Alpha adrenergic receptor agonists for treatment of inflammatory diseases

An epinephrine and agonist technology, used in anti-inflammatory agents, nervous system diseases, non-central analgesics, etc., can solve the problem that α-adrenergic receptor agonists are not widely recognized and can be effectively treated.

Active Publication Date: 2011-02-09
WARSAW ORTHOPEDIC INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] However, to date, alpha-adrenergic receptor agonists have not been widely recognized to be effective in the treatment of atherosclerosis cau

Method used

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  • Alpha adrenergic receptor agonists for treatment of inflammatory diseases
  • Alpha adrenergic receptor agonists for treatment of inflammatory diseases
  • Alpha adrenergic receptor agonists for treatment of inflammatory diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0280] Embodiment 1: preparation test

[0281] 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.

[0282] 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.

[0283] Table 1

[0284] Table 2

[0285] ta...

Embodiment 2

[0291]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.

[0292] 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.

[0293] Group No

deal with

dose

comment

1

Clonidine

0.02mg / kg SC

clonidine control

2

100DL 7E

0％

4 pellets (3mm×0.7mm)

3

100DL 7E

5％

Clonidine HCl; 4 pills (3

mm×0.7mm)

4

100DL 5E

5％

3 pills (3mm×0.7mm)

5

100DL 5E

7％

3 pills (3mm×0....

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PUM

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Abstract

Effective treatments of pain and/or inflammation from tendonitis, carpal tunnel syndrome, tarsal tunnel syndrome, osteoarthritis, bursitis and/or an oral-facial disease are provided. Through the administration of an effective amount of at least one alpha adrenergic agonist at or near a target site, one can reduce, prevent or treat pain and/or inflammation from tendonitis, carpal tunnel syndrome, tarsal tunnel syndrome, osteoarthritis, bursitis and/or an oral-facial disease.

Description

[0001] This application claims U.S. Patent Application 12 / 422,624, filed April 13, 2009, entitled "AlphaAdrenergic Recipor Agonists for Treatment of Inflammatory Diseases" and the filing date benefit of US Provisional Application 61 / 046,201, filed April 18, 2008, entitled "Clonidine Formulations In A Biodegradable Polymer Carrier." These entire disclosures are hereby incorporated by reference into this disclosure. Background technique [0002] Pain is typically experienced when free nerve endings of nociceptors are subjected to mechanical, thermal, chemical, or other nociceptive stimuli. These pain receptors are able to transmit signals along afferent neurons to the central nervous system and then to the brain. When a person experiences pain, any one or more of a number of problems may be associated with this sensation, including but not limited to reduced function, reduced activity, sleep pattern complications, and reduced quality of life. [0003] Causes of pain include, b...

Claims

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Application Information

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IPC IPC(8): A61K31/415A61K47/34A61P29/00A61K31/137
CPCA61K9/0024A61K9/14A61K31/4162A61K31/137A61K31/415A61P1/02A61P25/00A61P29/00Y02A50/30
Inventor J·M·扎内拉V·M·金C·M·霍博特W·F·麦克凯K·R·希尔德布兰德
Owner WARSAW ORTHOPEDIC INC
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