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Microcapsules for the delayed, controlled release of perindopril

A technology of slow-release peridole and microparticles, which is applied in the direction of microcapsules, capsule delivery, medical preparations of non-active ingredients, etc., and can solve the problem of controlled slow-release antihypertensive dosage forms that cannot inhibit angiotensin-converting enzymes Does not include the dual mechanism of release, low AI absorption, etc., to achieve optimal compliance, treatment of arterial hypertension and heart failure, and high bioavailability

Inactive Publication Date: 2007-10-31
SERVIER LAB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Obviously, such a situation is disadvantageous, since the AI ​​uptake is too low, or even zero, and therefore has no therapeutic effect, the consequences can be severe
[0057] Therefore, the prior art does not include a galenic system with sustained release through a dual mechanism of "time-dependent" and "pH-dependent" release and which does guarantee release of the active ingredient
[0058] On the other hand, there are currently no controlled-release antihypertensive dosage forms that inhibit angiotensin-converting enzymes

Method used

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  • Microcapsules for the delayed, controlled release of perindopril
  • Microcapsules for the delayed, controlled release of perindopril
  • Microcapsules for the delayed, controlled release of perindopril

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0113] Preparation of 1-perindopril microcapsules

[0114] Step A: Preparation of Perindopril Microparticles

[0115] 157 g of perindopril tert-butylamine salt and 17 g of hydroxypropylcellulose were dispersed or dissolved in 1300 g of acetone. The suspension was sprayed onto 1500 g of sugar microspheres with a mean diameter of 355-500 [mu]m using a Glatt GPCG3 spray coater. The film coating conditions are: product temperature: 37-39°C, spray feeding rate: 42g / min, atomization pressure: 1.8bar.

[0116] Step B: Preparation of Perindopril Microcapsules

[0117] The hydrophilic polymer A and the hydrophobic compound B were dissolved in isopropanol which had been heated to a temperature of 65-75°C. This solution was sprayed onto the perindopril microparticles prepared in step A using a Glatt GPCG3 sprayer. The film coating conditions are: product temperature: 36-41°C, spray feeding rate: 8-12g / min, atomization pressure: 1.5bar.

[0118] 2- Formulation Example

[0119] ...

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Abstract

The present invention relates to a microcapsule composition allowing the delayed and controlled release of perindopril, or of a pharmaceutically acceptable salt thereof, for administration by the oral route.

Description

technical field [0001] The present invention relates to oral microcapsules of controllable sustained-release perindopril or its pharmaceutically acceptable salt. [0002] More precisely, the present invention relates to a microparticle form of controlled release perindopril or a pharmaceutically acceptable salt thereof, wherein the controlled release period is controlled in a specific manner by a dual mechanism: "Time-dependent" release triggered after a specific residence time, and "pH-dependent" release triggered by pH changes after microparticles enter the small intestine. The microparticles of the present invention are microcapsules with a particle size measurement value of 100-1200 microns, they contain perindopril, and are individually coated with at least one layer of coating film, so that the controlled release of perindopril can be achieved. profit. Background technique [0003] Perindopril tert-butylamine salts have also been marketed, and they are used in the tr...

Claims

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Application Information

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IPC IPC(8): A61K31/40A61K9/50A61K31/401A61K38/55A61K47/32A61K47/34A61P9/12A61P9/04A61K9/14A61K9/26A61K9/48A61K9/62A61K31/404A61K31/405A61K47/14A61K47/26A61K47/36A61K47/38A61K47/42A61K47/44A61P9/00A61P43/00
CPCA61K9/5026A61K9/5078A61K9/5015A61K31/405A61P43/00A61P9/00A61P9/04A61P9/12A61K9/48A61K9/50
Inventor B·于埃德巴罗什P·武特里希V·勒格朗C·卡斯唐R·梅吕埃
Owner SERVIER LAB
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