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Colchicine soluble microneedle patch and preparation method thereof

A technology of colchicine and micro-needle stickers, applied in sheet delivery, pharmaceutical formulations, organic active ingredients, etc., can solve the problems of unloaded colchicine research and patents, complex raw materials, slow onset time, etc. The effect of microneedle drug loading, bioavailability improvement, and elimination of bubble interference

Active Publication Date: 2021-07-20
NANJING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Although previous studies have reported that other colchicine formulations are used for transdermal administration, for example, Chinese patent application 200710057506.6 discloses a "colchicine transdermal absorption patch for the treatment of acute gout", but the onset time is relatively slow , and the raw materials are complex
So far, there is no research or patent on the minimally invasive soluble polymer microneedle patch drug delivery system loaded with colchicine

Method used

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  • Colchicine soluble microneedle patch and preparation method thereof
  • Colchicine soluble microneedle patch and preparation method thereof
  • Colchicine soluble microneedle patch and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Embodiment 1 (preparation and effective puncture skin)

[0065] 1. Preparation of a soluble microneedle patch loaded with fluorescent substances

[0066] Preparation:

[0067] Add a magnetic stirrer in double distilled water and stir at 1000 rpm, and vacuumize at -0.1 MPa for 30 min. Add 320 mg of sodium hyaluronate (HA) and 8 mg of fluorescent substance sulforhodamine B (SRhB) into 8 mL of double-distilled water, and stir at room temperature at 400 rpm for 7 hours. Take 500μL of SRhB / HA mold solution and add it into the mold, vacuumize for 30min, and centrifuge at 3000rpm / 20min. Then add 300μL of SRhB / HA mold solution, vacuumize and centrifuge at 3000rpm / 10min. Remove excess mold liquid on the surface of the mold, centrifuge again at 3000rpm / 10min, and dry in an oven at 45°C for 1 hour.

[0068] Add 1.3mL blank HA mold liquid (concentration 0.04g / mL) to the mold with microneedle array, centrifuge at 3000rpm / 10min, dry at 45°C for 9h, peel off the microneedle from t...

Embodiment 2

[0075] Embodiment 2 (preparation and treatment on animal model)

[0076] 1. Preparation of a dissolvable microneedle patch loaded with colchicine

[0077] Add a magnetic stirrer in double distilled water and stir at 1000 rpm, and vacuumize at -0.1 MPa for 30 min. Add 320mg of sodium hyaluronate HA and 250mg of colchicine (Col) (the mass ratio of the two is 1.28:1) into 8mL of double-distilled water, and stir at room temperature at 400rpm for 7 hours. Take 500μL of Col / HA mold solution and add it into the mold, vacuumize for 30min, and centrifuge at 3000rpm / 20min. Then add 300μL of Col / HA mold liquid, vacuumize and centrifuge at 3000rpm / 10min. Remove excess mold liquid on the surface of the mold, centrifuge again at 3000rpm / 10min, and dry in an oven at 45°C for 1 hour.

[0078] Add 1.3mL blank HA mold liquid (concentration 0.04g / ml) to the mold with microneedle array, centrifuge at 3000rpm / 10min, dry at 45°C for 9h, peel off the microneedle from the mold and stick it on medi...

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Abstract

The invention belongs to the technical field of microneedle array transdermal drug delivery, and particularly provides a colchicine soluble microneedle patch and a preparation method thereof. The microneedle patch comprises a hyaluronic acid microneedle array containing medicine colchicine, a substrate and a medical adhesive tape, and microneedles are of conical or pyramid structures. The medicine is only added into a microneedle body, so that the cost is reduced. The microneedle patch can be pressed on the skin by fingers, so that quick drug release is realized, toxic and side effects of gastrointestinal tracts are avoided, and the bioavailability is improved.

Description

technical field [0001] The invention belongs to the technical field of transdermal administration, and in particular relates to a colchicine-loaded soluble microneedle patch for treating acute gout and a preparation method thereof. Background technique [0002] Gout is an inflammatory arthritis, mainly related to purine metabolism disorder and decreased uric acid excretion, which lead to persistent hyperuricemia. The deposition of needle-like monosodium urate (MSU) crystals in joints and their surrounding tissues triggers acute and chronic Inflammation. The clinical course of gout includes asymptomatic hyperuricemia, intermittent attacks of acute arthritis, and borderline gout. If hyperuricemia is not treated, it will form late gout. The clinical features are tophi and the simplicity of severe pain in the acute attack stage. Arthritis, chronic gouty arthritis, and joint damage, usually affecting the joints of the lower extremities. Acute gout typically presents as monoarti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/165A61K47/36A61P19/06
CPCA61K9/7023A61K9/0021A61K31/165A61K47/36A61P19/06A61K9/70A61M37/00
Inventor 丁智刘阳张峻峰
Owner NANJING UNIV
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