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Use of celecoxib composition for fast pain relief

A technology for relieving pain and composition, which is applied in the field of rapid pain relief of Selexib composition, which can solve the problems of not containing Selexib and unpredictable plasma concentration, etc., and achieve the effect of rapid pain relief

Inactive Publication Date: 2003-09-24
PHARMACIA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this reference neither contains any suggestion that the suspension composition may provide an effective pain-relieving amount of Selixix, nor can it be concluded from this reference that 250 ng / ml can be reached in a rapidly bioavailable formulation Conclusions for plasma or higher pain-relieving concentrations
Especially in view of the known extensive binding of selexib to plasma albumin after oral administration (Davies et al., Clin. Pharmacokinet. 38: 225-242, 2000), therefore, one cannot predict Specific plasma concentrations that produce analgesia

Method used

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  • Use of celecoxib composition for fast pain relief
  • Use of celecoxib composition for fast pain relief
  • Use of celecoxib composition for fast pain relief

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0097] A single-center, single-dose, double-blind, placebo-controlled, parallel-group 24-hour study of 200 patients experiencing moderate to severe post-operative pain was studied. The patient is in the postoperative phase after removal of 2 or more third molars requiring bone resection. Patients were stratified according to baseline pain intensity and randomized into 4 treatment groups, administered orally at the following doses:

[0098] 1. 200mg of Selixi capsules (Celebrex  200mg).

[0099] 2. 400 mg of ibuprofen capsules.

[0100] 3. 200mg fine suspension of Selixix.

[0101] 4. Placebos.

[0102] A fine suspension of Selixix was prepared by dissolving Selixix in ethanol containing 5% polysorbate 80 and adding the resulting mixture to apple juice. The fine suspension was administered within 5 minutes of preparation.

[0103] Individual patient assessments of pain relief on a patient visit basis were at the time of dosing and at 15, 30, 45 and 60 minutes after dosi...

Embodiment 2

[0114] 1 gram of the SF-1 formulation was individually filled into individual hard gelatin capsules (Capsugel) to form Test Composition 1.

[0115] For comparison, Selixix suspension was formulated as follows:

[0116] A. Add 5.0g Tween 80 into the volumetric flask.

[0117] B. Add ethanol (to 100ml) to form a mixture, and stir the mixture to form a homogeneous solution.

[0118] C. Transfer a 5 ml aliquot of this homogeneous solution to another flask containing 200 mg of Selexib to form a premix.

[0119] D. Add 75ml of apple juice to the premix to form the Selixix Suspension Intermediate.

[0120] E. The Selexib Suspension Intermediate was left to stand for 5 minutes and then shaken to form the Selexib Suspension for comparison.

[0121] In a 24-individual, randomized, four-period, symmetric, crossover study of human subjects, the bioavailability parameters obtained with the administration of the test composition 1 were compared with those obtained with the above-m...

Embodiment 3

[0123] Two selexib / caffeine suspensions were prepared as follows.

[0124] 1. PVP (K30) was added to water to form a PVP solution of 11.25 mg PVP / ml solution; two 12 ml portions of this PVP solution were taken and placed in separate containers (A and B).

[0125] 2. Add 180 mg of caffeine aliquots to container A and 900 mg of caffeine aliquots to container B to form caffeine suspensions A and B respectively; Sonicate.

[0126] 3. Prepare the Selixix suspension (in water) as a suspension containing 30% Selixix and PVP (K30) at a concentration of 11.25 mg PVP / ml solution; Dynomill the Selixix suspension Wet milling was performed to form a finely ground Selixix suspension.

[0127] 4. Take two 6ml portions of finely ground Selixix suspension and add them to Caffeine Suspensions A and B to form Selixix / Caffeine Suspensions A and B respectively.

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Abstract

The present invention provides a method of rapidly relieving pain in a mammalian subject, preferably a human. The method comprises orally administering to a subject a pain-relieving effective amount of a composition comprising Selexib formulated in such a way that when tested on fasted humans according to standard pharmacokinetic practice, it provides a A selexib plasma concentration profile that achieves a concentration of at least about 250 ng / ml within no more than about 30 minutes postdose.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Application 60 / 207,729, filed May 26,2000. field of invention [0003] The present invention relates to the new use of certain oral pharmaceutical preparations containing the selective cyclooxygenase-2 inhibitor drug Selexib in the rapid relief of pain, and the use in the manufacture of medicines for treating pain. Background of the invention [0004] A large number of compounds have been reported to selectively inhibit cyclooxygenase-2 for therapeutic and / or prophylactic action, and have been disclosed as having therapeutic or prophylactic properties for specific cyclooxygenase-2 mediated disorders or such general disease capacity. Many in this class are substituted pyrazolylbenzenesulfonamides as reported by Talley et al. in US Pat. Fluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide, also known herein as Selixix. Selixi...

Claims

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Application Information

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IPC IPC(8): A61J3/02A61J3/07A61K9/00A61K9/14A61J3/00A61K9/16A61K9/50A61K9/64A61K31/415A61K31/485A61K31/522A61K47/10A61K47/12A61K47/14A61K47/32A61K47/34A61K47/38A61P25/04A61P25/06A61P29/00A61P43/00
CPCA61K9/0095A61K9/14A61K31/415Y10S977/915Y10S977/775Y10S977/926A61P25/04A61P25/06A61P29/00A61P43/00
Inventor A·卡林P·高A·布鲁格尔F·哈桑J·福尔贝斯
Owner PHARMACIA CORP
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