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Intraorally disintegrating valdecoxib compositions

A technology of valdecoxib and its composition, which is applied in the field of treating cyclooxygenase-2-mediated diseases, and can solve problems such as low water solubility and delayed onset of treatment

Inactive Publication Date: 2005-06-29
PHARMACIA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since the aqueous solubility of valdecoxib is already extremely low, any further reduction in oral dissolution of valdecoxib cannot be expected to lead to improved sensory properties
Furthermore, an additional reduction in the aqueous solubility of valdecoxib would be expected to result in an unacceptable delay in the onset of treatment

Method used

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  • Intraorally disintegrating valdecoxib compositions
  • Intraorally disintegrating valdecoxib compositions
  • Intraorally disintegrating valdecoxib compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0125] Three kinds of valdecoxib composite granules (G1-G3) were prepared according to the following methods. Three batches of granulation fluid were prepared, as shown in Table 1, to prepare a dry powder blend comprising valdecoxib and at least one of Avicel PH101, PVP (K29-32) and sodium lauryl sulfate (SLS). The dry powder blend was wet granulated in a 2 liter Key Granulator.

[0126] Valdecoxib composite granules G1 were prepared using Eudragit(R) E PO, SLS and dibutyl sebacate and dispersed in 97.6 g of water; this dispersion was added to the dry powder blend over 4 minutes and mixed to form a mixture. An additional 30 g of water was then added to the mixture and the mixture was tray dried and hand passed through a 20 mesh screen to form valdecoxib composite granules.

[0127] Valdecoxib composite granules G2 were prepared using PVP as a dry binder. Water was added to the dry powder blend over 5 minutes. The granulation uniformity is poor, half of the raw material is s...

Embodiment 2

[0131] Prepare valdecoxib instant tablets (A batch, hereinafter also referred to as instant tablets A) according to the following method, and the components are shown in Table 2. Valdecoxib (457.75 g) and Avicel PH101 (226.92 g) were mixed together for 2 minutes in a Glatt granulator (main and cutter speeds set at 600 and 3000 rpm, respectively) to form a premix. Eudragit(R) E PO (49 g) and citric acid (16.33 g) were added to a vessel containing 250 g of water to form a solution. This solution was added to the premix at a substantially constant rate over 8.5 minutes (mixing continued) to form a wet mixture. After the solution addition was complete, the wet mixture was further mixed for 1 minute to form wet granules. The obtained wet granules are passed through a 18-mesh sieve, and dried in a 40° C. oven or a fluidized bed dryer to form a valdecoxib complex whose dissolution is retarded. Valdecoxib complex (98.31 g) was then blended with 483.69 g of placebo granules (composed...

Embodiment 3

[0134] Prepare valdecoxib instant tablets (batch B, hereinafter also referred to as instant tablets B) according to the following method, and the components are shown in Table 3. Valdecoxib (398.28 g) and Avicel PH101 (214.48 g) were mixed together for 2 minutes in a Glatt granulator (main and cutter speeds set at 600 and 3000 rpm, respectively) to form a premix. To a vessel containing 300 g of water was added Eudragit(R) E PO (112.15 g), sodium lauryl sulfate (7.88 g) and dibutyl sebacate (16.88 g) to form a dispersion. This dispersion was added to the premix at a substantially constant rate over 15 minutes (mixing continued) to form a wet mixture. After the addition of the dispersion was complete, the wet mixture was further mixed for 1 minute to form wet granules. The obtained wet granules are passed through a 18-mesh sieve, and dried in a 40° C. oven or a fluidized bed dryer to form a valdecoxib complex whose dissolution is retarded. Valdecoxib complex (112.99 g) was the...

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Abstract

Orally disintegrating valdecoxib fast-dissolving tablets and methods of preparing such dosage forms are provided. The compositions are useful for treating or preventing cyclooxygenase-2 mediated conditions and disorders.

Description

field of invention [0001] The present invention relates to orally disintegrating pharmaceutical compositions comprising valdecoxib as an active ingredient, methods of preparing such compositions and methods of treating cyclooxygenase-2 mediated disorders comprising the oral administration of such compositions to a subject. combination. Background of the invention [0002] Compound 4-(5-methyl-3-phenyl-4-isoxazolyl)benzenesulfonamide, also known as valdecoxib in this specification, U.S. Patent No.5,633,272 of Talley et al. discloses this compound and preparation It and methods of related compounds, this patent is hereby incorporated by reference. Valdecoxib has the following structure: [0003] [0004] The compounds reported in the above-mentioned U.S. Patent No. 5,633,272, including valdecoxib, are disclosed therein as useful anti-inflammatory, analgesic and antipyretic agents, and are effective for cyclooxygenase relative to cyclooxygenase-1 (COX-1). -2 (COX-2) inhib...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/20A61K31/42A61K31/421A61K9/26A61K47/00A61K47/10A61K47/26A61K47/32A61K47/34A61K47/38A61P29/00A61P29/02
CPCA61K9/0056A61K9/2077A61K9/2081A61K31/42A61P29/00A61P29/02A61K47/30
Inventor 特兰·T·李布莱克·C·路德维格约瑟夫·P·里奥尤迪·J·沙山本健
Owner PHARMACIA CORP
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