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Compositions and preparation methods for bioavailable oral aceclofenac dosage forms

A technology of aceclofenac and composition, applied in the field of pharmaceutical preparations, can solve the problems such as no clear improvement in solubility and dissolution rate, and no mention of efficacy and stability of pharmaceutical preparations

Inactive Publication Date: 2004-11-03
PHARM TECH RES +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

No clear improvement in solubility and dissolution in solid dispersion formulations containing aceclofenac
Moreover, there is no mention of the efficacy and stability of pharmaceutical formulations prepared using PVP

Method used

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  • Compositions and preparation methods for bioavailable oral aceclofenac dosage forms
  • Compositions and preparation methods for bioavailable oral aceclofenac dosage forms
  • Compositions and preparation methods for bioavailable oral aceclofenac dosage forms

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] 1 g of aceclofenac was dissolved in 20 ml of a mixture of acetone and ethanol at a volume ratio of 1:1, and then 1 g of PVP was added thereto and completely dissolved to obtain a transparent solution. Add 0.2 g of sodium lauryl sulfate and 5 ml of distilled water to the solution, dissolve completely until transparent. The obtained reaction mixture was sprayed using the procedure described in Experimental Example 1 below and then dried to obtain a solid powder formulation.

Embodiment 2

[0040] 1 g of aceclofenac was dissolved in 20 ml of a mixture of acetone and ethanol at a volume ratio of 1:1, and then 1 g of PVP was added thereto and completely dissolved to obtain a transparent solution. Add 2 g of sodium lauryl sulfate and 5 ml of distilled water to the solution, completely dissolve to obtain a transparent solution. The obtained mixture was sprayed using the procedure described in Experimental Example 1 below and then dried to obtain a solid powder preparation.

Embodiment 3

[0042] 1 g of aceclofenac was dissolved in 20 ml of a mixture of acetone and ethanol at a volume ratio of 1:1, and then 1 g of PVP was added thereto and completely dissolved to obtain a transparent solution. Add 4g of sodium lauryl sulfate and 5ml of distilled water to the solution, dissolve completely to obtain a transparent solution. The obtained mixture was sprayed using the procedure described in Experimental Example 1 below and then dried to obtain a solid powder preparation.

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PUM

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Abstract

There are provided compositions and preparation methods for bioavailable oral aceclofenac dosage forms. More particularly, the compositions containing water-insoluble aceclofenac, a polymeric base selected from the group consisting of polyvinyl, methyl cellulose, ethyl cellulose, hydroxypropylmethylcellulose, carboxy methyl cellulose, glyceryl monostearate, carbamer, and poloxamer, and surfactant. The compositions of the present invention can be formulated into compressed particles, granules, tablets, capsules or even semisolid preparations, which significantly increase the bioavilablity due to the improvement of dissolution of the drug in gastrointestinal tract, and reduce the manufacturing cost by simple process.

Description

technical field [0001] The present invention relates to pharmaceutical preparations containing aceclofenac (aceclofenac) for oral administration, in particular, to containing aceclofenac with poor water solubility, selected from polyvinylpyrrolidone, methylcellulose, ethylcellulose , polymer-based formulations of hydroxypropylmethylcellulose, carboxymethylcellulose, glyceryl monostearyl, carbamer and poloxamer, and surfactants. In addition, the present invention also relates to the preparation method of this kind of oral preparation. Background technique [0002] Aceclofenac represented by the following general formula 1 is a non-steroidal anti-inflammatory drug (NSAID), including WO99 / 62865 and WO99 / 55660 and the journal "Drugs" Vol. 52 (1), 113-124 ( 1996) disclosed its preparation method and efficacy in detail. [0003] Formula 1 [0004] [0005] However, when administered to humans, aceclofenac, which is poorly water-soluble, has low solubility and dissolution rat...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/16A61K31/216A61K47/02A61K47/04A61K47/10A61K47/12A61K47/14A61K47/18A61K47/20A61K47/30A61K47/32A61K47/34A61K47/36A61K47/38A61P29/00
CPCA61K31/216A61K9/1694A61K47/32A61P29/00A61K47/30
Inventor 李凡珍李东源金泰完
Owner PHARM TECH RES
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