Preparation method of exenatide microneedle

A technology of exenatide and microneedles, which is applied in the field of preparation of exenatide microneedles, can solve the problems of short half-life of exenatide and inconvenience for patients, and achieve the effect of complete needle shape and uniform drug loading

Pending Publication Date: 2021-04-13
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The purpose of the present invention is to aim at the shortcoming that exenatide has a short half-life, is administered twice a day, must be injected in multiple small doses to establish tolerance, and t

Method used

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  • Preparation method of exenatide microneedle
  • Preparation method of exenatide microneedle
  • Preparation method of exenatide microneedle

Examples

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Embodiment 1

[0053] Embodiment 1, the preparation of exenatide microneedle with PVA, 400kDa hyaluronic acid (HA) and 6000 dextran (Dextran) as material

[0054] figure 1 The preparation process of exenatide phase-inversion microneedles is disclosed, that is, the polymer solution is poured on the mold with a microhole array, the polymer solution fills the micropores, and the needle tip solution is pumped into the micropores by vacuuming In the process, exenatide microneedles can be obtained after several "freeze-thaw" cycles, and the exenatide microneedles can be obtained after drying. The preparation process is simple. Specific steps are as follows:

[0055]First prepare PVA solution (10%-35% PVA aqueous solution can be selected, select 18% PVA aqueous solution for use in the present embodiment) and the mixed aqueous solution of HA and Dextran (can contain 0.5%-5% HA, 0.3%-20% in the mixed aqueous solution Dextran; the mixed aqueous solution selected in this embodiment contains 1% HA and...

Embodiment 2

[0064] Embodiment 2, release kinetics of exenatide microneedles

[0065] In order to investigate the release of exenatide, the exenatide microneedle sheet prepared in the above example was punched out with a punching device into a microneedle disc with a diameter of 12 mm (about 170 microneedles), and the microneedle sheet was made of polytetrafluoroethylene Wrapped in vinyl fluoride and tin foil, the body of the microneedle is partially exposed. Add 2ml of pH 7.4 phosphate buffer solution to the 24-well plate, put the wrapped microneedle piece into the 24-well plate with the needle tip facing down, cover it, and put it in a constant temperature shaker at 37°C and 100rpm for in vitro For release experiments, samples were taken at 0.5h, 1h, 2h, 3h, 4h, 5h, 6h, 8h, 10h, 12h, 16h, 20h, and 24h. After each sample was taken, pour out the release solution remaining in the 24-well plate, wash the 24-well plate with new PBS buffer solution, and add 2ml of the release solution to cont...

Embodiment 3

[0074] Example 3, Investigation on the Uniformity of Drug Loading of Exenatide Microneedles

[0075] In order to verify the uniformity of dispersion of exenatide in different parts of the same mold, we investigated the uniformity of the drug loading of the microneedles. The release amount of exenatide in different parts of the microneedle tablets on the same mold was basically the same at each time point, the cumulative release curves basically overlapped, and the final in vitro release rate was about 70%. It shows that the error of in vitro release of the microneedle sheets of the same mold is small and the uniformity is good. The result is as Figure 8 ;Depend on Figure 8 It can be seen that the drug loading uniformity is good, and the drug release curves of microneedle tablets at different positions are close.

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Abstract

The invention discloses a preparation method of an exenatide microneedle. The preparation method comprises the following steps of: pouring an aqueous solution of a polymer material containing exenatide on a mould with a micropore matrix, filling all micropores with the polymer solution, performing freezing and thawing cycle on the mould poured with the exenatide solution for multiple times, and finally performing film uncovering and drying. Exenatide has the defects that the half-life period is relatively short, exenatide is administrated twice a day, tolerance needs to be established through multiple times of small-dose injection, and much inconvenience and pain are brought to patients due to frequent injection. An exenatide phase conversion microneedle transdermal patch not only can realize minimally invasive non-injection administration of exenatide, but also is relatively safe, more effective and convenient to use, improves the compliance of a patient, and is convenient for the patient to establish tolerance.

Description

technical field [0001] The invention belongs to the technical field of transdermal drug delivery systems, and relates to a method for preparing exenatide microneedles, which is a method for preparing exenatide microneedles that deliver drugs into the body by means of microneedle transdermal attachment . Background technique [0002] Exenatide is one of the first-choice drugs for the treatment of type 2 diabetes. As the first marketed glucagon-like peptide-1 receptor agonist, it has its unique characteristics compared with other commonly used type 2 diabetes drugs. Advantages, including glucose-dependent hypoglycemic effect, stimulating insulin secretion, inhibiting glucagon secretion, inhibiting islet β cell apoptosis, reducing gastric emptying, reducing appetite, etc., provide a new treatment for type 2 diabetes method. [0003] Microneedle refers to a small needle array with a length of less than 1mm. Since it only pierces the stratum corneum of the skin and does not tou...

Claims

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Application Information

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IPC IPC(8): A61K38/22A61K9/00A61K47/32A61K47/36A61P3/10A61M37/00
CPCA61K38/22A61K9/0021A61K47/32A61K47/36A61P3/10A61M37/0015A61M2037/0053A61M2037/0046
Inventor 金晓晖金拓王猛邹茜茜葛宇轩吴飞
Owner SHANGHAI JIAO TONG UNIV
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