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A rapidly dissolving microneedle based on water-soluble small molecules and its preparation and application

A technology of water-soluble small molecules and small molecules, which can be applied to medical preparations containing non-active ingredients, medical preparations containing active ingredients, organic active ingredients, etc. Solve problems such as slow dissolution rate, achieve the effect of simple and fast preparation process, suitable for large-scale production, and good solubility

Active Publication Date: 2021-05-18
武汉楚颜生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with the prior art, the microneedle matrix material used in the prepared small molecule soluble microneedle is a small molecule, which dissolves very quickly after piercing the skin, and can release the drug coated therein quickly, and the prepared microneedle The needle has good mechanical properties and is easy to pierce the skin. It solves the problems of slow dissolution and long application time of the existing soluble microneedles prepared by polymer materials, which can bring great convenience to patients.
Moreover, the small and medium molecule soluble microneedles of the present invention can coat hydrophilic drugs and hydrophobic drugs separately or at the same time, which solves the problem that it is difficult to coat hydrophobic drugs with current soluble microneedles

Method used

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  • A rapidly dissolving microneedle based on water-soluble small molecules and its preparation and application
  • A rapidly dissolving microneedle based on water-soluble small molecules and its preparation and application
  • A rapidly dissolving microneedle based on water-soluble small molecules and its preparation and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] This embodiment comprises the following steps:

[0031] (1) Preparation of maltose aqueous solution: a certain amount of maltose solid was dissolved in water, and stirred for several minutes to obtain a clear and transparent maltose aqueous solution with a mass fraction of 100w / v%.

[0032] (2) Fill the maltose aqueous solution into the microneedle mold: add the maltose aqueous solution prepared in step (1) to the surface of the microneedle mold (the length of a single microneedle is 300 microns), and utilize the method of molding to make the maltose aqueous solution enter And fill the mold base.

[0033] (3) Drying and demoulding to obtain rapidly dissolving maltose microneedles: drying the mold obtained in step (2) and demoulding to obtain maltose soluble microneedles.

Embodiment 2 to Embodiment 15

[0035] The parameters, conditions, etc. used in Embodiment 2 to Embodiment 15 are shown in the table below. Except for the specific parameters and condition settings given in the table, other unexplained parameters, conditions, processing methods, etc. are maintained with Embodiment 1. unanimous.

[0036] Table 1 embodiment 2 to the parameter that embodiment 15 adopts, list of conditions

[0037]

Embodiment 16

[0039] This embodiment comprises the following steps:

[0040] (1) Prepare a mixed aqueous solution of hydroxypropyl-β-cyclodextrin and hydrophilic model dye rhodamine B: dissolve a certain amount of hydroxypropyl-β-cyclodextrin and rhodamine B powder in water, stir for several minutes, A clear and transparent mixed aqueous solution with a mass fraction of hydroxypropyl-β-cyclodextrin of 100w / v% and a mass fraction of rhodamine of 0.1wt% was obtained.

[0041] (2) Fill the aqueous solution of hydroxypropyl-β-cyclodextrin mixed with rhodamine B into the microneedle mold: the hydroxypropyl-β-cyclodextrin mixed with rhodamine B prepared in step (1) The dextrin mixed aqueous solution is added to the surface of the microneedle mold (the length of a single microneedle is 450 microns), and the mixed aqueous solution is used to enter and fill the mold base by molding.

[0042] (3) Drying and demoulding to obtain rapidly dissolving hydroxypropyl-β-cyclodextrin microneedles: the mold o...

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Abstract

The invention belongs to the technical field of drug delivery devices, and discloses a rapidly dissolving microneedle based on water-soluble small molecules and its preparation and application. Then, the small molecule aqueous solution is filled into a microneedle mold, dried and demolded to obtain a rapidly dissolving microneedle based on the small molecule. In the present invention, by improving the overall process flow design of the preparation method and the conditions and parameters involved in each step (such as the type of small molecule and its aqueous solution concentration, etc.), it is possible to prepare a small molecule with an extremely fast dissolution rate and good mechanical properties. Compared with the existing technology, the soluble microneedles can effectively solve the problems of the time-consuming preparation process of the polymer soluble microneedles and the slow dissolving speed of the microneedles.

Description

technical field [0001] The invention belongs to the technical field of drug delivery devices, and more specifically relates to a rapidly dissolving microneedle based on water-soluble small molecules and its preparation and application. Background technique [0002] Transdermal drug delivery refers to a drug delivery method in which drugs are coated or applied on the skin surface. It has the advantages of simple and convenient operation, long-lasting drug effect, and no first-pass effect of drugs. However, due to the barrier function of the stratum corneum of the skin, the efficiency of transdermal administration is limited, and in many cases it cannot meet the needs of practical applications. Microneedle drug delivery is a new type of micro-invasive transdermal drug delivery method, which overcomes the barrier function of the stratum corneum of the skin and greatly improves the drug delivery efficiency and bioavailability of transdermal drug delivery. The length of the micr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K47/40A61K47/26A61K47/69A61K31/436
CPCA61K9/0021A61K31/436A61K47/26A61K47/40A61K47/6951
Inventor 朱锦涛王华张连斌陶娟
Owner 武汉楚颜生物科技有限公司
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