Method for preparing and using water-based steroid pheromone compositions

A composition and pheromone technology, which is applied in the directions of pharmaceutical combinations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., and can solve the problems of no instructions, no description of the preparation or use of solutions or suspensions, etc.

Inactive Publication Date: 2008-07-09
PHERO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, they do not describe any formulation or use of these solutions or suspensions, nor do they state that such compositions can be administered without the use of organic solvents or propellants

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The steroid pheromone androstenone was premixed with the monohydric alcohol by dissolving 1.52 g of androstenone in 157 g of 2-propanol. Diol 1,4-butanediol was mixed with surfactant by dissolving 500 g of dodecylbenzenesulfonic acid as its monoisopropylamine salt in 3,000 g of 1,4-butanediol pre-mixed. The two premixes were then mixed together with continuous stirring while adding in a slow stream an amount of water (96,341.48 g) sufficient to obtain 100% by weight to prepare the microemulsion.

[0029] The resulting microemulsion was stable when exposed to room temperature for 150 days, as determined by gas chromatographic analysis. Unexpectedly, microemulsions were also stable after three cycles of freezing at -15°C for 22-24 h and thawing at room temperature for 2 h, as determined by gas chromatographic analysis.

Embodiment 2

[0031] The steroidal pheromone androstenone was premixed with the monohydric alcohol by dissolving 0.76 g of androstenone in 78.5 g of 2-propanol. The diol 1,4-butanediol was premixed with the surfactant by dissolving 500 g of dodecylbenzenesulfonic acid in 3,000 g of 1,4-butanediol. The two pre-blends were then mixed together with constant stirring while an amount of water (96,420.74 g) was added in a slow stream, sufficient to obtain 100% by weight, to prepare the microemulsion.

[0032] The resulting microemulsion was stable when exposed to room temperature for 150 days, as determined by gas chromatographic analysis. Unexpectedly, microemulsions were also stable after three cycles of freezing at -15°C for 22-24 h and thawing at room temperature for 2 h, as determined by gas chromatographic analysis.

Embodiment 3

[0034] The steroid pheromone androstenone was premixed with the monohydric alcohol by dissolving 1.52 g of androstenone in 157 g of 2-propanol. The diol 1,4-butanediol was premixed with the surfactant by dissolving 500 g of nonylphenol ethoxylated with 9 moles of ethylene oxide in 3,000 g of 1,4-butanediol. produce microemulsions. The two pre-blends were then mixed together with continuous stirring while an amount of water (96,341.48 g) was added in a slow stream, sufficient to obtain 100% by weight.

[0035] 20 mL of the resulting microemulsion was placed in a 30 mL high density polyethylene bottle (AmpakDistribution Inc. Richmond, BC). The bottle fits a mechanical nebulizer that delivers approximately 0.13 mL of an aerosol containing approximately 2 μg of androstenone when the stopper is manually depressed. Two depressions deliver approximately 4 μg, which is well within the effective dose range of 2-20 μg established by Melrose et al. (1972). When sows were examined by v...

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Abstract

This invention relates to methods of formulating steroid pheromones as novel stable emulsions. These emulsions can be used for administration of the steroid pheromones to living organisms such as humans or pigs in place of current organic solvent or pressurized aerosol formulations that present hazards in both shipping and application. Uses relating to pigs are in stimulation of sexual maturation, diagnosis of the onset and timing of oestrus in female pigs, and inducing boars to accept dummy sows. The water-based emulsions can include 5 -androst-16-en-3-one and 3 -hydroxy-5a-androst-16-ene for administration to pigs. The use of water-based emulsions eliminates the need for formulation of the steroid pheromones in organic solvents, delivery of these pheromones as pressurized aerosols, and following the precautions required to reduce hazards during shipping and handling. The water-based emulsions allow for treatment of living organisms where a liquid organic solvent formulation or aerosol of the pheromones might be harmful to the organism or a substrate.

Description

field of invention [0001] The present invention relates to a process for formulating steroid pheromones into novel stable emulsions. These emulsions can be used to administer steroidal pheromones to living organisms, such as humans or pigs, in place of current organic solvent formulations or pressurized aerosol formulations which are hazardous in delivery and application. Uses involving pigs are stimulating sexual maturation in sows, diagnosing estrus onset and cycle, and inducing boars to accept model sows. Background of the invention [0002] Steroidal pheromones range from insoluble to slightly soluble in water (Hoover, 1975). Various organic solvents must be used to extract steroidal pheromones from mammalian subjects. These solvents include methanol (Brooksbank et al. 1974; Nixon et al. 1988), ethanol (Cutler et al. 1987, 1989, 1990, 1992; Preti et al. 1987), diethyl ether (Patterson 1968a,b; Gower et al. Patterson 1968b; Brooksbank et al. 1974), and ethyl acetate (N...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/568A61K9/107A61P5/24
CPCA61K9/12A61K9/1075A61K31/568A61K31/57A61K47/10A61K31/185A61P15/08A61P5/24A61K2300/00
Inventor 诺曼·阿夫利诺琼·P·拉方丹
Owner PHERO TECH
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