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Penetration enhancing and irritation reducing systems

A technology that promotes penetration and reduces irritation. It is used in medical preparations with non-active ingredients, medical preparations containing active ingredients, and aerosol delivery. It can solve problems such as weakening of skin penetration ability, stimulation and side effects, and reduce skin irritation. , to promote the effect of transdermal and/or topical administration

Inactive Publication Date: 2001-02-28
思特肯有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the skin penetration of transdermal systems is compromised by their possible irritating side effects

Method used

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  • Penetration enhancing and irritation reducing systems
  • Penetration enhancing and irritation reducing systems
  • Penetration enhancing and irritation reducing systems

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] The following examples illustrate a comparison between formulations using oleic acid and oleyl alcohol as the membrane fluidizing agent.

[0044] In vitro experiments with testosterone formulations with oleic acid or oleyl alcohol as the membrane fluidizer demonstrated the same level of drug delivery. Testosterone formulations were tested and it was shown that formulations containing oleyl alcohol produced much higher skin irritation than formulations of testosterone containing oleic acid. These experiments demonstrated that switching to oleic acid as the membrane fluidizer in PES not only maintained the system's ability to facilitate topical and transdermal drug delivery, but also had the unexpected result of reducing skin irritation.

[0045] Table I lists the preparations tested, and each preparation is expressed by its composition and weight percentage. Mean testosterone efflux and erythema total scores (± standard deviation) are given for each formulation. The ab...

Embodiment 2

[0059] The following examples illustrate preferred compositions for the gel products of the present invention.

[0060] Composition Range

[0061] Ethanol 0.1-50%

[0062] Propylene glycol 0.1-50%

[0063] Isopropanol 0.1-50%

[0064] Oleic acid 0.1-50%

[0065] Gelling agent 0.01-50%

[0066] Added irritation reducer 0.1-50%

[0067] Preservative 0 (the preparation can be preserved by itself)-0.1%

[0068] Drug 0% to saturation

Embodiment 3

[0070] The following examples illustrate preferred compositions for the ointment products of the present invention.

[0071] Composition Range

[0072] Propylene glycol 0.1-50%

[0073] Butanediol 0.1-50%

[0074] Isopropyl myristate 0.1-50%

[0075] Oleic acid 0.1-50%

[0076] Mygliol 0.1-50%

[0077] Vaseline 0.1-80%

[0078] Polawax 0.1-20%

[0079] Gelling agent 0.01-50%

[0080] Added irritation reducer 0.1-50%

[0081] Preservative 0 (the preparation can be preserved by itself)-0.1%

[0082] Drug 0% to saturation

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PUM

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Abstract

This invention lies in the technology of transdermal and topical drug delivery. In particular, the present invention relates to enhancement of the penetration of transdermally or topically applied drugs and with the reduction of skin irritation that often accompanies transdermal and topical drug delivery.

Description

field of invention [0001] The present invention relates to the technology of transdermal and topical administration. In particular, the present invention relates to enhancing the penetration of transdermal or topical administration and reducing skin irritation often associated with transdermal and topical administration. background of the invention [0002] The feasibility of a transdermal route of systemic drug delivery has been established over the past decade. Transdermal therapeutic systems include those containing scopolamine, nitroglycerin, clonidine, fentanyl, nicotine, and estradiol. However, drugs applied to the skin or mucous membranes have a disadvantage in that they often cause irritation. Furthermore, many of the essential components of topical, transdermal, and transmucosal formulations and delivery devices are irritating alone or in combination, such as solubilizers, suspending agents, dispersing agents, preservatives, animal and vegetable fats, oils, and wa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/06A61K31/047A61K31/565A61K31/568A61K47/10A61K47/12A61K47/32
CPCA61K31/047A61K47/12A61K31/565A61K47/10A61K9/0014A61K9/06A61K31/568A61K2300/00A61K31/56
Inventor V·H·W·马克S·格雷森
Owner 思特肯有限公司