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Kafe 바로가기국가/구분 | United States(US) Patent 등록 |
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국제특허분류(IPC7판) |
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출원번호 | US-0732024 (2012-12-31) |
등록번호 | US-9161916 (2015-10-20) |
발명자 / 주소 |
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출원인 / 주소 |
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대리인 / 주소 |
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인용정보 | 피인용 횟수 : 15 인용 특허 : 533 |
The present disclosure teaches unique formulations for topical administration of tetracycline antibiotics, in which the tetracycline antibiotics remain stable.
1. A topical composition comprising a foamable pharmaceutical composition and a propellant, the foamable pharmaceutical composition comprising: a) an unstable active agent;b) at least one emollient; or at least one liquid oil; ora combination of at least one emollient and at least one liquid oil;c)
1. A topical composition comprising a foamable pharmaceutical composition and a propellant, the foamable pharmaceutical composition comprising: a) an unstable active agent;b) at least one emollient; or at least one liquid oil; ora combination of at least one emollient and at least one liquid oil;c) at least one surfactant, wherein the surfactant comprises a fatty acid ester having a C8-C24 hydrocarbon chain; andd) optionally at least one foam adjuvant;wherein each component is compatible with the unstable active agent present in the composition;wherein the composition is free of one or more of PPG-15 stearyl ether, octyldodecanol, ethanol propylene glycol, glycerol, PEG 200, PEG 400, MCT oil, isostearic acid, polyoxyl 20 stearyl ether, polyoxyl 2 stearyl ether, methyl glycose sesquistearate, PEG 40 stearate, cocoglycerides, hexylene glycol, butylene glycol, sorbitan monolaurate, and dimethyl isosorbide,wherein the composition comprises less than about 2% by weight of the foamable pharmaceutical composition of water; andwherein at least 90% by mass of the unstable active agent is present in the foamable pharmaceutical composition when stored for 72 hours at 25° C. after mixing with the pharmaceutical composition. 2. The topical composition of claim 1, wherein the unstable active agent is a tetracycline antibiotic; wherein at least 90% by mass of the tetracycline antibiotic is present in the foamable pharmaceutical composition when stored for 72 hours at 25° C. after mixing with the pharmaceutical composition. 3. The composition of claim 2, wherein the weight ratio of the foamable pharmaceutical composition to the propellant is about 100:3 to about 100:35. 4. The topical composition of claim 2, wherein the emollient is selected from the group consisting of PPG-15 stearyl ether, octyldodecanol, diisopropyl adipate isostearic acid, cetearyl octanoate, and mixtures of any two or more thereof. 5. The topical composition of claim 2, wherein the liquid oil is selected from the group consisting of a plant-based oil, a mineral oil, a triglyceride, an essential oil, a light mineral oil, a MCT oil, a jojoba oil, a peppermint oil, and mixtures of any two or more thereof. 6. The topical composition of claim 2, wherein the fatty acid ester having a C8-C24 hydrocarbon chain is selected from the group consisting of a stearic acid ester, a monoglyceride, a diglyceride, glycerol monostearate, sorbitan monostearate, PEG 40 stearate, PEG 100 stearate, and mixtures of any two or more thereof. 7. The topical composition of claim 2, wherein the foam adjuvant is selected from the group consisting of a fatty alcohol, a C14-C18 fatty alcohol, oleyl alcohol, stearyl alcohol, myristyl alcohol, a fatty acid, cocoglycerides, and mixtures of any two or more thereof. 8. The topical composition of claim 2, wherein the tetracycline antibiotic is selected from the group consisting of a minocycline, a doxycycline, minocycline hydrochloride, doxycycline hyclate, doxycycline monohydrate, and mixtures of any two or more thereof. 9. The topical composition of claim 2 further comprising at least one of aluminum starch octenyl succinate, titanium dioxide, coconut alcohol, and hexylene glycol. 10. The topical composition of claim 2, wherein chemical stability is determined by observing a color change in the foamable pharmaceutical composition. 11. The topical composition of claim 2 comprising: a) about 0.1% to about 10% by weight of the foamable pharmaceutical composition of minocycline hydrochloride;b) about 60% to about 95% by weight of the foamable pharmaceutical composition of: at least one emollient selected from the group consisting of PPG-15 stearyl ether, octyldodecanol, diisopropyl adipate, and cetearyl octanoate; orat least one oil selected from the group consisting of a light mineral oil, a MCT oil, a jojoba oil, and a peppermint oil; ora combination of said at least one emollient and said at least one oil;c) about 0.01% to about 15% by weight of the foamable pharmaceutical composition of at least one surfactant selected from the group consisting of a stearic acid ester, a monoglyceride, a diglyceride, glycerol monostearate, sorbitan monostearate, PEG 40 stearate and PEG 100 stearate; andd) optionally 0% to about 10% by weight of the foamable pharmaceutical composition of at least one foam adjuvant comprising a fatty alcohol and or cocoglycerides, wherein the fatty alcohol is selected from the group consisting of oleyl alcohol, stearyl alcohol and myristyl alcohol;wherein each component is compatible with minocycline hydrochloride;wherein the composition is free of propylene glycol, glycerol, PEG 200, PEG 400, ethanol, isostearic acid, polyoxyl 20 stearyl ether, polyoxyl 2 stearyl ether, methyl glucose sesquistearate, hexylene glycol, butylene glycol, sorbitan monolaurate, and dimethyl isosorbide; andwherein the weight ratio of the foamable pharmaceutical composition to the propellant is about 100:3 to about 100:35. 12. The topical composition of claim 11, wherein less than about 1% by mass of a 4-epiminocycline is measured when the foamable pharmaceutical composition is stored for 72 hours at 25° C. compared to time 0. 13. The topical composition of claim 2 comprising either A): a) about 0.1% to about 10% by weight of the foamable pharmaceutical composition of doxycycline hyclate or doxycycline monohydrate;b) about 60% to about 95% by weight of the foamable pharmaceutical composition of: at least one emollient selected from the group consisting of PPG-15 stearyl ether, diisopropyl adipate, and cetearyl octanoate; orat least one oil selected from the group consisting of a mineral oil and a MCT oil; ora combination of said at least one emollient and said at least one oil;c) about 0.01% to about 15% by weight of the foamable pharmaceutical composition of at least one surfactant selected from the group consisting of a stearic acid ester, a monoglyceride, a diglyceride, glycerol monostearate, sorbitan monostearate, hydrogenated castor oil, and PEG 100 stearate; andd) optionally 0% to about 10% by weight of the foamable pharmaceutical composition of at least one foam adjuvant comprising a fatty alcohol and or a fatty acid selected from the group consisting of stearyl alcohol, oleyl alcohol, isostearic acid and myristyl alcohol; or B): a) about 0.1% to about 10% by weight of the foamable pharmaceutical composition of doxycycline hyclate or doxycycline monohydrate;b) about 60% to about 95% by weight of the foamable pharmaceutical composition of: at least one emollient selected from the group consisting of cetearyl octanoate, PPG-15 stearyl ether, propylene glycol, diisopropyl adipate, and isostearic acid; orat least one oil selected from the group consisting of light mineral oil, MCT oil, and hydrogenated castor oil;or a combination of said at least one emollient and said at least one oil;c) about 0.01% to about 15% by weight of the foamable pharmaceutical composition of at least one surfactant selected from the group consisting of a stearic acid ester, a monoglyceride, a diglyceride, glycerol monostearate, sorbitan monostearate, PEG 40 stearate, and PEG 100 stearate; andd) about 1% to about 10% by weight of the foamable pharmaceutical composition of at least one foam adjuvant comprising a fatty alcohol and or fatty acid selected from the group consisting of oleyl alcohol, stearyl alcohol, myristyl alcohol and stearic acid;wherein each component is compatible with doxycycline hyclate or doxycycline monohydrate;wherein the composition is free of octyldodecanol, propylene glycol, glycerol, PEG 200, PEG 400, butylene glycol, sorbitan monolaurate, and dimethyl isosorbide; andwherein the weight ratio of the foamable pharmaceutical composition to the propellant is about 100:3 to about 100:35. 14. The topical composition of claim 2 further comprising about 0.1% to about 5% by weight of the foamable pharmaceutical composition of a silicone oil or a cyclomethicone. 15. The topical composition of claim 2, wherein the tetracycline antibiotic is chemically stable in the foamable pharmaceutical composition, wherein at least 90% by mass of the tetracycline antibiotic is present in the foamable pharmaceutical composition when stored for about 3 weeks, wherein chemical stability is determined by measuring mass of the tetracycline antibiotic at three weeks compared to time 0. 16. The topical tetracycline antibiotic composition of claim 2 further comprising at least one tetracycline-compatible additional active agent. 17. A method of treating a bacterial infection or post-surgical adhesions, the method comprising topically administering the topical composition of claim 2 to a subject in need of treatment, wherein the topical composition is administered to one or more of skin, face, a mucosal membrane, a body cavity, the nose, the mouth, the eye, the ear canal, the respiratory system, the vagina, the rectum or a surgical site of the subject. 18. A method of treating a bacterial infection, the method comprising administering the topical composition of claim 11 to a subject in need of treatment, wherein the topical composition is administered topically to one or more of skin, a mucosal membrane, or a body cavity of the subject. 19. A method of treating a bacterial infection, the method comprising administering the topical composition of claim 13 to a subject in need of treatment, wherein the topical composition is administered topically to one or more of skin, a mucosal membrane, or a body cavity of the subject. 20. The topical composition of claim 2, wherein at least 90% by mass of the tetracycline antibiotic is present in the foamable pharmaceutical composition when stored for 72 hours at 40° C. after mixing with the pharmaceutical composition, wherein chemical stability is determined by measuring mass of the tetracycline antibiotic at 72 hours compared to time 0. 21. The topical composition of claim 1, wherein said unstable active agent is a water sensitive agent, an ester or amide prone to hydrolysis by water, an agent sensitive to free radical attack or oxidation, or sensitive to a specific pH level. 22. The topical composition of claim 1, wherein the composition is free of PPG-15 stearyl ether, octyldodecanol, MCT oil, isostearic acid, PEG 40 stearate, and cocoglycerides. 23. The topical composition of claim 1, wherein the composition is free of PPG-15 stearyl ether, MCT oil, isostearic acid, PEG 40 stearate, cocoglycerides and hexylene glycol. 24. The topical composition of claim 2, wherein the emollient is selected from the group consisting of diisopropyl adipate, cetearyl octanoate, and mixtures thereof. 25. The topical composition of claim 2, wherein the liquid oil is selected from the group consisting of a plant-based oil, a mineral oil, a triglyceride, an essential oil, a light mineral oil, jojoba oil, a peppermint oil, and mixtures of any two or more thereof.
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