Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form
Patent
1998-12-10
2000-11-21
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
514825, 514456, A61K 900, A61K 3135, A01N 4316
Patent
active
061499234
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to an antirheumatic agent comprising diethyl L-lysylcromoglycate or a nontoxic salt thereof as an active ingredient.
BACKGROUND ART
A typical rheumatic disease--chronic rheumatoid arthritis (hereinafter RA)--is a systemic connective-tissue disease having a main symptom of polyarthritis chronica, and is one of the autoimmune diseases. The disease type thereof is generally polyarthritis which is progressive and chronic. It includes various clinical types such as one showing spontaneous remission, one showing highly progressive destruction and absorption of joints (e.g., arthritis dissecans) and the like. Clinical symptoms thereof include arthritis, swelling of joint, pain, deformation, morning stiffness, rheumatoid nodule, angiitis and the like.
For internal therapy of RA at present, nonsteroidal antiflammatory agents (e.g., aspirin, indometacin, diclofenac sodium, ibuprofen, loxoprofen sodium, piroxicam, ampiroxicam, naproxen, and the like), adrenocorticosteroidal agents (e.g., intraarticular injection and oral administration of prednisolone, and the like), immunomodulators (e.g., gold preparation, D-penicillamine, bucillamine, actarit and the like), immunosuppressive agents (e.g., methotrexate, mizoribine and the like), and the like are used. These medicaments, nevertheless, fail to provide sufficient therapeutic effects, but rather, cause various side effects. For example, nonsteroidal antiinflammatory agents may cause peptic ulcer, nephropathy, hepatopathy and the like, adrenocorticosteroidal agents may induce and exacerbate infectious diseases, diabetes, moon face, peptic ulcer, adrenocortical insufficiency, thrombophlebitis, osteoporosis and the like, immunomodulators may cause dermatopathy, nephropathy, stomatitis and the like, and immunosuppressive agents may cause hepatopathy, leukopenia, thrombocytopenia and the like, some of which constituting severe side effects.
In view of the above-mentioned situation, there is a demand for the development of an antirheumatic agent effective for the alleviation and suppression of the symptoms of RA and causing fewer side effects.
It is therefore an object of the present invention to provide an antirheumatic agent that is delivered to local sites after oral administration, that is effective for the treatment of RA and that causes fewer side effects.
DISCLOSURE OF THE INVENTION
The present inventors have conducted various studies to solve the above-mentioned problems and found that cromoglycic acid derivatives of the following formula (I): ##STR2## namely, diethyl L-lysylcromoglycate and a nontoxic salt thereof, are efficiently absorbed from the digestive tract, delivered to local sites and suppress the symptoms of polyarthritis, which is the main symptom of RA, and developed further studies to result in the completion of the present invention.
That is, the present invention provides the following. nontoxic salt thereof as an active ingredient. organic acid. least one organic carboxylic acid selected from the group consisting of maleic acid, fumaric acid, tartaric acid, citric acid, succinic acid, malic acid, oxalic acid, mandelic acid, malonic acid and benzoic acid. diethyl L-lysylcromoglycate or a nontoxic salt thereof, and a pharmaceutically acceptable carrier. to (5) above, which is an oral preparation. to (5) or (6) above, further comprising an organic acid. to (7) above, wherein the organic acid is at least one organic carboxylic acid selected from the group consisting of maleic acid, fumaric acid, tartaric acid, citric acid, succinic acid, malic acid, oxalic acid, mandelic acid, malonic acid and benzoic acid. effective amount of diethyl L-lysylcromoglycate or a nontoxic salt thereof to a patient. the therapy of rheumatism. the production of a pharmaceutical agent for the therapy of rheumatism. therapy of rheumatism of any of (5)-(8) above and a written matter associated therewith, the written matter stating that said pharmaceutical composition can or should be used for the therapy of rheumatism.
In the p
REFERENCES:
patent: 4066756 (1978-01-01), Orr et al.
patent: 4847286 (1989-07-01), Tamaki et al.
Yoshimi et al Importance of Hydrolysis of Amino Acid Moiety in Water-Soluble Prodrugs of Disodium Cromoglycate for Increased Oral Bioavailability 1992 J. Pharmacobio-Dyn 15:339-345.
Mori et al Pro-drugs for the Oral Deliver of Disodium Cromoglycate 1988 Chem. Pharm. Bull. 36:338-344.
Fukata Fumio
Kobayashi Yuta
Okunishi Hideki
Shirahase Hiroaki
Yoshimi Akihisa
Kyoto Pharmaceutical Industries, Ltd.
Page Thurman K.
Ware Todd D.
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