Unlock instant, AI-driven research and patent intelligence for your innovation.

Compositions

A composition and compound technology, applied in the field of therapeutic application in the treatment of pain, can solve the problems of unrelieved evaluation and the like

Inactive Publication Date: 2016-11-09
GLOBALACORN
View PDF14 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, studies on potent P2X3-selective ligands with reasonable potent bioavailability are still lacking
To date, selective P2X3 receptor antagonists have not been successfully evaluated in the clinic for the relief of chronic nociceptive or neuropathic pain

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Compositions
  • Compositions
  • Compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0236] AppCH 2 Both ppA and AppNHppA are tetrabasic acids and thus can form pharmaceutically acceptable salts in combination with monobasic amino ester local anesthetics such as tetracaine, and / or with monobasic aminoamide local anesthetics such as lidocaine ( figure 1 ). These salts can be administered by direct injection, via a patch or in combination with minimally invasive techniques such as iontophoresis or microneedling (Elsabahy M, Foldvari M: Needle-free gene delivery through the skin: an overview of recent strategies. Current Pharma Design, (2013) Mar 12, manuscript in press).

Embodiment 2

[0238] AppCH 2 Both ppA and AppNHppA are tetrabasic acids and can be combined with the ABC / ABCD lipid-based nanoparticle system (LNP) for transdermal delivery (in salt or free acid form as described above). Referring to recent literature on formulations of small interfering RNA (siRNA) and other RNA interference (RNAi) effectors or DNA into ABC / ABCD LNPs, suitable formulations can be derived (Miller AD (2013) Delivery of RNAi therapeutics: work inprogress. Expert Rev. Med. Devices 10:781-811)( figure 2 ). These LNP formulations can then be delivered transdermally by direct injection, via a patch, or in combination with minimally invasive techniques such as iontophoresis or microneedles (Elsabahy M, Foldvari M: Needle-free gene delivery through the skin: an overview of recent strategies. Current Pharma Design, (2013) Mar 12, manuscript in press; Rodriguez-Cruz IM, et al. Polymeric nanospheres as strategy to increase the amount of triclosan retained in the skin: passive diffu...

Embodiment 3

[0240] Area is 10cm 2 The patch of is prepared by preparing the following composition comprising:

[0241](a) 0.2-2 mg of the compound as described in Example 1, wherein the compound constitutes 20% by weight of the composition;

[0242] (b) 30% by weight of a hydrophilic polymer, eg Eudragit E 100 TM ;

[0243] (c) 44% by weight non-swellable acrylate polymer, eg Durotack 280-2416 TM ;and

[0244] (d) 6% by weight of plasticizer, e.g. Brij 97 TM .

[0245] These components are added to acetone or ethanol or another suitable volatile organic solvent and mixed to obtain a viscous mass. The substance was spread on top of an aluminized polyester foil (23 microns thick) using conventional equipment to yield a film with a wet film thickness of 0.2 mm. The film was allowed to dry within 4-6 hours at room temperature. The aluminum foil was then cut into patches with an area of ​​approximately 10 cm2.

[0246] figure 1 : AppCH 2 Schematic representation of ppA and AppNHppA...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
diameteraaaaaaaaaa
diameteraaaaaaaaaa
sizeaaaaaaaaaa
Login to View More

Abstract

The present invention relates to administration of a dinucleoside polyphosphate analogue or a pharmaceutically acceptable salt thereof, topically in a formulation comprising a suitable excipient or using a device for transdermal delivery, and / or combined with a nanoparticle carrier. The present invention also relates to the therapeutic use of such compositions or devices, in particular in the treatment of painor epilepsy. The analogue may be combined with an anaesthetic (such as a salt form) or delivered in a nanoparticle.

Description

technical field [0001] The present invention relates to dinucleoside polyphosphate analogues or pharmaceutically acceptable salts thereof with (comprising suitable excipients) or capable of sustained and / or sustained release, using transdermal delivery devices and / or with nanoparticles Topical or transdermal administration in the form of formulations in combination with a vehicle and / or anesthetic. The invention also relates to the therapeutic use of such compositions or devices, especially in the treatment of pain. Background technique [0002] More than 270 million people worldwide suffer from chronic pain, which is still primarily managed with opioids and NSAIDs. While there have been small improvements in both the opioid and NSAID areas, they still suffer from significant adverse side effects and dependence problems. [0003] P2X3 receptors have been shown to be involved in various conditions of chronic pain, including inflammation and cancer-related pain. Previous st...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K31/7084A61P23/00A61P29/00
CPCA61K45/06A61K31/7084A61P23/00A61P23/02A61P25/04A61P29/00A61K2300/00A61K9/0014A61K9/0021A61K9/127A61K9/7061A61K31/09A61K31/167A61K31/245C12N15/1138C12N2310/14C12N2320/31C12N2320/32C12N2320/51
Inventor 安德鲁·大卫·米勒
Owner GLOBALACORN