CN1572294A - Oral gliclazide sustained release formulation - Google Patents
Oral gliclazide sustained release formulation Download PDFInfo
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- CN1572294A CN1572294A CN 03135098 CN03135098A CN1572294A CN 1572294 A CN1572294 A CN 1572294A CN 03135098 CN03135098 CN 03135098 CN 03135098 A CN03135098 A CN 03135098A CN 1572294 A CN1572294 A CN 1572294A
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- slow releasing
- releasing preparation
- gliclazide
- release
- bioerodable
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Abstract
An oral gliclazide sustained release formulation includes effective ingredient gliclazide and thinning agent, lubricant and flow aid agent. It is characterized in that the release formulation contains biology dissolve corrode framework material which is composed of at least one wax kind or saturated fat kind. In order to control the release better, the formulation can be added with surfactants. The formulation can release 50% of the total amount of the gliclazide in 4-6 hours, and will not be influenced by dissolve medium PH value.
Description
Technical field
The present invention relates to a kind of oral drug preparation, exactly is a kind of oral Gliclazide delayed-release preparation that contains the bioerodable skeleton.
Background technology
Gliclazide is second filial generation sulfonylurea hypoglycemic agent (having another name called gliclazide), is clinical blood sugar lowering commonly used, because its determined curative effect is put into national essential drugs catalogue and medical care insurance medication.Present clinical use for every oral ordinary tablet that contains 80mg dosage, conventional average recipe quantity is an administration every day secondary, each a slice is also looked the seriousness of diabetes sometimes, administration every day 1-4 sheet divides administration several times.This oral ordinary tablet discharges rapidly, and effective ingredient is in blood samples of patients high concentration a middle or short term (peak value), and slow releasing preparation can be avoided such peak value, makes the equalization of concentration of effective ingredient in blood samples of patients and stable, thus the side effect of avoiding peak value to cause.
CN1342068A discloses a kind of oral sustained release matrix tablet, is the hydrophilic skeleton, comprises at least a cellulose polymerizable compound and glucose syrup.
Summary of the invention
Oral Gliclazide delayed-release preparation provided by the present invention, comprise effective ingredient gliclazide and diluent, lubricant and fluidizer, it is characterized in that: contain the bioerodable framework material in this slow releasing preparation, described bioerodable framework material is made of at least a wax class or saturated fat class.
Described wax class is Cera Flava or synthetic wax or Brazil wax etc.
Described saturated fat class is hard fatty acids or hydrogenated vegetable wet goods.
The bioerodable framework material accounts for the 10%-40% of total formulation weight amount, is good with 15%-25%.
The effective ingredient gliclazide accounts for the 7.5%-25% of total formulation weight amount.Discharge for controlling Gliclazide delayed-release better, can also add surfactant in this slow releasing preparation, be sodium lauryl sulphate or Tweens etc.The 5%-10% of surfactant comprise total formulation weight amount.
Described diluent adopts known phosphate or acid phosphate or carbonate or acid carbonate, preferred sodium bicarbonate.Diluent accounts for the 20%-70% of total formulation weight amount, is good with 45%-65%.
Described lubricant adopts known stearic acid or its salt, preferred magnesium stearate.
Described fluidizer is selected known silicon dioxide for use.
Oral Gliclazide delayed-release preparation provided by the present invention adopts known freezing method preparation.Here it is at first mixes gliclazide, diluent, surfactant, then mixture is added in the bioerodable framework material of heating and melting stirring and evenly mixing, cool off, pulverize, sieve, add lubricant, fluidizer then, mixing, tabletting or record capsule and get final product.
Oral Gliclazide delayed-release preparation provided by the present invention adopts bioerodable framework material and surfactant and weakly alkaline diluent to make up, and its release in vitro meets the requirements.Gliclazide discharged 50% of total amount between 4-6 hour, and was not subjected to the influence (seeing accompanying drawing) of pH value.
Description of drawings:
Be the release profiles of gliclazide in the dissolve medium of different PH shown in the accompanying drawing, accompanying drawing 1 is the dissolve medium of PH6.8, and accompanying drawing 2 is the dissolve medium of PH7.8.
The slow release of gliclazide shown in the curve is not subjected to the influence of pH value.
The specific embodiment
Now to prepare 1000, every contains gliclazide 30mg is example, and non-limiting examples is described below
Example 1,
Gliclazide 30g
Sodium bicarbonate 130g
Cera Flava 35g
Tween 80 15g
Magnesium stearate 2g
Silica 1 g
Method for making: with Cera Flava in blender, put heating and melting in the water-bath, add premixed gliclazide, sodium bicarbonate, Tween 80, in the semisolid stirring and evenly mixing, stir on the limit, solid dispersion is made in the limit cooling, pulverizes the 40-60 mesh sieve, make granule with 50% ethanol, oven dry back adds lubricant, fluidizer, and mixing presses 1000 or fill 1000 capsules to get final product.
Made tablet (or capsule) adopts dissolution method first subtraction unit according to drug release determination method " 2000 editions two appendix XD first methods of Chinese Pharmacopoeia ", is medium with the phosphate buffer 1 000ml of pH6.8 and pH7.8,100 rev/mins of rotating speeds; Determination data sees the following form
Drug release determination data (%)
| ??1h | ??2h | ??4h | ??8h | ??12h | ||
| Embodiment 1 | ??PH6.8 | ??26 | ??38 | ??62 | ??88 | ??101 |
| ??PH7.8 | ??27 | ??39 | ??65 | ??90 | ??100 |
Example 2-example 6:
Hydrogenated vegetable oil is in blender; put heating and melting in the water-bath; add premixed gliclazide, sodium bicarbonate, sodium lauryl sulphate; in the semisolid stirring and evenly mixing; stir on the limit, the limit cooling; make solid dispersion and in waving granulation machine, cross the 20-24 mesh sieve, add magnesium stearate and silicon dioxide mixing, 1000 of flat stampings of 8mm or irritate 1000 capsules.
Example 2-example 6 made tablets (or capsule) adopt dissolution method first subtraction unit according to drug release determination method " 2000 editions two appendix XD first methods of Chinese Pharmacopoeia ", are medium with the phosphate buffer 1 000ml of pH6.8 and pH7.8,100 rev/mins of rotating speeds; Determination data sees the following form
Drug release determination data (%)
Claims (7)
1, a kind of oral Gliclazide delayed-release preparation comprises effective ingredient, diluent, lubricant and fluidizer, it is characterized in that: contain at least a bioerodable framework material of wax class or saturated fat apoplexy due to endogenous wind in this slow releasing agent.
2, slow releasing preparation according to claim 1 is characterized in that: described wax class is Cera Flava or synthetic wax or Brazil wax, and described saturated fat class is stearic acid or hydrogenated vegetable oil.
3, slow releasing preparation according to claim 1 and 2 is characterized in that: the bioerodable framework material accounts for the 10%-40% of total formulation weight amount.
4, slow releasing preparation according to claim 3 is characterized in that: the 15%-25% that the bioerodable framework material accounts for the total formulation weight amount is good.
5, slow releasing preparation according to claim 1 is characterized in that: contain surfactant in this slow releasing preparation.
6, slow releasing preparation according to claim 5 is characterized in that: described surfactant is sodium lauryl sulphate or Tweens.
7, according to claim 1 or 5 or 6 described slow releasing preparation, it is characterized in that: the 5%-10% of surfactant comprise total formulation weight amount.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB031350984A CN1294908C (en) | 2003-06-08 | 2003-09-28 | Oral gliclazide sustained release formulation |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN03131849 | 2003-06-08 | ||
| CN03131849.5 | 2003-06-08 | ||
| CNB031350984A CN1294908C (en) | 2003-06-08 | 2003-09-28 | Oral gliclazide sustained release formulation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1572294A true CN1572294A (en) | 2005-02-02 |
| CN1294908C CN1294908C (en) | 2007-01-17 |
Family
ID=34523632
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB031350984A Expired - Fee Related CN1294908C (en) | 2003-06-08 | 2003-09-28 | Oral gliclazide sustained release formulation |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1294908C (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101347414B (en) * | 2008-03-21 | 2011-11-23 | 瑟维尔实验室 | Divisible galenical preparation form capable of controlling release of active ingredient |
| CN101721392B (en) * | 2008-10-24 | 2012-02-08 | 天津市铭泰医药科技有限公司 | Method for preparing gliclazide slow-release capsule |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6056977A (en) * | 1997-10-15 | 2000-05-02 | Edward Mendell Co., Inc. | Once-a-day controlled release sulfonylurea formulation |
| AP1243A (en) * | 1999-02-01 | 2004-02-02 | Servier Lab | Core tablet for controlled release of gliclazide after oral administration. |
| EP1372614A4 (en) * | 2001-03-16 | 2007-10-31 | Andrx Pharmaceuticals Llc | Controlled release sulfonylurea formulation |
-
2003
- 2003-09-28 CN CNB031350984A patent/CN1294908C/en not_active Expired - Fee Related
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101347414B (en) * | 2008-03-21 | 2011-11-23 | 瑟维尔实验室 | Divisible galenical preparation form capable of controlling release of active ingredient |
| CN101721392B (en) * | 2008-10-24 | 2012-02-08 | 天津市铭泰医药科技有限公司 | Method for preparing gliclazide slow-release capsule |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1294908C (en) | 2007-01-17 |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C17 | Cessation of patent right | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20070117 Termination date: 20100928 |