Solid compositions suitable for oral administration comprising n

Details Solid compositions suitable for oral administration comprising n Solid compositions suitable for oral administration comprising n

1999-09-24

2000-09-26

Geist, Gary

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Radical -xh acid, or anhydride, acid halide or salt thereof...

514546, 514561, 560252, 560253, 562571, A61K 3138, A61K 3122, C07C 6702, C07C22900

Patent

active

061243604

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to stable, non-hygroscopic, pharmacologically acceptable salts of L-carnitine and lower alkanoyl-L-carnitines which favourably lend themselves to the preparation of solid, orally administrable compositions. The present invention also relates to such compositions.
Various therapeutic uses of L-carnitine and alkanoyl derivatives thereof are already known. For instance, L-carnitine is used in the cardiovascular field for the treatment of acute and chronic myocardial ischaemia, angina pectoris, heart failure and cardiac arrhythmias.
In the nephrological field, L-carnitine is administered to chronic uraemics undergoing regular haemodialytic treatment to combat myasthenia and the onset of muscular cramps.
Other therapeutic uses relate to the normalization of the HDL:LDL+VLDL ratio and total parenteral nutrition.
It is also known that the salts of L(-)-carnitine and its alkanoyl derivatives present the same therapeutic or nutritional activities as those of the so-called inner salts and can, therefore, be used in their place, provided these salts are "pharmacologically acceptable", i.e. they do not present unwanted toxic or side effects.
In practice, then, the choice between an "inner salt" and a true L(-)-carnitine or alkanoyl-L(-)-carnitine salt will depend essentially on availability, economical and pharmacy considerations rather than on therapeutic or nutritional considerations.
The object of the present invention is to provide stable and non-hygroscopic salts of L-carnitine and lower alkanoyl-L-carnitines which are endowed with an enhanced therapeutical and/or nutritional efficacy with respect to their inner salt counterparts.
It should, therefore, be clearly understood that the utility of the salts of the present invention is not confined to their lack of hygroscopicity and higher stability compared to the corresponding inner salts, but also resides in the contribution to the overall therapeutic and/or nutritional value of the salt in its entirety provided by their anionic moiety. This value is, therefore, no longer to be attributed exclusively to the "carnitine" moiety of the salt.
Because of their lack of hygroscopicity these salts can be easily compounded, particularly with a view of preparing solid, orally administrable compositions.
As is well known to experts in pharmacy, the processing of hygroscopic products entails the use of controlled-humidity chambers both for storage and for the processing itself.
Moreover, the finished products must be packed in hermetically sealed blisters in order to avoid unpleasant consequences due to humidity.
All this involves extra costs both for the storage of raw materials and for their processing and packaging.
Among the populations of the industrialised countries there is an increasingly widespread use of food supplements or "nutraceuticals" both by sportsmen (amateurs or professionals) and by people in good health.
The former use L-carnitine or food supplements containing L- carnitine because it facilitates the oxidation of fatty acids and makes a larger amount of energy available to skeletal muscle, thus allowing enhanced performance and giving rise to less accumulation of lactic acid in the athletes' muscles.
People in good health use these food supplements as health foods, i.e. for the purposes of favouring a reduction in serum fat levels and normalisation of the ratio between the various cholesterol fractions in order to prevent diseases related to lipid metabolism disorders.
It has been estimated that the amount of L-carnitine and its derivatives sold for non-ethical purposes is twice that sold for ethical purposes.
The US market for food supplements or nutraceuticals amount to approximately 250 billion dollars, whereas the estimated figure for the European market is approximately 500 billion dollars (Food Labeling News, 1994, "Nutraceuticals" Market said to be a vast one, March, Vol. 2, n.degree. 25; King Communications Group Inc., 1993, "Nutraceuticals" Foods, Drink in Global Market Food and Drink Daily, April, Vol. 3, n.degree.

REFERENCES:
patent: 4602039 (1986-07-01), Cavazza
patent: 4962121 (1990-10-01), Hamberger et al.
patent: 5571783 (1996-11-01), Montagne et al.
patent: 5589468 (1996-12-01), Lin et al.

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