Moisture-proof mite allergen soluble microneedle

An allergen, soluble technology, applied in the direction of allergen antigen components, microneedles, needles, etc., can solve the problems of poor mechanical properties, uncertainty in the selection of matrix materials, and no consideration of humidity factors, and achieve good mechanical strength. Effect

Pending Publication Date: 2021-10-26
微缔医药科技(杭州)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] For example, the Chinese patent with the publication number CN109715075A provides a preparation idea of ​​loading microneedles with a composition containing at least one allergen, and selects a specific matrix material hyaluronic acid for research, but the technical solution has shortcomings The reason is that this patent focuses on the changes in the preparation process of microneedles loaded with allergens, and does not examine the factors affecting humidity, different allergens, and different matrix materials, nor does it discuss any specific allergens (such as mite allergens) ) into dissolvable microneedles for formulation screening
Therefore, when the mite allergen is loaded into the soluble microneedles under specific humidity conditions, the difference in the mechanical properties of the soluble microneedles caused by the change of the formulation cannot be known from this patent
[0007] For example, the Japanese patent with the publication number JP2014156433A only generally introduced the possibility of allergen loading into microneedles, focusing on the change of microneedle structure, but the disadvantage of this technical solution is that there is no specific embodiment Prove that different matrix materials have different mechanical properties for the development of mite allergen soluble microneedles, and it is impossible to judge whether they are resistant to moisture
The conclusion of this document is very different from the common knowledge that "the greater the relative humidity, the worse the mechanical properties", but the technical shortcomings of this document are: ①Due to the difference in climate and region in daily life, the relative humidity of the air is also very different , while the literature only examined the relative humidity conditions of 43%RH and 86%RH, it is not enough to predict that the mechanical properties of Gantrez S-97 microneedles also meet the requirements of the formulation under other humidity conditions; ②Further, due to the mite allergen The physical and chemical properties are very different from those of vitamin K, so when using Gantrez S-97 drug-loaded mite allergen to make soluble microneedles, does it still comply with the law that "the mechanical properties of microneedles at 86% relative humidity are better than those at 43% relative humidity" , also unknown
[0010] It can be seen that under different humidity conditions, the selection of soluble microneedles made of different materials loaded with different drugs has different effects on the mechanical properties of the microneedles, which has brought great implications for the selection of matrix materials when developing soluble microneedles for mite allergens. uncertainty

Method used

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  • Moisture-proof mite allergen soluble microneedle
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  • Moisture-proof mite allergen soluble microneedle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Preparation of Mite Allergen Soluble Microneedle Female Mold

[0039] like figure 1 , the present invention adopts MEMS technology in combination with inverted mold method to prepare microneedle negative mold, and the steps are as follows:

[0040] 1) Preparation of monocrystalline silicon positive mold microneedles

[0041] The male mold microneedle is prepared by MEMS technology, the microneedle is listed as 10*10, the height of the needle is 600 μm, the diameter of the bottom is 300 μm, and the diameter of the needle tip is ≤10 μm.

[0042] 2) Preparation of polydimethylsiloxane mold

[0043] After mixing polydimethylsiloxane and curing agent at a mass ratio of 8:1, pour it into a cuboid container with a single crystal silicon positive mold microneedle; place the container in a vacuum drying oven at a vacuum degree of 0.1MPa Vacuumize for 3 minutes to remove the air bubbles in the mixture; put it into an oven, dry it at 80° C. for 3 hours, and take it ou...

Embodiment 2

[0044] Example 2 Preparation of Mite Allergen Soluble Microneedles

[0045] like figure 2 , the present invention adopts extrusion molding method to prepare mite allergen soluble microneedles, the steps are as follows:

[0046] 1) After mixing the matrix material and the mite allergen according to the prescription ratio, dissolve it with phosphate buffered saline (PBS) with a pH of 7.4 to form a uniform mixed solution (i.e. matrix solution), take an appropriate amount of matrix solution into a centrifuge tube, Put it in a centrifugal precipitator, centrifuge to remove the air bubbles in the matrix solution, and let it stand for later use.

[0047] 2) Take the matrix solution obtained after centrifugation in step 1), pour it on the polydimethylsiloxane mold prepared in Embodiment 1 of the present invention, then place the polydimethylsiloxane mold on a plane, and squeeze it with a roller The matrix solution above the mold goes back and forth several times, so that the matrix...

Embodiment 3

[0048] Example 3 Effects of Different Humidity Conditions on the Mechanical Properties and Activity of Mite Allergen Soluble Microneedles

[0049] In the present invention, the matrix material is intended to be a high-molecular polymer. Based on the research of the aforementioned literature, this embodiment intends to use methyl vinyl ether-maleic anhydride copolymer (Gantrez S-97) to load the mite allergen preparation Adult mite allergen-soluble microneedles, by measuring the mechanical strength and mite allergen activity changes of mite allergen-soluble microneedles under different humidity conditions, to explore the effect of humidity conditions on the mite allergen-soluble microneedles mechanical properties and effect on activity. Humidity conditions are selected from 10% to 90% relative humidity (10 to 90% RH). To provide a premise basis for the follow-up microneedle material composition, combination with allergens, and their relationship with each other on the impact of...

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Abstract

The invention discloses a moisture-proof mite allergen soluble microneedle. The moisture-proof mite allergen soluble microneedle comprises a needle body and a backing, wherein the needle body comprises mite allergen and a composite matrix material, the composite matrix material is a mixture of a methyl vinyl ether-maleic anhydride copolymer and polyvinyl alcohol, and the content ratio of the methyl vinyl ether-maleic anhydride copolymer to the polyvinyl alcohol is (1:1.5)-(2:1). According to the moisture-proof mite allergen soluble microneedle, by screening the appropriate matrix material type and content (Gantrez S-97+PVA) and the appropriate drug loading ratio, the prepared mite allergen soluble microneedle can still have good mechanical strength under a high-humidity condition, is easy to pierce into the skin for drug administration, and does not affect the activity of the mite allergen.

Description

technical field [0001] The invention relates to the technical field of administration of mite allergens, in particular to a moisture-resistant soluble microneedle for mite allergens. Background technique [0002] The incidence of allergies is very high, and literature reports that about one-third of people suffer from allergic diseases in their lifetime. According to the statistics of my country's Beijing area, the incidence of allergies in the general population is about 15%. Allergic disease is even as high as 50% in parts of the Pacific Ocean. Since entering the 21st century, the disease has become one of the most common global diseases. According to the data of the World Health Organization, 22% to 25% of people in the world suffer from allergic diseases at present, and the rate of increase is 23 times every 10 years. Therefore, allergy and anti-allergy are unavoidable serious problems faced by modern people. Antigenic substances that cause allergic reactions are cal...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K39/35A61K9/00A61K47/32A61M37/00A61P33/14
CPCA61K9/0021A61K39/35A61K47/32A61P33/14A61M37/0015A61M2037/0053A61M2037/0046
Inventor 不公告发明人
Owner 微缔医药科技(杭州)有限公司
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