Menthol complex patch

Abstract

The menthol composite patch is composed of an anti-adhesion layer, a first drug storage layer, a second drug storage layer and a backing layer in sequence; the first drug storage layer is composed of menthol and a pressure-sensitive adhesive matrix, and the weight percentage content of menthol in the first drug storage layer is 0.1%-2%. The second drug storage layer is composed of a pepper extract, cetearyl alcohol and a pressure-sensitive adhesive matrix, and the weight ratio of the pepper extract to cetearyl alcohol is 1:0.5-2, and the weight percentage content of the pepper extract in the second drug storage layer is 0.5-3%.

Description

Technical Field

[0001] This invention relates to a transdermal drug delivery formulation, and more particularly to a patch comprising menthol as an active ingredient. Background Technology

[0002] Menthol, also known as peppermint, is a terpenoid organic compound, a white crystalline substance extracted from the leaves and stems of peppermint, and is the main component of peppermint and spearmint essential oils. Externally, it is used for local analgesia, antipruritic effects, headaches, dizziness, and insect bites; nasal drops are used for nasal congestion due to colds. Due to its cooling effect, it can be used in soothing cold compresses to lower body temperature, constrict blood vessels, and reduce internal bleeding and swelling. However, after sports injuries, the condition changes over time, requiring further treatment such as anti-inflammatory, analgesic, and blood circulation-promoting therapies. Menthol alone is insufficient to meet these requirements. Therefore, providing a menthol-containing composite patch with sustained-acting properties is a problem that needs to be addressed in existing technologies. Summary of the Invention

[0003] To solve the aforementioned technical problems, the technical solution adopted by the present invention is as follows:

[0004] A menthol composite patch is provided, which consists of an anti-adhesive layer, a first drug storage layer, a second drug storage layer and a backing layer in sequence.

[0005] The first drug storage layer is composed of menthol and pressure-sensitive adhesive matrix, and the weight percentage content of menthol in the first drug storage layer is 0.1%~2%.

[0006] The second drug storage layer is composed of capsicum extract, cetearyl alcohol and pressure-sensitive adhesive matrix. The weight ratio of capsicum extract to cetearyl alcohol is 1:0.5~2, and the weight percentage content of capsicum extract in the second drug storage layer is 0.5~3%.

[0007] The menthol composite patch further comprises a first drug storage layer containing 0.2% to 0.5% menthol by weight.

[0008] The menthol composite patch further includes a second drug storage layer containing 0.8-1.5% capsicum extract by weight, and the preferred weight ratio of capsicum extract to cetearyl alcohol is 1:0.8-1.2.

[0009] Furthermore, in the menthol composite patch, the pressure-sensitive adhesive matrix is ​​a polyisobutylene pressure-sensitive adhesive matrix.

[0010] The menthol composite patch, further, is prepared using a method comprising the following steps:

[0011] 1) Mix menthol and polyisobutylene pressure-sensitive adhesive matrix evenly, coat it on the anti-adhesive layer to form the first drug storage layer, and dry it at 65-85℃;

[0012] 2) After heating cetearyl alcohol to 55~60℃, mix it evenly with capsicum extract and then with polyisobutylene pressure-sensitive adhesive matrix. Coat the surface of the first drug storage layer, dry it at 65-85℃, and then laminate it with the backing layer and cut it into patches.

[0013] The menthol composite patch provided by this invention adopts a dual-layer structure with a first drug storage layer and a second drug storage layer. When the patch is applied, the first drug storage layer containing menthol takes effect first, which cools and constricts blood vessels to prevent further damage. After the patch has been applied for a period of time, the capsicum extract in the second drug storage layer begins to exert its blood-activating effect, further promoting the recovery of the disease. Detailed Implementation

[0014] All percentages in all examples are by weight.

[0015] Example 1

[0016] In the first drug storage layer, 0.1% is menthol and the remainder is polyisobutylene pressure-sensitive adhesive matrix;

[0017] The second drug storage layer contains 0.5% capsicum extract, 0.5% cetearyl alcohol, and the remainder is polyisobutylene pressure-sensitive adhesive matrix.

[0018] The preparation method is as follows:

[0019] 1) Mix menthol and polyisobutylene pressure-sensitive adhesive matrix evenly, coat it on the anti-adhesive layer to form the first drug storage layer, and dry it at 65-85℃;

[0020] 2) After heating cetearyl alcohol to 55~60℃, mix it evenly with capsicum extract and then with polyisobutylene pressure-sensitive adhesive matrix. Coat the surface of the first drug storage layer, dry it at 65-85℃, and then laminate it with the backing layer. Cut it into patches to make menthol composite patches.

[0021] Example 2

[0022] In the first drug storage layer, 0.2% is menthol and the remainder is polyisobutylene pressure-sensitive adhesive matrix;

[0023] The second drug storage layer contains 0.8% capsicum extract, 0.8% hexadecyl alcohol, and the remainder is polyisobutylene pressure-sensitive adhesive matrix.

[0024] The preparation method is as follows:

[0025] 1) Mix menthol and polyisobutylene pressure-sensitive adhesive matrix evenly, coat it on the anti-adhesive layer to form the first drug storage layer, and dry it at 65-85℃;

[0026] 2) After heating cetearyl alcohol to 55~60℃, mix it evenly with capsicum extract and then with polyisobutylene pressure-sensitive adhesive matrix. Coat the surface of the first drug storage layer, dry it at 65-85℃, and then laminate it with the backing layer. Cut it into patches to make menthol composite patches.

[0027] Example 3

[0028] In the first drug storage layer, 0.5% is menthol and the remainder is polyisobutylene pressure-sensitive adhesive matrix;

[0029] The second drug storage layer contains 1.5% capsicum extract, 1.5% hexadecyl alcohol, and the remainder is polyisobutylene pressure-sensitive adhesive matrix.

[0030] The preparation method is as follows:

[0031] 1) Mix menthol and polyisobutylene pressure-sensitive adhesive matrix evenly, coat it on the anti-adhesive layer to form the first drug storage layer, and dry it at 65-85℃;

[0032] 2) After heating cetearyl alcohol to 55~60℃, mix it evenly with capsicum extract and then with polyisobutylene pressure-sensitive adhesive matrix. Coat the surface of the first drug storage layer, dry it at 65-85℃, and then laminate it with the backing layer. Cut it into patches to make menthol composite patches.

[0033] Example 4

[0034] In the first drug storage layer, 0.5% is menthol and the remainder is polyisobutylene pressure-sensitive adhesive matrix;

[0035] The second drug storage layer contains 0.8% capsicum extract, 0.8% hexadecyl alcohol, and the remainder is polyisobutylene pressure-sensitive adhesive matrix.

[0036] The preparation method is as follows:

[0037] 1) Mix menthol and polyisobutylene pressure-sensitive adhesive matrix evenly, coat it onto the release layer to form the first drug storage layer, and dry it at 65-85℃:

[0038] 2) After heating cetearyl alcohol to 55~60℃, mix it evenly with capsicum extract and then with polyisobutylene pressure-sensitive adhesive matrix. Coat the surface of the first drug storage layer, dry it at 65-85℃, and then laminate it with the backing layer. Cut it into patches to make menthol composite patches.

[0039] Example 5

[0040] In the first drug storage layer, 0.2% is menthol and the remainder is polyisobutylene pressure-sensitive adhesive matrix;

[0041] The second drug storage layer contains 1.5% capsicum extract, 1.5% hexadecyl alcohol, and the remainder is polyisobutylene pressure-sensitive adhesive matrix.

[0042] The preparation method is as follows:

[0043] 1) Mix menthol and polyisobutylene pressure-sensitive adhesive matrix evenly, coat it on the anti-adhesive layer to form the first drug storage layer, and dry it at 65-85℃;

[0044] 2) After heating cetearyl alcohol to 55~60℃, mix it evenly with capsicum extract and then with polyisobutylene pressure-sensitive adhesive matrix. Coat the surface of the first drug storage layer, dry it at 65-85℃, and then laminate it with the backing layer. Cut it into patches to make menthol composite patches.

[0045] The patch formulations in Examples 1-5 were examined and found to have uniformity of content, release rate, initial tack, holding power, and peel strength, all of which meet the relevant requirements for patches in Appendix IV of the 2015 edition of the Chinese Pharmacopoeia.

Claims

1. A menthol compound patch, characterized in that... The composite patch is composed of an anti-adhesive layer, a first drug storage layer, a second drug storage layer, and a backing layer in sequence. The first drug storage layer is composed of menthol and a pressure-sensitive adhesive matrix, and the weight percentage content of menthol in the first drug storage layer is 0.1%~2%; The second drug storage layer is composed of capsicum extract, cetearyl alcohol and pressure-sensitive adhesive matrix. The weight ratio of capsicum extract to cetearyl alcohol is 1:0.5~2, and the weight percentage content of capsicum extract in the second drug storage layer is 0.5~3%.

2. The menthol composite patch as described in claim 1, characterized in that, The weight percentage content of menthol in the first drug storage layer is 0.2%~0.5%.

3. The menthol composite patch as described in claim 1, characterized in that, The second drug storage layer contains 0.8-1.5% capsicum extract by weight, and the weight ratio of capsicum extract to cetearyl alcohol is 1:0.8-1.

2.

4. The menthol composite patch according to any one of claims 1 to 3, further wherein the pressure-sensitive adhesive matrix is ​​a polyisobutylene pressure-sensitive adhesive matrix.

5. The menthol composite patch as described in claim 4, characterized in that... The preparation method used includes the following steps: 1) Mix menthol and polyisobutylene pressure-sensitive adhesive matrix evenly, coat it on the anti-adhesive layer to form the first drug storage layer, and dry it at 65-85℃; 2) After heating cetearyl alcohol to 55~60℃, mix it evenly with capsicum extract and then with polyisobutylene pressure-sensitive adhesive matrix. Coat the surface of the first drug storage layer, dry it at 65-85℃, and then laminate it with the backing layer and cut it into patches.