# US 2014/0194677 A1 · Estrus synchronization preparations and effective cidr-less protocols

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- Number: US 2014/0194677 A1
- Document ID: US20140194677A1
- Status: Published application
- Kind: A1
- Application number: 14/090,450
- Filed: 2013-11-26
- Published: 2014-07-10
- Earliest claimed: 2009-01-26
- Inventors: Jennifer Yoakum; Hal Witt
- Web page: https://patentgrep.com/patent/US20140194677A1

## CPC

- A61K 31/57: substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 31/565: not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K 31/567: substituted in position 17 alpha, e.g. mestranol, norethandrolone
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61P 15/08: for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

An injectable preparation of estrogenic and progestrogenic hormonal compounds in an anhydrous excipient injected to synchronize estrus in non-menstruating placental female animals, and a five to nine day protocol to apply the unique preparation to achieve estrus synchronization.

## Claims

### Claim 1

An injectable composition for promoting CIDR-less estrus synchronization in a cycling female cow, comprising:
(a) a steroidal estrogenic compound in an amount effective to induce estrus in a mature, cycling female cow;
(b) a steroidal progestogen compound in an amount effective to preserve a corpus luteum intact of the cow for a period of at least five days after injection; and
(c) an anhydrous excipient;
wherein the composition is formulated for intramuscular injection.

### Claim 2 (depends on 1)

The composition of claim 1, wherein the estrogenic compound is selected from the group consisting of estradiol 17-β and estradiol benzoate, or a derivative, analog, agonist, or mixture.

### Claim 3 (depends on 1)

The composition of claim 1, wherein the progestogen compound is a progestin compound.

### Claim 4 (depends on 1)

The composition of claim 1, wherein the progestogen compound is selected from the group consisting of progesterone, hydroxyprogesterone, medroxyprogesterone, altrenogest, and norgestomet, levonorgestrel, or a derivative, analog, agonist or mixture thereof.

### Claim 5 (depends on 1)

The composition of claim 1, wherein the progestogen compound is present at a concentration of at least 30 mg/mL.

### Claim 6 (depends on 1)

The composition of claim 1, wherein the estrogenic compound is present at a concentration of:
(a) at least 0.025% by volume;
(b) about 0.05% to about 1.0% by volume; or
(c) about 0.06% to about 0.125% by volume.

### Claim 7

A method for improving estrus synchronization or fertilization rates in a cycling, female cow, the method comprising:
(a) administering on Day Zero to a cycling, female cow by intramuscular injection a first steroidal hormone composition comprising an estrogenic compound, a progestogen compound, and an anhydrous excipient in an amount effective to induce estrus in the cow, wherein Day Zero is at least 45 days postpartum;
(b) administering on Day X to the cow a second composition comprising prostaglandin, or a biologically functional equivalent thereto, in an amount effective to initiate estrus, wherein Day X is from 5 to 8 days after Day Zero; and
(c) administering on Day Y to the cow a third composition comprising an estrogenic compound in an amount effective to force ovulation, wherein Day Y is from 12 to 36 hours after administration of the second composition;
wherein the cow does not comprise a controlled intravaginal hormone release device.

### Claim 8 (depends on 7)

The method of claim 7, further comprising the additional step of attempting to impregnate the cow on Day Z, wherein Day Z is not less than twelve hours after administration of the third composition.

### Claim 9 (depends on 8)

The method of claim 8, wherein:
the first composition is administered within the first twelve hours on Day Zero;
the second composition is administered within four hours of 8:00 AM on Day X where Day X is 6 to 7 days after Day Zero;
the third composition is administered within four hours of 1:00 PM on Day Y; and
the attempting to impregnate comprises artificial insemination within four hours of 2:00 PM on Day Z.

### Claim 10 (depends on 9)

The method of claim 9, wherein:
the first composition is administered within the first twelve hours on Day Zero;
the second composition is administered within one hour of 9:00 AM on Day X where Day X is 6 days after Day Zero;
the third composition is administered within one hour of 1:00 PM on Day Y; and
the insemination is performed within one hour of 2:00 PM on Day Z.

### Claim 11 (depends on 7)

The method of claim 7, wherein the first steroidal hormone composition comprises:
(a) a steroidal estrogenic compound in an amount effective to induce estrus in the cow;
(b) a steroidal progestogen compound in an amount effective to preserve a corpus luteum intact of the cow for a period of at least five days after injection; and
(c) an anhydrous excipient;
wherein the composition is formulated for intramuscular injection.

### Claim 12 (depends on 11)

The method of claim 11, wherein the estrogenic compound of the first steroidal hormone composition is selected from the group consisting of estradiol 17-β and estradiol benzoate, or a derivative, analog, agonist, or mixture.

### Claim 13 (depends on 11)

The method of claim 11, wherein the progestogen compound of the first steroidal hormone composition is a progestin compound.

### Claim 14 (depends on 11)

The method of claim 11, wherein the progestogen compound of the first steroidal hormone composition is selected from the group consisting of progesterone, hydroxyprogesterone, medroxyprogesterone, altrenogest, norgestomet, and levonorgestrel, or a derivative, analog, agonist or mixture thereof.

### Claim 15 (depends on 11)

The method of claim 11, wherein the estrogenic compound is present in the first steroidal hormone composition at a concentration of:
(a) at least 0.025% by volume;
(b) about 0.05% to about 1.0% by volume; or
(c) about 0.06% to about 0.125% by volume.

### Claim 16

A method for improving estrus synchronization or fertilization rates in a virgin heifer, the method comprising:
(a) administering on Day Zero to a virgin heifer by intramuscular injection a first steroidal hormone composition comprising an estrogenic compound, a progestogen compound, and an anhydrous excipient in an amount effective to induce estrus in the heifer;
(b) administering on Day X to the heifer a second composition comprising prostaglandin, or a biologically functional equivalent thereto, in an amount effective to initiate estrus, wherein Day X is from 5 to 8 days after Day Zero;
(c) administering on Day Y to the heifer a third composition comprising an estrogenic compound in an amount effective to force ovulation, wherein administration occurs not less than 12 hours after administration of the second composition; and
(d) inseminating the heifer on Day Z, wherein insemination occurs not less than 12 hours after administration of the third composition;
wherein the heifer does not comprise a controlled intravaginal hormone release device.

### Claim 17 (depends on 16)

The method of claim 16, wherein:
the first composition is administered within the first twelve hours on Day Zero;
the second composition is administered within four hours of 8:00 AM on Day X where Day X is 6 to 7 days after Day Zero;
the third composition is administered within four hours of 1:00 PM on Day Y; and
insemination occurs within four hours of 2:00 PM on Day Z.

### Claim 18 (depends on 17)

The method of claim 17, wherein:
the first composition is administered within the first twelve hours on Day Zero;
the second composition is administered within one hour of 9:00 AM on Day X where Day X is 6 days after Day Zero;
the third composition is administered within one hour of 1:00 PM on Day Y; and
the insemination is performed within one hour of 2:00 PM on Day Z.