Microneedle percutaneous patch containing donepezil
Inventors
Kim, Tae Hyung • Lee, Booyong • Kim, Jung Dong • Jeong, Do Hyeon • Shin, DongChul • Hwang, Yongyoun • Nam, Yun-sun • Lee, Joo Han • An, Eun Jin
Assignees
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Publication Number
US-11737973-B2
Publication Date
2023-08-29
Expiration Date
Abstract
The present invention relates to a composition for preparing a microneedle, a soluble microneedle, and a microneedle percutaneous patch comprising the soluble microneedle. A soluble microneedle contained in a microneedle percutaneous patch of the present invention has a high drug loading capacity and excellent strength and thus may contain an effective amount of donepezil or a pharmaceutically acceptable salt thereof even with a small area of the microneedle. Accordingly, the present invention is economical and produces a lower level of skin irritation.
Core Innovation
The invention provides a soluble microneedle comprising a homogeneous composition of donepezil or a pharmaceutically acceptable salt thereof and hyaluronic acid or a pharmaceutically acceptable salt thereof. The composition is defined by a weight ratio range of the donepezil or salt to the hyaluronic acid or salt of 1:1.5 to 1:2.05, and the donepezil content is 43 wt % or less of the total weight of the composition.
The soluble microneedle further specifies quantitative formulation and material properties that support use as a biodegradable delivery format. Hyaluronic acid or a pharmaceutically acceptable salt is defined by an intrinsic viscosity range of 0.150 to 0.250 m3/kg, and the soluble microneedle has a strength between 0.058 N and 1.603 N.
The invention also provides a microneedle percutaneous patch including the soluble microneedle and a support layer with at least one soluble microneedle attached thereto. Patch-level performance is constrained by an insertion capacity into skin per unit area of 90% or more, and the content further relates to donepezil stability and performance characteristics such as elution profiles and precipitation observations connected with donepezil content.
Claims Coverage
The independent claim defines a homogeneous soluble microneedle formulation with specified donepezil-to-hyaluronic-acid weight ratio and a maximum donepezil content limit. The family further indicates dependent-claim refinements that add quantitative constraints on hyaluronic-acid intrinsic viscosity, strength, and patch-level insertion capacity, and defines a microneedle percutaneous patch with a support layer.
Homogeneous soluble microneedle composition of donepezil and hyaluronic acid
A soluble microneedle comprising a homogeneous composition of donepezil or a pharmaceutically acceptable salt thereof and hyaluronic acid or a pharmaceutically acceptable salt thereof, wherein a weight ratio of the donepezil or salt and the hyaluronic acid or salt is 1:1.5 to 1:2.05 and wherein the content of the donepezil or salt is 43 wt % or less of the total weight of the composition.
Microneedle intrinsic viscosity bound for hyaluronic acid
The intrinsic viscosity of hyaluronic acid or a pharmaceutically acceptable salt thereof is 0.150 to 0.250 m3/kg.
Microneedle donepezil formulation strength constraint
The soluble microneedle has a strength between 0.058 N and 1.603 N.
Microneedle percutaneous patch with support-attached microneedles
A microneedle percutaneous patch including the soluble microneedle and a support with at least one soluble microneedle attached thereto.
Patch insertion capacity threshold into skin
A microneedle percutaneous patch has an insertion capacity into skin per unit area of 90% or more.
Overall, the claim coverage centers on a homogeneous soluble microneedle formulation of donepezil or a salt and hyaluronic acid or a salt with a specified 1:1.5 to 1:2.05 weight ratio and donepezil content of 43 wt % or less, supported by quantitative refinements including hyaluronic-acid intrinsic viscosity, microneedle strength, and patch-level skin insertion capacity for a support-attached microneedle percutaneous patch.
Stated Advantages
Reduced skin irritation.
Biodegradability without removal.
Improved bioavailability compared with oral administration (reported about 2.0× to 2.5×).
Documented Applications
Treatment of dementia using a donepezil-loaded soluble microneedle and a corresponding microneedle percutaneous patch.
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