CN1294908C

CN1294908C - Oral gliclazide sustained release formulation

Info

Publication number: CN1294908C
Application number: CNB031350984A
Authority: CN
Inventors: 柏俊; 李华林; 孙备; 费勤志; 吕凌; 黄守正
Original assignee: ANHUI INSTITUTE OF MATERIA MEDICA; ANHUI MEDICINE SCIENCE AND TECHNOLOGY INDUSTRY Co
Current assignee: ANHUI INSTITUTE OF MATERIA MEDICA; ANHUI MEDICINE SCIENCE AND TECHNOLOGY INDUSTRY Co
Priority date: 2003-06-08
Filing date: 2003-09-28
Publication date: 2007-01-17
Anticipated expiration: 2023-09-28
Also published as: CN1572294A

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

Oral Gliclazide delayed-release preparation

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
		1h	2h	4h	8h	12h	Embodiment 1	PH6.8	26	38	62	88	101
PH7.8	27	39	65	90	100			PH6.8	26	38	62	88	101

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

1, a kind of oral Gliclazide delayed-release preparation, comprise effective ingredient gliclazide, diluent, lubricant and fluidizer, it is characterized in that: contain at least a bioerodable framework material in Cera Flava or synthetic wax or Brazil wax or the hydrogenated vegetable oil in this slow releasing agent, the bioerodable framework material accounts for 10%～40% of total formulation weight amount.

2, slow releasing preparation according to claim 1 is characterized in that: the bioerodable framework material accounts for 15%～25% of total formulation weight amount.

3, slow releasing preparation according to claim 1 and 2 is characterized in that: contain surfactant sodium lauryl sulphate or tween in this slow releasing preparation, 5%～10% of surfactant comprise total formulation weight amount.