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A micro -needle patch and preparation method containing Ren Er acid

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: 2022-08-09
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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  • A micro -needle patch and preparation method containing Ren Er acid
  • A micro -needle patch and preparation method containing Ren Er acid
  • A micro -needle patch and preparation method containing Ren Er acid

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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 includes at least the preparation step of the needle point solution, and specifically, includes the following steps:

[0052] The aqueous solution of azelaic acid and matrine are mixed, and a water-soluble matrix material is added at room temperature, and the needle tip solution is obtained after complete dissolution.

Embodiment 1

[0066] Preparation of layered microneedles containing azelaic acid

[0067] 1. Preparation process:

[0068] (1) Preparation of needle tip solution

[0069] Add 9.885mL of ultrapure water to 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 70°C water bath 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 and matrine is 1:1, after the solution temperature 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 to the centrifuge tube, use an electronic balance to weigh 2g of hydroxyethyl cellulose and 900.2g of PVP K into the centrifuge tube. Microneedle...

Embodiment 2

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

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

[0077] The microneedle height of the microneedle patch and the residual needle height aft...

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Abstract

The invention discloses a microneedle patch containing azelaic acid. A solution prescription for preparing microneedle tips comprises: an active ingredient, matrine and a water-soluble matrix material; the active ingredient comprises azelaic acid, and the The mass percentage content of azelaic acid in the needle tip solution is 0.1%-10%. The microneedle patch has high azelaic acid bioavailability, good skin mildness, avoids local skin irritation of azelaic acid, and does not affect the antibacterial activity of azelaic acid. The invention also discloses a preparation method of the microneedle patch.

Description

technical field [0001] The present 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 has good antibacterial, antioxidant, inhibiting oil secretion, inhibiting melanin production, inhibiting cell proliferation and preventing excessive keratinization of hair follicles. It is widely used in the fields of medicine, cosmetics and health care: for common acne, melanoma , malignant freckles, chloasma, rosacea and other diseases have a significant therapeutic effect; it also plays an important role in improving skin aging, brightening and whitening, and reducing pigmentation. In addition, azelaic acid has high safety and no systemic adverse reactions. Compared with common antibiotics and hormone anti-acne drugs, it has good human tolerance and is not prone to drug resistance and transmucosal and skin teratogenicity. It has br...

Claims

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Application Information

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