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Flurbiprofen cataplasm preparation

A technology of flurbiprofen and fillers, which is applied in the field of external preparations of non-steroidal anti-inflammatory drugs, and can solve the problems of uneven drug release speed, long drug action time of cataplasm and slow transdermal absorption speed, etc.

Inactive Publication Date: 2017-06-13
北京茗泽中和药物研究有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Chinese patent CN031164412 discloses a kind of flurbiprofen cataplasm, and discloses a plurality of prescriptions, after testing, we find that the specific prescriptions disclosed in this document all have the defects of slow transdermal absorption rate and uneven drug release rate , the advantages of fast onset of action and long duration of action of the cataplasm cannot be repeated

Method used

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  • Flurbiprofen cataplasm preparation
  • Flurbiprofen cataplasm preparation
  • Flurbiprofen cataplasm preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Pharmacological Example 1 In Vitro Release Experiment

[0020] According to the third method (paddle and disk method, used for transdermal patches) in the release determination method in the second appendix XD of the Chinese Pharmacopoeia 2010 edition, the emergency release of the patch obtained in Examples 3 and 4 was measured. The specific method is as follows

[0021] The test uses physiological saline as the release medium: add the release medium to the dissolution cup, pre-warm to (32±0.5°C), remove the protective layer from the cataplasm, cut it into a size of 2.5cmx7.5cm, and put it flat into the dialysis bag (MWCO 14,000), the release side faces up, and 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. Take 6mL samples from the dissolution vessel at 10min, 20min, 30min, 45min, 60min, 90min, 2h, 2.5h, 3h and 4h respectively, and add an equal volume of...

Embodiment 2

[0022] Pharmacological embodiment 2, in vitro transdermal experiment

[0023] Using the improved Franz diffusion cell method, using the abdominal skin of the isolated 3-month-old rat as a barrier, the cataplasms prepared in Examples 3 and 4 and the commercially available flurbiprofen cataplasm (as a positive control) were used for in vitro Transdermal test. The specific experimental method is:

[0024] After 3-month-old healthy rats were anesthetized and killed, the abdominal hair was removed with scissors, the undamaged skin was removed, and the subcutaneous tissue was removed. After washing, they were respectively fixed at the release port of the Franz diffusion cell, and pH 7.4 phosphoric acid was added to the receiving chamber. The buffer is used as a release medium to keep the endothelial layer in close contact with the solution. Put the cataplasm with the protective layer removed on the skin, adjust the water bath so that the temperature of the outer layer is constant ...

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Abstract

The invention relates to a flurbiprofen cataplasm preparation. The flurbiprofen cataplasm preparation consists of a back lining layer, a medicine depot and a protective layer, and is characterized in that the medicine depot is prepared from the following components in percentage by weight: 0.2% to 0.5% of flurbiprofen as an active ingredient and 5% to 10% of oil phase component; the oil phase component is prepared from caprin and glycerol monolaurate according to a mass ratio of 1:(0.3-0.4); the flurbiprofen is dispersed into the oil phase, and the part using as the water phase component is used for neutralizing with 5% to 10% of sodium polyacrylate as a water phase component, 20% to 40% of moisturizing agent, 0.5% to 1.5% of Carbomer 980, 1.5% to 3% of CMC-Na (sodium carboxymethylcellulose), 0.1% to 0.2% of NMP (N-methyl pyrrolidone), 0.2% to 0.4% of dihydroxyaluminum aminoacetate, 0.1% to 0.3% of EDTA-2Na, 1% to 3% of filling agent, and the balance of water.

Description

technical field [0001] The invention relates to an external preparation of a non-steroidal anti-inflammatory drug, in particular to a cataplasm. Background technique [0002] The molecular formula of flurbiprofen (CAS: 51543-40-9, flurbiprofen) is as follows: [0003] [0004] Flurbiprofen is a fluorine-containing non-steroidal anti-inflammatory drug, mainly used in the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, traumatic pain and other pain. Flurbiprofen acts as an anti-inflammatory and analgesic by inhibiting the activity of prostaglandin synthase cyclooxygenase. Compared with oral administration, when used for pain caused by trauma and inflammation of joints, soft tissues, and muscles, the use of external preparations can reduce the side effects of oral administration and accelerate the onset of the drug. [0005] Compared with other external plasters, Cataplasm has a large drug loading capacity, and has a stronger carrying capacity fo...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/192A61K47/14A61K47/22A61P29/00A61P19/02A61P19/08
CPCA61K9/7023A61K31/192A61K47/14A61K47/22
Inventor 姚永波李斐菲杨红伟
Owner 北京茗泽中和药物研究有限公司
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