CN104622822A (en) | 2014-12-23 | 2014-12-23 | Metformin hydrochloridetablet composition and preparation method thereof |
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| CN201410813845.2A CN104622822A (en) | 2014-12-23 | 2014-12-23 | Metformin hydrochloridetablet composition and preparation method thereof |
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Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108420807A (en) * | 2018-06-08 | 2018-08-21 | 重庆希尔安药业有限公司 | A kind of metformin hydrochloride medicinal composition preparation and preparation method thereof |
| CN109044988A (en) * | 2018-09-29 | 2018-12-21 | 哈尔滨珍宝制药有限公司 | A kind of metformin hydrochloride medicinal composition and its preparation method and application |
| CN109758431A (en) * | 2017-11-09 | 2019-05-17 | 郑州泰丰制药有限公司 | A kind of metformin hydrochloride tablet and preparation method thereof |
| CN110075077A (en) * | 2019-05-17 | 2019-08-02 | 贵州天安药业股份有限公司 | A kind of Dimethyldiguanide hydrochloride enteric solubility tablet of effective hypoglycemic |
| CN110731948A (en) * | 2019-12-06 | 2020-01-31 | 仁和堂药业有限公司 | Metformin hydrochloride fast-release agent tablet and application thereof |
| CN110840852A (en) * | 2019-10-16 | 2020-02-28 | 河北天成药业股份有限公司 | Metformin hydrochloride tablet and production process and production equipment thereof |
| CN110876728A (en) * | 2019-12-06 | 2020-03-13 | 仁和堂药业有限公司 | Preparation method of metformin hydrochloride quick-release preparation |
| CN112494441A (en) * | 2020-12-24 | 2021-03-16 | 迪沙药业集团有限公司 | Metformin hydrochloride composition |
-
2014
- 2014-12-23 CN CN201410813845.2A patent/CN104622822A/en active Pending
Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109758431A (en) * | 2017-11-09 | 2019-05-17 | 郑州泰丰制药有限公司 | A kind of metformin hydrochloride tablet and preparation method thereof |
| CN108420807A (en) * | 2018-06-08 | 2018-08-21 | 重庆希尔安药业有限公司 | A kind of metformin hydrochloride medicinal composition preparation and preparation method thereof |
| CN109044988A (en) * | 2018-09-29 | 2018-12-21 | 哈尔滨珍宝制药有限公司 | A kind of metformin hydrochloride medicinal composition and its preparation method and application |
| CN109044988B (en) * | 2018-09-29 | 2021-03-23 | 哈尔滨珍宝制药有限公司 | Metformin hydrochloride pharmaceutical composition and preparation method and application thereof |
| CN110075077A (en) * | 2019-05-17 | 2019-08-02 | 贵州天安药业股份有限公司 | A kind of Dimethyldiguanide hydrochloride enteric solubility tablet of effective hypoglycemic |
| CN110840852A (en) * | 2019-10-16 | 2020-02-28 | 河北天成药业股份有限公司 | Metformin hydrochloride tablet and production process and production equipment thereof |
| CN110731948A (en) * | 2019-12-06 | 2020-01-31 | 仁和堂药业有限公司 | Metformin hydrochloride fast-release agent tablet and application thereof |
| CN110876728A (en) * | 2019-12-06 | 2020-03-13 | 仁和堂药业有限公司 | Preparation method of metformin hydrochloride quick-release preparation |
| CN112494441A (en) * | 2020-12-24 | 2021-03-16 | 迪沙药业集团有限公司 | Metformin hydrochloride composition |
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Application publication date: 20150520 |