Cooling agents, pharmaceutical compositions having cooling agents and processes for making and using same
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-007/16
A61K-047/00
출원번호
US-0272710
(2002-10-17)
발명자
/ 주소
Zanone,John
Stier,Roger E.
출원인 / 주소
Firmenich SA
대리인 / 주소
Norris, McLaughlin &
인용정보
피인용 횟수 :
7인용 특허 :
10
초록▼
The invention pertains to cooling agents comprising N-substituted p-menthane-3-carboxamides, menthyl acetate and solubilizer, and methods for making the cooling agents. The invention also concerns pharmaceutical compositions comprising the cooling agents, including tablets, suspensions and liquid so
The invention pertains to cooling agents comprising N-substituted p-menthane-3-carboxamides, menthyl acetate and solubilizer, and methods for making the cooling agents. The invention also concerns pharmaceutical compositions comprising the cooling agents, including tablets, suspensions and liquid solutions having active pharmaceutical agents for treating upper gastrointestinal tract distress, and methods for treating upper gastrointestinal tract distress in humans.
대표청구항▼
What is claimed is: 1. A pharmaceutical composition comprising from about 1% to about 99% by weight of the pharmaceutical composition of at least one active pharmaceutical agent selected from the group consisting of antacid agents, acid secretion prevention agents, bismuth containing agents and mix
What is claimed is: 1. A pharmaceutical composition comprising from about 1% to about 99% by weight of the pharmaceutical composition of at least one active pharmaceutical agent selected from the group consisting of antacid agents, acid secretion prevention agents, bismuth containing agents and mixtures thereof and from about 1% to about 99% by weight of the pharmaceutical composition excipients comprising at least one cooling agent in spray dried form, wherein the cooling agent comprises a) N-substituted p-menthane-3-carboxamide of the formula: where R', when taken separately, is hydrogen or an aliphatic radical containing up to 25 carbon atoms; and R", when taken separately is hydroxy, or an aliphatic radical containing up to 25 carbon atoms, with the proviso that when R' is hydrogen R" may also be an aryl radical of up to 10 carbon atoms and selected from the group consisting of substituted phenyl, phenalkyl, substituted phenalkyl, naphthyl, substituted naphthyl, and pyridyl; and R' and R", when taken together with the nitrogen atom to which they are attached, represent a cyclic or heterocyclic group of up to 25 carbon atoms, b) menthyl acetate wherein the menthyl acetate and the N-substituted p-menthane-3-carboxamide act synergistically to provide a cooling effect, and c) solubilizer of mixed esters of capric and acrylic acids esterified on glycerin wherein said solubilizer is present in an amount sufficient to prevent the N-substituted p-methane-3-carboxamines from crystallizing out of solution during the spray drying process. 2. The pharmaceutical composition of claim 1 wherein the cooling agent comprises from about 1% to about 20% of the N-substituted p-menthane-3-carboxamide compounds, about 1% to about 10% of the menthyl acetate and about 60% to about 85% of the solubilizer all by weight of cooling agent components. 3. The pharmaceutical composition of claim 1 further comprising a carrier. 4. The pharmaceutical composition of claim 1 wherein the N-substituted p-menthane-3-carboxamide is N-ethyl p-methane-3-carboxamide. 5. The pharmaceutical composition of claim 1 wherein the excipients comprise menthol. 6. The pharmaceutical composition of claim 1 wherein the antacid agents are selected from the group consisting of aluminum carbonate, aluminum hydroxide, aluminum phosphate, aluminum hydroxy-carbonate, dihydroxy aluminum sodium carbonate, aluminum magnesium glycinate, dihydroxy aluminum amino acetate, dihydroxy aluminum aminoacetic acid, calcium carbonate, calcium phosphate, aluminum magnesium hydrated sulfates, magnesium aluminate, magnesium alumina silicates, magnesium carbonate, magnesium glycinate, magnesium hydroxide, magnesium oxide, magnesium trisilicate, sucralfate, and mixtures thereof. 7. The pharmaceutical composition of claim 1 wherein the acid secretion prevention agents are selected from the group consisting of cimetidine, ranitidine, famotidine, omeprazole, and mixtures thereof. 8. The pharmaceutical composition of claim 1 wherein the bismuth containing agents are selected from the group consisting of bismuth subsalicylate, bismuth aluminate, bismuth citrate, bismuth subcitrate, bismuth nitrate, bismuth subcarbonate, bismuth subgalate, and mixtures thereof. 9. A method for treating upper gastrointestinal tract distress in humans comprising orally administering through an ingestible composition a safe and effective amount of at least one active pharmaceutical agent selected from the group consisting of antacid agents, acid secretion prevention agents, bismuth containing agents and mixtures thereof, and a cooling agent in spray dried form comprising a) N-substituted p-menthane-3-carboxamide of the formula: where R', when taken separately, is hydrogen or an aliphatic radical containing up to 25 carbon atoms; and R", when taken separately is hydroxy, or an aliphatic radical containing up to 25 carbon atoms, with the proviso that when R' is hydrogen R" may also be an aryl radical of up to 10 carbon atoms and selected from the group consisting of substituted phenyl, phenalkyl, substituted phenalkyl, naphthyl, substituted naphthyl, and pyridyl; and R' and R", when taken together with the nitrogen atom to which they are attached, represent a cyclic or heterocyclic group of up to 25 carbon atoms, b) menthyl acetate wherein the menthyl acetate and the N-substituted p-menthane-3-carboxamide act synergistically to provide a cooling effect, and c) solubilizer of mixed esters of capric and acrylic acids esterified on glycerin wherein said solubilizer is present in an amount sufficient to prevent the N-substituted p-methane-3-carboxamines from crystallizing out of solution during the spray drying process. 10. The method of claim 9 wherein the ingestible composition is in the form of tablet.
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이 특허에 인용된 특허 (10)
Luo Shiuh J. (Livingston NJ), Breath-freshening edible compositions comprising menthol and an N-substituted-P-menthane carboxamide and methods for pre.
Cherukuri Subraman R. (Towaco NJ) Raman Krishna (Randolph NJ) Mansukhani Gul (Staten Island NY) Cifrese Ralph (Wharton NJ) Wong Lucy L. (Jackson Heights NY), Breath-freshening edible compositions of methol and a carboxamide.
Upson James G. (Springdale OH) Russell Carmelita M. (Cincinnati OH), Ingestible pharmaceutical compositions for treating upper gastrointestinal tract distress.
Record David (River Forest IL) Tyrpin Henry (Midlothian IL) Broderick Kevin (Berwyn IL) Johnson Sonya (Brookfield IL), Mint flavored chewing gum having reduced bitterness and methods for making same.
Watson Hugh R. (Wargrave GB2) Rowsell David G. (Staines GB2) Spring David J. (Datchet GB2), P-Menthane carboxamides having a physiological cooling effect.
Watson Hugh R. (Wargrave EN) Rowsell David G. (Staines EN) Spring David John (Datchet EN), Tobacco and tobacco-containing manufactures containing an ingredient having physiological cooling activity.
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