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Loxoprofen sodium cataplasm

A technology of cataplasms and fillers, applied in the field of loxoprofen sodium cataplasms, which can solve the problems of lack of delayed hypersensitivity reactions

Inactive Publication Date: 2018-06-01
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

Loxoprofen sodium itself is a non-steroidal anti-inflammatory drug. In its indications, patients with rheumatoid arthritis, frozen shoulder and other diseases are often in the middle of delayed hypersensitivity. In the actual application process, For patients with delayed hypersensitivity, they are prone to symptoms of contact dermatitis such as skin redness, itching, and rash. Since traditional skin irritation experiments all use healthy animal models, there is a lack of research on delayed hypersensitivity. A loxoprofen sodium cataplasm that can reduce the skin irritation of patients with delayed hypersensitivity has become an urgent problem in the prior art

Method used

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  • Loxoprofen sodium cataplasm

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Pharmacological Example 1 In Vitro Release Experiment

[0027] According to the method provided in the third method (paddle and disk method, used for transdermal patch) in the second appendix XD of the Chinese Pharmacopoeia 2010 edition, the emergency release of the patch obtained in Examples 1 to 6 is measured . The specific method is as follows

[0028] In the test, physiological saline was used as the release medium, and the release medium was added into the dissolution cup, pre-warmed to (32±0.5°C) to remove the protective layer of the cataplasm, cut into a size of 2.5cmx7.5cm, and put it flat into a dialysis bag (molecular weight cut-off 14,000 ), with the release side facing up, placed between two layers of discs, so that the edges of the disc clamp the two ends of the dialysis bag, and then wrap and fix with rubber bands to fix the disc. At 10min, 20min, 30min, 45min, 60min, 90min, 2h, 2.5h, 3h and 4h, 6mL samples were taken from the dissolution vessel respecti...

Embodiment 2

[0029] Pharmacological Example 2 New Zealand Rabbit Animal Model Skin Irritation Experiment of Delayed Hypersensitivity

[0030] 1. Experimental animals: select New Zealand white rabbits, weighing 2.0-2.5 kg, male or female, 10 rabbits in each group.

[0031] 2. Modeling, the model group uses potassium dichromate (K 2 Cr 2 o 7 ) for immunization, each rabbit was injected intramuscularly with 1% K 2 Cr 2 o 7 + Freund's complete adjuvant mixture (volume ratio 1:1) 0.5ml. At the same time, 0.1ml of the mixed solution was injected intradermally in 4 places, and after continuous injection for 7 days, the back was treated with K 2 Cr 2 o 7 / 40% dimethyl sulfoxide solution for skin application. In the third week after the first injection, 0.5ml of 0.5% K2Cr2O7 solution was injected intramuscularly to strengthen the hypersensitivity reaction.

[0032] 3. Experimental method

[0033] After the last injection, cut off most of the rabbit hair on both sides of the spine with sc...

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Abstract

The invention discloses a loxoprofen sodium cataplasm. The loxoprofen sodium cataplasm is composed of a back sheet layer, a drug storage cavern, and a protection layer; the drug storage cavern is composed of, by weight, 0.9 to 1.2% of loxoprofen sodium which is taken as an active component, 5 to 10% of an oil phase component which is composed of castor oil, propylene glycol, and tocopheryl acetate, 5 to 10% of a partially neutralized sodium polyacrylate, 15 to 20% of glycerol, 0.2 to 0.4% of dihydroxyaluminum aminoacetate, 0.4 to 0.6% of calcium disodium edetate, 1 to 1.5% of carbomer 934, 1.5to 3% of hydroxypropyl methyl cellulose (HPMC), 1 to 2% of pH conditioning agent ascorbic acid, 0.05 to 0.1% of nicotinamide, 1 to 3% of a filter, and the balance water.

Description

technical field [0001] The present invention relates to loxoprofen sodium cataplasm. Background technique [0002] Loxoprofen Sodium (CAS: 80382-23-6, Monosodium [0003] 2-{4-[(2-oxocyclopentyl)methyl]phenyl}propanoatedihydrate, 2-[4-(2-oxocyclopentyl-1-ylmethyl)phenyl]propanoate dihydrate) belongs to phenylpropanoid Acid NSAIDs, whose molecular formula is as follows: [0004] [0005] Loxoprofen sodium was successfully developed by Japan's Daiichi Sankyo Co., Ltd. in 1986, and it was listed in Japan in 1986. It can be widely used clinically for anti-inflammation of rheumatoid arthritis, low back pain, frozen shoulder, neck, shoulder and wrist syndrome, etc. Analgesia etc. The external preparations of loxoprofen sodium are mainly patches and cataplasms produced by Daiichi Sankyo. The specifications of the cataplasm are 100mg / 10g paste / 10cm×14cm. Loxoprofen sodium itself is a non-steroidal anti-inflammatory drug. In its indications, patients with rheumatoid arthritis...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/216A61K47/22A61P29/00A61P19/02
CPCA61K9/7023A61K31/216A61K47/22
Inventor 杨红伟姚永波李斐菲
Owner 北京茗泽中和药物研究有限公司
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