Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1998-11-30
1999-09-14
Kumar, Shailendra
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
514556, 560196, 562553, A61K 3120, C07C 6934
Patent
active
059523794
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to stable, non-hygroscopic salts of L(-)carnitine and alkanoyl L(-)-carnitines, a process for their preparation and solid, orally administrable compositions containing such salts.
These salts lend themselves to the preparation of solid pharmaceutical compositions suitable for oral administration, such as pills, tablets, chewable tablets, capsules, granulates, powders and the like, of which L(-)carnitine or the alkanoyl L(-)carnitines, optionally formulated with the usual pharmacologically acceptable excipients, constitute the active ingredient.
These stable, non-hygroscopic salts also facilitate the production of solid compositions which may contain other active ingredients, e.g. with a nutritional and/or dietetic effect. These compositions which are administered orally constitute by far the most preferable administration form for a vast range of users and are increasingly establishing themselves on the so-called health food, medical food or nutraceutical market. These terms, which have yet to be rigorously defined from the regulatory point of view, denote foods or food components such as food supplements, dietetic products, energy foods, and the like, i.e. formulations which are not addressed to mainly or exclusively therapeutic purposes but which are aimed rather at enhancing well-being and at producing a general improvement in fitness and performance on the part of the consumer or at preventing metabolic disorders caused by dietary deficiencies or by the inadequate biosynthesis of essential endogenous substances as a result of advancing age.
The growing interest in L(-)carnitine and its derivatives in this field, too, stems from the increasingly widespread recognition, corroborated by scientific evidence, that L(-)carnitine and the lower alkanoyl L(-)carnitines, in addition to their well-known therapeutic value in the treatment of various diseases, make a marked contribution towards supplying energy to the skeletal musculature and increasing the resistance to prolonged, intense stress in professional athletes or in any subject practising sport also at amateur level, enhancing the performance capability of such subjects.
In addition, L(-)carnitine or its lower alkanoyl derivatives constitute indispensable nutritional supplements for vegetarians, whose diets have a low carnitine content as well as a low content of the two amino acids, lysine and methionine, which are the precursors of the biosynthesis of L(-)carnitine in the kidneys and liver.
The same considerations apply not only to those subjects who have to live on a diet poor in protein for prolonged periods of time, but, in general, also to those subjects who, though not presenting any clearly definable pathological condition, feel debilitated, experiencing a particular state of stress or physical and/or mental fatigue.
All these applications indicate that the solid orally administrable compositions are the preferred presentation form, inasmuch as they make it particularly easy for users to take the substances and comply with optimal dosage regimens.
Of growing interest, moreover, is the use of L(-)carnitine and its derivatives in the veterinary field and as animal feed supplements in the breeding of livestock, some species of fish, and, most notably, valuable animals such as racehorses and thoroughbreds.
It has long since been known that L(-)carnitine and its alkanoyl derivatives are extremely hygroscopic and not very stable when they occur as inner salts (or "betaines") as represented by the formula ##STR2## wherein R.dbd.H or C.sub.1 -C.sub.5 lower alkanoyl.
This leads to complex problems of processing, stability and storage both of the raw materials and of the finished products. For example, L(-)carnitine tablets have to be packaged in blisters to keep them out of contact with the air, since, otherwise, even in the presence of normal humidity conditions, they would undergo alterations, swelling up and becoming pasty and sticky. In addition, owing to the inadequate stability, traces of trimethylamine are released whi
REFERENCES:
patent: 4602039 (1986-07-01), Cavazza
Kumar Shailendra
Oh Taylor Victor
Sigma-Tau Industrie Farmaceutiche
LandOfFree
Stable, non-hygroscopic salts of L(-)carnitine and alkanoyl L(-) does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Stable, non-hygroscopic salts of L(-)carnitine and alkanoyl L(-), we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Stable, non-hygroscopic salts of L(-)carnitine and alkanoyl L(-) will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1510285