Gastro-retentive oral pharmaceutical compositions

A drug and tablet technology, which is applied in the field of oral galenic preparations of three types of BCS molecules such as baclofen, can solve the problems of long time and achieve the effect of improving floating

Active Publication Date: 2016-08-03
ETHYPHARM SA
View PDF6 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because of the prolonged time required for the tablets to float, it was observed that these tablets were also excreted by gastric emptying

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
  • Gastro-retentive oral pharmaceutical compositions
  • Gastro-retentive oral pharmaceutical compositions
  • Gastro-retentive oral pharmaceutical compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0062] 1. Example of composition according to patent EP1745775 (comparative example)

[0063] In this example, the composition of the tablet follows the quantities described in patent EP1745775.

[0064] Table 1: Similar percentage composition as described in patent EP1745775

[0065]

[0066]

[0067] Baclofen was mixed with xanthan gum, Avicel CL611, mannitol SD200, and grain. After drying and sizing on a 425 μm mesh vibrating sieve, the granulated active ingredient was mixed with the excipient mixture in a multidirectional mixer (Turbula 2L) for 10 minutes, then lubricated with magnesium stearate for an additional 1 minute. The final blend was then compressed on a rotary tablet press (SVIACPR12) equipped with 12 mm diameter round punches and a pressure feed system.

[0068] Tablets were produced using a compression force of 18kN and had a hardness of 105N.

[0069] Table 2 shows the dissolution results in 500 ml of pH 4.5 media according to USP test II (100 rpm...

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

PropertyMeasurementUnit
hardnessaaaaaaaaaa
hardnessaaaaaaaaaa
hardnessaaaaaaaaaa
Login to view more

Abstract

The invention relates to a pharmaceutical matrix tablet which can be administered orally once or twice per day with gastro-retentive controlled release of Baclofen.

Description

technical field [0001] The present invention relates to an oral galénique preparation of BCS class III molecules such as baclofen in the form of a gastric retention controlled release tablet. These compositions can be administered once or twice daily. Background technique [0002] When developing a new pharmaceutical entity, the oral route is the first route envisioned because of its benefits in promoting treatment adherence. However, this approach has been abandoned for many molecules in development due to the low oral bioavailability of these molecules. This may be due to various factors related to the properties of the molecule itself, or to the physiology of the gastrointestinal tract (Fasinu, et al., 2011). Over the past 10 years, various approaches (including physical or chemical methods) to increase the oral bioavailability of these molecules have been investigated. [0003] The Biopharmaceutics Classification System (BCS) is an important tool in the pharmaceutical...

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
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/197A61K9/00A61P25/32A61K9/20
CPCA61K9/0065A61K31/197A61K9/2009A61K9/2018A61K9/205A61K9/2054A61K9/2077A61P25/32A61K47/00A61K47/26A61K9/0053A61K9/2013
Inventor C·埃里P·孔塔曼
Owner ETHYPHARM SA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products