Drug – bio-affecting and body treating compositions – Designated organic nonactive ingredient containing other... – Solid synthetic organic polymer
Patent
1997-09-16
2000-05-16
Kulkosky, Peter F.
Drug, bio-affecting and body treating compositions
Designated organic nonactive ingredient containing other...
Solid synthetic organic polymer
424486, A61K 3179
Patent
active
060638214
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to transparent rapid release compositions of non-steroidal analgesics with antipyretic and antiinflammatory action, obtainable by extrusion of a melt comprising, besides one or more active substances, Fikentscher K value of 30, mixtures thereof, and sodium or of potassium, subsequent shaping.
The invention furthermore relates to a process for producing such compositions.
Rapid release of the active substance is of crucial importance particularly with analgesics in order to achieve a rapid onset of the pain-relieving action.
In the case of active substances with low solubility in water, as represented, for example, by the organic acids with analgesic activity, rapid release of sufficient doses is often not simple to achieve.
EP-A 607 467 proposes to promote rapid release of ibuprofen by adding basic salts which are applied during the pelleting process in the form of aqueous solutions to the active substance which has previously been mixed with an ancillary substance. The pellets are subsequently compressed to tablets in a conventional way. However, this procedure is relatively elaborate and therefore rather unfavorable economically.
It is furthermore known that drug forms can be produced in a very economic manner by extrusion of polymer melts which contain active substances, with subsequent continuous shaping.
EP-B 240 904 describes such a process for producing solid pharmaceutical forms by extrusion of polymer melts which contain active substances, using as polymers homo- or copolymers of N-vinylpyrrolidone.
However, a fundamental problem in the process of this type is that the matrix-forming polymers on the one hand are sufficiently melt-processible, or become processible by addition of a plasticizing substance, at the processing temperatures but, on the other hand, lead to stable drug forms under the usual storage conditions, with which no cold flow occurs.
This problem is all the more difficult to solve when the intention is to produce rapid release drug forms. Normally suitable for this purpose are, in particular, relatively low molecular weight polymers which rapidly dissolve in the digestive juices. However, it is precisely these which show the phenomenon of cold flow of the finished drug forms to a pronounced extent. High molecular weight polymers do not usually show rapid release and can scarcely be extruded without plasticizers because the glass transition temperature (DIN 52324) is considerably higher.
An additional problem arises when the intention is to produce transparent drug forms by melt extrusion. The active substance is completely uniformly distributed without compartmentalization only in transparent forms. This is indispensable for rapid release. In addition, the use of transparent forms simplifies quality control and patient compliance.
It is an object of the present invention to find transparent rapid release compositions of non-steroidal analgesics which can be produced in a simple manner by melt extrusion with subsequent shaping and have good storage stability.
We have found that this object is achieved by the compositions defined at the outset.
Suitable active substances according to the invention are non-steroidal analgesics with antipyretic and antiinflammatory effect, as also used for symptomatic antirheumatic therapy.
Suitable active substances are, accordingly, derivatives of salicylic acid such as acetylsalicylic acid and derivatives of other organic acids and pyrazole derivatives. Thus, suitable active substances are aryl acid derivatives such as diclofenac, tolmetin or zomepirac, also arylpropyl acid derivatives such as ibuprofen, naproxen, fenoprofen, flurbiprofen or ketoprofen, or else indole- and indeneacetic acid derivatives such as indometacin or sulindac. Examples of suitable pyrazole derivatives are for example phenazone, aminophenazone, metamizole, propyphenazone, phenylbutazone or oxyphenbutazone.
Preferred active substances are ibuprofen, acetylsalicylic acid and ketoprofen, sulindac, indometacin, flurbiprofen.
It is also possible to u
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Breitenbach Jorg
Rosenberg Joerg
Sanner Axel
BASF - Aktiengesellschaft
Kulkosky Peter F.
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