Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1990-04-16
1992-09-15
Brown, Johnnie R.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
514 25, 514 27, 536 168, 536 181, 435 72, 435825, A61K 3171, C07H 1704
Patent
active
051478587
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
The present invention concerns a new acidic polycyclic ether antibiotic having the absolute stereochemical formula ##STR1## wherein Me.dbd.CH.sub.3 ; pharmaceutically acceptable cationic salts thereof; nutrient feed compositions comprising said antibiotic for poultry, cattle or swine; its use as an anticoccidial agent in poultry, or as a growth promotant in cattle or swine; a fermentation method for its preparation; and the Actinomadura sp. microorganism which produces said antibiotic in said fermentation method.
The compound (I) is a new member of the acidic polycyclic ether group of antibiotics. This family includes such well known agents as monensin (The Merck Index, 10the Ed., Merck and Co.,Inc., Rahway, N.J., 1983, monograph no. 6100), nigericin (loc. cit., monograph no. 6390), narasin (loc. cit., monograph no. 6271), lasalocid (loc. cit., monograph no. 5204), and salinomycin (loc. cit., monograph no. 8193). The subject has been reviewed by Westley, "Polyether Antibiotics", Adv. Appl. Microbiol., vol. 22, pp. 177-223 (1977). These compounds are generally known as coccidiostats and/or as feed additive-growth promotants.
SUMMARY OF THE INVENTION
A culture of Actinomadura sp., ATCC 53676, when fermented under aerobic conditions in aqueous media, produces a new acidic polycyclic ether antibiotic, a compound having the formula (I), as specified above.
The present invention is directed to said compound of the formula (I), including the pharmaceutically-acceptable cationic salts thereof, and to a process for its preparation which comprises fermentation of said Actinomadura sp. ATCC 53676 in an aqueous nutrient medium comprising an assimilable source of carbon and nitrogen until a recoverable amount of said compound of the formula (I) is formed, preferably under submerged aerobic conditions. For use as an anticoccidial agent and/or a growth promotant, the compound (I) is not necessarily separated from the fermentation and isolated in substantially pure form, but is alternatively used in crude form, either in precipitated form admixed with mycelium (recovered by filtration of the fermentation medium), or in solids obtained by spray- or freeze-drying the entire fermentation medium.
Said pharmaceutically-acceptable cationic salts include, but are not limited to, those of sodium, potassium, calcium, ammonia, N,N'-dibenzylethylenediamine, N-methylglucamine (meglumine) and diethanolamine. The preferred cationic salts are those of potassium and sodium.
The present invention is also directed to nutrient feed compositions, one for cattle or swine which comprises the compound of the formula (I) in an amount effective to promote growth and/or improve the feed utilization of said cattle or swine, and the other for poultry which comprises the compound of the formula (I) in an amount effective to control coccidial infection in said poultry.
The present invention is further directed to a method for promoting growth and/or increasing the efficiency of feed utilization in swine or cattle which comprises administering to said swine or cattle a growth promoting or feed-utilization efficiency promoting amount of the compound of the formula (I), particularly in the form of a nutrient feed composition; and to a method for controlling coccidial infections in poultry which comprises administering to said poultry an anticoccidially effective amount of the compound of the formula (I), particularly in the form of a nutrient feed composition.
Finally, the present invention is directed to a biologically pure culture of Actinomadura sp. ATCC 53676, said culture being capable of producing the compound of the formula (I) in a recoverable quantity upon fermentation in an aqueous nutrient medium comprising assimilable sources of carbon and nitrogen; including said culture in freeze-dried form.
DETAILED DESCRIPTION OF THE INVENTION
The culture capable of producing the present polycyclic ether antibiotic of the formula (I) is designated Actinomadura sp., and has been deposited in The American Type Culture Coll
REFERENCES:
patent: 4148882 (1979-04-01), Celmer et al.
patent: 4195079 (1980-03-01), Celmer et al.
patent: 4746650 (1988-05-01), Cullen et al.
Chemical Abstracts, vol. 104, 166918w (1986).
Cullen Walter P.
Dirlam John P.
Maeda Hiroshi
Tone Junsuke
Brown Johnnie R.
Lumb J. Trevor
McFarlin D. Stuart
Peselev Elli
Pfizer Inc
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