Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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
View PDF4 Cites 2 Cited by
  • 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 to increase the dose for each individual patient, he must perform extensive titration experiments, because the physician cannot be sure that the release profile of the two components will be the same. constant
Accordingly, the range of therapeutically useful amounts of analgesics available to physicians will be limited

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com