CARRIERS, FORMULATIONS, METHODS FOR FORMULATING UNSTABLE ACTIVE AGENTS FOR EXTERNAL APPLICATION AND USES THEREOF
First Claim
Patent Images
1. A topical tetracycline antibiotic composition comprising a foamable pharmaceutical composition and a propellant, the foamable pharmaceutical composition comprising:
- a) about 0.1% to about 10% by weight of a tetracycline antibiotic;
b) about 60% to about 95% by weight of;
at least one oily emollient;
at least one oil, wherein the oil is a liquid hydrocarbon-based oil;
ora combination of at least one oily emollient and at least one oil;
c) about 0.01% to about 15% by weight of at least one surfactant, wherein the surface active agent is an ester of a C8-C24 saturated hydrocarbon;
d) optionally 0.01% to about 10% by weight of at least one foam adjuvant, wherein the foam adjuvant is a 14C to 18C fatty alcohol; and
wherein each component is tetracycline-compatible;
wherein the composition is substantially non-aqueous;
wherein the tetracycline antibiotic is chemically stable in the foamable pharmaceutical composition when stored for 72 hours at about at least 25°
C. after mixing with the pharmaceutical composition; and
wherein the weight ratio of the foamable pharmaceutical composition to the propellant is about 100;
5 to about 100;
35.
11 Assignments
0 Petitions
Accused Products
Abstract
The present disclosure teaches unique formulations for topical administration of tetracycline antibiotics, in which the tetracycline antibiotics remain stable.
144 Citations
48 Claims
-
1. A topical tetracycline antibiotic composition comprising a foamable pharmaceutical composition and a propellant, the foamable pharmaceutical composition comprising:
-
a) about 0.1% to about 10% by weight of a tetracycline antibiotic; b) about 60% to about 95% by weight of; at least one oily emollient; at least one oil, wherein the oil is a liquid hydrocarbon-based oil;
ora combination of at least one oily emollient and at least one oil; c) about 0.01% to about 15% by weight of at least one surfactant, wherein the surface active agent is an ester of a C8-C24 saturated hydrocarbon; d) optionally 0.01% to about 10% by weight of at least one foam adjuvant, wherein the foam adjuvant is a 14C to 18C fatty alcohol; and wherein each component is tetracycline-compatible; wherein the composition is substantially non-aqueous; wherein the tetracycline antibiotic is chemically stable in the foamable pharmaceutical composition when stored for 72 hours at about at least 25°
C. after mixing with the pharmaceutical composition; andwherein the weight ratio of the foamable pharmaceutical composition to the propellant is about 100;
5 to about 100;
35. - View Dependent Claims (2, 3, 4, 5, 8, 9, 10, 11, 25, 26, 27, 28, 31, 44)
-
-
6-7. -7. (canceled)
-
12. (canceled)
-
13. A topical tetracycline antibiotic composition comprising a foamable pharmaceutical composition and a propellant, the foamable pharmaceutical composition comprising:
-
a) about 0.1% to about 10% by weight of minocycline hydrochloride; b) about 60% to about 95% by weight of; at least one emollient selected from the group consisting of PPG-15 stearyl ether, octyldodecanol, diisopropyl adipate, and Cetearyl Octanoate; at least one oil selected from the group consisting of Light mineral oil, MCT oil, Hydrogenated Castor Oil, jojoba oil, and peppermint oil;
ora combination of at least one emollient and at least one oil; c) about 0.01% to about 15% by weight of at least one surfactant selected from the group consisting of Glycerol monostearate, Sorbitan monostearate, PEG 40 Stearate, and PEG 100 Stearate; d) optionally about 0% to about 10% by weight of at least one foam adjuvant selected from the group consisting of Oleyl alcohol, Stearyl alcohol, Myristyl alcohol and Cocoglycerides; and wherein each component is minocycline-compatible; wherein the composition is substantially non-aqueous; wherein the minocycline hydrochloride is chemically stable in the foamable pharmaceutical composition when stored for 72 hours at about at least 25°
C. after mixing with the carrier or with the agent; andwherein the weight ratio of the foamable pharmaceutical composition to the propellant is about 100;
5 to about 100;
35. - View Dependent Claims (17, 45, 47)
-
-
14-16. -16. (canceled)
-
18. A topical tetracycline antibiotic composition comprising a foamable pharmaceutical composition and a propellant, the foamable pharmaceutical composition comprising either A):
-
a) about 0.1% to about 10% by weight of doxycycline hyclate; b) about 60% to about 95% by weight of; at least one emollient selected from the group consisting of PPG-15 stearyl ether, diisopropyl adipate, and Cetearyl Octanoate; at least one oil selected from the group consisting of mineral oil and MCT oil;
ora combination of at least one emollient and at least one oil; c) about 0.01% to about 15% by weight of at least one surfactant selected from the group consisting of Glycerol monostearate, Sorbitan monostearate, hydrogenated castor oil, and PEG 100 Stearate; d) optionally about 0% to about 10% by weight of at least one foam adjuvant selected from the group consisting of steryl alcohol, oleyl alcohol, isostearic acid and myrystyl alcohol; or B); a) about 0.1% to about 10% by weight of doxycycline monohydrate; b) about 60% to about 95% by weight of; at least one emollient selected from the group consisting of cetearyl octanoate, PPG-15 stearyl ether, propylene glycol, octyldodecanol, diisopropyl adipate, and isostearic acid; at least one oil selected from the group consisting of light mineral oil, MCT oil, and hydrogenated castor oil; or a combination of at least one emollient and at least one oil; c) about 0.01% to about 15% by weight of at least one surfactant selected from the group consisting of Glycerol monostearate, Sorbitan monostearate, and PEG 100 Stearate; d) about 1% to about 10% by weight of at least one foam adjuvant selected from the group consisting of oleyl alcohol, stearyl alcohol, myristyl alcohol and stearic acid; wherein each compound is doxycycline-compatible; wherein the composition is substantially non-aqueous; wherein the doxycycline hyclate or the doxycycline monohydrate is chemically stable in the foamable pharmaceutical composition when stored for 72 hours at about at least 25°
C. after mixing with the foamable pharmaceutical composition; andwherein the weight ratio of the foamable pharmaceutical composition to the propellant is about 100;
5 to about 100;
35. - View Dependent Claims (46, 48)
-
-
19-24. -24. (canceled)
-
29-30. -30. (canceled)
-
32-43. -43. (canceled)
Specification