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Device for delivery of TRPV1 agonists

A delivery device, agonist technology, applied in the direction of anti-inflammatory agent, capsule delivery, sheet delivery, etc., can solve problems such as undescribed

Inactive Publication Date: 2008-05-28
NEUROGESX INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the use of such water escape and non-hydrophilic penetration enhancers to enhance the thermodynamic activity of drug depots has not been described.

Method used

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  • Device for delivery of TRPV1 agonists
  • Device for delivery of TRPV1 agonists
  • Device for delivery of TRPV1 agonists

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0096] Example 1: Preparation of a Microreservoir-Type Device Containing 0.04% by Weight Capsaicin in the Drug Depot

[0097] 16.0 g of oleyl alcohol was added to 80 mg of capsaicin and the ingredients were mixed. Next, 200 mg of ethylcellulose was added and mixed well, then left for 2 hours. Add 36.74 g Bio-PSA  4201 and 146.98 grams of Bio-PSA  4301. Vigorously mix the mass until the gelled mixture of oleyl alcohol, capsaicin, and ethyl cellulose is uniformly dispersed in the adhesive as microspheres. The resulting adhesive matrix was then coated on a release liner 3M™ Scotchpak TM On 1022, dry the solvent n-heptane by hot air at a temperature of 35-40°C. Coat weight after removal of n-heptane is about 273.6 g / m 2 . Then use 3M TM Scotchpak TM A 9733 polyester liner was laminated to the dried film, and the finished drug delivery device (5 cm x 5 cm) was punched out. The flushed drug delivery device is then enclosed in sachets of a primary packaging stack.

Embodiment 2

[0098] Example 2: Preparation of a Microreservoir-Type Device Containing 2.0% by Weight Capsaicin in the Drug Depot

[0099] 20.0 g oleyl alcohol was added to 4 g capsaicin and the ingredients were mixed. Next, 200 mg of ethylcellulose was added and mixed well, then left for 2 hours. Add 175.80 g Bio-PSA  4301. Vigorously mix the mass until the gelled mixture of oleyl alcohol, capsaicin, and ethyl cellulose is uniformly dispersed in the adhesive as microspheres. The resulting adhesive matrix was then coated on a release liner 3M TM Scotchpak TM On 1022, dry the solvent n-heptane by hot air at a temperature of 35-40°C. Coat weight after removal of n-heptane is about 277.9 g / m 2 . Then use 3M TM Scotchpak TM A 9733 polyester liner was laminated to the dried film, and the finished drug delivery device (5 cm x 5 cm) was punched out. The flushed drug delivery device is then enclosed in sachets of a primary packaging stack.

Embodiment 3

[0100] Example 3: Preparation of a microreservoir-type device containing 4 wt% capsaicin in the drug reservoir

[0101] Add 36.0 g oleyl alcohol to 8.0 g capsaicin and mix these ingredients. Next, 2.0 g of ethylcellulose was added and mixed well, then left for 2 hours. Add 154.0 g Bio-PSA  4301. Vigorously mix the mass until the gelled mixture of oleyl alcohol, capsaicin, and ethyl cellulose is uniformly dispersed in the adhesive as microspheres. The resulting adhesive matrix was then coated on a release liner 3M TM Scotchpak TM On 1022, dry the solvent n-heptane by hot air at a temperature of 35-40°C. Coat weight after removal of n-heptane is about 218.4 g / m 2 . Then use 3M TM Scotchpak TM A 9733 polyester liner was laminated to the dried film, and the finished drug delivery device (5 cm x 5 cm) was punched out. The flushed drug delivery device is then enclosed in sachets of a primary packaging stack.

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Abstract

Described herein are drug delivery devices comprising a occluded liner and a drug depot comprising a TRPVl agonist and a non-hydrophilic solvent. The depot can take different forms, such as a viscous polymer matrix, a liquid reservoir, or microreservoir droplets. Methods of making and using the drug delivery device are also described.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Provisional Patent Application Serial No. 60 / 652,923, filed February 14, 2005, the entire contents of which are hereby incorporated by reference. technical field [0003] The devices and methods described herein are in the field of drug delivery. More specifically, the devices and methods relate to the transdermal administration of capsaicin and other TRPVl agonists for pain relief. Background technique [0004] The transient receptor potential vanilloid 1 receptor (TRPV1) is a capsaicin-sensitive ligand-gated cation channel selectively expressed on small unmyelinated peripheral nerve fibers (cutaneous nociceptors) (see Caterina and Julius, 2001, "The Vanilloid Receptor: A Molecular Gateway to the Pain Pathway", Annu Rev Neurosci, 24:487-517; and Montell et al., 2002, "A unified nomenclature for the superfamily of TRP cationchannels", Mol Cell, 9:229 -31). When TRPV1 is activat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61F13/00A61K31/565
CPCA61K31/16A61K9/7084A61K31/565A61K36/81A61P17/00A61P29/00A61K9/48A61K31/165
Inventor N·穆罕默德G·C·贾米森K·R·布雷
Owner NEUROGESX INC
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