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A lidocaine gel emplastrum

A technology of lidocaine gel plaster and lidocaine, applied in the direction of medical preparations with non-active ingredients, organic active ingredients, oil/fat/wax non-effective ingredients, etc., can solve the problem of systemic effects and risks Large and low bioavailability

Inactive Publication Date: 2019-01-15
北京茗泽中和药物研究有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when it is used for local pain, the systemic effect of lidocaine is actually a side effect, which needs to be avoided by various technical means. If the blood concentration is too high (>150ng / mL), it is easy to cause systemic effects, especially when the affected area is large and needs to be applied on a large area for labor pain
[0004] Chinese literature - the development and pharmacokinetics research of lidocaine hydrochloride cataplasm (Liu Tingting, Huazhong University of Science and Technology master's thesis, May 2007) discloses a kind of cataplasm of lidocaine hydrochloride as active ingredient, its After using lidocaine hydrochloride as the active ingredient, although the release rate of the main drug was improved, the blood drug concentration decreased rapidly after reaching the peak, and the bioavailability was lower than that of the LIDODERM gel patch as the reference drug. At the same time, the peak blood drug concentration is also higher, and the risk of lidocaine plasma concentration reaching the threshold of systemic reaction is greater

Method used

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  • A lidocaine gel emplastrum
  • A lidocaine gel emplastrum
  • A lidocaine gel emplastrum

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Pharmacological Example 1, in vitro transdermal experiment

[0020] For details of the method, please refer to the new dosage form of transdermal administration in "New Drug Forms and New Technology" edited by Lu Bin. The modified Franz diffusion cell method was used to use the isolated 3-month-old rat abdomen skin as a barrier, and the bab patches prepared in Examples 1 to 6 and Comparative Examples 1 to 6 were used for in vitro skin penetration tests. The specific experimental methods are:

[0021] Three-month-old healthy rats were put to death by anesthesia, the abdominal hair was removed with scissors, the undamaged skin was removed, and the subcutaneous tissues were removed. After washing, they were fixed to the release ports of the Franz diffusion cell, and pH 7.4 phosphoric acid was added to the receiving chamber. The buffer is used as the release medium to keep the endothelial layer in close contact with the solution. Put the gel patch with the protective layer rem...

Embodiment 2

[0024] Pharmacological Example 2, Pharmacokinetic Experiment (Rabbit)

[0025] Take Japanese big-eared white rabbits, weighing 2.0±0.2kg, and randomly divided into groups. Each group uses both male and female, with 8 rabbits in each group. The hair on both sides of the rabbit's back spine was removed with a depilatory one day before the administration. The area of ​​the depilation was about 25cm×15cm. At the same time, it was fasted for 12 hours before administration. The dosage of each group was 50mg / kg, and the patch was applied to both sides of the back spine. Rabbit ears were taken at 15min, 30min, 1, 2, 3, 4, 6, 8, 12, 24h after administration. The marginal venous blood was 2mL, and the blood drug concentration (ng / mL) was detected. The data is expressed in terms of mean±standard deviation, and the data is processed by Excel.

[0026] The grouping and test results are as follows (ng / mL) (n=8, means±s)

[0027]

[0028]

[0029] The experimental results show that, compared wit...

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Abstract

A lidocaine gel emplastrum comprise a backing layer, a drug store and a protective layer, and is characterized in that that drug store consists of the following components in percentage by weight: 3 to 6 % of lidocaine as an active ingredient; 7 to 12 % of oil phase component consisting of castor oil and castor oil polyoxyethylene ether with the ratio of 1:0.2-0.4; 5-10% of partially neutralized sodium polyacrylate as a water phase component, 15-20 % of glycerin, 1.5 to 2 % of sodium carboxymethyl cellulose, 0.3 to 0.5 % of triethyl citrate, 0.1 to 0.2 % of cinnamic acid, 0.1 to 0.2 % of citric acid, 0.2 to 0.4 % of dihydroxyaluminum aminoacetate, 0.1 to 0.3 % of calcium sodium edetate, and 1 to 3 % of filler, with the balance being water. The partially neutralized sodium polyacrylate is NP700, 30 to 50 % of the lidocaine is dispersed in the oil phase, and the rest of the lidocaine is dispersed in the aqueous phase.

Description

Technical field [0001] The invention relates to a lidocaine gel plaster. Background technique [0002] Lidocaine (2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide, CAS:137-58-6, lidocaine, LDC) is a common local anesthetic that can be used For local analgesia. Gel patch (Cataplasm) has the advantages of large drug loading, promoting drug penetration through the skin, no allergic reaction and irritation to the skin, no pain and no residue when peeling off. The existing lidocaine gel patch product was first marketed and produced by Endo Pharma, and its specification is 700mg / 13g paste / 140cm 2 . The auxiliary materials used are aluminum dihydroxyglycolate (aluminum glycolate) EDTA-2Na, glycerin, kaolin, methyl paraben, polyacrylic acid, polyvinyl alcohol, propylene glycol, propyl paraben, CMC-Na, sodium polyacrylate, Sorbitol, tartaric acid and urea. However, it is known from the reported pharmacokinetic literature that when the preparation is administered according to the recom...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/167A61K47/44A61K47/14A61K47/12A61P29/00A61K9/107
CPCA61K9/107A61K9/7076A61K31/167A61K47/12A61K47/14A61P29/00
Inventor 李斐菲姚永波杨红伟
Owner 北京茗泽中和药物研究有限公司
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