Sustained-release microparticles containing deslorelin, and preparation method therefor
Inventors
Assignees
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Publication Number
US-12251419-B2
Publication Date
2025-03-18
Expiration Date
Abstract
According to sustained-release microparticles containing deslorelin, and a preparation method therefor, of the present invention, sustained-release microparticles containing deslorelin in a formulation for subcutaneous administration are provided so that pain can be relieved during administration to animals, and a chemical castration effect can last for 2 to 36 months. In addition, the present invention is effective as a chemical castration agent for 2 to 8 months so as to have an excellent of removing boar taint.
Core Innovation
The invention relates to sustained-release microparticles containing deslorelin for chemical castration, with deslorelin released continuously after subcutaneous or intramuscular injection to relieve pain and maintain chemical castration effects. The core microparticle composition is a biodegradable polymer matrix containing deslorelin evenly distributed within an O1(Oil)/O2(Oil)/W(Water) emulsion or a W1(Water)/O(Oil)/W2(Water) emulsion.
A core aspect is preparing the microparticles by injecting a first mixture into a channel in a linear direction and injecting a second mixture into a channel formed on either side or one side to form a cross-point with the linear-flow channel, then crossing the flow in the linear direction with the flow in a lateral direction. This cross-point flow mixing produces microparticles in which deslorelin is evenly distributed.
The process includes removing an organic solvent present on the surface of the collected microparticles and washing and drying the microparticles. The disclosed compositions can additionally include an osmotic pressure regulator in the second mixture, and the sustained-release period is described as 2 to 36 months for continuous release and 2 to 8 months for boar taint removal in male pigs.
Claims Coverage
The provided document includes one independent claim. It covers a method for preparing sustained-release deslorelin microparticles by cross-point mixing of two channel flows to form specified emulsion types, yielding microparticles with an average diameter of 25 to 140 μm.
Cross-point mixing to evenly distribute deslorelin
Preparing microparticles by injecting a first mixture into a channel in a linear direction and allowing the first mixture to flow, then injecting a second mixture so as to form a cross-point with the linear-direction channel and allowing the second mixture to flow, and crossing the linear-direction flow with a lateral-direction flow to prepare microparticles in which deslorelin is evenly distributed.
Specific emulsion type microparticles
Wherein the prepared microparticles are an O1(Oil)/O2(Oil)/W(Water) emulsion or a W1(Water)/O(Oil)/W2(Water) emulsion.
Microparticle size range
Wherein the microparticles have an average diameter of 25 to 140 μm.
Sustained-release microparticles containing deslorelin in biodegradable polymer
Preparing a first mixture by mixing an active pharmaceutical ingredient mixture in which deslorelin is dissolved in a first solvent and a biodegradable polymer mixture in which a biodegradable polymer is dissolved in a second solvent, and preparing the microparticles as sustained-release microparticles containing deslorelin.
Overall, the claim coverage is directed to producing sustained-release deslorelin microparticles by cross-point channel flow mixing to achieve even deslorelin distribution, forming specified double-emulsion types, and obtaining microparticles with an average diameter of 25 to 140 μm.
Stated Advantages
Relieve pain during subcutaneous or intramuscular injection.
Maintain chemical castration effects via continuous deslorelin release.
Provide continuous drug release for 2 to 36 months.
Provide boar taint removal for 2 to 8 months in male pigs.
Achieve evenly distributed deslorelin in the microparticles.
Enable particle uniformity and prevention of aggregation.
Documented Applications
Subcutaneous or intramuscular injection for relieving pain and maintaining chemical castration effects.
Boar taint removal in male pigs using sustained-release deslorelin microparticles.
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