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Flexible slow-release micro-needle patch and preparation method thereof

A micro-needle sticking, flexible technology, applied in the field of medicine, can solve the problems of inability to meet the production of large-dose pharmaceutical preparations, low drug loading of micro-needles, organic solvent residues, etc., and achieves easy control of solubility, simple process, and conditions. mild effect

Inactive Publication Date: 2017-02-22
BEIJING CAS MICRONEEDLE TECH LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this method is cumbersome in process operation, and may cause organic solvent residues in the microsphere production process, which affects safety. At the same time, the microneedles produced by this method have low drug loading, which cannot meet the production of large-dose drug preparations

Method used

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  • Flexible slow-release micro-needle patch and preparation method thereof
  • Flexible slow-release micro-needle patch and preparation method thereof
  • Flexible slow-release micro-needle patch and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1: Preparation of sustained-release microneedle patch for intradermal administration

[0044] 1) Weigh 0.5 g of carboxymethyl cellulose with a molecular weight of 200 KDa, add 4.5 ml of water, and prepare a carboxymethyl cellulose aqueous solution with a mass fraction of 10%.

[0045] 2) Grinding the raw material medicine of paclitaxel in crystal form and sieving to obtain drug crystals with a particle size of about 10 μm. Weigh 100 mg of the sieved drug crystal and add it to the above-mentioned carboxymethyl cellulose aqueous solution, and magnetically stir (1500rpm, 12h) to obtain a microneedle emulsion (ie, microneedle injection molding solution) with a mass ratio of matrix material to drug of 5:1. .

[0046] 3) Add 80 μl of microneedle emulsion into the microneedle mold, and make the microneedle emulsion enter the microneedle pinholes by vacuuming.

[0047] 4) Dry the above-mentioned microneedle mold with the microneedle emulsion added under the conditions...

Embodiment 2

[0051] Example 2: Preparation of sustained-release microneedle patch for intradermal administration

[0052] 1) Weigh 2 g of PVP K30, add 4 ml of water, and prepare an aqueous solution of polyvinylpyrrolidone with a mass fraction of 33%.

[0053] 2) Grinding and sieving the bulk drug in the crystal form of etonogestrel to obtain drug crystals with a particle size of about 15 μm. Weigh 100 mg of sieved drug crystals and add them to the aqueous solution of PVP K30, and magnetically stir (2000 rpm, 6 h) to prepare a microneedle emulsion (microneedle injection molding solution) with a mass ratio of matrix material to drug of 20:1.

[0054] 3) Add 150 μl of microneedle emulsion into the microneedle mold, and pressurize the microneedle emulsion into the microneedle pinholes. Microneedle patch 100 needles / square centimeter, needle length 0.50mm.

[0055] 4) Dry the above-mentioned microneedle mold with the microneedle emulsion added under the conditions of 25° C. and 30% humidity f...

Embodiment 3

[0059] Example 3: Preparation of sustained-release microneedle patch for intradermal administration

[0060] 1) Weigh 0.5 g of sodium hyaluronate with a molecular weight of 1500 KDa, add 9.5 ml of water, and prepare an aqueous solution of sodium hyaluronate with a mass fraction of 5%.

[0061] 2) Grinding the raw material drug of artemether in crystal form and then sieving to obtain the drug in crystal form with a particle size of 20 μm. Weighed 50 mg of the sieved drug in crystal form and added it to the aqueous solution of hyaluronic acid, and stirred it magnetically (1000 rpm, 12 h) to prepare a microneedle emulsion with a mass ratio of matrix material to drug of 10:1.

[0062] 3) Add 100 μl of microneedle emulsion into the microneedle mold, and make the microneedle emulsion enter the microneedle pinholes by vacuuming. The microneedle patch has 169 needles / square centimeter, and the needle length is 0.85mm.

[0063] 4) Put the above-mentioned microneedle mold added with t...

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Abstract

The invention discloses a flexible slow-release micro-needle patch and a preparation method thereof. The micro needle patch comprises a micro-needle, a substrate and a back lining, wherein the micro-needle and the substrate form a micro-needle array; a base material of the micro-needle or a base material of the micro-needle array contains a drug in a crystal form; the solubility of the drug in the crystal form in water is less than 100 microgram / ml. The micro-needle patch has the characteristics of simple process, high preparation safety, low process cost and high drug loading capacity.

Description

technical field [0001] The invention belongs to the technical field of medicine, and more specifically relates to a flexible sustained-release microneedle patch and a preparation method thereof. Background technique [0002] The transdermal drug delivery system is a dosage form in which drugs are administered through the skin. This dosage form has unique advantages over general dosage forms such as oral administration and injection. Microneedle is one of the physical penetration enhancement methods for transdermal drug delivery. Microneedles alter the permeability of the skin by creating micron-sized channels in the skin that allow drug molecules to pass through. Soluble microneedle is to blend the drug with the soluble matrix material. After the microneedle penetrates into the skin, the drug is released as the matrix material dissolves or degrades. At the same time, the microneedle patch can be peeled off after the needle tip dissolves in the skin, It does not require lon...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61M37/00A61K9/70A61K31/337A61K31/357A61K31/567
CPCA61K31/337A61K9/0021A61K31/357A61K31/567A61K47/32A61M2037/0053A61M37/0015A61K9/7023A61M2207/00
Inventor 高云华贺美琳
Owner BEIJING CAS MICRONEEDLE TECH LTD
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