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Highly concentrated pourable aqueous solutions of potassium ibuprofen, their preparation and their uses

A technology of ibuprofen potassium and liquid, which is applied in the field of new highly concentrated aqueous liquid compositions, and can solve problems such as complex processing steps, sodium salt or potassium salt cannot be realized, etc.

Inactive Publication Date: 2007-01-17
ALBEMARLE CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

While a solution with a concentration higher than about 8% by weight is obtained according to the method of the above-mentioned patent, unfortunately the maximum concentration of dissolved potassium ibuprofen is shown to be about 24.2% by weight, and this is achieved by less than about 50% ibuprofen converted to potassium salt
Complete conversion to the sodium or potassium salts of these components was also not possible due to undesired reactions with polyethylene glycol solvents resulting from attempts to react at higher concentrations
In order to minimize undesired side reactions, complex processing steps are used in the method

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Potassium carbonate (69.1 grams) was weighed in a stainless steel mixing bowl. To this was added 75 grams of deionized water, the bowl was placed in a homogenizer (Dispermat CV by VMA-Getzmann) equipped with a high shear dispersing impeller and mixed immediately. K 2 CO 3 After being substantially dissolved in water, 206 grams of ibuprofen (Albemarle Corporation) powder was added to the mixing bowl with continued mixing. Then 80 grams of absolute ethanol was added to the mixture and mixing was continued for an additional 30 minutes. After the mixing was discontinued, the mixing bowl was rinsed with an additional 220 grams of absolute ethanol and the contents of the bowl were quantitatively transferred to a 2 liter round bottom flask. The flask was mounted on a Rotavapor RE11 (manufactured by Buchi) and heated to 70°C under rotation until the mixture became clear (or at least slightly cloudy or turbid). After the contents of the flask became clear (or at least slight...

Embodiment 2

[0057] The operation of Example 1 was repeated in substantially the same manner. Typically, a clear, stable liquid composition containing about 83.2% by weight potassium ibuprofen, about 10.8% by weight water, and about 6.0% by weight ethanol as analyzed by NMR. In this case, the weight ratio of ethanol to water is about 0.65:1.

Embodiment 3

[0059] The operation of Example 1 was repeated in substantially the same manner, except that agitation was performed in a Hobart mixer and solvent removal by an aspirator pump was performed in a smaller amount than in Example 1. Typically, the resulting clear, stable liquid composition contains about 81.7% by weight potassium ibuprofen, about 11.3% by weight water, and about 7.1% by weight ethanol as shown by NMR analysis. The weight ratio of ethanol to water is about 0.65:1.

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PUM

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Abstract

Concentrated pourable potassium ibuprofen liquid compositions and their preparation are described. They are comprised of (i) potassium ibuprofen, (ii) water; and (iii) methanol, ethanol, 1-propanol, 2-propanol, 1,1-dimethylethanol, or a mixture of any two or more of them. The amount of dissolved potassium ibuprofen in the composition is in the range of about 60 to about 90 wt%. These compositions are suitable for use in the preparation of pharmaceutical dosage form such as liquid-filled soft gelatin capsules, syrups, elixirs, suspensions; solid dosage forms such as tablets or caplets; and topically-applied products such as lotions, creams or ointments.

Description

technical field [0001] The present invention relates to novel highly concentrated aqueous liquid compositions of potassium 2-(4-isobutylphenyl)propionate believed to be at least partially solubilized and / or at least partially ionized and / or at least complexed. Accordingly, it is believed that the composition may contain at least some potassium cations and 2-(4-isobutylphenyl)propionate anions. If one removes all liquid from these compositions, the resulting solids will contain at least predominantly potassium 2-(4-isobutylphenyl)propionate. [0002] Therefore, for convenience and convenience only, the term "dissolved" is often used in this document in relation to potassium ibuprofen. The term is used in its ordinary sense to indicate that a certain amount of potassium ibuprofen has gone into solution. The term is not intended to represent that indeed such 2-(4-isobutylphenyl)propionic acid is in the liquid composition. Rather, the term is used to describe that by removing a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K31/19A61K31/192
CPCA61K31/192A61K31/19A61K9/4858A61P29/00A61K9/08A61K31/185
Inventor 帕特里克·C.·胡格雷戈里·H.·兰贝思阿西里奥·J.·马尔科姆
Owner ALBEMARLE CORP
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