Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Reexamination Certificate
1999-03-22
2002-12-24
Badio, Barbara P. (Department: 1616)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
C514S171000, C514S178000, C514S182000, C514S450000, C552S625000, C552S646000, C552S650000, C549S269000
Reexamination Certificate
active
06498153
ABSTRACT:
Sustained release pharmaceutical compositions containing growth promoters for use in food animals are described in U.S. Pat. No. 3,939,265 issued to J. A. Grandadam on Feb. 17, 1976 and U.S. Pat. No. 5,288,496 issued to D. H. Lewis on Feb. 22, 1994. The rate of release of the growth promoters of these compositions, however, generally does not comport with the growth periods of food animals in feedlots, the rate of release of the promoters declining over the growth period and becoming markedly reduced before the expiration of the period. To overcome this deficiency in feedlot growth promotion, it would be desirable to provide an extended release composition, from which the growth promoters are uniformly released over the growth period of the food animal in the feedlot, thereby enhancing the weight gain of the animal and improving the feed efficiency of the formulation. It has now been found that a composition comprising a first composition comprising growth promoters and a second composition comprising growth promoters and a biodegradable polymer releases the promoters over an extended period of time corresponding to the growth period of feedlot animals.
The present invention relates to an extended release composition comprising a first composition comprising growth promoters and a second composition comprising growth promoters and a biodegradable polymer. More specifically, the present invention relates to a composition comprising a first composition comprising a compound of formula 1
wherein R is loweralkyl; the ester derivatives, geometric isomers, stereoisomers, or optical isomers thereof, a compound of formula 2
wherein R
1
, and R
2
are loweralkyl; the ester derivatives, geometric isomers, stereoisomers, or optical isomers thereof, a compound of formula 3
wherein R
3
and R
4
are loweralkyl; the geometric isomers, stereoisomers, or optical isomers thereof, a compound of formula 4
wherein R
5
is loweralkyl; the ester derivatives, geometric isomers, stereoisomers, or optical isomers thereof; or a compound of formula 5
wherein R
6
is loweralkyl; the ester derivatives, geometric isomers, stereoisomers, or optical isomers thereof; and a second composition comprising a compound of formula 1
wherein R is loweralky; the ester derivatives, geometric isomers, stereoisomers, or optical isomers thereof, a compound of formula 2
wherein R
1
and R
2
are loweralkyl; the ester derivatives, geometric isomers, stereoisomers, or optical isomers thereof, a compound of formula 3
wherein R
5
is loweralkyl; the ester derivatives, geometric isomers, stereoisomers, or optical isomer thereof, a compound of formula 4
wherein R
3
and R
4
are loweralkyl; the geometric isomers, stereoisomers, or optical isomers thereof, and a compound of formula 5
wherein R
6
is loweralkyl; the ester derivatives, geometric isomers, stereoisomers, or optical isomers thereof; and a biodegradable polymer selected from the group consisting of homopolymers and copolymers of &ggr;-butyrolactone, &dgr;-valerolactone, &egr;-caprolactone, glycolide, DL-lactide, L-lactide, glycolic acid, DL-lactic acid, L-lactic acid, and combinations thereof, polydioxanones, polyorthesters, polyanhydrides, polycarbonates, polyesteramides, and polyphosphazines, useful for the promotion of weight gain in food animals. The present invention also relates to a pharmaceutical dosage form containing the composition, a method of preparing the dosage form utilizing the composition, as well as pellets of the composition for implantation in food animals.
Preferred compositions of growth promoters are those wherein R, R
1
, R
2
, R
3
, and R4, R
5
and R
6
are methyl and the aroyl or alkanoyl ester derivatives thereof, where applicable.
More preferred compositions are those wherein the growth promoters are;
(a) 17&bgr;-acetoxyestra-4,9,11-trien-3-one;
(b) 17&bgr;-benzoyloxyestra-4,9,11-trien-3-one;
(c) 17&bgr;-propionyloxy-4-androsten-3-one;
(d) pregn-4-en-3,20-dione;
(e) estra-1,3,5(10)-trien-3,17&bgr;-diol;
(f) 17&bgr;-benzoyloxyestra-1,3,5(10)-trien-3-ol;
(g) 3,4,5,6,9,10,11,12-decahydro-7,14,16-trihydroxy-3-methyl-1H(2)-benzoxacyclotetradecin 1-one.
Preferred biodegradable polymers are homopolymers and copolymers of glycolide, DL-lactide, L-lactide, glycolic acid, DL-lactic acid and L-lactic acid and combinations thereof.
More preferred biodegradable polymers are copolymers of DL-lactide and glycolide, copolymers of L-lactide and glycolide, polymers of L-lactide and polymers of DL-lactide, designated polylactides.
As used throughout the specification and appended claims, the term “alkyl” refers to a straight or branched chain hydrocarbon radical containing no unsaturation and having 1 to 5 carbon atoms. Examples of alkyl groups are methyl, ethyl, 1-propyl, 2-propyl, 1-butyl, 2-butyl, 1-pentyl, 3-pentyl, and the like; the term “alkanoic acid” refers to a compound formed by combination of a carboxyl group and a hydrogen atom or alkyl group. Examples of alkanoic acid are formic acid, acetic acid, propanoic acid, 1-methylpropanoic acid, 2,2-dimethylacetic acid, pentanoic acid, and the like; the term “alkanoyl” refers to the radical formed by removal of the hydroxyl group from an alkanoic acid. Examples of alkanoyl groups are formyl, acetyl, propanoyl, 2-methylpropanoyl, 2,2-dimethylacetyl, pentanoyl, and the like. The term “aryl” refers to an unsubstituted or a substituted phenyl group. Examples of aryl groups are benzene, 2-methylbenzene, 3-chlorobenzene, 4-hydroxybenzene, 3-methoxybenzene, methoxybenzene, 3-nitrobenzene, 2-trifluorobenzene, and the like. The term “aroic acid” refers to a compound formed by combination of an carboxyl group with an aryl group. Examples of aroic acids are benzoic acid, 2-methylbenzoic acid, 3-chlorobenzoic acid, 4-hydroxybenzoic acid, 3-methoxybenzoic acid, 3-nitrobenzoic acid, 2-trifluorobenzoic acid, and the like. The term “aroyl” refers to the radical formed by removal of the hydroxyl group from an aroic acid. Examples of aroyl are benzoyl, 2-methylbenzoyl, 3-chlorobenzoyl, 4-hydroxybenzoyl, 3-methoxybenzyol, 2-nitrobenzoyl, 2-trifluoromethylbenzoyl, and the like. The term “lower” as applied to any of the aforementioned groups or compounds refers to a group or compound having a carbon skeleton containing up to and including 5 carbon atoms. The expression “ester derivatives” refers to esters of the hydroxy group or groups of compounds of the present invention and an alkanoyl or aroyl group. Examples of ester derivatives are esters of formic acid, acetic acid, propanoic acid, 1-methylpropanoic acid, 2,2-dimethylacetic acid, pentanoic acid, benzoic acid, 2-methylbenzoic acid, 3-chlorobenzoic acid, 4-hydroxybenzoic acid, 3-methoxybenzoic acid, 2-nitrobenzoic acid and 2-trifluoromethylbenzoic acid and the like.
The compounds of the compositions of the present invention which lack an element of symmetry exist as optical antipodes and as the racemic forms thereof. The optical antipodes may be prepared from the corresponding racemic forms by standard optical resolution techniques or by synthesis from optically active precursors.
The present invention comprehends all optical isomers and racemic forms thereof and all stereoisomers of the compounds of the compositions disclosed and claimed herein. The formulas of the compounds shown herein are intended to encompass all possible optical and stereoisomers of the compounds so depicted.
The expression “food animal” refers to an animal raised for the purpose of providing a source of protein in the diet of humans or other animals. Examples of food animals are bovine animals, such as cows, cattle, steers, calves, and the like, ovine animals such as sheep; porcine animals such as pigs, and the like and avians such as chickens, turkeys and the like.
The expression “conventional drug delivery” refers to the temporally uncontrolled release of a drug into the blood of an animal resulting in a short duration of action, the blood levels of the drug being either initially high (intravenous administration) and falling off rapidly, or initially low (extramuscular administratio
Cady Susan Mancini
Gibson John W.
Macar Claude
Akzo Nobel N.V.
Badio Barbara P.
Blackstone William M.
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