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Micro-needle patch containing azelaic acid and preparation method of micro-needle patch

A technology of azelaic acid and microneedle sticking, which is applied in the field of medicine, can solve the problems of slowing down the skin metabolism rate, time-consuming, skin irritation, etc., and achieve the goal of improving the effective utilization of drugs, avoiding cross-infection, and reducing the dosage concentration Effect

Active Publication Date: 2021-03-12
BEIJING CAS MICRONEEDLE TECH LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The existing formulations of azelaic acid on the market include: cream, gel and mucilage, all of which are applied locally. The azelaic acid in the preparation penetrates the stratum corneum of the skin through osmosis and reaches the epidermis and dermis. So as to exert the drug effect, but the limited penetration makes the effective utilization rate of the drug low, so it is necessary to increase the concentration of azelaic acid to achieve the effect (the content of azelaic acid in the marketed products: 10%-20%), but it is easy to cause erythema , itching, scaling, burning sensation and other local skin irritation
In addition, azelaic acid itself has poor water solubility, making it difficult to formulate
[0004] Chinese patent CN106420787A discloses a preparation method of an acne cream containing azelaic acid. By blending active ingredients such as azelaic acid with an oily matrix material, the solubility and skin permeability of azelaic acid are improved, but for sebum For acne-prone skin with strong secretion, the use of a large amount of oily substrate is undoubtedly worse, it is easy to clog the skin pores, slow down the skin metabolism rate, and aggravate the deterioration of skin diseases
The use of high-concentration 1,3-propanediol can not only improve the solubility of azelaic acid, but also act as a penetration enhancer, which can increase the skin’s absorption of active ingredients, but the use of large doses of alcohols has a certain stimulating effect on the skin, and 2 The pH of %ZEN hydrogel is about 5.8, which itself is an acidic environment, and a large amount of acidic drugs such as azelaic acid and salicylic acid are added, which makes the overall acidity of the gel relatively high, and will also cause certain irritation to the skin sex
[0006] Chinese patent CN108187070A discloses a preparation method of azelaic acid hydroxypropyl-β-cyclodextrin inclusion compound, which has the advantages of improving the solubility of azelaic acid and enhancing the stability of the drug, but the preparation process is complicated and needs to be reacted first. The two-step process of high-temperature mixing in the kettle and spray drying takes a long time, which is not conducive to the industrial production of new formulations of azelaic acid

Method used

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  • Micro-needle patch containing azelaic acid and preparation method of micro-needle patch
  • Micro-needle patch containing azelaic acid and preparation method of micro-needle patch
  • Micro-needle patch containing azelaic acid and preparation method of micro-needle patch

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preparation example Construction

[0051] On the other hand, another embodiment of the present invention provides a method for preparing a microneedle patch containing azelaic acid, the method at least includes the preparation step of the needle tip solution, specifically, includes the following steps:

[0052] Mix the aqueous solution of azelaic acid and matrine, add the water-soluble matrix material at room temperature, and wait for complete dissolution to obtain the needle tip solution.

Embodiment 1

[0066] Fabrication of layered microneedles containing azelaic acid

[0067] 1. Preparation process:

[0068] (1) Preparation of needle tip solution

[0069] Add 9.885mL of ultrapure water into the centrifuge tube, use an electronic balance to weigh 0.05g of azelaic acid dissolved in water, and then place the centrifuge tube in a water bath environment at 70°C to promote the dissolution of azelaic acid. After it is completely dissolved, add 0.065g matrine. At this time, the molar ratio of azelaic acid to matrine is 1:1. After the temperature of the solution drops to room temperature, add 0.1g of sodium carboxymethylcellulose (CMC), weigh 0.1g of trehalose and add , stirred to dissolve, and then placed in a centrifuge to remove air bubbles to obtain a microneedle tip solution.

[0070] (2) Preparation of base solution

[0071] Add 7.8mL of ultrapure water into the centrifuge tube, weigh 2g of hydroxyethyl cellulose with an electronic balance, and add 0.2g of PVP K900 into the...

Embodiment 2

[0075] The layered needle microneedle patch is prepared according to the method of Example 1, the difference is that the formulation of the needle tip solution is different, and the formulation, dissolution and pH are as shown in Table 2 (in Table 2, the components not shown in the balance are water ).

[0076] The prepared microneedle patch was applied to the arms of volunteers with sensitive skin for 10 minutes, and then removed to observe whether the skin was allergic. The effect was as follows: image 3 As shown in a, the skin is slightly red (the area where the microneedle is applied is a normal phenomenon due to the puncture of the stratum corneum of the skin by the microneedle). After about 2 hours, the redness gradually subsides, and there is no itching, swelling, diffuse allergy, etc. Stimulation response; the surface morphology of the obtained microneedle patch after acting for 10 minutes is as follows: Figure 4 shown.

[0077] The microneedle height of the micron...

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Abstract

The invention discloses a micro-needle patch containing azelaic acid. A solution formula for preparing a micro-needle tip comprises an active component, sophocarpidine and a water-soluble matrix material, wherein the active component comprises azelaic acid, and the mass percentage of azelaic acid in the needle tip solution is 0.1%-10%. The azelaic acid in the micro-needle patch is high in bioavailability and good in skin mildness, local skin irritation of azelaic acid is avoided, and the antibacterial activity effect of azelaic acid is not affected. The invention further discloses a preparation method of the micro-needle patch.

Description

technical field [0001] The invention relates to the technical field of medicine. More specifically, it relates to a microneedle patch containing azelaic acid and a preparation method thereof. Background technique [0002] Azelaic acid is widely used in the fields of medicine, cosmetics and health care because of its good antibacterial, antioxidative, oil secretion, melanin production, cell proliferation and hair follicle hyperkeratosis prevention effects: common acne, melanoma , malignant freckles, chloasma, rosacea and other diseases have significant therapeutic effects; it also plays an important role in improving skin aging, skin brightening and whitening, and reducing pigmentation. In addition, azelaic acid has high safety and no systemic adverse reactions. Compared with common antibiotics and hormonal anti-acne drugs, it has good human tolerance and is less prone to drug resistance and teratogenicity through mucous membranes and skin. The role of azelaic acid and pote...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/191A61K31/4375A61K45/06A61K47/38A61P17/10A61P31/02A61P31/04
CPCA61K9/0021A61K31/191A61K31/4375A61K45/06A61K47/38A61P17/10A61P31/02A61P31/04A61K2300/00
Inventor 江林邢梦真杨国忠高云华
Owner BEIJING CAS MICRONEEDLE TECH LTD
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