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Celecoxib compositions

a composition and celecoxib technology, applied in the field of oral deliveryable pharmaceutical compositions, can solve the problems of undesirably large aggregates of celecoxib in the composition, difficult to prepare a pharmaceutical composition containing celecoxib that has the desired blend uniformity, and complicated formulation of celecoxib for effective oral administration to a subject. achieve the effect of relative bioavailability

Inactive Publication Date: 2005-12-01
GD SEARLE & CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0062] Compositions of the invention are especially useful as anti-inflammatory agents, such as for the treatment of arthritis, with the additional benefit of having significantly less harmful side effects than compositions of conventional nonsteroidal anti-inflammatory drugs (NSAIDs).

Problems solved by technology

The formulation of celecoxib for effective oral administration to a subject has hitherto been complicated by the unique physical and chemical properties of the compound, particularly its low solubility and factors associated with its crystal structure, including cohesiveness, low bulk density and low compressibility.
Even when blended with other substances, the celecoxib crystals tend to separate from the other substances and agglomerate together during mixing of the composition resulting in a non-uniformly blended composition containing undesirably large aggregates of celecoxib.
Therefore, it is difficult to prepare a pharmaceutical composition containing celecoxib that has the desired blend uniformity.
Further, handling problems are encountered during the preparation of pharmaceutical compositions comprising celecoxib.
For example, the low bulk density of celecoxib makes it difficult to process the small quantities required during formulation of the pharmaceutical compositions.

Method used

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  • Celecoxib compositions
  • Celecoxib compositions
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Examples

Experimental program
Comparison scheme
Effect test

example 1

100 mg Dose Capsule

[0327] A capsule was prepared having the following composition:

TABLE 1WeightIngredientfraction (%)Amount (mg)Celecoxib37.04100Lactose monohydrate (NF, Ph Eur)55.46149.75Sodium lauryl sulfate (NF, Ph Eur)38.1Povidone (K29-32 USP)2.56.75Croscarmellose sodium (NF, Ph Eur)12.7Magnesium stearate (NF, Ph Eur)12.7Total capsule fill weight100270

[0328] The above unit dose composition was placed in a hard gelatin capsule (white opaque, size #2) comprising titanium dioxide (USP), gelatin (NF), and blue ink (SB-6018).

[0329] The lactose monohydrate used in each of the examples herein is commercially available from Formost Farms, Baraboo, Wis. The Ac-Di-Sol brand of croscarmellose sodium used in each of the examples herein is commercially available from FMC Corporation, Chicago, Ill. The sodium lauryl sulfate used in each of the examples herein is commercially available from Henkel Corporation, Cincinnati, Ohio. The povidone (polyvinylpyrrolidone) used in each of the exampl...

example 2

200 mg Dose Capsule

[0331] A capsule was prepared having the following composition:

TABLE 2IngredientWeight fraction (%)Amount (mg)Celecoxib74.07200Lactose monohydrate (NF, Ph Eur)18.4349.75Sodium lauryl sulfate(NF, Ph Eur)38.10Povidone (K29-32 USP)2.56.75Croscarmellose sodium12.7Magnesium stearate (NF, Ph Eur)12.7Total capsule fill weight100270

[0332] The above unit dose composition was placed in a hard gelatin capsule (white opaque, size #2) comprising titanium dioxide (USP), gelatin (NF), and blue ink (SB-6018).

example 3

100 mg Dose Tablet

[0333] Tablets were prepared having the following composition:

TABLE 3Amount / tabletWeightAmount / batchIngredient(mg)fraction (%)(kg)Celecoxib100406.40Lactose monohydrate (NF)101.8840.756.52Sodium lauryl sulfate (NF)7.530.48Povidone (K29 / 32, USP)6.252.50.40Croscarmellose sodium7.530.48(Type A, NF)Microcrystalline cellulose25101.60(Avicel PH-102, NF)Magnesium stearate (NF)1.880.750.12Total250.0110016Opadry White YS-1-18027A7.50

[0334] The tablets prepared were 0.210 inch×0.465 inch (5.0 mm×11.2 mm) modified oval shaped tablets.

[0335] The Avicel brand of microcrystalline cellulose was used in the preparation of the tablets of Examples 3 and 4 and is commercially available from FMC Corporation, Philadelphia, Pa.

[0336] Tablet dose strengths between 25 mg to 225 mg can be accomodated by increasing or decreasing the amounts of celecoxib and each of the carrier materials described above so as to maintain the same weight fractions exemplified above.

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Abstract

Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising particulate celecoxib in an amount of about 10 mg to about 1000 mg in intimate mixture with one or more pharmaceutically acceptable excipients. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and disorders.

Description

[0001] This application claims the benefit of U.S. provisional application Ser. No. 60 / 110,333 filed Nov. 30, 1998 and to U.S. application Ser. No. 09 / 451,641 filed Nov. 30, 1999.FIELD OF THE INVENTION [0002] The present invention relates to orally deliverable pharmaceutical compositions containing celecoxib as an active ingredient, to processes for preparing such compositions, to methods of treatment of cyclooxygenase-2 mediated disorders comprising orally administering such compositions to a subject, and to the use of such compositions in the manufacture of medicaments. BACKGROUND OF THE INVENTION [0003] The compound 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide (also referred to herein as celecoxib) was previously reported in Talley et al., U.S. Pat. No. 5,466,823 which describes and claims a class of 1,5-diaryl pyrazoles and their salts together with processes for the preparation of such compounds. Celecoxib has the structure: [0004] The 1,5-diary...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61KA61K9/20A61K9/14A61K9/48A61K31/135A61K31/167A61K31/415A61K31/451A61K31/485A61K31/55A61K31/7056A61PA61P1/04A61P1/16A61P3/10A61P7/06A61P9/10A61P11/06A61P17/02A61P17/04A61P17/06A61P19/02A61P19/08A61P19/10A61P21/04A61P25/04A61P25/28A61P27/02A61P29/00A61P31/18A61P35/00A61P37/08B02C13/22
CPCA61K9/2054A61K9/4866A61K9/2018A61K9/4858A61K9/2027A61K31/415A61K9/2013A61P1/00A61P1/04A61P1/16A61P11/00A61P11/06A61P13/12A61P15/00A61P17/00A61P17/02A61P17/04A61P17/06A61P17/10A61P17/16A61P19/02A61P19/04A61P19/08A61P19/10A61P21/04A61P25/00A61P25/04A61P25/06A61P25/28A61P27/02A61P27/06A61P27/14A61P29/00A61P31/18A61P35/00A61P37/00A61P37/06A61P37/08A61P43/00A61P7/04A61P7/06A61P9/00A61P9/10A61P3/10A61K9/1694A61K9/0053A61K9/2095A61K31/635A61K45/06
Inventor GAO, DANCHENHLINAK, ANTHONY J.MAZHARY, AHMAD M.TRUELOVE, JAMES E.VAUGHN, MARGARET B.
Owner GD SEARLE & CO
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