FR2488799A2 - ZOOTECHNIC COMPOSITIONS COMPRISING ZERANOL ON THE ONE HAND AND STEROID ON THE OTHER 4, 9, 11-TRIENIC - Google Patents

Abstract

THE SUBJECT OF THE INVENTION IS ZOOTECHNICAL COMPOSITIONS, AS DEFINED IN CLAIM 1 OF FRENCH PATENT APPLICATION 2388560, CHARACTERIZED IN THAT THEY CONTAIN A QUANTITY BETWEEN 10 AND 50MG OF ZERANOL FOR A QUANTITY BETWEEN 5 AND 50MG OF PRODUCT OF FORMULA I. (CF DRAWING IN BOPI) IN WHICH R REPRESENTS AN ALCOHYL RADICAL CONTAINING 1 TO 3 CARBON ATOMS, X REPRESENTS HYDROGEN, A SATURATED OR UNSATURATED ALCOHYL RADICAL CONTAINING FROM 1 TO 6 CARBON ATOMS OF WHICH ONE OF THE CARBON ATOMS MAY BE REPLACED BY AN OXYGEN ATOM, OR X STILL REPRESENTS A RADICAL ACYL DERIVED FROM A CARBOXYLIC ACID CONTAINING 1 TO 18 CARBON ATOMS. ZOOTECHNICAL COMPOSITIONS ARE MORE PARTICULARLY INTENDED FOR ADMINISTRATION IN PIGS TO IMPROVE WEIGHT GAIN.

Description

In the French patent application 2,388,560,

  On April 27, 1977, the Applicant Company described and claimed the technical compositions characterized by

  they contain zeranol and, on the other hand,

  of formula I ROX wherein R represents an alkyl radical containing from

  1 to 3 carbon atoms, X represents hydrogen, a

  Dical saturated or unsaturated alkyl containing from 1 to 6 atoms

  which one of the carbon atoms may be replaced by

  O represents an acyl radical derived from a carboxylic acid containing from 1 to 18 carbon atoms.

carbon atoms.

  These compositions are intended to promote the

  weight gain in farm animals, such as cattle

and pigs.

  The simultaneous presence of the two active ingredients

  force, unexpectedly, the favorable action on the growth

  The result is that the weight of the animals of both active ingredients increases, resulting in a significantly higher weight gain than would be expected given the known properties of the components. For cattle, and more particularly beef, the compositions

  may contain between 10 and 100 mg of zeranol and, preferably,

  between 20 and 60mg; and between 50 and 400mg of the product of

  Formula I and preferably between 100 and 300 mg.

  For administration to livestock, the compositions of the invention may be deposited as an implant in the dermis, preferably at the base of the ear. They are deposited for example from twenty days to four months before slaughter, from

  preferably one to three months before this one.

  In the application for the first certificate of addition, compositions according to the application of the main patent have been described, characterized in that they contain, in addition, other active ingredients involved in improving the - 1 -

  resorption of the compositions. This application for second

  certificate of addition relates to new

  zootechnical requirements as defined in the

main patent application.

  The main patent application generally claims all the combinations containing zeranol and

  a steroid of formula I, and more particularly described

  associations containing between 10 and 100 mg of zerals

  and preferably between 20 and 60 mg and between 50 and 400 mg of tablets of formula I and preferably between 100 and 300 mg. The main patent application envisages, more particularly, the compositions containing a steroidal amount of formula I which is much larger than the

amount of granol.

  We have just discovered that it was possible to obtain excellent results on pork growth, particularly on weight gain, by administering to pigs zootechnical compositions in which the quantity

  steroid of formula I is lower.

  The subject of the invention is zootechnical compositions

  as defined in claim 1 of the request for

  French patent 2,388,560, characterized in that they contain an amount of between 10 and 50 mg of zeranol

  for a quantity of between 5 and 50 mg of

mule I R (I)

/ OX

  in which R represents an alkyl radical containing 1 to 3 carbon atoms, X represents hydrogen, a radical

  saturated or unsaturated alkyl having from 1 to 6 carbon atoms

  wherein one of the carbon atoms can be replaced by an oxygen atom, X is still an acyl radical derived from a carboxylic acid having from 1 to 18 carbon atoms; The subject of the invention is more particularly the - 2 -

  compositions characterized in that they contain a

  rolde of formula I, wherein R represents a radical

  methyl; as well as those characterized in that they

  ferment a steroid of formula I, wherein X represents an acyl radical derived from an organic carboxylic acid having from 1 to 18 carbon atoms;

  The subject of the invention is more specifically

  characterized in that the steroid of formula I is 3-oxo 17M-acetoxy estra 4,9,11-triene;

  The subject of the invention is especially the

  characterized by the fact that they contain a quantity

  between 10 and 40 mg of zeranol, for a quan-

  between 10 and 30 mg of 3-oxo-17-acetoxy-estra 4,9,11-triene, and in particular the compositions characterized in that they contain from 10 to 40 mg of zeranol, for 20 mg of

  3-oxo 17, -acetoxy estra 4,9,11-triene.

  Naturally, the invention is particularly

  the subject of the compositions described below, in the

  experimental part. As noted above,

  The positions of the invention make it possible to obtain very good results in pigs. The subject of the invention is therefore the zootechnical compositions defined above, characterized in that they are intended for administration in the

- pork.

  The compositions of the invention are nevertheless not limited to the administration in pigs, they can also be administered in cattle, sheep and

Poultry.

  The compositions of the invention are preferably administered in the form of implants. These implants can be

  administered in the necks of animals or in the fis-

  siers.Ils are deposited for example from 20 days to 4 months before

  slaughter, preferably 1 to 3 months before slaughter.

  The compositions of the invention may also be

  either in the form of solutions or suspen-

  ingested; implants have the advantage

to be better resorbed.

  The zootechnical compositions, as defined above, also show interesting properties - 3 - - 4 -

- 2488799

  pharmacological properties, including anabolic properties and,

  more particularly, anabolic properties proti-

  diques. These properties make zootechnical compositions

  of the invention suitable for use as veterinary medicaments, in particular to increase the general organic resistance to aggression of all kinds, to combat

  against stunting, weight loss,

  general organic diseases related to a state of senescence and

  to fight secondary diseases

  infectious, parasitic and nutritional.

  The subject of the invention is therefore also, as a

  veterinary medicinal product, the zootechnical

  above, and in particular zootechnical compositions

  wherein the compound of formula I is 3-oxo-17;

  acetoxy estra 4,9,11-triene. The invention also

  pharmaceutical compositions containing, as the main

  active ingredient, at least one of the previously defined medicinal

  is lying. The active ingredient contents of the compositions and medi-

  The invention may vary according to the animal species.

  The compounds used in the compositions of the invention

  are known products; zeranol or zearalanol (see Merck Index 1976, 9th edition 9781) can be prepared, for example, according to the process described in US Pat. No. 3,239,345. The compounds of formula I can be prepared according to the processes described in US Pat. French Patents 1,380,414 and 1,492,985, as well as in Belgian Patent 696,084 The following examples illustrate the invention, but without limiting it:

  Example 1: zootechnical composition in the form of implant.

  An implant containing zeranol 36mg 3-oxo 17) -acetoxy estra 4,9,11-triene 20mg was prepared.

  Example 2: zootechnical composition in the form of implant.

  An implant containing zeranol 24mg 3-oxo 17J-acetoxy estra 4,9,11-triene 20mg was prepared.

  Example 3: zootechnical composition in the form of implant.

  An implant containing: zeranol 12mg

- 5 - 2488799

  3-oxo 17M-acetoxy estra 4,9,11-triene 2Omg

  Example 4: Effect on livestock of zootech compositions

  picnics. The test was carried out on LargeWhite-Landrace castrated male pigs. The animals are fattened in industrial pigs and are housed in pens that can contain 7 to 10 pigs. The animals are divided into 4 batches - a control batch, - a batch to which the implant of example 1 is administered, - a batch to which the implant of example 2 is administered,

  a batch to which the implant of example 3 is administered.

  Implants are introduced into the subcutaneous tissue,

  the ear, 63 days before slaughter. All the animals

receive the same food.

  The results obtained are as follows: AInnim, who received the Treatment Control implant of 11 'on

1 1 2 3 II

  Conclusion: The zootechnical compositions of Examples 1, 2 and 3 make it possible to improve very clearly the gain of

daily weight.

Time before slaughter 63 63 63 63

(in days) up to.

  Batch No. 1 2 3 4 Number of animals 15 14 15 14 Number of days of fattening Average weight on day 65.53 65.07 64.67 65.00 of treatment (Kg) Average weight at end of treatment test (Kg) 101.40 102.79 106.13 102.36 Average weight gain 35.87 37.72 41.46 37.36 Average weight gain 0.569 0, 599 0.658 0.59 daily (Kg) 0, 6 _, 99_, 5 -6-

Claims (1)

1, zootechnical compositions, as defined in claim 1 of the French patent application 2,388,560, characterized in that they contain an amount between 10 and 50 mg zeranol, for a quantity between 5 and 50 mg of product of formula I (1) in which R represents an alkyl radical containing from 1 to 3 carbon atoms, X represents hydrogen, a saturated or unsaturated alkyl radical containing from 1 to 6 carbon atoms of which one of the carbon atoms may be replaced by an oxygen atom, or X is still an acyl radical derived from a carboxylic acid containing from 1 to 18 carbon atoms; 2. The zootechnical compositions as defined in claim 1, characterized in that they contain a steroid of formula 1, in which R represents a methyl radical; The zootechnical compositions as defined in claim 1 or 2, characterized in that they contain a steroid of formula I, in which X represents an acyl radical derived from an organic carboxylic acid having 1 to 18 carbon atoms. ; 4. The zootechnical compositions as defined in claim 3, characterized in that the steroid of formula I is 3-oxo-179-acetoxy estra 4,9,11-triene; 5. zootechnical compositions, as defined in claim 4, characterized in that they contain an amount of between 10 and 40 mg of zeranol, for an amount of between 10 and 30 mg of 3-oxo-17-acetoxy estra 4, 9,11-triene; 6. The zootechnical compositions as defined in claim 5, characterized in that they contain from 40 mg of zeranol to 20 mg of 3-oxo 17f-acetoxy estra 4.9, 11-triene; The zootechnical compositions as defined in any one of claims 1 to 6, characterized in that they are intended for administration in pigs; 8.- As medicament, zootechnical compositions, as defined in any one of the claims 1-7;   9.- Pharmaceutical compositions containing, as a primary   active ingredient, at least one drug defined in claim 8.