Matrix for sustained, invariant and independant release of active compounds

A matrix and composition technology, applied in the direction of organic active ingredients, digestive system, drug combination, etc., can solve the problems of limited range of analgesic dosage, different release distribution, and inability to ensure release distribution, etc., to reduce side effects and simplify the preparation method Effect

Inactive Publication Date: 2007-03-28
EURO-CELTIQUE SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A disadvantage of this known formulation is that, given the same mass ratio but different absolute amounts of tolitidine and naloxone will show different release profiles if the release is measured at a certain pH value
Therefore, even if the physician does not change the mass ratio of tolitidine to naloxone, if he wants

Method used

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  • Matrix for sustained, invariant and independant release of active compounds
  • Matrix for sustained, invariant and independant release of active compounds
  • Matrix for sustained, invariant and independant release of active compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0161] Example 1 - By spray granulation to produce different hydroxyl groups in non-swellable diffusion matrices Codone / naloxone dosage tablet

[0162] The following component amounts can be used to make the oxycodone / naloxone tablets of the present invention.

[0163] Preparation (name)

[0164] The Surelease(R) E-7-7050 polymer blend used had the following composition.

[0165] Surelease®

[0166] For the preparation of tablets, Oxycodone HCl, Naloxone HCl, Povidone 30 and Lactose FlowLac100 were mixed in a tumbler mixer (Bohle) followed by spray granulation with Surelease® in a fluid tank granulator (GPCG3) change. This material was screened through a Comill 1.4 mm sieve. An additional granulation step was performed with molten fatty alcohol in a high-cutting mixture (Collette). All tablet cores made by this procedure had a weight of 123 mg on a dry matter basis.

Embodiment 2

[0167] Embodiment 2-by extruding to make have oxycodone and nalox in non-swellable diffusion matrix ketone dose tablets

[0168] The following component amounts can be used to make the oxycodone / naloxone tablets of the present invention.

[0169] Preparation (name)

Oxy / Nal-Extr

Oxycodone HCl

20mg

Naloxone HCl

10mg

Kollidone 30

6 mg

Lactose Flow Lac100

49.25 mg

Ethyl cellulose 45cpi

10mg

stearyl alcohol

24 mg

Talc

2.5 mg

Magnesium stearate

1.25 mg

[0170] The above amounts of Oxycodone HCl, Naloxone HCl, Ethylcellulose 45 cpi, Kollidone 30, Stearyl Alcohol and Lactose Flow Lac100 were mixed in a drum mixer (Bohle). The mass was subsequently extruded with a counter-rotating twin-screw extruder of type Micro 18GGL (Leistritz AG, Nuernberg, Germany). The temperature of heating zone 1 was 25°C, heating zone 2 was 50°C, heating zone 3 to 5 was 60°C, heating zone 6 to 8 ...

Embodiment 3

[0172] Example 3 - Release Profile of Oxycodone / Naloxone Tablets Taken from Example 1:

[0173] The release of the active compound was measured over a period of 12 hours using HPLC at pH 1.2 and applying the Basket method of USP. Test tablets Ox / Nal-0, Ox / Nal-5 or Ox / Nal-10.

[0174] From Figure 2 and the values ​​listed in the table, it follows that in the case of non-swellable expanded matrices based on Surelease(R), the release rate of different amounts of oxycodone remains the same regardless of the amount of naloxone. Correspondingly, a constant release profile of naloxone was observed at different oxycodone amounts.

[0175] time

[0176] Release values ​​refer to oxycodone or naloxone (row 2) and are expressed as a percentage. The average release of naloxone at 420 minutes was 92.7%. The maximum error value is 1% at 420 minutes. Oxy and Nal stand for oxycodone and naloxone and denote the active compounds to be measured.

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Abstract

The invention concerns a storage stable pharmaceutical formulation comprising preferably two active compounds in a non-swellable diffusion matrix, whereby the compounds are released from the matrix in a sustained, invariant and, if several compounds are present, independent manner and the matrix is determined with respect to its substantial release characteristics by ethylcellulose and at least one fatty alcohol. The invention also concerns methods for producing such pharmaceutical formulations.

Description

[0001] This application is a divisional application of the Chinese patent application with application number 03807177.0 and application date of April 04, 2003. technical field [0002] The present invention relates to a storage-stable pharmaceutical formulation comprising at least one pharmaceutically active compound in a substantially non-swellable diffusion matrix, wherein the compound is present in a continuous, constant and independent (if several compounds are present) released from the matrix. As regards its intrinsic release properties, the matrix is ​​formed from ethylcelluloses and at least one fatty alcohol. [0003] The present invention also relates to a process for the manufacture of storage-stable pharmaceutical formulations containing at least one pharmaceutically active compound in a non-swellable diffusion matrix, wherein said at least one compound is released from the matrix in a sustained and invariant manner. released from the matrix, and also in an indep...

Claims

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Application Information

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IPC IPC(8): A61K31/439A61K9/16A61K9/20A61K9/22A61P1/00A61K9/26A61K9/28A61K31/485
CPCA61K9/2013A61K9/2054A61K31/485A61K9/2018A61K9/2866A61P1/00
Inventor 比安卡·布罗格曼西尔克·米劳克里斯托弗·斯皮茨利
Owner EURO-CELTIQUE SA
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