US4719239A — Pharmaceutical multicomponent systems and method …

Claim 1

Independent Claim 159 words

A multicomponent system for pharmaceutical use comprising: at least one pharmaceutically active agent, 0 to 70% by weight of at least one oil component, 2 to 60% by weight of at least one physiologically acceptable surfactant selected from the group consisting of nonionic surfactants with an HLB value higher than 8 and amphoteric surfactants, and 0 to 78% by weight of at least one cosurfactant selected from the group consisting of partial esters and ethers of polyhydric alcohols with saturated or unsaturated fatty acids and fatty alcohols with 6 to 22 C-atoms said at least one cosurfactant being liquid below 40° C., wherein the individual components are present in such quantities in said system that at room temperature stable, liquid, single-phase systems are formed, which contain said at least one pharmaceutically active agent in dissolved form, and wherein the sum of said at least one oil component and said at least one cosurfactant is at least 10% by weight.

Claim 2

Dependent Claim 159 words

A multicomponent system for pharmaceutical use comprising: at least one pharmaceutically active agent, 0 to 70% by weight of at least one oil component, 2 to 60% by weight of at least one physiologically acceptable surfactant selected from the group consisting of nonionic surfactants with an HLB value higher than 8 and amphoteric surfactants, and 0 to 78% by weight of at least one cosurfactant selected from the group consisting of partial esters and ethers of polyhydric alcohols with saturated or unsaturated fatty acids and fatty alcohols with 6 to 22 C-atoms said at least one cosurfactant being liquid below 40° C., wherein the individual components are present in such quantities in said system that at room temperature stable, liquid, single-phase systems are formed, which contain said at least one pharmaceutically active agent in dissolved form, and wherein the sum of said at least one oil component and said at least one cosurfactant is at least 10% by weight.

Claim 3

Dependent Claim 49 words

A multicomponent system according to claim 1, wherein said at least one surfactant is selected from the group consisting of ethoxylated glycerol partial esters and ethers with aliphatic carboxylic acids and alcohols with 2 to 22 C-atoms and with more than 7 and up to 40 ethylene oxide units.

Claim 4

Dependent Claim 43 words

A multicomponent system according to claim 1, wherein said at least one surfactant is selected from the group consisting of polyethylene glycol esters and ethers with aliphatic carboxylic acids with 6 to 22 C-atoms and with aliphatic alcohols with 6 to 22 C-atoms.

Claim 5

Dependent Claim 30 words

A multicomponent system according to claim 1, wherein said at least one surfactant is selected from the group consisting of ethoxylated cyclopentano-perhydrophenanthrene derivatives with 5 to 50 ethylene oxide units.

Claim 6

Dependent Claim 22 words

A multicomponent system according to claim 1, wherein said at least one surfactant is selected from the group consisting of polyoxyethylene/polyoxypropylene copolymers.

Claim 7

Dependent Claim 29 words

A multicomponent system according to claim 1, wherein said at least one surfactant is selected from the group consisting of acid-amidoalkyl-betaines with (C 2 -C 22 ) fatty acids.

Claim 8

Dependent Claim 38 words

A multicomponent system according to claim 1, wherein said at least one cosurfactant is selected from the group consisting of partial esters and ethers of polyhydric alcohols with saturated fatty acids and alcohols with 8 to 10 C-atoms.

Claim 9

Dependent Claim 36 words

A multicomponent system according to claim 1, wherein said at least one cosurfactant is selected from the group consisting of glycerol partial esters and ethers with fatty acids and fatty alcohols with 8 to 10 C-atoms.

Claim 10

Dependent Claim 33 words

A multicomponent system according to claim 1, wherein said at least one cosurfactant is selected from the group consisting of caprylic and capric acid glycerol esters, and mixed capric-caprylic acid glycerol partial esters.

Claim 11

Dependent Claim 45 words

A multicomponent system according to claim 1, wherein said at least one surfactant is selected from the group consisting of PEG (20 EO)-oleic acid glycerol partial esters, and said at least one cosurfactant is selected from the group consisting of capric-caprylic acid glycerol partial esters.

Claim 12

Dependent Claim 85 words

A multicomponent system according to claim 1, wherein said at least one oil component is selected from the group consisting of oleyl alcohol and polar esters of monohydric alcohols with 2 to 4 C-atoms with fatty acids having 8 to 12 C-atoms and, said at least one surfactant is selected from the group consisting of low molecular weight polyoxyethylene/polyoxy propylene copolymers with a PEG proportion of 20 to 50% by weight, based on the copolymer, and a propylene fraction molecular weight of 600 to 1400.

Claim 13

Dependent Claim 24 words

A multicomponent system as in claim 11 wherein said at least one oil component serves as said at least one cosurfactant in said system.

Claim 14

Dependent Claim 25 words

A multicomponent system according to claim 1, further comprising at least one member from the group consisting of water and at least one hydrophilic component.

Claim 15

Dependent Claim 34 words

A multicomponent system according to claim 13, wherein said at least one hydrophilic component is selected from the group consisting of an aliphatic monohydric or polyhydric C 2 -C 4 -alcohol, urea and water.

Claim 16

Dependent Claim 17 words

A multicomponent system according to claim 1, further comprising from 1 to 85% by weight of water.

Claim 17

Dependent Claim 16 words

A multicomponent system according to claim 1, further comprising 35 to 95% by weight of water.

Claim 18

Dependent Claim 30 words

A multicomponent system according to claim 1 for use in preparations of pharmaceutical formulations for cutaneous, peroral, parenteral, vaginal or rectal administration, as well as inhalations, balneotherapeutics and cosmetic products.

Claim 19

Dependent Claim 27 words

A multicomponent system according to claim 17, wherein said system is an anhydrous system for use under occlusive conditions for the transdermal application of lipophilic active agents.

Claim 20

Dependent Claim 27 words

A multicomponent system according to claim 17, wherein said system is an aqueous system for application in open form for the transdermal application of hydrophilic active agents.

Claim 21

Dependent Claim 19 words

A multicomponent system according to claim 17, wherein said system is an aqueous system used for local cutaneous application.

Claim 22

Dependent Claim 81 words

A multicomponent system according to claim 1 wherein said at least one surfactant is physiologically acceptable, and is selected from the group consisting of nonionic surfactants with an HLB value higher than 8, and amphoteric surfactants, and wherein at least one compound selected from the group consisting of oleyl alcohol and polar esters of monohydric alcohols with 2 to 4 C-atoms with 8 to 18 C-atoms, function(s) as both said at least one oil component and said at least one cosurfactant.

Claim 23

Dependent Claim 25 words

A multicomponent system according to claim 21 wherein said at least one surfactant is selected from the group consisting of low molecular weight polyoxyethylene/polyoxypropylene copolymers.

Claim 24

Dependent Claim 168 words

A multicomponent system for pharmaceutical use comprising 0.1-15% by weight solid or up to 65% by weight liquid of at least one pharmaceutically active agent, up to 85% weight of at least one oil component, 0-50% by weight of at least one physiologically acceptable surfactant selected from the group consisting of nonionic surfactants with an HLB value higher than 8 and amphoteric surfactants, and up to 80% by weight of at least one cosurfactant selected from the group consisting of partial esters and ethers of polyhydric alcohols with saturated or unsaturated fatty acids and fatty alcohols with 6 to 22 C-atoms said at least one cosurfactant being liquid below 40° C., and wherein the sum of said at least one cosurfactant and said at least one oil component is at least 2.5% by weight, and the individual components are present in such quantities in said system that at room temperature stable, liquid, single-phase systems are formed, which contain said at least one pharmaceutically active agent in dissolved form.

Claim 25

Dependent Claim 168 words

A multicomponent system for pharmaceutical use comprising 0.1-15% by weight solid or up to 65% by weight liquid of at least one pharmaceutically active agent, up to 85% weight of at least one oil component, 0-50% by weight of at least one physiologically acceptable surfactant selected from the group consisting of nonionic surfactants with an HLB value higher than 8 and amphoteric surfactants, and up to 80% by weight of at least one cosurfactant selected from the group consisting of partial esters and ethers of polyhydric alcohols with saturated or unsaturated fatty acids and fatty alcohols with 6 to 22 C-atoms said at least one cosurfactant being liquid below 40° C., and wherein the sum of said at least one cosurfactant and said at least one oil component is at least 2.5% by weight, and the individual components are present in such quantities in said system that at room temperature stable, liquid, single-phase systems are formed, which contain said at least one pharmaceutically active agent in dissolved form.

Claim 26

Dependent Claim 182 words

Process for the preparation of a multicomponent system for pharmaceutical use comprising: at least one pharmaceutically active agent, 0 to 70% by weight of at least one oil component, 2 to 60% by weight of at least one physiologically acceptable surfactant selected from the group consisting of nonionic surfactants with an HLB value higher than 8 and amphoteric surfactants, and 0 to 78% by weight of at least one cosurfactant selected from the group consisting of partial esters and ethers of polyhydric alcohols with saturated or unsaturated fatty acids and fatty alcohols with 6 to 22 C-atoms, said at least one cosurfactant being liquid below 40° C., wherein the individual components are present in such quantities in said system that at room temperature stable, liquid, single-phase systems are formed, which contain said at least one pharmaceutically active agent in dissolved form, said process comprising the steps of: intermixing said at least one surfactant, said at least one cosurfactant, and said at least one oil component, and subsequently, dissolving said at least one pharmaceutically active agent in the mixture, and then adding water.

Claim 27

Dependent Claim 182 words

Process for the preparation of a multicomponent system for pharmaceutical use comprising: at least one pharmaceutically active agent, 0 to 70% by weight of at least one oil component, 2 to 60% by weight of at least one physiologically acceptable surfactant selected from the group consisting of nonionic surfactants with an HLB value higher than 8 and amphoteric surfactants, and 0 to 78% by weight of at least one cosurfactant selected from the group consisting of partial esters and ethers of polyhydric alcohols with saturated or unsaturated fatty acids and fatty alcohols with 6 to 22 C-atoms, said at least one cosurfactant being liquid below 40° C., wherein the individual components are present in such quantities in said system that at room temperature stable, liquid, single-phase systems are formed, which contain said at least one pharmaceutically active agent in dissolved form, said process comprising the steps of: intermixing said at least one surfactant, said at least one cosurfactant, and said at least one oil component, and subsequently, dissolving said at least one pharmaceutically active agent in the mixture, and then adding water.

Claim 28

Dependent Claim 28 words

A process as in claim 24 wherein said dissolving step comprises the step of dissolving said at least one pharmaceutically active agent, accompanied by heating, in the mixture.

Annuity Stage	Window Opens	Payment Deadline	Surcharge Period Until	Estimated Fee	Status
3.5 Years (Year 4)	1991-01-11	1991-07-13	1992-01-12	$2000.00	Window Closed / Lapsed
7.5 Years (Year 8)	1995-01-11	1995-07-13	1996-01-12	$3760.00	Window Closed / Lapsed
11.5 Years (Year 12)	1999-01-11	1999-07-13	2000-01-12	$7700.00	Window Closed / Lapsed

Pharmaceutical multicomponent systems and method of preparing same

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