Fast-implantable sustained-release microneedle patch and preparation method of fast-implantable sustained-release microneedle

A micro-needle and sustained-release technology, applied in the field of medicine, can solve the problems of complex process, cumbersome operation and high cost, and achieve the effects of wide range of drugs, reduction of process cost, and increase of drug load.

Pending Publication Date: 2020-03-10
BEIJING CAS MICRONEEDLE TECH LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The method is to inject microspheres made of biodegradable polymer materials into the mold, and prepare porous or multi-layer microneedles through extrusion and ultrasonic welding or thermal welding technology. The microneedles must first be produced by spray drying technology or Preparation of microspheres by emulsification method, complex process
The porous, multi-layered microneedles are weaker and more brittle than a single microneedle, making it difficult to effectively release them from the mold
[0008] To sum up, at present, taking polylactic acid microneedles as an example, the production of microneedles can be divided into two categories. One is to make polylactic acid degradable polymer materials and drugs into microspheres, and then add them to the microneedle mold. Then heat, melt and cool to form a microneedle with a certain mechanical strength. This kind of microneedle can load drugs, but it needs to be made into microspheres and then formed into a microneedle. The operation is cumbersome and the cost is high; the other is to directly add polylactic acid powder On the needle mold, it is heated and melted (above 200°C) and then cooled to form a microneedle, which is difficult to load drugs

Method used

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  • Fast-implantable sustained-release microneedle patch and preparation method of fast-implantable sustained-release microneedle
  • Fast-implantable sustained-release microneedle patch and preparation method of fast-implantable sustained-release microneedle
  • Fast-implantable sustained-release microneedle patch and preparation method of fast-implantable sustained-release microneedle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Embodiment 1 Preparation of rapidly implantable sustained-release microneedles

[0049] 1. Weigh 0.3g of PLGA (80 / 20) with a molecular weight of 20kDa, add 0.7ml N-methylpyrrolidone, and prepare a PLGA solution with a mass fraction of 30%; weigh 100mg of etonogestrel, add 1ml of N-methylpyrrolidone Pyrrolidone, be mixed with the etonogestrel solution of 100mg / ml; Above-mentioned etonogestrel solution 0.5ml is mixed with above-mentioned PLGA solution 0.5ml, is mixed with the 15% PLGA solution containing etonogestrel (50mg / ml), as needle tip injection Mold fluid.

[0050] 2. Weigh 0.25g of polyvinylpyrrolidone with a molecular weight of 10kDa, add 4.75ml of water to prepare an aqueous solution of 5% polyvinylpyrrolidone by mass fraction as the intermediate layer injection molding solution; weigh 3.5g of polyvinyl alcohol with a molecular weight of 50kDa. Add 6.5ml of water, heat at 80°C for 2 hours, and prepare a polyvinyl alcohol aqueous solution with a mass fraction of...

Embodiment 2

[0059] Embodiment 2 Preparation of rapidly implantable sustained-release microneedles

[0060] 1. Weigh 0.4g of polylactic acid (PLA) with a molecular weight of 10kDa, add 0.6ml of N-methylpyrrolidone to prepare a PLA solution with a mass fraction of 40%; weigh 10mg of red fluorescent dye, add 1ml of N-methylpyrrolidone , be prepared into a fat-soluble analog drug red fluorescent dye solution with a mass fraction of 10 mg / ml; mix 0.5 ml of the red fluorescent dye solution with 0.5 ml of the PLA solution, and prepare a 20% PLA solution containing the red fluorescent dye 5 mg / ml, As a needle tip injection molding fluid.

[0061] 2. Weigh 0.05g of pullulan, add 9.95ml of water, and prepare a pullulan aqueous solution with a mass fraction of 0.5%, as the intermediate layer injection molding solution; weigh 2.5g of sodium carboxymethyl cellulose with a molecular weight of 200kDa, add 7.5ml of water was prepared as an aqueous solution of 25% sodium carboxymethyl cellulose in mass f...

Embodiment 3

[0067] Example 3 Preparation of Rapidly Implantable Sustained Release Microneedles

[0068] 1. Weigh 0.3g of PLGA (75 / 25) with a molecular weight of 10kDa, add 0.7ml N-methylpyrrolidone, and prepare a PLGA solution with a mass fraction of 30%; weigh 15mg of interferon a-2b and dissolve it in sterile water for injection , add 35 mg of zinc hydroxide after micronization and sterilization, vortex and mix for 10 minutes to form 1 g of zinc salt interferon a-2b solution; add 1 g of zinc salt interferon a-2b solution to the above 30% PLGA The solution is stirred to form a drug-loaded sol system, which is used as a needle tip injection molding solution.

[0069] 2. Weigh 0.25g of trehalose, add 4.75ml of water to make an aqueous solution of trehalose with a mass fraction of 5%, and use it as the intermediate layer injection molding solution; weigh 3g of polyvinyl alcohol with a molecular weight of 70kDa, add 7ml of water, and place Heat at 85° C. for 2 hours, and prepare an aqueous ...

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Abstract

The invention discloses a fast-implantable sustained-release microneedle patch and a preparation method of a fast-implantable sustained-release microneedle. The invention firstly discloses the fast-implantable sustained-release microneedle, the fast-implantable sustained-release microneedle includes a needle tip, an intermediate layer, a needle body and a base, the needle tip is formed of a substrate containing a biodegradable water-insoluble polymer material, the intermediate layer is formed of a substrate containing a hydrophilic material, and the needle body and the base are formed of a substrate containing a biocompatible polymer material. The invention also discloses the preparation method of the microneedle. According to the microneedle or microneedle patch provided by the invention,the biodegradable water-insoluble polymer material is used to prepare the needle tip, the hydrophilic material is used to prepare the intermediate layer, and the biocompatible polymer material is used to prepare the needle body and the base, so that the multi-layered microneedles with water-insoluble needle tips are formed; and water is absorbed after the microneedles act on skin, the needle tipsand the needle bodies are quickly separated from the base within 1 h, after the base is removed, the needle tips remain in the skin, and the long-term release of a drug in vivo can be ensured withoutapplying the microneedle patch to a user for a long time.

Description

technical field [0001] The invention relates to the technical field of medicine. More specifically, it relates to a rapidly implantable sustained-release microneedle patch and a preparation method thereof. Background technique [0002] Transdermal drug delivery preparation is a dosage form in which drugs are administered through the skin, which can avoid the interference of the gastrointestinal environment on drug efficacy and the "first-pass effect" of the liver, maintain a constant optimal blood concentration or physiological effect, and prolong the effective time of action. The frequency of medication is reduced, patients can administer medication independently, and the compliance is better. However, the stratum corneum on the outer layer of the skin will hinder the absorption of drugs, and the drugs are not easy to penetrate into the body, resulting in a very limited choice of drugs. In recent years, microneedle technology has received widespread attention. It is one o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/34A61K8/02A61K8/88A61K8/85A61M37/00A61Q19/00
CPCA61K9/0021A61K47/34A61K8/0204A61K8/88A61K8/85A61M37/00A61Q19/00A61K9/00A61K8/02A61K9/70A61K47/42A61K47/32A61K47/26A61K47/36A61K47/38A61M37/0015A61M2037/0046A61M2037/0053
Inventor 高云华杨国忠张锁慧
Owner BEIJING CAS MICRONEEDLE TECH LTD
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