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Irbesartan gastric retention sustained-release pharmaceutical composition

A technology for slow-release drugs and retention in the stomach, which is applied in drug combination, drug delivery, and pharmaceutical formulations, and can solve problems such as limited action time and inability to fully utilize the advantages of slow-release preparations

Inactive Publication Date: 2007-08-08
GUANGZHOU PUIS PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Due to the influence of gastric emptying and intestinal transit, the usual sustained and controlled release preparations have limited action time in the human body and cannot fully utilize the advantages of sustained and controlled release preparations

Method used

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  • Irbesartan gastric retention sustained-release pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Irbesartan 75g

[0065] Hypromellose 14g

[0066] cetyl alcohol 7g

[0067] Calcium carbonate 20g

[0068] Microcrystalline Cellulose 30g

[0069] Lactose 20g

[0070] Magnesium stearate 1.8g

[0071]

[0072] Makes 1000 pieces

[0073] Preparation:

[0074] Weigh the above-mentioned raw materials and auxiliary materials, sieve them, mix them well, and press them into tablets.

Embodiment 2

[0076] (1) Tablet core prescription

[0077] Irbesartan 150g

[0078] Hypromellose 20g

[0079] Cetyl Alcohol and Stearyl Alcohol Mixture 10g

[0080] Magnesium carbonate 20g

[0081] Poloxamer 2g

[0082] Microcrystalline Cellulose 40g

[0083] Talc powder 2.5g

[0084]

[0085] Makes 1000 pieces

[0086] (2) Prescription of coating solution (1000 tablets dosage)

[0087] Opadry 5g

[0088] 85% ethanol appropriate amount

[0089] Preparation:

[0090] 1. Weigh the raw materials and auxiliary materials according to the tablet core prescription, sieve them separately, mix them evenly, and press them into tablets;

[0091] 2. Prepare coating solution: slowly add Opadry to an appropriate amount of 85% ethanol solution, stir evenly and continue stirring for several minutes, set aside;

[0092] 3. Coating the prepared tablet core with the above-mentioned coating solution according to the conventional process.

Embodiment 3

[0094] Irbesartan 150g

[0095] Hypromellose 20g

[0096] Cetyl and stearyl alcohol mixture 12g

[0097] Calcium carbonate 20g

[0098] Microcrystalline Cellulose 45g

[0099] Povidone 4g

[0100] Magnesium Stearate 2.5g

[0101] 50% ethanol appropriate amount

[0102]

[0103] Makes 1000 pieces

[0104] Preparation:

[0105] Weigh the above-mentioned other raw materials and auxiliary materials except magnesium stearate, sieve them separately, mix well, add povidone 50% ethanol solution to granulate, add magnesium stearate after drying, mix well, and press into tablets Instantly.

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PUM

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Abstract

The invention relates to a method for preparing erbesatan stomach-held slow-release drug compound, which comprises the erbestan and acceptable medical shaping agents, to control the stop time in the stomach, to confirm the stable blood drug density of patient, improve safety and effect.

Description

technical field [0001] The invention relates to a sustained-release pharmaceutical composition retained in the stomach, in particular to a sustained-release pharmaceutical composition retained in the stomach of the antihypertensive drug irbesartan and a preparation method thereof. Background technique [0002] Irbesartan (Irbesartan) its chemical name is: 2-butyl-3-[4-[2-(1H-tetrazol-5-yl)phenyl]benzyl]-1,3-diaminospiro -[4.4]Non-1-en-4-one. It is a new type of angiotensin II receptor antagonist, which can specifically antagonize the angiotensin II (AngII) receptor AT 1 , for AT 1 Receptor selectivity is AT 2 8500-fold by selectively antagonizing AngII and AT 1 Receptor binding, inhibition of vasoconstriction and aldosterone release, resulting in antihypertensive effects. It is suitable for various degrees of essential hypertension. Compared with other antihypertensive drugs, the efficacy of irbesartan is similar or slightly superior to that of enalapril, amlodipine, a...

Claims

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Application Information

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IPC IPC(8): A61K31/4184A61K9/22A61K9/28A61K47/38A61K47/36A61P9/12
CPCA61K9/0065A61K31/4178A61P9/12
Inventor 贝庆生
Owner GUANGZHOU PUIS PHARMA FACTORY
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