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

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

Example Embodiment

[0159] Example 1: Preparation of propylene glycol, ethanol and water formulations containing 2% minoxidil, which contains or does not contain alpha hydroxy acid and sodium sulfate

[0160] The beaker contains 4ml of propylene glycol, 12ml of ethanol and 4ml of water. Under normal temperature and pressure, 0.4g of minoxidil (USP / NF, purchased from Spectrm Quality Products, Inc., Gardena, CA) is added with stirring to produce 2% ( wt / v) Minoxidil formulation. The preparation is incompatible with the "ROGAINE" purchased from Upjohn TM "the same.

[0161] To prepare a preparation containing α-hydroxy acid (used in Example 12), 360 μl of DL-lactic acid was added to the above-mentioned ROGAINE-type preparation under normal temperature and pressure.

[0162]To prepare a preparation containing alpha hydroxy acid and sodium sulfate (used in Example 12), 0.626 g of sodium sulfate was added to the aforementioned preparation containing alpha hydroxy acid under normal temperature and pressure....

Example Embodiment

[0163] Example 2: Preparation of polyoxyethylene-10 stearyl ether containing 2% minoxidil

[0164] In a beaker, melt 0.5 g of polyoxyethylene-10 stearyl ether (available from ICI Surfactants, Wilmington, DE, trade name "BRIJ 76") at 50°C, and add 10 ml of the Minoxidil prepared in Example 1 to it Stir until the mixture is cooled to room temperature to produce a preparation containing 2% (wt / v) minoxidil and 5% non-ionic lipid.

Example Embodiment

[0165] Example 3: Preparation of a tri-nonionic lipid preparation containing 2% minoxidil

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

[0167] Add 10 ml of the minoxidil preparation prepared in Example 1 to the nonionic lipid mixture obtained above 0.5, and stir until the mixture drops to room temperature to produce 2% (wt / v) minoxidil and 5% Preparation of non-ionic 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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