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Methods and compositions for treating pain

A composition and compound technology, applied in the directions of drug combinations, active ingredients of heterocyclic compounds, pharmaceutical formulations, etc., can solve the problems such as frequency and intensity of pain at the injection site, and no disclosure of phlebitis.

Inactive Publication Date: 2008-06-25
THERAQUEST BIOSCIENCES LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Administration of intramuscular injections in volumes of 3 mL exceeds the recommended maximum volume of 2 mL and may therefore result in increased frequency and intensity of pain at the injection site
However, the following options have not been clearly mentioned: 1) Minimizing the risk of phlebitis after intravenous administration of NSAIDs; 2) Prolonged intravenous infusion of NSAIDs through preparation A bolus injection that is at least as well tolerated or preferably more tolerated than that to achieve a more rapid IV onset of action (faster peak concentration and higher peak concentration); or 3) by taking the NSAID tolerable dose Delivered as a direct bolus instead of a 15-120 minute infusion to reduce the cost of IV administration, requiring prior dilution and administration via a volume control device
Furthermore, for non-steroidal anti-inflammatory drugs, there is no disclosure in the art about candidate salts, compounded Evaluation, detection and selection of compounds, di-salts, hydrotropes, buffers, surfactants and co-solvents

Method used

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  • Methods and compositions for treating pain
  • Methods and compositions for treating pain
  • Methods and compositions for treating pain

Examples

Experimental program
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Embodiment approach

[0156]Administer intramuscularly. Once a common method of administration, the intramuscular (IM) route is less commonly used than it used to be due to improved oral drug availability and the convenience of intravenous administration. This method of administration involves injecting the drug directly into the muscle tissue, where the drug is gradually absorbed throughout the body. For intramuscular administration of non-stimulating drugs requiring only a single injection, the intramuscular route remains a viable route, especially in outpatient settings. The intravenous route is preferred when repeated dosing is required or when rapid and reliable onset of action is desired, since repeated intramuscular administration is painful and inconvenient. Typically, the deltoid, gluteus maximus, and vastus lateralis are the sites used for intramuscular injections.

[0157] Subcutaneous injection. Subcutaneous injections involve injection into the fatty tissue under the skin. The meth...

Embodiment 1

[0302] Ketoprofen-piperazine (1:2) complex

[0303] An aqueous mixture of 0.5M ketoprofen and 1.0M piperazine was sonicated until a clear solution was obtained. The solution was then filtered through a 0.45 micron syringe filter (the pH of the filtered aliquot was approximately 10.00). Small aliquots (approximately 0.250 mL) were placed in 12-well spot ceramic plates. The physical mixture precipitated out within a few days (2-3 days) at ambient temperature.

[0304] The ketoprofen-piperazine complex forms a semisolid (physical mixture) with a water solubility greater than 360 mg / mL and a pH of approximately 9.4 (for a saturated solution).

Embodiment 2

[0306] Ketoprofen-ethylenediamine (1:2) complex

[0307] A mixture of 0.5M ketoprofen and 1.0M ethylenediamine was sonicated until a clear solution was obtained. The solution was then filtered through a 0.45 micron syringe filter (the pH of the filtered aliquot was approximately 10.00). Small aliquots (approximately 0.250 mL) were placed in 12-well spot ceramic plates. The physical mixture precipitated out within a few days (2-3 days) at ambient temperature.

[0308] The ketoprofen-ethylenediamine complex forms a semi-solid form with a water solubility greater than 500 mg / mL and a pH of about 7.3 (for a saturated solution).

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Abstract

The present invention provides a method of treating or preventing pain, inflammation or fever comprising administering to a subject in need of such treatment or prevention a therapeutically effective amount of one or more selected NSAIDs, in racemic, enantiomeric excess, or enantiomeric form, in combination with ethylenediamine and / or piperazine.

Description

[0001] This application claims priority to US Provisional Application 60 / 675,442, filed April 28, 2005, which is hereby incorporated by reference in its entirety. field of invention [0002] The present invention relates to the field of pharmaceutical compositions and their use in the treatment and prevention of pain, inflammation and fever. Background technique [0003] The medical condition of pain is a complex physiological process involving many sensory and neural mechanisms. Pain can be defined as an unpleasant sensory or emotional experience associated with or described in terms of actual or potential tissue damage. [0004] Pain is usually classified according to duration or mechanism as acute pain, inflammatory pain, visceral pain, penetrating pain, nociceptive pain, neuropathic pain, chronic pain, or cancer-related pain. Acute pain is a normal and predictable physiological response to undesirable chemical, thermal or mechanical stimuli. Acute pain is usually self-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/19A61K31/54A61K31/495A61K31/34A61K31/355
CPCA61K31/495A61K31/5415A61K31/501A61K31/13A61K45/06A61K31/4535A61P25/00A61P25/04A61P29/00A61K2300/00A61K31/355A61K31/34A61K31/54
Inventor N·巴布尔
Owner THERAQUEST BIOSCIENCES LLC