Alpha adrenergic receptor agonists for treatment of degenerative disc disease

An epinephrine, agonist technology for bone disease, neurological disease, resistance to vector-borne diseases, etc., to solve problems that are not widely evaluated as an effective treatment for pain and inflammation

Inactive Publication Date: 2010-09-22
WARSAW ORTHOPEDIC INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] However, to date, alpha adrenergic receptor agonists have not been widely evaluated as an effective treatment for pain and inflammation caused by degenerative disc disease and / or articular surface pain and inflammation

Method used

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  • Alpha adrenergic receptor agonists for treatment of degenerative disc disease
  • Alpha adrenergic receptor agonists for treatment of degenerative disc disease
  • Alpha adrenergic receptor agonists for treatment of degenerative disc disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0279] Embodiment 1: preparation test

[0280] The inventors prepared a number of formulations of clonidine in which they varied polymer type, drug loading, excipients (including some formulations where no excipients were present), pellet size, and processing. These formulations are described in Table 1, Table 2 and Table 3 below. Multiple assays were performed on these formulations, including in vitro release assays measuring the microgram quantities released and the cumulative percent release of clonidine. The results of these experiments are presented in Figure 7-3 6 in.

[0281] In vitro efflux studies were performed in phosphate buffered saline (PBS, pH 7.4) at 37°C. Briefly, sticks (n=3) were weighed before immersion in 5 mL of PBS. At regular intervals, PBS was removed for analysis and replaced with 5 mL of fresh PBS. The PBS-run-out buffer was analyzed for clonidine content using a UV-Vis spectrophotometer.

[0282] Table 1

[0283] Table 2 table 3 ...

Embodiment 2

[0289] In the Chronic Constriction Injury Model in rats, the inventors evaluated the efficacy of a 5-month clonidine / polymer depot formulation. The animal model is the Bennett model (Wistar rat). Objective: To determine whether a 5-month polymeric clonidine efflux long-acting formulation can improve pain-related behavioral responses in a rat model of neuropathic pain.

[0290] Experimental Design: Four loose chromic bowel bandages, 1 mm apart, were tied around the common sciatic nerve at the mid-thigh. Each animal received either the test treatment or the control article treatment - dosing as described in Table 5.

[0291] Group No

deal with

dose

comment

1

Clonidine

0.02mg / kg SC

clonidine control

2

100DL 7E

0％

4 pellets (3mm×0.7mm)

[0292] Group No

deal with

dose

comment

3

100DL 7E

5％

Clonidine HCl; 4 pills (3

mm×0.7mm)

4

100DL 5E...

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Abstract

Effective treatments of pain and / or inflammation from degenerative disc disease and / or facet joint are provided. Through the administration of an effective amount of at least one alpha adrenergic agonist at or near a degenerative disc and / or facet joint, one can reduce, prevent or treat pain and / or inflammation caused by the degenerative disc disease and / or facet joint.

Description

[0001] This application claims U.S. Patent Application No. 12 / 420,192, filed August 2009, entitled "Alpha Adrenergic Receptor Agonists for Treatment of Degenerative Disc Disease" and Filing date benefit of U.S. Provisional Application No. 61 / 046,201, filed April 2008, entitled "Clonidine Formulations In A Biodegradable Polymer Carrier." The entire disclosures of these applications are hereby incorporated by reference into this disclosure. Background technique [0002] The human spine is formed by 26 connected vertebrae. Each of these vertebrae is separated from any adjacent vertebrae by an intervertebral disc that cushions shock and prevents each vertebra from directly impinging on the other. At the center of each disc is the nucleus pulposus which contains proteoglycans. Surrounding the nucleus pulposus is an outer ring called the annulus fibrosus. Degenerative disc disease refers to any general degenerative condition of the lower spine that involves disc degeneration. Di...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61P29/00A61K31/415A61K47/34A61P19/00
CPCA61K9/1647A61K9/0024A61K31/415A61K31/4168A61P19/00A61P19/02A61P25/00A61P25/02A61P29/00A61P43/00Y02A50/30
Inventor W·F·麦克凯
Owner WARSAW ORTHOPEDIC INC
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