Ibuprofen for Topical Administration

a technology of ibuprofen and topical administration, which is applied in the field of topical compositions of ibuprofen, can solve the problems of inability to tolerate oral intake of ibuprofen, ineffective dosing, and limited use of ibuprofen in its free acid form

Inactive Publication Date: 2010-06-03
BIOCHEMICS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010]In accordance with another embodiment of the invention is a method of preparing a pharmaceutical composition by solubilizing ibuprofen in a pharmaceutically acceptable solvent, creating an active drug-containing solution by combining the solubilized ibuprofen with a skin conditioner and a preservative, creating an aqueous solution containing a conditioner, a pH stabilizer and a preservative, creating an emollient phase by combining an emulsifier, a preservative, an oil and a stabilizer, combining the emollient phase and the aqueous solution, homogenizing to create a homogenized m

Problems solved by technology

Use of ibuprofen in its free acid form has been limited to formulations intended for oral administration, e.g., Motrin® in tablet and oral suspension.
However, some individuals are unable to tolerate oral intake of ibuprofen.
Fo

Method used

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  • Ibuprofen for Topical Administration
  • Ibuprofen for Topical Administration

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0046]

TABLE 1Wt % (ofexcipient)Phase AL-Arginine Base0.2Methylparaben0.2Water5Phase BIBU (USP grade)3.5Menthol2Eucalyptus Oil2N-methyl-2-pyrrolidone1Phenoxyethanol0.7Phase CCetyl Alcohol5Soybean Oil17.5Glyceryl Stearate6Beeswax22Petrolatum10Ethyl Oleate12.8Vitamin E TPGS2Capric Glyceride10Propylparaben0.1TOTAL:100

[0047]The formulation of Example 1 is prepared as follows. In Tank 1, dissolve (±)-2-(4-isobutylphenyl)propionic acid into N-methyl-2-pyrrolidone until completely solubilized. Add the remaining ingredients of Phase B and mix until completely dissolved. In the Main tank, add the ingredients of Phase C, mix while heating to 70° C. In tank 2, add the ingredients of Phase A, mix while heating to 70° C. Transfer the contents in Tank 2 into the main tank, mix for 10 minutes, and cool to 40° C. (degrees Celsius) or less. Transfer contents in Tank 1 into Main Tank at 40° C. (degrees Celsius) or less. Mix until blended (˜20 minutes).

example 2

[0048]

TABLE 2Wt % (ofexcipient)Phase AL-Arginine Base0.2Methylparaben0.2Water5Phase BIBU (USP grade)20Menthol2Soybean Oil14.8Eucalyptus oil2Phenoxyethanol0.7Dimethylacetamide2Phase CBeeswax18Petrolatum10Glyceryl Stearate5Cetyl Alcohol5Vitamin E TPGS2Capric Glyceride10Ethyl Oleate3Propylparaben0.1TOTAL:100

[0049]The formulation of Example 2 is prepared as follows. In Tank 1, dissolve menthol into eucalyptus oil until completely solubilized; add remaining ingredients of Phase B and pass through nano-equipment to reduce the particle size. In the main tank, add the ingredients of Phase C, mix while heating to 70° C. In tank 2, add the ingredients of Phase A, mix while heating to 70° C. Transfer the contents from Tank 2 into Main Tank, mix for 10 minutes; cool to 40° C. (degrees Celsius) or less. Transfer the contents of Tank 1 into the Main Tank at 40° C. (degrees Celsius) or less. Mix until blended (˜20 minutes).

example 3

[0050]

TABLE 3Preparation of Batch No. 176ZX03(% w / w)Ibuprofen in free acid form10KOH2L-Arginine Base0.5Carbopol ® 980NF (2.5%)4Veegum ® HV (10%)35Methylparaben0.2Syloid 244 FP4Phenoxyethanol0.7Water14Menthol5Eucalyptol5N,N-dimethylacetamide3Olive Oil5Lemon Oil0.5Vitamin E TPGS2Propylparaben0.1Glyceryl Monostearate7DC Elastomer 102TOTAL100

[0051]One hundred grams (100 g) of a 2.5% Carbopol® 980NF solution is prepared as follows. While heating 97.5 g water to 70° C., add 2.5 g Carbopol® 980NF powder with strong mixing (i.e.,. such that a vortex should turn). Mixing is continued until the solution is hydrated and free of clumps at 70° C. The solution is removed from heat and left at room temperature overnight, and then mixed again before use.

[0052]One hundred grams (100 g) of a 10% Veegum® HV solution is prepared as follows. While heating 90 g of water to 70° C., 10 g Veegum® HV is added with strong mixing (i.e., a vortex should turn). Mixing is continued for 30 minutes at 70° C. The mi...

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Abstract

Set forth herein is a preparation of ibuprofen (2-(4-isobutylphenyl)propionic acid) in the free acid form that is suitable for topical administration. The topical ibuprofen formulation is prepared by dissolving the free acid form of ibuprofen, or preparing a homogeneous suspension of the free acid form of ibuprofen, in the presence of a pharmaceutically acceptable solvent so as to produce a topical drug formulation compatible with the penetration of 2-(4-isobutylphenyl) propionic acid through the skin tissue. Topical formulations of ibuprofen can be based on a pharmaceutically acceptable solvent such as, e.g., a pyrrolidone solvent or dimethylacetamide.

Description

REFERENCE TO RELATED APPLICATION[0001]This application claims benefit of the filing date of U.S. provisional application Ser. No. 61 / 095,672, filed Sep. 10, 2008, hereby incorporated by reference.TECHNICAL FIELD[0002]The present invention relates to topical compositions of ibuprofen and methods for making and using the compositions.BACKGROUND[0003]Ibuprofen, an anti-inflammatory, analgesic, and anti-pyretic agent, is a member of a group of drugs known as non-steroidal anti-inflammatory drugs (NSAIDs). Past formulations of ibuprofen have chiefly made use of the water-based form (salt form) of ibuprofen. Ibuprofen in its salt form forms the basis of such drug products as Advil® (potassium salt form of ibuprofen). Use of ibuprofen in its free acid form has been limited to formulations intended for oral administration, e.g., Motrin® in tablet and oral suspension. IBU® Ibuprofen Tablets USP (Knoll Laboratories, Mount Olive, N.J.) is supplied in tablets for oral administration.[0004]NSAID...

Claims

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Application Information

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IPC IPC(8): A61K31/192A61P29/00
CPCA61K9/0014A61K47/32A61K9/7023A61K31/192A61P29/00A61K47/16A61K47/22
Inventor CARTER, STEPHEN G.ZHU, ZHENPATEL, KANUKOZWICH, DIANE L.
Owner BIOCHEMICS
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