Microparticles containing dutasteride, and preparation method therefor
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Assignees
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Publication Number
US-11911508-B2
Publication Date
2024-02-27
Expiration Date
Abstract
The present invention relates to: sustained-release microparticles capable of maintaining, for a long time, effects of preventing, treating or alleviating benign prostatic hyperplasia and prostate cancer and effects of preventing hair loss and promoting hair growth according to the administration of microparticles containing dutasteride; and a preparation method therefor, and according to the use of a method for administering the particles to a patient through an injection, a patient does not have to directly store or handle the microparticles, unlike an oral dosage form, and thus storage and handling are simple. In addition, drug effects are maintained for a long period of time of 1-3 months and, simultaneously, administration through injection can be facilitated since foreign body sensation and pain are reduced when being administered to a patient through injection because of the constant average diameter of the particles.
Core Innovation
The invention relates to dutasteride-containing microparticles comprising dutasteride and a biodegradable polymer. The microparticles have dutasteride evenly distributed in a spherical biodegradable polymer and have an average particle diameter of 20 to 70 μm. The microparticles contain the biodegradable polymer and dutasteride at a weight ratio of 3:1 to 9:1.
The microparticles are capable of preventing an initial excessive release of dutasteride after injection into a body and of maintaining a drug administration effect of dutasteride according to an initial release after injection into the body. The disclosed formulations include continuous release targets of 1 to 3 months, and the biodegradable polymer may be selected from biodegradable polymer materials listed in the disclosure.
A preparation concept using microchannels is described for forming spherical particles, where microchannel geometry and operating conditions affect particle size, uniformity, and aggregation. The disclosure includes examples using biodegradable polymers such as PLGA with dutasteride-containing microparticles and provides experimental release evaluation results demonstrating sustained drug release aligned with the 1 to 3 month target.
Claims Coverage
The claims include one independent claim directed to dutasteride-containing spherical biodegradable polymer microparticles with defined particle and composition parameters, plus dependent claims that add specific duration of continuous release, polymer selection constraints, and medical-use compositions. The independent claim includes five inventive features focusing on evenly distributed dutasteride, spherical biodegradable polymer particles of a defined size range, a defined drug-to-polymer weight ratio, and release behavior after injection.
Equally distributed dutasteride in spherical biodegradable polymer
The microparticles have a dutasteride drug evenly distributed in a spherical biodegradable polymer.
Defined spherical particle diameter range
The microparticles have an average particle diameter of 20 to 70 μm.
Defined dutasteride-to-polymer weight ratio
The microparticles contain the biodegradable polymer and dutasteride at a weight ratio of 3:1 to 9:1.
Prevention of initial excessive dutasteride release after injection
The microparticles are capable of preventing an initial excessive release of dutasteride after injection into a body.
Maintenance of dutasteride administration effect based on initial release
The microparticles are capable of maintaining a drug administration effect of dutasteride according to an initial release after injection into the body.
Overall, the claim set centers on spherical dutasteride-containing biodegradable polymer microparticles with dutasteride evenly distributed, a specified particle size range, and a specified dutasteride:polymer weight ratio, combined with release control after injection that prevents an initial excessive release while maintaining a sustained drug administration effect.
Stated Advantages
Prevents an initial excessive release of dutasteride after injection.
Maintains a drug administration effect of dutasteride according to an initial release after injection.
Reduced foreign body sensation/pain and uniform particle size are stated as advantages in the disclosure.
Documented Applications
Treating or preventing benign prostatic hyperplasia using dutasteride-containing microparticles.
Treating or preventing prostate cancer using dutasteride-containing microparticles.
Treating and preventing hair loss and promoting hair growth using dutasteride-containing microparticles.
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