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Transdermal delivery system for alkaloids of aconitum species

A technology of aconitine and alkaloids, which can be used in nervous system diseases, antipyretics, drug combinations, etc., and can solve the problem of low success rate

Inactive Publication Date: 2003-10-22
美国爱科赛尔制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

While this type of treatment does alleviate many of the withdrawal symptoms associated with detoxification in patients, it takes months and is therefore not very successful in helping addicts wean themselves off their drug dependence for good

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0041] The term "matrix", "matrix system" or "matrix patch" as used herein refers to dissolving or suspending a certain amount of aconitine alkaloid in or in a polymeric carrier. In addition, pressure-sensitive The adhesive may also contain other ingredients, or penetration enhancers or other health benefit substances dissolved or suspended in the pressure sensitive adhesive. This definition is meant to include embodiments where such polymeric phases are laminated to pressure sensitive adhesives, or where adhesives are used to make adhesive matrix-type patches with depots. These matrix patches usually consist of an adhesive layer with an impermeable backing film on the outside and a release liner on the inside, which is to be removed before use. The backing film is the polymeric phase that protects the backbone patch and prevents the delivery of drugs and / or accelerators to the external environment. The release liner acts like a backing film, but is removed as described above...

Embodiment 1-3

[0128] Examples 1-3 comprise a plurality of transdermal matrix patches containing aconitine alkaloid according to the present invention

[0129] The permeability of the embodiment.

[0130]

preparation

Composition (%, w / w)

Permeability (t=24h)

(μg / cm 2 / t) *

Adhesive / LAP

97.5 / 2.5

3.7±2.6

Adhesive / LAP / SMO

87.5 / 2.5 / 10

8.2±4.6

Adhesive / LAP / L-DEA

87.5 / 2.5 / 10

47.9±18.0

Adhesives / LAP / GMO / LA

87.5 / 2.5 / 10

7.9±4.1

Adhesive / LAP / oleic acid

87.5 / 2.5 / 10

14.9±7.4

[0131] Adhesive: pressure-sensitive acrylic copolymer; LAP: homogenate

[0132] SMO: sorbitan monooleate;

[0133] L-DEA: Lauramide DEA

[0134] GMO / LA: Glyceryl Monooleate / Lauryl Alcohol

[0135] * (mean ± SD), n = 3 skin donors, 12 diffusion tanks

[0136] The above results clearly show that application of a penetration enhancer can significantly increase the sk...

Embodiment 2

[0138] Formulation Two (1)

[0139] * A single Eudragit and a mixture of different levels of Eudragit. Eudragit can be selected from: NE30D, L100, L12 / 5, S100, S12 / 5, L30D-55, E100, E12 / 5, RL100, RL12 / 5, R100, RLPO, PLPM, RL30D, RS100, RS12 / 5, RSPM , RSPO, RS30D, etc. Example 3

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Abstract

The present invention provides a composition of transdermally administered aconitine alkaloids for ameliorating pain and inflammation. In one aspect, an aconitine alkaloid is delivered in a sufficient amount to achieve and maintian a blood plasma aconitine alkaloid level of about 0.5 ng / mL to about 400 ng / mL. Aconitine alkaloids may be delivered by themselves, or in combination with other elements, such as additional analgesics, other drugs, or positive health promoting substances. Various formulations for the transdermal delivery of aconitine alkaloids are disclosed, and may include selected penetration enhancers.

Description

technical field [0001] The present invention generally relates to compositions and methods capable of ameliorating pain and inflammation. More particularly, the present invention relates to compositions for improving pain and inflammation containing alkaloid compounds extracted from plants of the genus Aconitum. Background of the invention [0002] Everyone has experienced pain of one kind or another in their life. Pain and inflammation accompany most diseases and physical injuries. Pain can be sharp, dull, intermittent, or chronic. Because pain is something people don't want to encounter, people are always exploring various treatments. Research and search for analgesics and anti-inflammatory agents with maximum efficacy and minimum side effects (such as drug dependence) are still ongoing until now. [0003] Among various types of pain, chronic pain caused by malignant and inflammatory diseases is unbearable due to its persistence. Many diseases such as cancer and arthr...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K9/70A61K31/435A61K31/439A61K45/06
CPCA61K9/7069A61K9/7053A61K9/7061A61K9/06A61K31/439A61K31/435A61K45/06A61P25/04A61P29/00A61K31/00A61K2300/00
Inventor 熊伟弘狄奈希·C·帕泰尔
Owner 美国爱科赛尔制药有限公司
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