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Hydroxide-releasing agents as skin permeation enhancers

a technology of hydroxide-releasing agents and skin permeation enhancers, which is applied in the direction of inorganic non-active ingredients, peptide/protein ingredients, drug compositions, etc., to achieve the effect of enhancing the rate of an active agen

Inactive Publication Date: 2006-05-04
LUO ERIC C +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0008] It is thus a primary object of the invention to address the above-described need in the art by providing a novel method for enhancing the rate at which an active agent administered to a patient's body surface permeates into and / or through the body surface.
[0010] It is still another object of the invention to provide such a method wherein the amount of hydroxide-releasing agent employed is optimized to enhance permeation while minimizing or eliminating the possibility of skin damage, irritation or sensitization.

Problems solved by technology

However, it is the cells of the stratum corneum which present the primary barrier to absorption of topical compositions or transdermally administered drugs.

Method used

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  • Hydroxide-releasing agents as skin permeation enhancers
  • Hydroxide-releasing agents as skin permeation enhancers
  • Hydroxide-releasing agents as skin permeation enhancers

Examples

Experimental program
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Effect test

example 1

[0153] An in vitro skin permeation study was conducted using three estradiol transdermal systems. The formulations used to prepare these systems are listed in Table 1, which includes weight and weight percent of each component of the formulations. The weight of sodium hydroxide was 0 g, 0.0155 g, and 0.025 g for formulation #Est-P18, #Est-P19 and #Est-P20 respectively. Each formulation was coated onto a release liner and dried in an oven at 55° C. for two hours to remove water and other solvents. The dried drug-in-adhesive / release liner film was laminated to a backing film. The backing / drug-in-adhesive / release liner laminate was then cut into discs with a diameter of 11 / 16 inch. The theoretical percent weight for each ingredient after drying (calculated assuming all volatile ingredients were completely removed during drying) is set forth in Table 2.

[0154] The in vitro permeation of estradiol through human cadaver skin from these discs was performed using Franz-type diffusion cells ...

example 2

[0159] An in vitro skin permeation study was conducted using four ketoprofen transdermal systems. The formulations used to prepare these systems are listed in Table 4, which includes weight and weight percent of each component of the formulations. The weight of sodium hydroxide was 0 g, 0.19 g, 0.215 g, and 0.225 g for formulation #Keto-P3H16, -P3H17, P3H18, and -P3H19, respectively. Each formulation was coated on a release liner and dried in an oven at 55° C. for two hours to remove water and other solvents. The dried drug-in-adhesive / release liner film was laminated to a backing film. The backing / drug-in-adhesive / release liner laminate was then cut into discs with a diameter of 11 / 16 inch. The theoretical percent weight for each ingredient after drying (calculated assuming all volatile ingredients were completely removed during drying) is set forth in Table 5.

[0160] The in vitro permeation of ketoprofen through human cadaver skin from these discs was performed using Franz diffusi...

example 3

[0167] An in vitro skin permeation study was conducted using four phenylpropanolamine hydrochloride (PPA-HCl) transdermal systems. The formulations used to prepare these systems are listed in Table 7, which includes weight and weight percent of each component in the formulations. The weight of sodium hydroxide was 0 g, 0.165 g, 0.195 g, and 0.23 g for formulation #PPA-N7, -N1, -N2, -and -N5, respectively. Each formulation was coated onto a release liner and dried in an oven at 55° C. for two hours to remove water and other solvents. The dried drug-in-adhesive / release liner film was laminated to a backing film. The backing / drug-in-adhesive / release liner laminate was then cut into round discs with a diameter of 11 / 16 inch. The theoretical percent weight for each component after drying (calculated assuming all the volatile ingredients were completely removed during drying) is listed in Table 8.

[0168] The in vitro permeation of PPA-HCl through human cadaver skin from these discs was pe...

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Abstract

A method is provided for increasing the permeability of skin or mucosal tissue to topically or transdermally administered pharmacologically or cosmeceutically active agents. The method involves use of a specified amount of a hydroxide-releasing agent, the amount optimized to increase the flux of the active agent through a body surface while minimizing the likelihood of skin damage, irritation or sensitization. Topically applied formulations and drug delivery devices employing hydroxide-releasing agents as permeation enhancers are provided as well.

Description

CROSS REFERENCE TO RELATED APPLICATIONS [0001] This is a divisional application of U.S. Ser. No. 09 / 738,410, filed Dec. 14, 2000; which is a continuation-in-part of U.S. Ser. No. 09 / 569,889, filed May 11, 2000, now abandoned; which is a continuation-in part of U.S. Ser. No. 09 / 465,098, filed Dec. 16, 1999, now abandoned; the disclosures of which are incorporated by reference.TECHNICAL FIELD [0002] This invention relates generally to the topical and transdermal administration of pharmacologically active agents, and more particularly relates to methods and compositions for enhancing the permeability of skin or mucosal tissue to topically applied pharmacologically active agents. BACKGROUND ART [0003] The delivery of drugs through the skin provides many advantages; primarily, such a means of delivery is a comfortable, convenient and noninvasive way of administering drugs. The variable rates of absorption and metabolism encountered in oral treatment are avoided, and other inherent inconv...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/70A61K9/00A61K31/137A61K47/02
CPCA61K9/0014A61K9/7023A61K9/7038A61K9/7053A61K31/137A61K47/02Y10S514/947A61K9/703A61K38/09A61K31/568A61K31/192A61K31/196A61K31/216A61K31/565A61K38/28A61K38/095A61K2300/00
Inventor LUO, ERIC C.JACOBSON, ERIC C.HSU, TSUNG-MIN
Owner LUO ERIC C
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