Pharmaceutical composition containing flurbiprofen and patch

A technology of flurbiprofen and its composition, which is applied in the field of pharmaceutical preparations, can solve the problems of poor compatibility between tackifying resins and drugs, damage to the cohesion of adhesive matrix, and poor drug-loading ability of patches, etc., to prolong storage time and effective action time, excellent transdermal absorption performance, and good sticking effect

Active Publication Date: 2021-11-16
江苏乐明医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the release of flurbiprofen was poor due to the inability of several binder components to dissolve flurbiprofen and the crystalline state of flurbiprofen in the formulation
In order to improve the state of the drug in the matrix, WO93 / 04677 patent publication discloses a method of using L-menthol as a dissolving agent for flurbiprofen, however, with the volatilization of L-menthol, flurbiprofen remains There is a possibility of crystallization
Japanese Patent Laid-Open No. 7-309749 discloses the use of lactic acid ester as a dissolving agent, but it destroys the cohesive force of the adhesive matrix, and then produces a paste residue on the skin, causing skin irritation
The patent document CN102028673A stabilizes the drug by adjusting the ratio of the tackifying resin in the matrix, thereby inhibiting the crystallization of flurbiprofen into the adhesive layer, but the tackifying resin is poorly compatible with the drug, and can only be applied to the patch. The stability is extended to about 3 months, and the drug-loading ability of the patch is poor, which can only maintain the effective release of the drug for about 8 hours. Clinical application needs three times a day, and the frequency of administration is too frequent

Method used

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  • Pharmaceutical composition containing flurbiprofen and patch
  • Pharmaceutical composition containing flurbiprofen and patch
  • Pharmaceutical composition containing flurbiprofen and patch

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0089] The flurbiprofen pressure-sensitive adhesive patch that present embodiment provides is made up of backing (9100 type, Japanese vilene Co., Ltd.), paste and anti-adhesive layer (KL12 type, Japan DYNIC Co., Ltd.), and the component of paste is as follows: Table 1 shows.

[0090] Table 1

[0091]

[0092]

[0093] Preparation Process:

[0094] (1) Add SIS, polyisobutylene and liquid paraffin into the reaction vessel, mix and swell at 150-160°C for more than 30 minutes, this step is carried out under nitrogen or vacuum conditions;

[0095] (2) Put terpene resin, L-menthol, calcium hydroxide, BHT and hydrogenated rosin glyceride into the mixture obtained in step (1) successively, and stir until melting at 150°C. Carry out under vacuum condition;

[0096] (3) In another reaction vessel, add flurbiprofen and poloxamer F68, heat up to 150°C, mix and stir to form a solid mixture of flurbiprofen and poloxamer;

[0097] (4) Add the solid mixture obtained in step (3) into...

Embodiment 2

[0100] The flurbiprofen pressure-sensitive adhesive patch provided in this example consists of a backing, a paste and an anti-adhesive film, and the components of the paste are shown in Table 2.

[0101] Table 2

[0102] Components and their sources Dosage Flurbiprofen (above 99.5% purity, British AESICA) 13.28g SIS (Vector 4111, DEXCO, USA) 20.29g Polyisobutylene (Oppanol B-10, BASF, Germany) 6.01g Terpene resin (A135, American PINOVA) 9.02g Hydrogenated Rosin Glycerides (HYDROGRAL-G5, French DRT) 3.01g Poloxamer F68 (BASF, Germany) 13.28g L-menthol (US SIGMA) 1.50g Liquid paraffin (Shanghai aladdin) 33.21g Calcium hydroxide (Shanghai aladdin) 0.04g BHT (MERCK, Germany) 0.38g total 100.02g

[0103] Preparation Process:

[0104] (1) Add SIS, polyisobutylene and liquid paraffin into the reaction vessel, mix and swell at 150-160°C for more than 30 minutes, this step is carried out under nitrogen or...

Embodiment 3

[0110] The flurbiprofen pressure-sensitive adhesive patch provided in this example consists of a backing, a paste and an anti-adhesive film. The components of the paste are shown in Table 3.

[0111] table 3

[0112] Components and their sources Dosage Flurbiprofen (above 99.5% purity, British AESICA) 13.28g SIS (Vector 4111, DEXCO, USA) 22.12g Polyisobutylene (Oppanol B-10, BASF, Germany) 6.55g Terpene resin (A135, American PINOVA) 9.83g Hydrogenated Rosin Glycerides (HYDROGRAL-G5, French DRT) 3.28g Polyvinylpyrrolidone K-90 (MERCK, Germany) 6.64g L-menthol (US SIGMA) 1.64g Liquid paraffin (Shanghai aladdin) 36.21g Calcium hydroxide (Shanghai aladdin) 0.04g BHT (MERCK, Germany) 0.41g total 100.00g

[0113] Preparation Process:

[0114] (1) Add SIS, polyisobutylene and liquid paraffin into the reaction vessel, mix and swell at 150-160°C for more than 30 minutes, this step is carried out under nit...

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PUM

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Abstract

The invention discloses a pharmaceutical composition containing flurbiprofen and a patch, namely a pharmaceutical composition. The pharmaceutical composition contains flurbiprofen serving as an active ingredient and pharmaceutically acceptable auxiliary materials, and the pharmaceutically acceptable auxiliary materials at least comprise a stabilizer, wherein the weight ratio of the flurbiprofen to the stabilizer is 1: (0.5-2). In the pharmaceutical composition, the flurbiprofen is dispersed in an amorphous manner, wherein all the components are matched with one another, so that the hot-melt pressure-sensitive adhesive transdermal preparation containing the composition has the characteristics of good stability of active components and excellent transdermal absorption performance.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a pharmaceutical composition and patch containing flurbiprofen. Background technique [0002] Flurbiprofen is a propionic acid non-steroidal anti-inflammatory drug (NSAIDs), which mainly exerts therapeutic effects by inhibiting prostaglandin synthase, and has good analgesic and anti-inflammatory effects. It is often used clinically for inflammation, fever and mild to moderate Symptomatic treatment of severe pain, can be used to treat aspirin ineffective or intolerable patients. [0003] Products containing flurbiprofen currently on the market include tablets, granules, injections and external preparations. Among them, the oral preparation of flurbiprofen is absorbed quickly, but the biological half-life in the body is short, only 3-5 hours. During the long-term treatment of rheumatoid arthritis, frequent administration is required, which cannot meet the purpose of long...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/192A61K9/70A61K47/10A61K47/32A61P29/00
CPCA61K31/192A61K47/10A61K47/32A61K9/7023A61P29/00Y02A50/30
Inventor 顾丹辉李冬智尹威赵拓
Owner 江苏乐明医药有限公司
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