Slow release capsule of compound metformin pyrrolidone and preparation method

A technology of metformin pioglitazone and sustained-release capsules, which is applied in the field of compound metformin pioglitazone sustained-release capsules and its preparation, can solve problems such as no literature reports, and achieve the effects of improving abnormal blood lipid metabolism, constant drug release, and reducing insulin resistance

Inactive Publication Date: 2006-02-01
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] According to the literature search, there is no literature report on the technology of making sustai

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Compound Sustained Release Capsules Containing Metformin Hydrochloride 250mg Pioglitazone Hydrochloride 7.5mg

[0032] (1) Preparation of metformin hydrochloride-containing pill core

[0033] Take 150 g of glyceryl monostearate and disperse in hot distilled water, heat to about 80° C., and add 250 g of metformin hydrochloride at a constant stirring speed until a slurry is formed. The hot slurry was mixed with 100 g of microcrystalline cellulose in a planetary mixer for 10 minutes, and then the powder was extruded into an extrudate with a diameter of 1 mm and a length of 4 mm with a plunger extruder at a rate of 30.0 cm / min. Rotate in a spheronizer at a speed of 1000r / min for 10 minutes to obtain round pellets, put the wet pellets in a fluidized bed and dry at 40°C for 30 minutes, and finally sieve, and take the ones with a diameter of 1.18-1.70mm.

[0034] (2) Metformin Hydrochloride Sustained Release Coating Layer

[0035] The above ball cores are placed in a fluidiz...

Embodiment 2

[0044] Compound Sustained Release Capsules Containing Metformin Hydrochloride 425mg Pioglitazone Hydrochloride 7.5mg

[0045](1) Preparation of metformin hydrochloride-containing pill core

[0046] Get metformin hydrochloride 425g and microcrystalline cellulose 40g and mix in planetary mixer for 5 minutes, add 5% PVP in right amount, mix for 5 minutes, operate by embodiment 1, prepare containing pill core with plunger extruder.

[0047] (2) Metformin hydrochloride drug-containing pill core coated with slow-release coating layer

[0048] The above ball cores are placed in a fluidized bed, and the polymer solution spray coating is prepared according to the following prescription. The coating gained about 10% in weight. Dry at 40°C for 1 hour.

[0049] Cellulose acetate 5g

[0050] Eudragit S 100 0.1g

[0051] Sodium chloride 0.2g

[0052] Triethyl citrate 0.25g

[0053] Ethanol 100ml

[0054] (3) Pioglitazone hydrochloride coating drug application

[0055] According to ...

Embodiment 3

[0059] Compound Sustained Release Capsules Containing Metformin Hydrochloride 250mg Pioglitazone Hydrochloride 7.5mg

[0060] (1) Preparation of Metformin Hydrochloride Sustained-release Small Tablets

[0061] Get metformin hydrochloride 250g, hydroxypropyl methylcellulose (METHOCEL K100MCR) 100g, sodium carboxymethylcellulose 25g, microcrystalline cellulose 20g, mix well, add 5% PVP ethanol solution to make granules, add after drying 0.5% magnesium stearate, compressed into 3mm small tablets, each tablet contains 12.5mg of metformin hydrochloride, and the tablet weight is 20mg. Put the above-mentioned small tablets in a fluidized bed, and coat with the following coating solution, and the weight of the coating is increased to about 7-8%.

[0062] Eudragit RS 100 5g

[0063] Eudragit S 100 0.1g

[0064] Triethyl citrate 0.25g

[0065] Ethanol 100ml

[0066] (2) Pioglitazone hydrochloride coating drug application

[0067] Take pioglitazone hydrochloride fine powder, add it...

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PUM

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Abstract

A slow-releasing capsule of compound fluamine pyrrolinone for treating diabetes is composed of the central slow-releasing fluamine microball or small tablet and the coated fast-releasing pyrrolinone layer. Its advantages are high curative effect and no toxic by-effect.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a compound metformin pioglitazone sustained-release capsule and a preparation method thereof. Background technique [0002] Metformin is a biguanide antihyperglycemic drug. It reduces insulin resistance and lowers blood sugar by inhibiting hepatic glucose production and increasing peripheral glucose uptake. Pioglitazone is a thiazolidinedione insulin sensitizer, its mechanism of action is related to the presence of insulin, it can reduce insulin resistance in peripheral tissues and liver, increase insulin glucose processing, and reduce glycogen output. [0003] When Metformin is used alone to treat hyperglycemia, in order to maintain effective therapeutic blood concentration, reduce side effects, and increase patient compliance, Metformin Hydrochloride is made into a sustained-release preparation taken once a day, such as Bristol-Myers Glucophagrtm XR of Squib...

Claims

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Application Information

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IPC IPC(8): A61K31/4439A61K9/52A61P3/10A61K31/155
Inventor 王杏林张俊伟陈志华杨志强
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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