Compositions and methods for dermally treating pain

A skin and drug technology, applied in the field of preparations for the treatment of musculoskeletal pain or neuropathic pain, can solve the problems of expensive storage capsules, hindering skin stretching, discomfort, etc.

Inactive Publication Date: 2013-12-18
NUVO RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] With regard to liquid reservoir patches, even when the drug is compatible with the specific liquid or semisolid solvent system carried in the thin pouch of the patch, the solvent system must still be compatible with the The adhesive layer is compatible, otherwise the drug may be adversely affected by the adhesive layer or the drug / solvent system may reduce the adhesion of the adhesive layer
In addition to these formulation considerations, it is generally more expensive to manufacture a reservoir patch than a matrix patch
[0006] Another disadvantage of skin (including transdermal) patches is that they are usually not stretchable or flexible, since the backing membrane (in matrix patches) and thin fluid pockets (in bladder patches) are generally made of Made of polyethylene or polyester, both of which are relatively non-stretchable materials
If the patch is applied to an area of ​​skin that is significantly stretched during body movement, such as a joint, separation between the patch and the skin may occur, thus disrupting drug delivery
In addition, patches present on the surface of the skin may hinder the stretching of the skin during body movements and cause discomfort
For these additional reasons, patches are not an ideal dosage form for areas of skin over muscles and joints that are intended to expand and stretch during physical activity

Method used

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  • Compositions and methods for dermally treating pain
  • Compositions and methods for dermally treating pain
  • Compositions and methods for dermally treating pain

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0099] As noted, hairless mouse skin (HMS) or human epidermal membrane (HEM) were used as model membranes for the in vitro flux studies described here. Hairless mouse skin (HMS) was used as a model membrane for the in vitro flux study described here. The newly isolated epidermis from the abdomen of hairless mice was carefully placed between the supply chamber and the receiving chamber of the Franz diffusion cell. The receiving chamber was filled with phosphate buffered saline (PBS) of pH 7.4. The experiment was initiated by placing the test formulation on the stratum corneum (SC) of the skin sample. The Franz cell was placed on a heating table maintained at 37°C and the temperature of the HMS was maintained at 35°C. At preset time intervals, aspirate 800 μL aliquots and replace them with fresh PBS solution. Determine the skin flux (μg / cm) from the steady-state slope of the cumulative penetration versus time curve 2 / h). The placement of the skin and the sampling technique u...

Embodiment 2

[0101] Non-volatile solvent system

[0102] By placing 200 mcL on the stratum corneum side (supply cell) of hairless mouse skin, the steady-state flux of ropivacaine base in the above-mentioned non-volatile solvent was obtained. The in vitro study was performed as described in Example 1. According to Table 2, the non-volatile solvents glycerin and Tween 20 have low steady-state flux values ​​and are not considered "flux favorable". However, mineral oil and isostearic acid are flux-favorable solvents, and are good candidates for evaluating curing agents and volatile solvents to design acceptable release formulations. Surprisingly, Span 20 has a much higher steady-state flux value and will also be qualified as a highly flux-favorable solvent.

Embodiment 3

[0104] Non-volatile solvent system

[0105] By placing 200 mcL on the stratum corneum side (supply cell) of hairless mouse skin, a steady-state flux of diclofenac sodium from the above-mentioned non-volatile solvent was obtained. The in vitro study was performed as described in Example 1. According to Table 3, the non-volatile solvent glycerin has a value of 1mcg / cm 2 The estimated treatment steady-state flux value of / h is equivalent to the steady-state flux value and can be considered as a solvent with favorable flux. However, the steady-state flux values ​​of isopropyl myristate, ethyl oleate, propylene glycol, and Span 20 are at least 10 times the reported flux value of glycerol and are considered favorable for flux.

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PUM

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Abstract

The present invention is drawn to solidifying formulations for dermal delivery of a drug for treating pain, such as musculoskeletal pain, inflammation, joint pain, or neuropathic pain. The formulation can include a drug selected from certain drug classes, a solvent vehicle, and a solidifying agent. The solvent vehicle can include a volatile solvent system comprising at least one volatile solvent, and a non-volatile solvent system comprising at least one non-volatile solvent, wherein the evaporation of at least some of the volatile solvent converts the formulation on the skin into a solidified layer and the non-volatile solvent system is capable of facilitating the topical delivery of the drug(s) at therapeutically effective rates over a sustained period of time.

Description

Invention field [0001] The present invention generally relates to formulations and methods for treating musculoskeletal pain or neuropathic pain. More specifically, the present invention relates to a viscous preparation having a viscosity suitable for application to the skin surface and forming a solidified layer for transdermal drug delivery on the skin. Background of the invention [0002] Pain can be caused by many sources. For example, neuropathic pain can be caused by diseases such as viral infections and diabetes. For example, post herpetic neuralgia (post herpetic neuralgia) is caused by herpes virus infection and typically causes moderate to severe pain in the infected skin of an infected person. Topical products, such as creams or patches containing appropriate drugs, can be used to control neuropathic pain; however, patches as well as traditional semi-solid preparations such as creams and ointments have significant disadvantages. Semi-solid preparations usually conta...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A01N37/12
Inventor J·张K·S·华纳K·莎玛
Owner NUVO RES
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