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Topital delivery system for active agents

A substance and composition technology, applied in the direction of organic active ingredients, drug combination, drug delivery, etc., can solve the problems of irritation, dry skin, etc., achieve the effects of less skin irritation, lighten skin pigmentation, and avoid signs of aging

Inactive Publication Date: 2001-07-11
JOHNSON & JOHNSON CONSUMER PROD INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these alcohols absorb lipids from the surface of the skin, causing excessive dryness and irritation

Method used

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  • Topital delivery system for active agents
  • Topital delivery system for active agents
  • Topital delivery system for active agents

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0159] Example 1: Preparation of 2% Minoxidil in Propylene Glycol, Ethanol and Water with or without Alpha Hydroxy Acid and Sodium Sulfate

[0160] Contain 4ml propylene glycol in the beaker, 12ml ethanol and 4ml water, under normal temperature and pressure, stir and add 0.4g minoxidil (U.S.P. / N.F., purchased from Spectrm Quality Products, Inc., Gardena, CA) wherein, generate 2% ( wt / v) minoxidil formulation. The preparation is the same as "ROGAINE" purchased from Upjohn TM "same.

[0161] To prepare an alpha hydroxy acid-containing formulation (for Example 12), 360 µl of DL-lactic acid was added to the above ROGAINE-type formulation at normal temperature and pressure.

[0162]To prepare the formulation containing α-hydroxy acid and sodium sulfate (for Example 12), add 0.626 g of sodium sulfate to the above-mentioned formulation containing α-hydroxy acid at normal temperature and pressure.

Embodiment 2

[0163] Embodiment 2: preparation contains the polyoxyethylene-10 stearyl ether of 2% minoxidil

[0164] In a beaker, melt 0.5g of polyoxyethylene-10 stearyl ether (purchased from ICI Surfactants, Wilmington, DE, trade name "BRIJ 76") at 50°C, and add 10ml of the minoxidil-containing product prepared in Example 1 to it. The formulation of minoxidil was stirred until the mixture was down to normal temperature to generate a formulation containing 2% (wt / v) minoxidil and 5% nonionic lipid.

Embodiment 3

[0165] Embodiment 3: preparation contains the three non-ionic lipid formulations of 2% minoxidil

[0166] 50°C, in a beaker, 0.225g glycerol dilaurate (Van Dyk & Company, Inc., Belleville, NJ, trade name "Emulsynt GDL"), 0.075g cholesterol (Croda, Inc., New York, NY, Trade name "Cholesterol NF") and 0.2 g of polyoxyethylene-10 stearyl ether in Example 2 were mixed until a homogeneous 45:15:40 (wt%) molten nonionic lipid mixture was obtained.

[0167] The minoxidil-containing preparation prepared by 10ml embodiment 1 is added in the nonionic lipid mixture obtained above 0.5, stirred until the mixture is down to normal temperature, and a mixture containing 2% (wt / v) minoxidil and 5% minoxidil is generated. Preparation of nonionic lipids.

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PUM

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Abstract

This invention relates to a method for enhancing the transmembrane penetration of benefit agents using a certain non-ionic lipid / surfactant-containing formulation as an enhancing agent, and the compositions used therein. Various active agents, such as anti-dandruff agents, hair growth agents, hair inhibitor agents, anti-acne agents, anti-aging agents, depilatory agents, and depigmentation agents, may be effectively delivered into the skin, hair follicles and sebaceous glands using the compositions of the present invention.

Description

[0001] related application [0002] This application is based on US Application 60 / 095,289 filed August 4, 1998, which application is incorporated herein in its entirety. field of invention [0003] The present invention relates to methods and compositions for the surface delivery of active substances such as drugs. More specifically, the present invention relates to methods for enhancing the transmembrane penetration of beneficial substances using nonionic lipid / surfactant-containing formulations as enhancers, and to the compositions used. Background of the invention [0004] Surface delivery of an active substance such as a drug in a carrier is a multi-step process involving: 1) dissolution, diffusion, or release of the substance from the carrier; 2) transfer of the substance to the site of absorption; 3) penetration of the substance through a restrictive barrier at the target site osmosis; and finally 4) the substance is eliminated by the blood circulation. In order for...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K8/00A61K8/02A61K8/06A61K8/14A61K8/19A61K8/20A61K8/23A61K8/30A61K8/33A61K8/34A61K8/35A61K8/36A61K8/362A61K8/365A61K8/368A61K8/37A61K8/39A61K8/42A61K8/44A61K8/49A61K8/58A61K8/60A61K8/63A61K8/64A61K8/67A61K8/72A61K8/73A61K8/86A61K8/90A61K8/92A61K8/97A61K31/505A61K31/74A61K47/10A61K47/14A61K47/28A61K47/34A61K47/44A61Q5/00A61Q5/02A61Q7/00A61Q7/02A61Q19/00A61Q19/02A61Q19/08A61Q19/10
CPCA61K8/602A61K8/678A61K8/63A61K8/19A61K8/90A61K8/365A61Q5/006A61Q19/08A61K8/92A61K8/49Y10S514/946A61K8/731A61K8/355A61K8/4946A61Q19/02A61K8/368A61K8/34A61K8/375A61Q19/10A61K8/671Y10S514/947A61K8/37A61K8/4953A61K8/42A61Q7/02A61Q19/00A61K8/0291A61Q7/00A61K8/345A61K8/86A61P17/10A61P17/14
Inventor S·M·尼米克J·C·T·王S·J·维希涅夫斯基K·S·斯藤陆光伟
Owner JOHNSON & JOHNSON CONSUMER PROD INC
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