Topical antimicrobial pharmaceutical compositions and methods

• US 5,208,257 A
• Filed: 06/23/1992
• Issued: 05/04/1993
• Est. Priority Date: 04/21/1986
• Status: Expired due to Term

• Current Assignee: Jon J. Kabara
• Original Assignee: Jon J. Kabara
• Inventors: Kabara, Jon J.
• Primary Examiner(s): Schenkman, Leonard
• Application Number:
  US07/902,767
• Time in Patent Office: 315 Days
• Field of Search: 514/552, 514/558
• US Class Current: 514/552
• CPC Class Codes: A01N 37/12 containing the group , wherein Cn means a carbon skeleton not containing a ring; Thio analogues thereof
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/20 having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
• CPC Class Codes: A61K 31/23 of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• CPC Class Codes: A61K 31/25 with polyoxyalkylated alcohols, e.g. esters of polyethylene glycol

Abstract

The present invention discloses a topical antimicrobial and anti-parasite pharmaceutical composition and methods of using the same. The topical antimicrobial pharmaceutical composition includes a safe and effective amount of an ethoxylated or propoxylated glycerol fatty acid ester and a pharmaceutically acceptable carrier. Also disclosed is a topical antimicrobial pharmaceutical composition including a safe and effective amount of a tertiary mixture including, a glycerol fatty acid ester, a binary mixture of fatty acids including a first fatty acid antimicrobial agent selected from C₆ to C₁₈ fatty acids, and a second fatty acid antimicrobial agent selected from C₆ to C₁₈ fatty acids, and a pharmaceutically acceptable carrier. Further disclosed is a topical antimicrobial pharmaceutical composition including a safe and effective amount of an ethoxylated or propoxylated glycerol fatty acid ester, a binary fatty acid mixture including, a first fatty acid antimicrobial agent selected from C₆ to C₁₈ fatty acid and the second fatty acid antimicrobial agent selected from C₆ to C₁₈ fatty acids, where the second fatty acid is not the same as the first fatty acid, and a pharmaceutically acceptable carrier. Further disclosed is a method of treating and preventing microbial related skin conditions in humans or lower animals comprising topically applying, to the afflicted situs of a human of lower animal in need of such treatment, a safe and effective amount of the above composition.

Claims

1. A topical antimicrobial or antiparasitic pharmaceutical composition comprising a safe and effective amount of a mixture comprising:

(a) a glycerol monoester of lauric acid present in an amount of about 0.05 to about 2.0 percent by weight of the composition;

(b) a binary mixture of fatty acids comprising;

(i) a first fatty acid comprising capric acid, and

(ii) a second fatty acid comprising caprylic acid;

wherein (a) and (b) are present at a level such that the weight;

weight ratio of (a);

(b) is about 10;

1 to 1;

10, and wherein (i) and (ii) are present in a weight;

weight ratio of about 1;

10 to about 10;

1 and said binary mixture is present in an amount of about 0.5 to about 8.0 percent by weight of the composition;

(c) a pharmaceutically-acceptable carrier which includes lactic acid; and

(d) a surfactant which comprises a block copolymer of propylene oxide and ethylene oxide.

2. A topical pharmaceutical composition according to claim 1 wherein said monoester is present at a level of about 0.1 to about 1 percent of the composition.

3. A topical pharmaceutical composition according to claim 1 wherein said monoester is present at a level of about 1 percent of the composition.

4. A topical pharmaceutical composition according to claim 1 wherein said carrier additionally comprises at least one additional carrier component selected from the group consisting of alcohols, parabens, phenols, water, and mixtures thereof.

5. A method of treating and preventing microbial-, viral-, or parasite-related skin conditions in humans or lower animals comprising topically applying to the afflicted situs of a human or lower animal in need of such treatment a safe and effective amount of a composition according to claim 4.

6. A topical pharmaceutical composition according to claim 1 wherein the pharmaceutical carrier additionally comprises an alcohol selected from the group consisting of propylene glycol, phenoxyethanol, methanol, ethanol, isopropyl alcohol, and mixture thereof.

7. A topical pharmaceutical composition according to claim 6 wherein said alcohol or alcohols are present in an amount of about 5 percent to about 60 percent by volume.

8. A topical pharmaceutical composition according to claim 1 wherein a second chelating agent is present and is selected from the group consisting of polyphosphoric acid and its salts, EDTA, EDTA(Na)₂, EDTA(Na)₄, citric acid and its salts, and mixtures thereof.

9. A topical pharmaceutical composition according to claim 1 wherein the surfactant is selected from the group consisting of dioctyl sodium sulfosuccinate, sarcosinates, amine oxides, Pluronics, sodium lauryl sulfate and mixtures thereof.

10. A topical pharmaceutical composition according to claim 1 wherein the pharmaceutical carrier additionally comprises a paraben selected from the group consisting of methyl parabens, propyl parabens, BHA, BHT, and mixtures thereof.

11. A topical pharmaceutical composition according to claim 10 wherein said phenols or parabens are present in an amount of about 0.05 percent to 0.5 percent by weight.

12. A topical pharmaceutical composition according to claim 1 wherein the surfactant is present at a level of about 0.25 percent to about 20 percent by weight.

13. A topical pharmaceutical composition according to claim 1 wherein a chelating agent is present in an amount of about 0.05 percent to about 7.5 percent by weight.

14. The topical pharmaceutical composition according to claim 1 wherein said monoester is monolaurin.

15. The topical pharmaceutical composition according to claim 1 wherein the glyceryl ester has been ethoxylated or propoxylated at a level of at least about 0.25 to about 5 moles of ethoxylate or propoxylate per mole of glyceryl ester.

16. A method of treating and preventing microbial-, viral- or parasite-related skin conditions in humans or lower animals comprising topically applying to the afflicted situs of a human or lower animal in need of such treatment a safe and effective amount of a composition according to claim 1.

17. A method of treating and preventing mastitis in an animal in need of such treatment or prevention comprising applying a composite according to claim 1 to at least one test of said animal.

18. A topical antimicrobial or antiparasitic pharmaceutical composition comprising a safe and effective amount of a mixture comprising:

(a) a polyhydric alcohol monoester of lauric acid present in an amount of about 0.05 to about 2.0 percent by weight of the composition;

(b) a binary mixture of fatty acids comprising;

(i) a first fatty acid comprising capric acid, and

(ii) a second fatty acid comprising caprylic acid;

wherein (i) and (ii) are present in weight;

weight ratio of about 1;

10 to about 10;

1 and said binary mixture present in an amount of about 0.5 to about 8.0 percent by weight of the composition;

(c) a pharmaceutically-acceptable carrier which includes a chelating agent; and

(d) a surfactant which comprises a block copolymer of propylene oxide and ethylene oxide and which is present at a level of about 0.25 to about 10% by weight.