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Preparation method for soluble microneedle for poorly water soluble drugs

A water-insoluble and soluble technology, applied in the field of microneedle, can solve the problems of microneedle organic solvent residue, drug waste, difficult polymer and other problems, and achieves increased drug utilization rate, reduced environmental pollution, and accurate dosing. Effect

Inactive Publication Date: 2016-11-09
PUTIAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] 1. The existing preparation method of soluble microneedles uses water as a solvent, so that most of the insoluble drugs cannot be prepared into soluble microneedles, which greatly limits the application of soluble microneedles
[0004] 2. It is difficult to find polymers that are soluble in both water and organic solvents by directly replacing them with organic solvents; and in this method, the drug is evenly dispersed in the needle body and the back scale of the microneedle, while the microneedle When the needle is used, the effective part is the needle body, and a large amount of medicine remains in the back scale, which will cause inaccurate administration and waste of medicine
[0005] 3. If the organic solvent is directly used as the solvent, the amount of organic solvent will be large, which will pollute the environment, and organic solvent residues are likely to exist in the microneedle

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] A method for preparing soluble microneedles for poorly water-soluble drugs, comprising the following steps:

[0027] S1. Weighing the insoluble drug with a mass of 0.01% of the total mass of the needle solution and polyvinylpyrrolidone with a mass of 1% of the total mass of the needle solution and dissolving them in an organic solvent to obtain a needle solution;

[0028] Most of the drugs in this embodiment are poorly water-soluble drugs, because the characteristics of poorly water-soluble drugs are poorly soluble in water and soluble in organic solvents.

[0029] Polyvinylpyrrolidone is very soluble in water and halogenated hydrocarbon solvents, alcohols, amines, nitroalkanes and low molecular fatty acids, etc., that is, polyvinylpyrrolidone can be dissolved in both water and organic solvents.

[0030] Specifically, the organic solvent in the step 1 is methanol, ethanol, N,N-dimethylformamide, dimethyl sulfoxide, methylene chloride, toluene, any one or a combination o...

Embodiment 2

[0047] A method for preparing soluble microneedles for poorly water-soluble drugs, comprising the following steps:

[0048] S1. Weigh the insoluble drug whose mass accounts for 5% of the total mass of the needle solution and polyvinylpyrrolidone whose mass accounts for 12% of the total mass of the needle solution, and dissolve them in an organic solvent to obtain a needle solution;

[0049] The organic solvent selected in this embodiment is toluene.

[0050] S2. Inject the needle body solution into the micropores of the microneedle mold by vacuum method or positive air pressure method, and dry by vacuuming or heating until the organic solvent is fully volatilized to obtain a microneedle mold containing the needle body;

[0051] In this embodiment, the needle body solution was injected into each micropore of the microneedle mold by the positive air pressure method, and the microneedle mold was dried in an oven at 50° C. for 4 hours.

[0052] Further, the drying temperature in st...

Embodiment 3

[0059] A method for preparing soluble microneedles for poorly water-soluble drugs, comprising the following steps:

[0060] S1. Weighing insoluble drugs whose mass accounts for 10% of the total mass of the needle solution and polyvinylpyrrolidone whose mass accounts for 30% of the total mass of the needle solution are dissolved in an organic solvent to obtain a needle solution;

[0061] The organic solvent selected in this embodiment is dichloromethane.

[0062] S2. Inject the needle body solution into the micropores of the microneedle mold by vacuum method or positive air pressure method, and dry by vacuuming or heating until the organic solvent is fully volatilized to obtain a microneedle mold containing the needle body;

[0063] The needle body solution was injected into each micropore of the microneedle mold by a vacuum method, and the microneedle mold was placed in an oven at 50° C. for 4 hours to cure.

[0064] Further, the drying temperature in step 2 by vacuuming or h...

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Abstract

The invention relates to a preparation method for a soluble microneedle for poorly water soluble drugs. The method comprises the steps that poorly water soluble drugs and polyvinylpyrrolidone are dissolved into an organic solvent, and a needle body solution is prepared; a vacuum method or positive gas pressure method is adopted for injecting a needle body solution into a microhole of a microneedle mold to obtain a needle body portion of the microneedle; a water-soluble polymer is taken to be dissolved into water, a direct appellation solution is prepared, the direct appellation solution is added into a microneedle mold containing the needle body, drying and demolding are performed, and the soluble microneedle for poorly water soluble drugs is obtained. According to the preparation method, preparation of the soluble microneedle for poorly water soluble drugs is achieved, medicine waste is avoided, and the medicine utilization rate is increased; consumption of an organic solvent is reduced, safety is improved, the method is environmentally friendly, and the water-soluble polymer for manufacturing the soluble microneedle can still be used for manufacturing a water-insoluble microneedle.

Description

technical field [0001] The invention relates to the technical field of microneedles, in particular to a method for preparing soluble microneedles for poorly water-soluble drugs. Background technique [0002] In recent years, the popularity of cosmetic microneedling has made more and more people understand microneedle technology. In the prior art, the preparation method of dissolvable microneedles is as follows: the drug is dissolved in water-soluble polymers to form a solution, and then the solution is injected into the microneedle mold by a specific method, and after drying, the mold is demoulded to obtain Soluble microneedles. Since the first step in the production process of soluble microneedles is to dissolve the drug in water-soluble polymers, this requires the drug to have strong water solubility. However, most of the drugs are organic molecules with poor water solubility, especially It is some water-insoluble drugs, and the prepared microneedles contain low drug con...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K47/32A61M37/00
CPCA61K9/0021A61K47/32A61M37/0015A61M2037/0053
Inventor 陈健敏黄梅萍杨周琰
Owner PUTIAN UNIV
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