Lanoline derivatives as penetration enhancing substances

Details Lanoline derivatives as penetration enhancing substances Lanoline derivatives as penetration enhancing substances

1993-11-12

1996-02-20

Phelan, D. Gabrielle

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Web, sheet or filament bases; compositions of bandages; or...

514946, 514947, A61F 1300

Patent

active

054926980

DESCRIPTION:

BRIEF SUMMARY
The invention relates to lanoline derivatives on their own or in a mixture with polyethyleneglycol ethers of fatty alcohols with longer chains as penetration enhancing substances in formulations containing pharmaceutical substances or other biologically active substances.
Transdermal application offers a series of advantages for a multitude of pharmaceutical substances or other biologically active substances: application, is avoided, resulting in negligible secondary action therapeutic index, is guaranteed.
Some pharmaceutical substances which, owing to their high "first-pass" effect, their low dosage and their high effective potential, would otherwise be regarded as ideal, possess, in many cases, such a low skin permeation that it is not possible to obtain therapeutic plasma values. In the case of all these pharmaceutical substances it is necessary to add so-called penetration enhancers to the system. Along these lines a multiplicity of substances is described, listed in the following Patent Spefications: U.S. Pat. No. 4,130,643, U.S. Pat. No. 4,405,616, U.S. Pat. No. 4,335,115, U.S. Pat. No. 4,130,667, U.S. Pat. No. 3,903,256, U.S. Pat. No. 4,379,454, U.S. Pat. No. 3,527,864, U.S. Pat. No. 3,952 099, U.S. Pat. No. 3,896 238, U.S. Pat. No. 3 472 931.
In Addition to being able to fulfil their specific function, penetration enhancing substances must possess the following properties: even when they remain on the skin for a long time, at occlusive conditions, they must be tolerated by the skin, must not produce any allergies and must be compatible with the active substances involved.
The enhancers known from the literature can be assigned to various chemical classes: azacycloalkanone) N,N-diethyl-m-toluamide monolaurate, diethyl sebacate, propylene glycol esters of saturated fatty acids
The existence of such a multitude of different substances of all possible chemical structures, all said to possess a penetration enhancing effect, makes a single working mechanism seem unlikely. Various thereof are, therefore, under discussion. mechanisms or combinations thereof are, therefore, under discussion. lipides.
Bearing in mind both the multitude of interactions taking place within the skin and the varying chemical qualities manifested by the active substances concerned, the penetration enhancing properties of all these so-called enhancers in relation to one active substance can only be predicted with difficulty.
From previous experience it can be said that a penetration enhancing substance or a certain mixture only very rarely comply with the characteristics required by several pharmaceutical substances or pharmaceutical substance groups.
From JP-A-61024517 a transdermal therapeutic system for diseases of circulatory organs is known, comprising a plaster with an adhesive layer, a penetration enhancing substance, as well as a beta blocker as active substance. Isopropyl myristate and/or isopropyl lanolate are employed as penetration enhancers. The advantage of this system is said to be a long-lasting administration of the beta-blocking agent, without irritation of the skin occurring. The active substance reaches the blood circulation directly without passing the liver, which means that harmful side effects are avoided. For production of the system, the penetration enhancing substance is incorporated into the adhesive layer, which layer contains the beta blocker as active substance.
From FR-A-21 32 130 cosmetic formulation such as sun creams, facial, body or hand creams are known, in particular, as moisturizers. These are emulsions of the "water in oil" type. To stabilize these emulsions, mixtures of lanolates, such as magnesium lanolate, calcium, lithium, zink and aluminium lanolate are used. It is the object of the formulation to achieve improved hydration of the epidermis and improved protection thereof. According to example 1, one formulation, for example, contains magnesium lanolate, alcohol of lanoline, isopropyl palmitate, paraffine oil, almond oil, ozokerit, water and parahydroxybenzoate of methyl. The use of po

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