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Skin-permeable selective cyclooxygenase-2 inhibitor composition

A technology of composition and monohydric alcohol, which is applied in the direction of active ingredients of heterocyclic compounds, drug combinations, non-central analgesics, etc., can solve the problems such as the difficulty in formulating therapeutic effect COX-2 inhibitory pharmaceutical compositions

Inactive Publication Date: 2004-11-17
PHARMACIA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0032] Therefore, regardless of whether a systemic or local therapeutic effect is desired, when not greater than about 400cm 2 It remains difficult to formulate therapeutically effective and selective COX-2 inhibitory pharmaceutical compositions when administered to skin areas

Method used

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  • Skin-permeable selective cyclooxygenase-2 inhibitor composition
  • Skin-permeable selective cyclooxygenase-2 inhibitor composition
  • Skin-permeable selective cyclooxygenase-2 inhibitor composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0067]According to the first embodiment of the present invention, the skin penetration rate of the therapeutic drug of the composition is at least equal to that provided by a reference solution of the therapeutic drug dissolved in 70% ethanol aqueous solution, preferably the rate is not less than about 10 μg / cm 2 ·sky. When skin penetration rates, or ranges for such rates, are specified herein, it is understood that rates are determined by standard testing, for example using human cadaver skin.

[0068] As an example of such a test, a Franz diffuser cell (cadaveric skin film of suitable area, eg, a 20mm diameter disc) and a suitable recipient fluid, described in more detail in the Examples below, may be used. Those skilled in the art are able to select a suitable receptor fluid, but the preferred receptor fluid of the present invention is 1% Tween 80 solution and 6% polyethylene glycol (20) oleyl ether (oleth-20) solution. The receptor fluid is maintained at a suitable temp...

Embodiment 1

[0156] Saturated solutions of celecoxib were prepared in the following solvents: 70% ethanol (EtOH) in water, ethanol, PEG-400, and propylene glycol (PG). The skin penetration performance of the solutions was tested according to the above method, and each test solution was tested with 250 μl droplets. The results are shown in Table 1.

Embodiment 2

[0158] Saturated solutions of valdecoxib were prepared and tested exactly as described in Example 1 for the celecoxib solution. The results are shown in Table 1.

[0159] drug

Celecoxib

Valdecoxib

solvent

70%

EtOH

EtOH

PEG-

400

PG

70%

EtOH

EtOH

PEG-

400

PG

concentration

(mg / ml)

15.2

91.4

297

33.3

12.7

7.48

210

23.6

skin flux

(μg / cm 2 ·sky)

15.7

±3.83

5.62

±1.49

ud

ud

12.8±

4.96

1.44±

0.54

ud

ud

[0160] ud = not detected

[0161] No skin penetration of celecoxib and valdecoxib was observed over a 24 hour period when PEG-400 or propylene glycol were used as solvents.

[0162] Surprisingly, 70% ethanol in water provided greater skin flux for both celecoxib and valdecoxib than ethanol alone. With this solvent, t...

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Abstract

A dermally deliverable pharmaceutical composition comprises at least one selective cyclooxygenase-2 (COX-2) inhibitory drug or prodrug thereof solubilized in a pharmaceutically acceptable carrier that comprises a low molecular weight monohydric alcohol, and exhibits a skin permeation rate of the therapeutic agent at least equal to that exhibited by a reference solution of the therapeutic agent in 70% aqueous ethanol. A method of effecting targeted delivery of a selective COX-2 inhibitory drug to a site of pain and / or inflammation in a subject comprises topically administering such a composition to skin of the subject, preferably at a locus overlying or adjacent to the site of pain and / or inflammation. A method of effecting systemic treatment of a subject having a COX-2 mediated disorder comprises transdermally administering such a composition, preferably by contacting the composition with an area of skin of the subject not greater than about 400 cm2.

Description

field of invention [0001] The present invention relates to pharmaceutical compositions containing selective cyclooxygenase-2 (COX-2) inhibitory drugs, and in particular to such compositions suitable for administration to the skin for local or systemic therapeutic effect. The invention also relates to methods of preparing such compositions, and to methods of treatment comprising administering such compositions to the skin of a patient in need thereof. Background of the invention [0002] Cyclooxygenase (COX) inhibition is believed to be at least the primary mechanism by which non-steroidal anti-inflammatory drugs (NSAIDs) exert their characteristic anti-inflammatory, antipyretic and analgesic effects through inhibition of prostaglandin synthesis. Conventional NSAIDs such as ketorolac, diclofenac, naproxen and their salts in therapeutic amounts inhibit both constitutively expressed COX-1 and the inflammation-associated or inducible COX-2 isoform of cycl...

Claims

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Application Information

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IPC IPC(8): A61KA61K9/00A61K9/06A61K9/08A61K9/107A61K9/12A61K31/122A61K31/196A61K31/352A61K31/365A61K31/415A61K31/42A61K31/44A61K31/4418A61K31/444A61K31/465A61K31/50A61K31/635A61K31/74A61K45/06A61K47/08A61K47/10A61K47/14A61K47/26A61K47/32A61K47/38A61PA61P29/00A61P43/00
CPCA61K31/50A61K45/06A61K47/38A61K47/26A61K9/0014A61K31/352A61K31/4418A61K47/32A61K31/44A61K31/465A61K31/122A61K31/365A61K31/415A61K31/42A61K47/14A61K31/444A61K31/635A61K31/74A61K47/10A61P29/00A61P43/00
Inventor G·W·卢G·D·埃温P·泰尔B·M·斯托勒R·戈科哈尔A·加德尔
Owner PHARMACIA CORP
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