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Directly compressible composition comprising microcrystalline cellulose

a technology of microcrystalline cellulose and composition, applied in the direction of pill delivery, etc., can solve the problems of unsatisfactory hardness of tablets which cannot be handled in pharmaceutical practice, inconvenient and expensive granulation steps, and the need to remove solvents necessary for wet granulation with high energy input, etc., to achieve low ejection force, low friabilities, and high tablet hardness

Inactive Publication Date: 2017-07-27
MERCK PATENT GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides directly compressible retardation matrices that eliminate the need for time-consuming granulation processes. These matrices can be easily converted into a directly compressible state using PVAs or commercially available PVA grades. Additionally, by blending a fine-grained PVA / MCC matrix with a poorly compressible active compound and a very small amount of magnesium stearate as lubricant, tablets of adequate hardnesses with low mechanical abrasion can be obtained. These tablets have been found to have extended release of active compound over several hours. The technical effects of this invention are the simplification of tablet manufacturing processes and the ability to provide controlled release of active compounds.

Problems solved by technology

A particular problem in this connection thus consists in the production in a simple manner of tablets which principally consist of corresponding PVAs as active compound excipient in which the active compound is homogeneously distributed.
The latter is associated with the disadvantage that the solvents necessary for wet granulation have to be removed again with high input of energy.
However, known pulverulent PVAs are per se not directly compressible and give tablets of unsatisfactory hardness which cannot be handled in pharmaceutical practice, since, for example, they have an undesired tendency to break or have excessively high abrasion.
Excipient materials of this type would make inconvenient and expensive granulation steps, which are usually necessary in order to make the tableting mixtures compressible, superfluous.

Method used

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  • Directly compressible composition comprising microcrystalline cellulose
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  • Directly compressible composition comprising microcrystalline cellulose

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[0091]The present description enables the person skilled in the art to apply the invention comprehensively. Even without further comments, it is therefore assumed that a person skilled in the art will be able to utilise the above description in the broadest scope.

[0092]If anything is unclear, it goes without saying that the publications and patent literature cited should be consulted. Accordingly, these documents are regarded as part of the disclosure content of the present description.

[0093]For better understanding of the invention and in order to illustrate it, examples are given below which are within the scope of protection of the present invention. These examples also serve to illustrate possible variants. Owing to the general validity of the inventive principle described, however, the examples are not suitable for reducing the scope of protection of the present application to these alone.

[0094]Furthermore, it goes without saying to the person skilled in the art that, both in t...

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Abstract

The present invention relates to a directly compressible composition for the production of tablets which comprise fine-grained polyvinyl alcohols (PVAs) and fine-grained microcrystalline celluloses (MCCs) in a co-mixture. The present invention also relates to the use of this mixture and to a process for the preparation thereof.

Description

[0001]The present invention relates to a directly compressible composition for the production of tablets which comprise fine-grained polyvinyl alcohols (PVAs) and fine-grained microcrystalline celluloses (MCCs) in a co-mixture. The present invention also relates to the use of this mixture and to a process for the preparation thereof.PRIOR ART[0002]Polyvinyl alcohols (PVAs) are synthetic polymers which are available in various grades, in particular with respect to degree of polymerisation and their viscosity. Polyvinyl alcohols are obtained by alkaline hydrolysis of polyvinyl acetate. Polyvinyl acetate is in turn obtained by free-radical polymerisation from vinyl acetate. Through different chain lengths and different degrees of hydrolysis of the polyvinyl acetates employed, polyvinyl alcohols (PVAs) having a very wide variety of physical properties can be obtained.[0003]Polyvinyl alcohols are employed, in particular, as film formers, adhesive gels and as viscosity modulator, in a mul...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/20
CPCA61K9/2027A61K9/2054A61K9/2095
Inventor OGNIBENE, ROBERTOBAUER, FINNWEDEL, THORSTENMODDELMOG, GUENTER
Owner MERCK PATENT GMBH
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