Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1997-08-27
1999-04-20
Spivack, Phyllis G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
514569, 514448, A61K 3119, A61K 3138
Patent
active
058957898
DESCRIPTION:
BRIEF SUMMARY
The object of the present invention consists of pharmaceutical compositions suitable for parenteral administration which contain alkylammonium salts of 2-arylpropionic acids.
In particular, although the parenteral pharmaceutical compositions of the invention are suitable to be obtained with any 2-arylpropionic acid having antiinflammatory activity, they preferably contain, as 2-arylpropionic acid, ketoprofen or 3-benzoyl-.alpha.-methylbenzeneacetic acid, ibuprofen or 2-(4-isobutylphenyl)propionic acid, naproxen or (S)-6-methoxy-.alpha.-methyl-naphthaleneacetic acid and tiaprofenic acid or 5-benzoyl-.alpha.-methyl-2-thiopheneacetic acid, the ketoprofen being the 2-arylpropionic acid particularly preferred.
One of the advantages of the pharmaceutical compositions of the invention is that it allows for the administration of the non-steroid antiinflammatory substance by a route of administration, the parenteral one, which does not show side effects as shown by the pharmaceutical forms administered by topical route such as, for example, creams, lotions, gels or ointments which, because of their easy methods of application, are widely used. It is in fact known from literature on the subject that topical administration of non-steroid anti-inflammatory drugs can, in a more or less serious manner, provoke damage to the patient's skin due to the photolability of the drug which, in the presence of light, undergoes a degradation process, the products of which interfere negatively on the cellular membrane by the formation of free radicals.
The pharmaceutical compositions of the invention represent, moreover, a notable improvement as far as stability and convenience of use and safety are concerned with respect to the compositions already on the market containing the same anti-inflammatory drugs.
A decisively more advantageous aspect of said pharmaceutical compositions is that their administration causes uneasiness which is tolerable, compared to the pain, sometimes intense, caused by the compositions for parenteral use on the market containing the same anti-inflammatory drugs.
In particular, as far as ketoprofen is concerned, the relatively small side effects and the recognised effectiveness in the symptomatic treatment of rheumatoid arthritis, in osteoarthritis, in anchylosing spondylitis, of acute painful articular and periarticular symptoms of the musculoskeletal system, in gout and in dysmenorrhea, in the treatment of pain and inflammation which accompanies or follows orthopedic operations, have made such a drug one of the most frequently used active principles in oral administration among anti-inflammatory non-steroid drugs of current therapeutical use.
The analgesic and anti-inflammatory effect of ketoprofen has been, in a large measure, correlated to its capacity, or more specifically, to the capacity of its S-enantiomer, to inhibit the synthesis of prostaglandin. More recently, it has been recognised that the R-enantiomer, which in human beings does not undergo an appreciable metabolic conversion in the S-antipode, has its own analgesic property, mediated by mechanisms of action which, even though not fully clarified, seem to be completely independent from the prostaglandin synthesis block.
Pharmaceutical formulations for parenteral use containing as active principle ketoprofen and/or its enantiomers are thought to be particularly useful in the treatment of acute exacerbations of painful manifestations and as adjuvant in the symptomatic therapy of pain in persons suffering from terminal cancer, in individual therapeutic treatment and in association with muscle relaxants, pain-killers and central analgesics.
The 2-arylpropionic acids with anti-inflammatory activity of the present invention are made up of highly lipophilic carboxylic acids and as such are scarcely soluble in water. Nonetheless it is possible to prepare solutions of said acids, after salification in aqueous vehicles containing a surplus of a hydrate, of a bicarbonate and/or of an alkaline carbonate or an earth alkaline carbonate such as, for exampl
REFERENCES:
patent: 4877620 (1989-10-01), Loew et al.
patent: 5206262 (1993-04-01), Donati et al.
Chemical Abstracts, vol. 91 (1981) CA94: 162745 q.
Boltri Luigi
Clavenna Gaetano
Gentile Marco
Dompe' SpA
Spivack Phyllis G.
LandOfFree
Parenteral pharmaceutical compositions containing ammoniomalkyl does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Parenteral pharmaceutical compositions containing ammoniomalkyl , we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Parenteral pharmaceutical compositions containing ammoniomalkyl will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2247987