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Reconstitutable parenteral composition containing COX-2 inhibitor

A technology of COX-2 and composition, which is applied in the preparation of the dilutable preparation, prepared as a powder, parenteral administration preparation, the preparation prepared by diluting in an aqueous carrier before parenteral administration, injection Preparations, in the field of parecoxib, can solve problems such as not describing injection preparations

Inactive Publication Date: 2004-07-14
PHARMACIA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] While these and other selective COX-2 inhibitory drugs and prodrugs have been broadly proposed for parenteral administration, no pharmaceutically acceptable injectable formulations of said drugs or prodrugs have been described to date.

Method used

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  • Reconstitutable parenteral composition containing COX-2 inhibitor
  • Reconstitutable parenteral composition containing COX-2 inhibitor
  • Reconstitutable parenteral composition containing COX-2 inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0258] Dilutable formulation powder compositions, designated herein as Formulations A-D, containing parecoxib in the form of parecoxib sodium in doses of 5, 10, 20 and 40 mg, respectively, were prepared as follows.

[0259] First, solutions for freeze-drying having compositions shown in Table 1 were prepared. Solutions A-D for lyophilization correspond to formulations A-D, respectively.

[0260] Element

[0261] When preparing each of the above solutions for lyophilization, dissodium hydrogen phosphate heptahydrate was dissolved in an appropriate volume of water for injection, and the pH of the resulting solution was adjusted to 8.1 with 1M phosphoric acid. Dissolve parecoxib sodium in this solution. Check the pH, if necessary, adjust the pH again with 1M phosphoric acid or 1N sodium hydroxide, add water, and adjust the volume to the target volume to form a solution for lyophilization. The volume of each prepared solution was sufficient to prepare several unit dos...

Embodiment 2

[0272] Dilutable formulation powder compositions referred to herein as Formulations E-J, each containing 20 mg of parecoxib in the form of parecoxib sodium, were prepared as follows. First, a solution for freeze-drying having the composition shown in Table 5 was prepared. Solutions E-J used for lyophilization correspond to formulations E-J, respectively. The solutions and the lyophilized powder compositions were prepared using procedures similar to those used to prepare Formulations A-D of Example 1.

[0273] It can be noted that Formulations E-J each contain more than about 10% of excipient ingredients other than buffer (disodium phosphate or tromethamine). These formulations are presented herein for comparison purposes.

[0274] Element

E

F

G

H

I

J

Parecoxib sodium (mg)

21.18

21.18

21.18

21.18

21.18

21.18

Disodium hydrogen phosphate heptahydrate

(mg) ...

Embodiment 3

[0280] Plasma concentrations of valdecoxib in human subjects were determined in pharmacokinetic studies. In 11 healthy adult subjects, a 20 mg dose of parecoxib in the form of parecoxib sodium in a 1 ml bolus was administered once intravenously (IV) or as an immediate-release tablet orally with 240 ml of water 20 mg dose of valdecoxib. The subjects drank 180ml of water 1 hour, 2 hours and 3 hours after taking the medicine.

[0281] Valdecoxib plasma concentrations were determined using a validated high performance liquid chromatography (HPLC) procedure. figure 1 Mean valdecoxib plasma concentrations from 0 to 24 hours after dosing are shown.

[0282] Maximum valdecoxib plasma concentrations were achieved earlier with intravenous administration of parecoxib sodium than with oral administration of valdecoxib.

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PUM

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Abstract

A pharmaceutical composition comprises, in powder form, (a) at least one water-soluble therapeutic agent selected from selective COX-2 inhibitory drugs and prodrugs and salts thereof, for example parecoxib sodium, in a therapeutically effective total amount constituting about 30% to about 90% by weight, (b) a parenterally acceptable buffering agent in an amount of about 5% to about 60% by weight, and optionally (c) other parenterally acceptable excipient ingredients in a total amount not greater than about 10% by weight, of the composition. The composition is reconstitutable in a parenterally acceptable solvent liquid to form an injectable solution. A lyophilization process is provided for preparation of such a composition.

Description

field of invention [0001] The present invention relates to water-soluble selective cyclooxygenase-2 (COX-2) inhibitory drugs and salts and prodrugs thereof, especially parecoxib, for example in the form of its sodium salt (parecoxib sodium). Parecoxib is a water-soluble prodrug of the selective COX-2 inhibitor valdecoxib. More specifically, the present invention relates to parenteral formulations, such as injectable formulations, of water-soluble selective COX-2 inhibitory drugs and salts and prodrugs thereof. Even more particularly, the invention relates to said formulations prepared as a powder for dilution in an aqueous vehicle prior to parenteral administration. The invention also relates to methods for the preparation of said dilutable formulations, methods of treatment using said formulations and the use of said formulations in the manufacture of medicaments. Background of the invention [0002] Cyclooxygenase (COX) inhibition is believed to be a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D237/16A61K9/00A61K9/08A61K9/19A61K31/00A61K31/122A61K31/352A61K31/365A61K31/415A61K31/42A61K31/444A61K31/50A61K45/08A61K47/02A61K47/04A61K47/12A61K47/18A61K47/36A61P29/00C07D213/61C07D231/12C07D261/08C07D307/58C07D311/58
CPCA61K31/42A61K9/0019A61K31/50A61K47/18A61K31/00A61K47/02A61K31/444A61K9/19A61K31/365A61K31/122A61K31/415A61K9/08A61K45/00A61P29/00A61K9/00
Inventor T·T·卡拉利S·内马A·卡林
Owner PHARMACIA CORP
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