Extended duration antacid product
AssigneeMicro-Pak, Inc.
InventorsDonald F. H. Wallach, Rajiv Mathur, Jean Philippot, Surendra Kumar
Life of this patent
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Abstract
An antacid product having extended duration of residence in the gastric and upper intestinal systems has been developed. This antacid product includes a blend of 10-70% by volume nonphospholipid lipid vesicles, with a particulate base. An antiflatulence agent may also be included. A method of providing extended duration amelioration of acid build up in the gastric and upper intestinal tract using this product is also disclosed.
Claims30
An antacid product having extended residence and duration in the gastric and upper intestinal systems comprising mixture of non-phospholipid lipid vesicles and an effective amount of a particulate base in a substantially aqueous solution, said lipid vesicles comprising 10-70% by weight of said product, and wherein said non-phospholipid is selected from the group consisting of:
- diethanolamides having the formula
- (HOCH.sub.2 --CH.sub.2).sub.2 NCO--R.sub.3
- where R.sub.3 is a radical of caprylic, lauric, myristic or linoleic acids;
- long chain acyl hexosamides having the formula
- R.sub.4 --NHCO--(CH.sub.2).sub.b --CH.sub.3
- where b ranges from 10-18 and R.sub.4 is a radical of a sugar molecule selected from a group consisting of glucosamine, galactosamine, and N-methylglucamine;
- and
- long chain acyl amino acid amides having the formula
- R.sub.5 --CH(COOH)--NHCO--(CH.sub.2).sub.c --CH.sub.3
- where c ranges from 10-18 and R.sub.5 is a radical of an amino acid side chain;
- long chain acyl amides having the formula
- HOOC--(CH.sub.2).sub.d --N(CH.sub.3)--(CH.sub.2).sub.3 --NHCO--R.sub.6
- where R.sub.6 is an acyl chain having 12-20 carbon and not more than two unsaturations, and d ranges from 1-3;
- glycerol monostearate;
- polyoxyethylene fatty esters having the formula
- R.sub.1 --COO(C.sub.2 H.sub.4 O).sub.n H
- where R.sub.1 is a radical of lauric, myristic, cetyl, stearic, or oleic acid and
- n=2-10;
- polyoxyethylene fatty acid ethers, having the formula
- R.sub.2 --CO(C.sub.2 H.sub.4 O).sub.m H
- where R.sub.2 is a radical of lauric, myristic, or cetyl acids, single or double unsaturated octadecyl acids, or double unsaturated eicodienoic acids and m ranges from 2-4;
- polyoxyethylene (20) sorbitan mono- or trioleate;
- polyoxyethylene glyceryl monostearate with 1-10 polyoxyethylene groups;
- betaines;
- and
- sarcosinamides.
A method of ameliorating acid build up in the gastric and upper intestinal tracts comprising, administering to a human host an effective amount of an antacid product comprising an effective amount of a mixture of non-phospholipid lipid vesicles and an effective amount of a particulate base in a substantially aqueous solution, said lipid vesicles comprising 10-70% by weight of said product, and wherein said non-phospholipid is selected from the group consisting of:
- diethanolamides having the formula
- (HOCH.sub.2 --CH.sub.2).sub.2 NCO--R.sub.3
- where R.sub.3 is a radical of caprylic, lauric, myristic or linoleic acids;
- long chain acyl hexosamides having the formula
- R.sub.4 --NHCO--(CH.sub.2).sub.b --CH.sub.3
- where b ranges from 10-18 and R.sub.4 is a radical of a sugar molecule selected from a group consisting of glucosamine, galactosamine, and N-methylglucamine;
- and
- long chain acyl amino acid amides having the formula
- R.sub.5 --CH(COOH)--NHCO--(CH2).sub.c --CH.sub.3
- where c ranges from 10-18 and R5 is a radical of an amino acid side chain;
- long chain acyl amides having the formula
- HOOC--(CH.sub.2).sub.d --N(CH.sub.3)--(CH.sub.2).sub.3 --NHCO--NHCO--R.sub.6
- where R.sub.6 is an acyl chain having 12-20 carbons and not more than two unsaturations, and d ranges from 1-3;
- glycerol monostearate;
- polyoxyethylene fatty esters having the formula
- R.sub.1 --COO(C.sub.2 H.sub.4 O).sub.n H
- where R.sub.1 is a radical of lauric, myristic, cetyl, stearic, or oleic acid and n=2-10;
- polyoxyethylene fatty acid ethers, having the formula
- R.sub.2 --CO(C.sub.2 H.sub.4 O).sub.m H
- where R.sub.2 is a radical of lauric, myristic, or cetyl acids, single or double unsaturated octadecyl acids, or double unsaturated eicodienoic acids and m ranges from 2-4;
- polyoxyethylene (20) sorbitan mono- or trioleate;
- polyoxyethylene glyceryl monostearate with 1-10 polyoxyethylene groups;
- betaines;
- and
- sarcosinamides.
An antacid product having extended residence and duration in the gastric and upper intestinal systems comprising a mixture of non-phospholipid lipid vesicles and an effective amount of a particulate base in a substantially aqueous solution, said lipid vesicles comprising 10-70% by weight of said product, and wherein said non-phospholipid is selected from the group consisting of:
- a blend of two distinct lipids, a primary lipid and a secondary lipid,
- wherein the primary lipid, which forms the greatest proportion by weight of any lipid is 50% or higher by weight of lipid in the vesicle, is selected from the group consisting of C.sub.12 -C.sub.18 fatty alcohols, C.sub.12 -C.sub.18 glycol monoesters, C.sub.12 -C.sub.18 glyceryl mono- and diesters, and mixtures thereof;
- and
- wherein the secondary lipid must be present in an amount sufficient to allow formation of the lipid vesicles, and is selected from the group consisting of quaternary dimethyldiacyl amines, polyoxyethylene acyl alcohols, polyglycerols, sorbitan fatty acid esters, fatty acids and their salts, and mixtures thereof.
A method of ameliorating acid build up in the gastric and upper intestinal tracts comprising, administering to a human host an effective amount of an antacid product comprising an effective amount of a mixture of non-phospholipid lipid vesicles and an effective amount of a particulate base in a substantially aqueous solution, said lipid vesicles comprising 10-70% by weight of said product, and wherein said non-phospholipid is selected from the group consisting of:
- a blend of two distinct lipids, a primary lipid and a secondary lipid,
- wherein the primary lipid, which forms the greatest proportion by weight of any lipid is 50% or higher by weight of lipid in the vesicle, is selected from the group consisting of C.sub.12 -C.sub.18 fatty alcohols, C.sub.12 -C.sub.18 glycol monoesters, C.sub.12 -C.sub.18 glyceryl mono- and diesters, and mixtures thereof;
- and
- wherein the secondary lipid must be present in an amount sufficient to allow formation of the lipid vesicles, and is selected from the group consisting of quaternary dimethyldiacyl amines, polyoxyethylene acyl alcohols, polyglycerols, sorbitan fatty acid esters, fatty acids and their salts, and mixtures thereof.
Dependencies are inferred from the claim text.