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Transdermal system for varenicline

A transdermal, skin-based technology, applied in the field of pharmaceutical compositions for medical use, can solve problems such as reactivity

Inactive Publication Date: 2008-07-30
PFIZER PRODS ETAT DE CONNECTICUT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Finally, the reactivity of varenicline with the excipient itself or with trace impurities of the excipient (i.e., degradants) can be particularly problematic due to the high dilution with the diluent

Method used

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  • Transdermal system for varenicline
  • Transdermal system for varenicline

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] As a method for determining the skin penetration properties of the active ingredient, a human cadaver skin membrane and a receiving liquid such as 1.0 M phosphate buffered saline are used for the Franz diffusion cell. Fill the receiving chamber of the Franz diffusion cell with receiving liquid and maintain the diffusion cell at 34.5°C. Cut off human corpse skin to provide a surface area of ​​1.767cm 2 的膜。 The film. The HPLC analysis of the liquid is used to determine the amount of active ingredient that penetrates through the membrane at different times ranging from 6 to 48 hours. Repeat each test several times. Table 1 shows the calculated average skin flow rate and average penetration amount per square centimeter for formulations I and II after 24 to 48 hours. These test results obtained by the Franz diffusion cell method show that, based on the theoretical active ingredient, 0.3 to 5 μg / cm 2 The skin flow rate per hour can realize the transdermal delivery of the compound...

Embodiment 2

[0081] Example 2-Matrix type transdermal

[0082] The active ingredient was mixed with an aqueous dispersion of NACOR 72-9965 (National Starch's hydrophobic acrylic copolymer) to achieve a concentration of 2% (w / w) in the dried film after the film was molded. The adhering mixture was shaped onto the released coating polymer film (Rexam Release Technologies; W. Chicago, IL), dried in a convection oven at 60°C, and cut to achieve a 2 mgA dose of active ingredient. The dried film was laminated into a laminate of polyester film (SCOTCHPACK #1012, 3M Pharmaceuticals; St. Paul, MN).

Embodiment 3

[0083] Example 3-Matrix type transdermal system

[0084] (1) Dissolve or disperse the alkali form or salt form of the active ingredient in a polyacrylate solution, such as Duro-Tak(R) 387-2052 adhesive. Add appropriate solvents, accelerators and / or fillers to the adhesive dispersion and mix well. The gas is removed from the resulting mixture and laminated to a release liner such as Medirelease(R) 2228 to form a coating with a thickness of 0.5-2 mm. The adhesive layer is dried at room temperature for 5-10 minutes, and then dried at 40-80°C for 15-30 minutes to remove all volatile solvents. A backing sheet such as Mediflex(R) 1200 is applied to the adhesive side. Store the resulting patch of the desired size in a closed package.

[0085] (2) The base form or the salt form of the active ingredient is dissolved or dispersed in an isobutylene (PIB)-based adhesive such as Duro-Tak(R) 87-6173. The following method is similar to that described in the previous section.

[0086] (3) Dissolv...

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Abstract

The present invention provides transdermal compositions comprising varenicline or a pharmaceutically acceptable salt or prodrug form thereof.

Description

Technical field [0001] The present invention relates to a pharmaceutical composition for medical use. Background technique [0002] Varenklin has the following structure: [0003] [0004] Varenicline is also called 5,8,14-triazatetracycline [10.3.1.0 2，11 .0 4，9 ]-Hexadecane-2(11), 3,5,7,9-pentaene or 7,8,9,10-tetrahydro-6,10-methylene-6H-pyrazine[2,3- h][3]-Benzazepine. Varenicline and its pharmaceutically acceptable acid addition salts are mentioned in International Patent Publication WO99 / 35131 published on July 15, 1999, the contents of which are incorporated herein by reference. [0005] Varenicline binds to neuronal nicotinic acetylcholine specific receptor sites and can be used to regulate cholinergic function. Therefore, the compound can be used to treat various diseases or disorders, including but not limited to inflammatory bowel disease (including but not limited to ulcerative colitis, pyoderma gangrenosum and Crohn’s disease), irritable bowel syndrome , Spastic dys...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/4995A61K9/12
CPCA61K9/0014A61K9/12A61K9/7061A61K9/7084A61K31/4995A61P1/00A61P1/04A61P25/00A61P25/06A61P25/08A61P25/14A61P25/16A61P25/20A61P25/22A61P25/24A61P25/28A61P25/30A61P25/32A61P25/34A61P25/36A61P29/00A61P3/00A61P3/04A61P43/00A61P9/00A61P9/06A61P9/12A61K9/70
Inventor B·A·约翰逊C·B·齐格勒
Owner PFIZER PRODS ETAT DE CONNECTICUT
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