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Claims for Patent: 3,966,949

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Claims for Patent: 3,966,949

Title: Pharmaceutical compositions and preparing same
Abstract:Water-insoluble therapeutic agents having a tertiary nitrogen capable of being protonated are stabilized and solubilized via the formation of water-soluble lipophilic liquid fatty acid salts.
Inventor(s): Webb, Jr.; Norval Ellsworth (Cincinnati, OH)
Assignee: Richardson-Merrell Inc. (Wilton, CT)
Application Number:05/406,013
Patent Claims: 1. A method of preparing a stabilized aqueous parenteral composition of a water-insoluble therapeutic agent containing a tertiary amine capable of being protonated which comprises reacting said therapeutic agent with at least a stabilizing amount of a lipophilic liquid fatty acid having from 14 to 24 carbon atoms to form a lipophilic, fatty acid liquid salt; incorporating a nonionic surfactant with said liquid salt; and incorporating water to effect a solution suitable for injection.

2. A pharmaceutical composition which forms a clear solution when added to water, prepared by treating a water-insoluble therapeutic agent containing a tertiary amine capable of being protonated, with a lipophilic fatty acid which is liquid at room temperature and contains from 14 to 24 carbon atoms in a weight to weight ratio of about one part of said therapeutic agent to one part of said fatty acid and not more than one part of said therapeutic agent to two parts of said fatty acid, to form a homogenous, monophasic oil; and incorporating a nonionic surfactant in an amount sufficient to solubilize said oil when combined with an aqueous vehicle.

3. A composition according to claim 2 wherein the water-insoluble therapeutic agent is a compound having the formula: ##SPC6##

in which R is selected from the group consisting of methyl and chlorine.

4. A composition according to claim 2 wherein said water-insoluble therapeutic agent is .alpha.-(p-t-butylphenyl)-4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)-1-piper idinebutanol.

5. A composition according to claim 2 wherein said nonionic surfactant is selected from the group consisting of the condensation products of ethylene oxide with a hydrophobic base prepared by the condensation of propylene oxide with propylene glycol, polyoxyethylated lanolin, polyoxyethylene lanolin alcohols, sorbitan fatty acid esters and polyoxyethylated vegetable oils.

6. A composition according to claim 2 wherein the lipophilic fatty acid is oleic acid and the nonionic surfactant is a polyoxyethylated vegetable oil.

7. A pharmaceutical composition which forms a clear solution when added to water, comprising a homogenous monophasic oil formed by the reaction of a water-insoluble therapeutic agent having a tertiary amine capable of being protonated with at least a stabilizing amount of a lipophilic fatty acid which is liquid at room temperature and contains from 14 to 24 carbon atoms; a pharmaceutical carrier; and a nontoxic nonionic surfactant selected from the group consisting of the condensation products of ethylene oxide with a hydrophobic base prepared by the condensation of propylene oxide with propylene glycol, polyoxyethylated lanolin, polyoxyethylene lanolin alcohols, sorbitan fatty acid esters and polyoxyethylated vegetable oils in an amount sufficient to solubilize said oil in said carriers.

8. A pharmaceutical composition according to claim 7 wherein the water-insoluble therapeutic agent is a compound having the formula: ##SPC7##

in which R is selected from the group consisting of methyl and chlorine.

9. A pharmaceutical composition according to claim 7 wherein the water-insoluble therapeutic agent is .alpha.-(p-t-butylphenyl)-4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)-1-piper idinebutanol.

10. A pharmaceutical composition according to claim 7 wherein the lipophilic fatty acid is oleic acid and the nonionic surfactant is a polyoxyethylated vegetable oil.
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