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Indomethacin cataplasm and composition thereof

A technology of indomethacin and indomethacin, applied in the direction of drug combinations, anti-inflammatory agents, non-central analgesics, etc., can solve the problems of poor transdermal absorption performance, low solubility, easy decomposition, etc., and increase transdermal absorption Performance, increased transdermal absorption, long-term moisturizing effect

Inactive Publication Date: 2015-02-25
和心医药科技(上海)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] For example, CN102526001A utilizes ion pairing technology to form indomethacin and organic amines into salts to increase its solubility, but the salts synthesized by such methods are easily decomposed and have poor stability due to the influence of temperature, pH and other conditions; there are also solubilizers and Transdermal penetration enhancers, such as alkylpyrrolidone, azone + propylene glycol (CN1973836A), however, indomethacin has low solubility in aqueous media, and crystallization may occur after long-term storage, resulting in poor transdermal absorption of the drug

Method used

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  • Indomethacin cataplasm and composition thereof
  • Indomethacin cataplasm and composition thereof
  • Indomethacin cataplasm and composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] The indomethacin cataplasm provided in this embodiment is composed of a backing, a paste and an anti-adhesive film, and the composition of the paste includes:

[0050]

[0051] Dissolve 2.0g of sodium carboxymethylcellulose in glycerin and partially purified water, then add 1.0g of polyoxyethylene monolaurate and 0.1g of Tween 80, heat to 40°C, and stir well to obtain component A;

[0052] Dissolve 1g of gelatin in partially purified water, heat to 60°C after swelling is complete, stir evenly until translucent colloid, and obtain component B;

[0053] Dissolve 5.0g of partially neutralized sodium polyacrylate, 0.06g of aluminum hydroxide and 0.15g of disodium edetate in glycerin, stir and mix evenly to obtain component C;

[0054] Add 0.12 g of tartaric acid into purified water, then add indomethacin solution pre-dissolved in crotamiton and N-methylpyrrolidone, mix and stir evenly to obtain component D;

[0055] Take the remaining purified water in the prefabricated...

Embodiment 2

[0057] The indomethacin cataplasm provided in this embodiment is composed of a backing, a paste and an anti-adhesive film, and the composition of the paste includes:

[0058]

[0059] Dissolve 2.0g of sodium carboxymethylcellulose in glycerin and partially purified water, then add 1.0g of polyoxyethylene monolaurate and 0.1g of Tween 80, heat to 40°C, and stir well to obtain component A;

[0060] Dissolve 2.0g of gelatin in partially purified water, heat to 60°C after swelling is complete, and stir evenly until translucent colloid is obtained to obtain component B;

[0061] Dissolve 6.0g of partially neutralized sodium polyacrylate, 0.05g of aluminum hydroxide and 0.15g of disodium edetate in glycerin, stir and mix evenly to obtain component C;

[0062] Add 0.12 g of tartaric acid into purified water, then add indomethacin solution pre-dissolved in crotamiton and N-methylpyrrolidone, mix and stir evenly to obtain component D;

[0063] Take the remaining purified water in a...

Embodiment 3

[0065] The indomethacin cataplasm provided in this embodiment is composed of a backing, a paste and an anti-adhesive film, and the composition of the paste includes:

[0066]

[0067]

[0068] Dissolve 2.0g sodium carboxymethylcellulose in glycerin and partially purified water, then add 1.0g carboxyvinyl polymer, 0.3g polyoxyethylene hydrogenated castor oil and 0.1g Tween 80, heat to 40°C, stir well, Get A component.

[0069] Dissolve 1.0g of gelatin in partially purified water, heat to 60°C after swelling is complete, and stir evenly until translucent colloid is obtained to obtain component B;

[0070] Dissolve 6.0g of partially neutralized sodium polyacrylate, 0.05g of aluminum hydroxide and 0.15g of disodium edetate in glycerin, stir and mix evenly to obtain component C;

[0071] Add 0.12 g of tartaric acid into purified water, then add indomethacin solution pre-dissolved in crotamiton and N-methylpyrrolidone, mix and stir evenly to obtain component D;

[0072] Take...

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Abstract

The invention provides an indomethacin cataplasm, which is composed of a backing, a paste body, and an anti-sticking film, wherein the paste body is composed of indomethacin, crotamiton, N-methyl pyrrolidone, and hydrogel matrix; the content of the indomethacin in the paste body is 0.1 to 3 wt%, the weight of crotamiton is 0.1 to 6 times as heavy as that of indomethacin, the weight of N-methyl pyrrolidone is 1 to 15 times as heavy as that of indomethacin, and the balance being hydrogel matrix. The mixed solvent of crotamiton and N-methyl pyrrolidone can increase the solubility of indomethacin so as to completely dissolve indomethacin, the indomethacin is evenly dispersed in hydrogel matrix and will not crystallize for a long time, moreover the skin penetrating performance of indomethacin is improved, and indomethacin can be more easily absorbed by the skin. Furthermore, a skin penetration promoter and a wetting agent are added to ensure that the cataplasm has a high water content and remains wet for a long time, and the skin penetration and absorption of the drugs are also promoted. The provided indomethacin cataplasm can be used to treat arthralgia diseases such as rheumatic arthritis, gouty arthritis, rigidity myelitis, tenosynovitis, and the like.

Description

technical field [0001] The invention relates to a hydrophilic cataplasm, in particular to an indomethacin cataplasm with high water content, good stability and skin penetration and an indomethacin composition. Background technique [0002] Indomethacin (Indomethacin) is one of the typical non-steroidal anti-inflammatory analgesic drugs, which mainly produces analgesic, anti-inflammatory and antipyretic effects by inhibiting the synthesis of prostaglandins (PG) in the body. Clinically, it is often used in the treatment of acute and chronic rheumatoid arthritis, gouty arthritis, ankylosing myelitis and bursitis, tenosynovitis and osteoarthritis, cervical spondylosis, muscle pain, low back pain and other diseases. [0003] It is clinically found that long-term oral administration of indomethacin has serious side effects on the gastrointestinal tract, such as irritating the mucous membrane of the digestive tract, leading to gastric bleeding or gastric ulcer; in addition, it also...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/405A61K47/22A61K47/18A61P29/00A61P19/02A61P21/00
Inventor 龙本威汤秀珍龚力平山内仁史吉田敏行蔡金花
Owner 和心医药科技(上海)有限公司
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