Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Liposomes
Patent
1995-09-01
1998-04-28
Azpuru, Carlos
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Liposomes
424439, A61K 9127, A61K 4742
Patent
active
057441570
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a preparation for maintaining and/or increasing muscular power and body cell mass. The preparation contains a thiol compound, particularly cysteine, a derivative and/or analogue thereof as well as conventional excipients.
The muscular mass of a body influences not only its muscular power but also the entire protein metabolism of the body. The heavy loss of muscular mass and the accompanying reduction of the body cell mass and the most important amino acid reservoir of the body are frequent and life-threatening complications in the case of carcinoses and infectious diseases, such as the immunological deficiency AIDS. Furthermore, a progressive loss of skeletal muscular mass is found in patients suffering from non-insulinogenic diabetes (type 2 diabetes) as well as in the case of amyotrophic lateral sclerosis. When persons get older, they also undergo a progressive loss of skeletal muscular mass and muscular power. This is accompanied by diverse and constantly increasing symptoms which cover the wide range from muscle strains, impairments of the vertebral column to physical decline resulting from old age and acute need of care. The patients generally feel the cachectic processes to be especially burdening. There is no satisfactory treatment for this by now. Also in the case of slighter muscular troubles such as lumbago, overstretching and accompanying secondary complaints such as backache and impairments of the vertebral column, it has not yet been possible to correct satisfactorily one of the most important causes of these problems, namely the progressive loss of muscular cell mass and muscular power, respectively.
Thus, the object of the present invention is to provide a preparation with which the above-mentioned problems can be treated successfully.
According to the invention this is achieved by providing a preparation which contains a thiol compound, particularly cysteine, a derivative and/or analogue thereof as well as conventional excipients. Glutathione is also to be counted among the favorable thiol compounds. N-acetylcysteine and homocysteine as well as a thiazolidine derivative of cysteine, e.g. 2-oxo-4-thiazolidine carboxylate, are also to be mentioned as being especially suitable.
In a preferred embodiment the preparation according to the invention includes a substance which improves the absorption of the active compound(s) by the cell. It is possible to use conventional substances for this purpose, which facilitate the substance transport into the cells. It is preferred to use liposomes, into the lumina of which the active compound(s) are incorporated. Liposomes are produced according to usual processes described in the literature.
In another preferred embodiment the preparation according to the invention includes a substance which increases the effectiveness of active compound(s). Such a substance is e.g. a hormone such as insulin or insulin-like growth factor, a vitamin, a nutrient such as glucose, or an amino acid, or a conventional, sarcoplastic drug such as an anabolic steroid.
The preparation according to the invention usefully contains 5-95, preferably 30-70, and in particular 40-60, % by weight of active compound or active compounds, and 95-5, preferably 70-30, and in particular 60-30, % by weight of conventional excipients. The preparation can be applied in the usual ways e.g. orally, parenterally or locally, the oral application being preferred. Furthermore, the preparation can be applied in conventional forms e.g. as a solution, suspension, emulsion, powder, tablet, capsule or ointment, with enteric-coated capsules being preferred. In addition, the excipients used may be the conventional ones such as drug carriers, binders, blasting agents, lubricating agents, solvents, solutizers, release accelerators, release retarders, emulsifiers, stabilizers (e.g. antioxidants, buffers), coloring agents or taste improvers. The solvent preferred is pyrogen-free water or physiological saline solution, a concentration of 10.sup.-5 to 10.sup.-1 preferably 10.sup.-3 to
REFERENCES:
patent: 5292773 (1994-03-01), Hirsch et al.
Azpuru Carlos
The German Cancer Research Institute
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