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Strong hydrophilic microneedle base material, drug-loaded microneedle and application of drug-loaded microneedle in disease treatment

A microneedle and base material technology, applied in the field of microneedles, can solve the problems of complicated process, low drug utilization rate, and poor comprehensive benefit, and achieve the effects of simple process, guaranteed drug quality, and high utilization rate

Active Publication Date: 2021-09-24
尹忠
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In summary, the main technical problems of drug microneedles are: mixed material drug loading method, low drug utilization rate, poor overall benefit; small drug loading, In particular, the packaged drug load is smaller and easy to fall off; many cases have to be subjected to high temperature, which is not suitable for many drugs; the process is relatively complicated, requiring precise control of various conditions, and it is difficult to scale up in mass production

Method used

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  • Strong hydrophilic microneedle base material, drug-loaded microneedle and application of drug-loaded microneedle in disease treatment
  • Strong hydrophilic microneedle base material, drug-loaded microneedle and application of drug-loaded microneedle in disease treatment
  • Strong hydrophilic microneedle base material, drug-loaded microneedle and application of drug-loaded microneedle in disease treatment

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preparation example Construction

[0100] Further, the present invention provides a method for preparing a strongly hydrophilic blank microneedle, wherein the polyvinyl alcohol powder and the small molecule polyol powder are weighed according to the hydroxyl ratio (converted into a weight ratio) Perform blending at room temperature to form a blended powder, hot press the blended powder into a molding material, and hot press the molded material into a mold to form a blank microneedle; or use the blended powder at a certain temperature to Blending mechanical hot-mixing and melt-extruding into profiles, and hot-pressing the profiles into molds to form blank microneedles (see attached Figure 6 And attached Figure 7 : 700 is the whole blank microneedle, 701 is the blank microneedle body).

[0101] The mold used in an optimized embodiment of the present invention is on a flat plate with a thickness of 0.2 to 3 mm, with one or more groups of microhole arrays, and the microholes are through holes; the material of th...

Embodiment 1

[0121] Example 1: Testing and Control of Microneedle Composition Substrate Molding Temperature Range

[0122] According to the composition of the microneedle composition base material of the present invention: the ratio of the small molecule polyhydroxy compound to the polyvinyl alcohol is blended to obtain the blended powder, and on the microneedle preparation equipment of Example 2, in a certain pressure range (28- 32kg / cm 2 ), in order to obtain better prefabricated discs and / or microneedle molding, adjust the temperature to conduct experiments to obtain a lower limit temperature with better operability, and the results are organized as follows Figure 23 As shown in the table in the table, the table shows that at 28-32kg / cm 2 Under pressure conditions, the prefabricated disc and / or microneedle molding temperature of different hot extrusion materials, the proportion is the weight ratio, and the unit is w / w.

[0123] After adding small molecular polyols such as mannitol, s...

Embodiment 2

[0124] Embodiment 2: Preparation device and process method of prefabricated discs, blank microneedles and other material discs used for testing

[0125] According to attached figure 1 Shown is a schematic diagram of an example of a microneedle preparation device used in the present invention. The test blank microneedle and the test sample disk of the present invention are all completed on the device.

[0126] Such as figure 1 As shown, the special microneedle preparation device includes, from top to bottom, an upper compression plate 1, a mold plate 2, an isolation layer 3, and an air extraction plate 4. The isolation layer 3 is made of a gas-permeable and liquid-impermeable material, and the mold plate 2 is provided with a microporous area 21 corresponding to the needle of the microneedle, the micropore is a through hole, and a cavity 41 is provided in the air pumping plate 4, and the corresponding microporous area 21 on the air pumping plate 4 The position is provided wit...

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Abstract

The invention discloses a micro-needle made of a strong hydrophilic base material, and particularly relates to a micro-needle and a drug-loaded micro-needle which are prepared by using a composition of polyvinyl alcohol and a micromolecular polyhydroxy compound as a base material and have a strong hydrophilic surface, and an application of the micro-needle and the drug-loaded micro-needle in disease treatment. The polyhydroxy high-molecular substance polyvinyl alcohol is compatible with the micromolecular polyhydroxy compound, the microneedle with the strong hydrophilic surface can be obtained, a medicine can be strongly adsorbed as long as the microneedle is in contact with the medicine, the microneedle is unlikely to fall off, a technology is simple, mass production is easy, a drug loading capacity is obviously increased, medicine use efficiency is high, blank microneedle preparation and medicine loading are carried out in different stages, a high temperature is avoided in a drug loading stage, and therefore, the drug-loaded microneedle can be effectively applied to drug loading and drug release for treating diseases and is easy in mass production. The microneedle base material composition, the blank microneedle prepared from the microneedle base material composition and application of the blank microneedle to drug loading can keep the inherent surface strong hydrophilic polarity of polyvinyl alcohol, so that the drug loading capacity of wrapped drug loading and a penetration amount of drugs entering the body are obviously improved.

Description

technical field [0001] The invention relates to a microneedle made of a strongly hydrophilic substrate, more particularly to a microneedle with a strongly hydrophilic surface prepared using a composition of polyvinyl alcohol and a small molecule polyhydroxy compound as a substrate. Drug-loaded microneedles and their application in the treatment of diseases. Background technique [0002] Drug microneedles, as a way of loading and releasing drugs, have developed rapidly in recent years, but the actual application of mass production is still relatively slow. Although various existing technologies are different in the preparation and drug loading methods of microneedles, their application is limited by the molding method and drug release method of microneedles. [0003] There are two main drug loading methods for drug microneedles. 1. Mixed drug loading: mix the drug and microneedle base powder, and then process the mixed material containing the drug into microneedles; 2. Encap...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61M37/00A61K9/00A61K38/22A61K38/28A61K45/00A61K47/10A61K47/26A61K47/32A61P3/10
CPCA61M37/0015A61K9/0021A61K45/00A61K38/28A61K38/22A61K47/32A61K47/26A61K47/10A61P3/10A61M2037/0053A61M2037/0046A61K45/06A61K31/58A61K38/26A61K2300/00A61M2037/0061A61M2037/0023
Inventor 尹忠
Owner 尹忠
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