MXPA96002270A - Orally applicable pharmaceutical composition - Google Patents
Orally applicable pharmaceutical compositionInfo
- Publication number
- MXPA96002270A MXPA96002270A MXPA/A/1996/002270A MX9602270A MXPA96002270A MX PA96002270 A MXPA96002270 A MX PA96002270A MX 9602270 A MX9602270 A MX 9602270A MX PA96002270 A MXPA96002270 A MX PA96002270A
- Authority
- MX
- Mexico
- Prior art keywords
- weight
- composition
- pharmaceutical composition
- active substance
- composition according
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 20
- 239000000203 mixture Substances 0.000 claims abstract description 146
- 239000000126 substance Substances 0.000 claims abstract description 68
- 230000001458 anti-acid Effects 0.000 claims abstract description 31
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 24
- 241000209134 Arundinaria Species 0.000 claims abstract description 22
- 235000000346 sugar Nutrition 0.000 claims abstract description 22
- 239000007788 liquid Substances 0.000 claims abstract description 19
- 239000004615 ingredient Substances 0.000 claims abstract description 13
- 239000002904 solvent Substances 0.000 claims abstract description 10
- 239000003159 antacid agent Substances 0.000 claims description 30
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 19
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 18
- 239000007787 solid Substances 0.000 claims description 14
- 125000003118 aryl group Chemical group 0.000 claims description 9
- VTHJTEIRLNZDEV-UHFFFAOYSA-L Magnesium hydroxide Chemical compound [OH-].[OH-].[Mg+2] VTHJTEIRLNZDEV-UHFFFAOYSA-L 0.000 claims description 6
- VTYYLEPIZMXCLO-UHFFFAOYSA-L calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 6
- 239000000347 magnesium hydroxide Substances 0.000 claims description 6
- 229910001862 magnesium hydroxide Inorganic materials 0.000 claims description 6
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 5
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 5
- 239000000600 sorbitol Substances 0.000 claims description 5
- 235000010356 sorbitol Nutrition 0.000 claims description 5
- 229920001285 xanthan gum Polymers 0.000 claims description 5
- CZMRCDWAGMRECN-UGDNZRGBSA-N D-sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 4
- CZMRCDWAGMRECN-GDQSFJPYSA-N Sucrose Natural products O([C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](CO)O1)[C@@]1(CO)[C@H](O)[C@@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-GDQSFJPYSA-N 0.000 claims description 4
- 239000008247 solid mixture Substances 0.000 claims description 4
- 239000005720 sucrose Substances 0.000 claims description 4
- 229960003563 Calcium Carbonate Drugs 0.000 claims description 3
- ZLNQQNXFFQJAID-UHFFFAOYSA-L Magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 claims description 3
- 229910000019 calcium carbonate Inorganic materials 0.000 claims description 3
- 239000001095 magnesium carbonate Substances 0.000 claims description 3
- 239000011776 magnesium carbonate Substances 0.000 claims description 3
- 229910000021 magnesium carbonate Inorganic materials 0.000 claims description 3
- 239000002562 thickening agent Substances 0.000 claims description 3
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2R,3R,4S,5R,6S)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2S,3R,4S,5R,6R)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2R,3R,4S,5R,6R)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims description 2
- CWSZBVAUYPTXTG-UHFFFAOYSA-N 5-[6-[[3,4-dihydroxy-6-(hydroxymethyl)-5-methoxyoxan-2-yl]oxymethyl]-3,4-dihydroxy-5-[4-hydroxy-3-(2-hydroxyethoxy)-6-(hydroxymethyl)-5-methoxyoxan-2-yl]oxyoxan-2-yl]oxy-6-(hydroxymethyl)-2-methyloxane-3,4-diol Chemical compound O1C(CO)C(OC)C(O)C(O)C1OCC1C(OC2C(C(O)C(OC)C(CO)O2)OCCO)C(O)C(O)C(OC2C(OC(C)C(O)C2O)CO)O1 CWSZBVAUYPTXTG-UHFFFAOYSA-N 0.000 claims description 2
- WNROFYMDJYEPJX-UHFFFAOYSA-K Aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 claims description 2
- 229910000014 Bismuth subcarbonate Inorganic materials 0.000 claims description 2
- 229920002907 Guar gum Polymers 0.000 claims description 2
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 2
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 2
- GVALZJMUIHGIMD-UHFFFAOYSA-H Magnesium phosphate tribasic Chemical compound [Mg+2].[Mg+2].[Mg+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O GVALZJMUIHGIMD-UHFFFAOYSA-H 0.000 claims description 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 2
- UIIMBOGNXHQVGW-UHFFFAOYSA-M NaHCO3 Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims description 2
- XAPRFLSJBSXESP-UHFFFAOYSA-N Oxycinchophen Chemical compound N=1C2=CC=CC=C2C(C(=O)O)=C(O)C=1C1=CC=CC=C1 XAPRFLSJBSXESP-UHFFFAOYSA-N 0.000 claims description 2
- QORWJWZARLRLPR-UHFFFAOYSA-H Tricalcium phosphate Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims description 2
- HRXKRNGNAMMEHJ-UHFFFAOYSA-K Trisodium citrate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O HRXKRNGNAMMEHJ-UHFFFAOYSA-K 0.000 claims description 2
- SXSTVPXRZQQBKQ-UHFFFAOYSA-M aluminum;magnesium;hydroxide;hydrate Chemical compound O.[OH-].[Mg].[Al] SXSTVPXRZQQBKQ-UHFFFAOYSA-M 0.000 claims description 2
- MGLUJXPJRXTKJM-UHFFFAOYSA-L bismuth subcarbonate Chemical compound O=[Bi]OC(=O)O[Bi]=O MGLUJXPJRXTKJM-UHFFFAOYSA-L 0.000 claims description 2
- 229940036358 bismuth subcarbonate Drugs 0.000 claims description 2
- 239000001506 calcium phosphate Substances 0.000 claims description 2
- 229910000389 calcium phosphate Inorganic materials 0.000 claims description 2
- 235000011010 calcium phosphates Nutrition 0.000 claims description 2
- 239000001913 cellulose Substances 0.000 claims description 2
- 229920002678 cellulose Polymers 0.000 claims description 2
- 235000010980 cellulose Nutrition 0.000 claims description 2
- PWZFXELTLAQOKC-UHFFFAOYSA-A dialuminum;hexamagnesium;carbonate;hexadecahydroxide;tetrahydrate Chemical compound O.O.O.O.[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Al+3].[Al+3].[O-]C([O-])=O PWZFXELTLAQOKC-UHFFFAOYSA-A 0.000 claims description 2
- 239000000665 guar gum Substances 0.000 claims description 2
- 235000010417 guar gum Nutrition 0.000 claims description 2
- 229960002154 guar gum Drugs 0.000 claims description 2
- 229960001545 hydrotalcite Drugs 0.000 claims description 2
- 229910001701 hydrotalcite Inorganic materials 0.000 claims description 2
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 2
- 229940071676 hydroxypropylcellulose Drugs 0.000 claims description 2
- 229960004018 magaldrate Drugs 0.000 claims description 2
- 239000004137 magnesium phosphate Substances 0.000 claims description 2
- 229910000157 magnesium phosphate Inorganic materials 0.000 claims description 2
- 229960002261 magnesium phosphate Drugs 0.000 claims description 2
- 235000010994 magnesium phosphates Nutrition 0.000 claims description 2
- 229920000609 methyl cellulose Polymers 0.000 claims description 2
- 239000001923 methylcellulose Substances 0.000 claims description 2
- 235000010981 methylcellulose Nutrition 0.000 claims description 2
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 2
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 2
- 239000001509 sodium citrate Substances 0.000 claims description 2
- 239000011778 trisodium citrate Substances 0.000 claims description 2
- 229940091250 Magnesium supplements Drugs 0.000 claims 1
- VQHSOMBJVWLPSR-WUJBLJFYSA-N Maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 claims 1
- FKHIFSZMMVMEQY-UHFFFAOYSA-N Talc Chemical compound [Mg+2].[O-][Si]([O-])=O FKHIFSZMMVMEQY-UHFFFAOYSA-N 0.000 claims 1
- GJCOSYZMQJWQCA-UHFFFAOYSA-N Xanthene Chemical compound C1=CC=C2CC3=CC=CC=C3OC2=C1 GJCOSYZMQJWQCA-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 235000010216 calcium carbonate Nutrition 0.000 claims 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims 1
- 239000011777 magnesium Substances 0.000 claims 1
- 229910052749 magnesium Inorganic materials 0.000 claims 1
- 235000014380 magnesium carbonate Nutrition 0.000 claims 1
- 235000012254 magnesium hydroxide Nutrition 0.000 claims 1
- 239000000391 magnesium silicate Substances 0.000 claims 1
- 229940099273 magnesium trisilicate Drugs 0.000 claims 1
- 229910000386 magnesium trisilicate Inorganic materials 0.000 claims 1
- 235000019793 magnesium trisilicate Nutrition 0.000 claims 1
- 239000000845 maltitol Substances 0.000 claims 1
- 235000010449 maltitol Nutrition 0.000 claims 1
- 229940035436 maltitol Drugs 0.000 claims 1
- 235000019263 trisodium citrate Nutrition 0.000 claims 1
- 238000009472 formulation Methods 0.000 description 20
- 239000000725 suspension Substances 0.000 description 10
- PNEYBMLMFCGWSK-UHFFFAOYSA-N al2o3 Chemical compound [O-2].[O-2].[O-2].[Al+3].[Al+3] PNEYBMLMFCGWSK-UHFFFAOYSA-N 0.000 description 6
- 238000004519 manufacturing process Methods 0.000 description 5
- 239000000230 xanthan gum Substances 0.000 description 4
- 235000010493 xanthan gum Nutrition 0.000 description 4
- 229940082509 xanthan gum Drugs 0.000 description 4
- 206010013911 Dysgeusia Diseases 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- 235000020374 simple syrup Nutrition 0.000 description 3
- BJHIKXHVCXFQLS-UYFOZJQFSA-N Fructose Natural products OC[C@@H](O)[C@@H](O)[C@H](O)C(=O)CO BJHIKXHVCXFQLS-UYFOZJQFSA-N 0.000 description 2
- GUBGYTABKSRVRQ-YOLKTULGSA-N Maltose Natural products O([C@@H]1[C@H](O)[C@@H](O)[C@H](O)O[C@H]1CO)[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 GUBGYTABKSRVRQ-YOLKTULGSA-N 0.000 description 2
- 210000002784 Stomach Anatomy 0.000 description 2
- 206010047700 Vomiting Diseases 0.000 description 2
- HEBKCHPVOIAQTA-SCDXWVJYSA-N Xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 2
- 229960002675 Xylitol Drugs 0.000 description 2
- 230000000875 corresponding Effects 0.000 description 2
- 238000005189 flocculation Methods 0.000 description 2
- 230000016615 flocculation Effects 0.000 description 2
- 238000011081 inoculation Methods 0.000 description 2
- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Chemical compound [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 description 2
- 230000002906 microbiologic Effects 0.000 description 2
- 230000001264 neutralization Effects 0.000 description 2
- 238000005020 pharmaceutical industry Methods 0.000 description 2
- 230000002335 preservative Effects 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- 238000004062 sedimentation Methods 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
- 238000003860 storage Methods 0.000 description 2
- 239000000811 xylitol Substances 0.000 description 2
- 235000010447 xylitol Nutrition 0.000 description 2
- VUKAUDKDFVSVFT-UHFFFAOYSA-N 2-[6-[4,5-bis(2-hydroxypropoxy)-2-(2-hydroxypropoxymethyl)-6-methoxyoxan-3-yl]oxy-4,5-dimethoxy-2-(methoxymethyl)oxan-3-yl]oxy-6-(hydroxymethyl)-5-methoxyoxane-3,4-diol Chemical compound COC1C(OC)C(OC2C(C(O)C(OC)C(CO)O2)O)C(COC)OC1OC1C(COCC(C)O)OC(OC)C(OCC(C)O)C1OCC(C)O VUKAUDKDFVSVFT-UHFFFAOYSA-N 0.000 description 1
- 229940069428 ANTACIDS Drugs 0.000 description 1
- 206010000087 Abdominal pain upper Diseases 0.000 description 1
- 206010001584 Alcohol abuse Diseases 0.000 description 1
- 241000228245 Aspergillus niger Species 0.000 description 1
- 206010006784 Burning sensation Diseases 0.000 description 1
- 229940095731 Candida albicans Drugs 0.000 description 1
- 241000222122 Candida albicans Species 0.000 description 1
- GZCGUPFRVQAUEE-KCDKBNATSA-N D-(+)-Galactose Natural products OC[C@@H](O)[C@H](O)[C@H](O)[C@@H](O)C=O GZCGUPFRVQAUEE-KCDKBNATSA-N 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N D-Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- FBPFZTCFMRRESA-KAZBKCHUSA-N D-Mannitol Natural products OC[C@@H](O)[C@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KAZBKCHUSA-N 0.000 description 1
- 208000002173 Dizziness Diseases 0.000 description 1
- 206010015137 Eructation Diseases 0.000 description 1
- 241000588722 Escherichia Species 0.000 description 1
- 239000005715 Fructose Substances 0.000 description 1
- 229920001908 Hydrogenated starch hydrolysate Polymers 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- GUBGYTABKSRVRQ-UUNJERMWSA-N Lactose Natural products O([C@@H]1[C@H](O)[C@H](O)[C@H](O)O[C@@H]1CO)[C@H]1[C@@H](O)[C@@H](O)[C@H](O)[C@H](CO)O1 GUBGYTABKSRVRQ-UUNJERMWSA-N 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- 210000003254 Palate Anatomy 0.000 description 1
- 108010009736 Protein Hydrolysates Proteins 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 208000007107 Stomach Ulcer Diseases 0.000 description 1
- 206010043903 Tobacco abuse Diseases 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 201000003082 alcohol use disease Diseases 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- 230000000845 anti-microbial Effects 0.000 description 1
- 230000001580 bacterial Effects 0.000 description 1
- 230000000711 cancerogenic Effects 0.000 description 1
- 231100000315 carcinogenic Toxicity 0.000 description 1
- 230000005591 charge neutralization Effects 0.000 description 1
- 230000001143 conditioned Effects 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 230000003247 decreasing Effects 0.000 description 1
- 230000003292 diminished Effects 0.000 description 1
- 150000002016 disaccharides Chemical class 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 230000035622 drinking Effects 0.000 description 1
- 235000021271 drinking Nutrition 0.000 description 1
- 201000006549 dyspepsia Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 230000004634 feeding behavior Effects 0.000 description 1
- 201000005917 gastric ulcer Diseases 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 230000000968 intestinal Effects 0.000 description 1
- KFZMGEQAYNKOFK-UHFFFAOYSA-N iso-propanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- 239000000395 magnesium oxide Substances 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 150000002772 monosaccharides Chemical class 0.000 description 1
- 238000006386 neutralization reaction Methods 0.000 description 1
- 229920001542 oligosaccharide Polymers 0.000 description 1
- 150000002482 oligosaccharides Polymers 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 238000004321 preservation Methods 0.000 description 1
- 230000002035 prolonged Effects 0.000 description 1
- BDERNNFJNOPAEC-UHFFFAOYSA-N propanol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 description 1
- 230000000069 prophylaxis Effects 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 238000009331 sowing Methods 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- WQZGKKKJIJFFOK-PHYPRBDBSA-N α-D-galactose Chemical compound OC[C@H]1O[C@H](O)[C@H](O)[C@@H](O)[C@H]1O WQZGKKKJIJFFOK-PHYPRBDBSA-N 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N β-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
Abstract
The present invention discloses an orally applicable pharmaceutical composition, wherein the composition contains at least an anti-acid active substance, as well as additional ingredients. The composition has a liquid to semisolid consistency, said composition mainly being preservative-free. However, the composition comprises as additional ingredients more than 45 percent by weight of a sugar and/or cane alcohol, relative to the final composition, and up to 40 percent by weight of a pharmaceutically innocuous solvent, relative to same final composition.
Description
ORALLY APPLIED PHARMACEUTICAL COMPOSITION
DESCRIPTION OF THE INVENTION
The present invention is directed to a pharmaceutical composition applicable orally, with the characteristics of the generic part of patent claim 1. Pharmaceutical compositions orally applicable with at least one antacid active substance are known and commercially available for a long time. Depending on each active substance, respectively in each active substance mixture, these known antacids are used as tablets, coated tablets or as a powder for prophylaxis and / or for the treatment of stomach problems, particularly for dizziness treatments, stomach cramps , burning sensation or heartburn, feeling of rejection or vomiting, acid belching, vomiting, tympanitis, gastric ulcer and / or for the treatment of problems after alcohol or nicotine abuse. Therefore it is then necessary for the patient to chew or suck the corresponding tablets or coated tablets before they are swallowed, which usually leads to the adhesion of components of the tablet, respectively the covered tablet, to the dental area. and / or area of the mouth palate, so most patients do not like it and agree not to apply such compositions, even knowing that it is necessary. In order to solve these problems for the application of the known pharmaceutical compositions, until now it has been tried to generate a suspension of the active substance, in such a way that the suspensions are offered in their liquid form to the patient. It is therefore necessary that the known liquid composition contains a relatively high portion of aromatic substances in order to avoid the bad taste of the antacid active substance, respectively the mixture of the active substance. However, known suspensions always need a condom, so that condoms that have been customary have so far drastically decreased the taste of the known liquid composition or can cause allergic reactions and / or are suspected to be carcinogenic. The present invention has the objective of creating a liquid or semisolid pharmaceutical composition, with an active substance antacid, so that the composition has a particularly pleasant taste. This objective was carried out according to the invention, for a pharmaceutical composition with the significant characteristics of claim 1 of the patent.
The inventive composition contains, as initially mentioned in the prior art, at least one of the antacid active substances, respectively a mixture of the antacid active substance and still more other ingredients. An essential aspect of the inventive composition is that the inventive composition has a liquid to semi-solid consistency, whereby the inventive composition does not primarily contain preservatives. However, the inventive composition contains as other ingredients more than 45% by weight of sugar and / or cane alcohol, relative to the ready-to-use composition and up to 40% by weight of a pharmaceutically innocuous solvent, relative to the composition ready to be used. The inventive composition has a number of advantages. A first advantage is that the inventive composition is particularly easy to apply, due to its liquid to semi-solid consistency, since the problems described above do not occur in the known solid compositions, which means that it is not necessary to chew or suck with the mouth the inventive composition due to the liquid, respectively semi-solid consistency of the inventive composition. The inventive composition leads, due to its liquid to semi-solid consistency, a single dose, which is not easily carried out with respect to the known compositions. It can be diminished, conditioned by the fact that the inventive composition to an extensive degree of condoms, meaning that the inventive composition is generally preservative-free, taste problems do not occur in such liquid, respectively semi-solid inventive composition as this is the case of known suspensions. In the inventive composition the bad taste comes from the antacid active substance, respectively, the mixture of the antacid active substance is rather canceled out by the fact that the inventive composition contains at least 45% by weight of a sugar and / or an alcohol of cane, in such a way that this sugar, respectively cane alcohol, in the inventive composition not only cancels the bad taste of the active substance, but also gives a very pleasant taste to the inventive composition, when the inventive composition contains small amounts of sugar. a condom, such as 0.01% by weight and approximately 0.1% by weight. It was surprisingly observed that the inventive composition is microbiologically stable and thus self-sterilizable also without any preservative, therefore this positive property of the inventive composition refers to the high concentration of the sugar mentioned in the above, respectively the cane alcohol. In spite of the relatively large portion of sugar, respectively of cane alcohol, the inventive composition does not tend towards sedimentation or lumping of the antacid active substance, respectively the mixture of the active substance, in such a way that the inventive composition liquid to semisolid is stable per se, it is not necessary to stir the inventive composition before application to cause it to make a homogeneity of the active substance, respectively the mixture of the active substance. Furthermore, the consistency of the liquid to semisolid inventive composition causes the fact that the active substance antacid, respectively, the mixture of the active substance can be dispersed after the application of the inventive composition, very quickly and homogeneously on the stomach of the patients and the intestinal tract, in such a way that the inventive composition leads to a rapid elimination of pain and a rapid cure. Due to its liquid to semi-solid formulation the inventive composition can also be dosed very precisely and reproducibly or it can also be packaged in single doses, which is correspondingly the standardized manufacturing process. A first embodiment of the inventive composition is characterized in that the content of the solid substance of the liquid to semi-solid composition falls to a high percentage of 88% by weight, relative to the ready-to-use composition. In such a way that one embodiment of the inventive composition contains as active substances at least one antacid active substance, respectively, the mixture of the active substance, as well as the sugar and / or cane alcohol at the concentration mentioned above, therefore the inventive composition contains a suspending agent, respectively, as an emulsifier, at least 12% by weight of the pharmaceutically innocuous solvent mentioned in the above, relating to the ready-to-use composition. Thus, one embodiment has a high content of solid substance, it was surprisingly observed that in this embodiment no lumping and / or sedimentation of the antacid active substance occurs, even when the content of the solid substance varies between 65% by weight and 88% by weight, relative to the composition of the list to be used. In such a way, a modality provided for a homogeneous composition and. a regular distribution of the antacid active substance respectively, the mixture of the active substance, also after a storage time of several months. With respect to the solvent containing the inventive composition, it is noted that it is particularly a pharmaceutically innocuous solvent. The inventive composition preferably contains water as solvent, ethanol, propanol-1 and / or propanol-2 each alone or a mixture thereof, therefore the solvents mentioned above, particularly water, is preferably due to their absolute innocuous. Within the present invention the term water means all aqueous systems. A particularly suitable and highly effective inventive composition contains as the pharmaceutically innocuous solvent between 12% by weight and 35% by weight of water, relative to the ready-to-use composition. Here it is observed that this embodiment of the inventive composition is particularly pleasing to apply, since this embodiment has a very pleasant neutral taste, moreover due to the unpleasant taste characteristics of the antacid active substance, respectively mixture of the active substance, It is completely canceled by the high concentrations of sugar and / or cane alcohol. In such a liquid to semisolid formulation of the inventive composition a flocculation of the active substance, respectively mixture of the active substance or a phase of separation of the composition could not be observed, even if the inventive composition is stored for a long time without being shake Also with respect to the concentration of the antacid active substance, respectively the mixture of the antacid active substance, in the inventive composition, it is noted that this concentration depends on which daily doses are used of the inventive composition. The inventive composition contains in particular between 5% by weight and 43% by weight, preferably between 12% by weight and 30% by weight of the active substance antacid, whereby each of the concentrations mentioned in the above relate to the List composition to be used. With respect to at least one antacid active substance, respectively the mixture of the antacid active substance, which the inventive composition contains, it is important to note that this is a known antacid active substance, preferably aluminum hydroxide, magnesium hydroxide, trisilicate magnesium carbonate, magnesium carbonate, magnesium phosphate, calcium carbonate, calcium phosphate, sodium citrate, magnesium oxide, magaldrate, hydrotalcite, sodium acid carbonate and / or bismuth subcarbonate, whereby the active substance concentrations mentioned in the above, refer to anhydrous active substances. As mentioned in the above, the inventive composition contains as another ingredient more than 45% by weight of sugar and / or cane alcohol, relative to the ready-to-use composition. In the inventive composition, the concentration of sugar and / or cane alcohol varies between 45% by weight and 80% by weight, preferably 60% by weight and 80% by weight. Despite this relatively high concentration of sugar and / or cane alcohol in the inventive composition, the inventive composition in liquid to semi-solid form additionally has impeccable stability, so that flocculation, lumping or precipitation of the substance does not occur. active antacid, respectively the mixture of the antacid active substance, either during the manufacturing process, nor during extremely prolonged storage. In addition, the modalities mentioned in the above of the inventive composition having a sugar content, respectively a concentration of cane alcohol of between 45% by weight and 80% by weight, have an extremely pleasant taste and this in addition is self-sterilizable in such a manner. way in patients, particularly young patients, want to use it. Within the present application the term sugar means all monosaccharides, disaccharides and / or oligosaccharides, however, preferably sucrose
(sucrose), glucose, fructose, maltose, lactose, galactose and / or starch hydrolysates that are used in the pharmaceutical industry. One embodiment of the inventive composition is characterized in that it contains particularly sucrose as sugar. Within the present application the term cane alcohol means all the monomers, dimers and oligomers of known hydrogenated sugars, however, preferably sorbitol, mannitol, xylitol, malitol and / or hydrogenated starch hydrolysates which are used in the pharmaceutical industry. A particularly suitable embodiment of the inventive composition contains sorbitol, xylitol and / or malitol at the concentrations mentioned above, such as cane alcohol. Therefore, this embodiment is characterized particularly in the fact that they have a very pleasant taste and a high microbiological stability in such a way that this embodiment of the inventive composition is used favorably and without problems. In order to make the application of the simple inventive composition, a particularly developed advantage of the inventive composition is characterized in that it has a gelatinous consistency. Particularly if such gelatinous composition is packaged in simple doses, for example packaged and sealed in corresponding bags, the patient can, if necessary, use a measured amount of the inventive composition very quickly and simply, without risking a loss of part of the inventive composition. With respect to the other ingredients of the inventive composition, it is noted that these are pharmaceutically used ingredients and that they normally exist in a liquid to semi-solid composition. In order to ensure, for example, a desired consistency in the] 1
inventive composition, as for example the gelatinous consistency mentioned in the foregoing, the inventive composition may contain at least one suitable thickening agent, particularly between 0.2% by weight and 2% by weight, therefore xanthan gum is in particular provided herein, guar gum and / or cellulose derivatives, preferably microcrystalline cellulose, methylcellulose, hydroxyethylcellulose, methylhydroxypropylcellulose and / or particularly suitable hydroxypropylcellulose. It is further recommended that the inventive composition contain, however, as an ingredient between 2% by weight and 8% by weight of glycerol as well as between 0.05% by weight and 0.7% by weight of an aromatic substance. A particularly suitable formulation of the inventive composition contains as main substances 12% by weight - 28% by weight of the active substance antacid, respectively the mixture of the active substance, 46% by weight - 58% by weight of the sugar and / or alcohol of cane, as well as 18% by weight - 30% by weight of water, therefore then this composition contains, if necessary 0 - 10% by weight of other components, particularly glycerol, thickening agents and / or aromatic substances. The development of the advantages of the inventive composition are indicated in the subclaims.
32-
In the following the inventive composition is described in more detail by three examples.
Example 1
A gelatinous formulation was manufactured in such a way that it contains the following ingredients: 13.33 g of aluminum oxide, hydrated with a concentration of approximately 50% by weight of AI2O3 (dry); 13.33 g of magnesium hydroxide powder, anhydrous; 52.5 g of a sorbitol solution, 70% by weight in non-crystalline water; 15.0 g of a solution of malitol, 80% by weight in water (licasine); 5.34 g of glycerol, 85% by weight; 0.35 g of xanthan gum; and 0.15 g of aromatic substances. For the preparation of this gelatinous formulation first all the glycerol is added to the solution of the cane alcohols. After this the hydrous aluminum oxide as well as the magnesium hydroxide are suspended in this mixture. The aromatic substances are added to the prepared mixture which was then taken to]
through stirring and then the mixture is thickened with xanthan gum. The gelatinous formulation manufactured in this way has a concentration of antacid active substances of 26.7% by weight, a water content of 19.6% by weight as well as a content of cane alcohol of 48.8% by weight, so all these concentrations they relate to the list composition to be used.
Example 2
A second gelatinous formulation was manufactured, having the following main components: 10.00 g of aluminum oxide, hydrated, with a solids content, of Al203 of 50% by weight; 10.00 g magnesium hydroxide powder, anhydrous; 79.86 g of sugar syrup (64% by weight of dry substance); and 0.14 g of aromatic substances. For the manufacture of this formulation the aqueous sugar syrup was subjected. The hydrous aluminum oxide and the powdered magnesium hydroxide are suspended in this aqueous sugar syrup. Subsequently the aromatic substances are added. After completely mixing, a resulting gelatinous formulation having a concentration of the antacid active substance mixture of 20% by weight (calculated as an anhydrous substance), a water content of 28.7% by weight and a sugar content of 51.1% by weight (calculated as the anhydrous substance), each relative to the ready-to-use composition.
Example 3
A third semi-solid formulation was manufactured, whereby this semisolid formulation contains the following ingredients: 13.3 g of calcium carbonate; 62.0 g of a sorbitol solution in water, 70% by weight, non-crystalline; 17.8 g of a solution of malitol in water, 80% by weight (licasine); 6.31 g of glycerol, 85% by weight; 0.42 g of xanthan gum; and 0.17 g of aromatic substances. The production according to Example 3 was carried out exactly as described above for the manufacture of the composition according to Example 1. Ready-to-use semisolid formulation 3 contains a concentration of 13.3% by weight of the active antacid active substance. (calculated as an anhydrous substance), 22.3% by weight of water, as well as 57.6% by weight of cane alcohol (calculated as anhydrous substance). For acceptance verification, the gelatinous formulation, according to the example 1 that had the highest concentration of the acid-proofing substances of the taste test, was distributed to 50 volunteers, so they were compared with a suspension normally existing in the market, it was used for this flavor-oriented test. In order to objectify this test examination, the 50 test subjects first received the formulation three times according to example 1, therefore a period of one week was determined between each of the single tests. After a taste neutralization phase, which means a three-hour break and repeated drinking of water, the normal suspension was then given to the test persons. In each of the three tests, 47 test persons reported that the formulation according to example 1 had an essentially better taste than the normal suspension, therefore 44 test persons reported that the formulation according to example 1 did not cause them No effect of the sweet residue few minutes after the test.
The phase 3 test described in the above was repeated after one month, therefore the same persons of the test, first tested the normal suspension and after a period of three hours they tested the formulation according to example 1, although several water drinks were repeated. Therefore 49 people unanimously reported that the formulation according to Example 1 had an essentially better taste, while the normal suspension had an unpleasant taste even though they were rinsed several times with water. In order to test the microbiological stability of the formulation according to example 1, the following examination was carried out: A verification of the formulation according to example 1, was carried out with respect to antimicrobial preservation according to the DAB 10, 3. published in 1994. The result of the examination of this verification is indicated in the following table, so that the inoculation was carried out with 0.3 ml of germ suspension.
-u- Table 1
Strain culture of bacterial number per g / ml deposit sowing after a period of
immediately 4 dig? Red.F. 28 days i 4,909,000 4,800,000 240 10 '230
2 4,991,000 800,000 230 10 '260
3 3,569,000 275,660 200 10 '250' 4 3,169,000 36,036 220 10 '250 5 1,500,000 900,000 180 > ? o- 100 6 3,918,000 1,703,000 200 164 7 1,455,000 53,423 250 800 6 250 200 170
1 = Staph. aureue 2 = Escherichia col i 3 = Ps. aeruginosa 4 = Candida albicans 5 = Aspergillus niger 6 = Zygosacch. rouxii 7 = dirty water 8 = control, without inoculation
Having described the invention as above, property is claimed as contained in the following:
Claims (12)
1. An orally applicable pharmaceutical composition, whereby the composition contains at least one antacid active substance, as well as other ingredients, characterized in that the composition has a liquid to semi-solid consistency, so that the composition is mainly preservative-free and that the composition contains as other ingredients more than 45% by weight of a sugar and / or cane alcohol, relative to the ready-to-use composition and up to 40% by weight of a pharmaceutically innocuous solvent, relative to the ready-to-use composition. .
2. The pharmaceutical composition according to claim 1, characterized in that the content of the solid substance of the liquid to semi-solid composition falls to a maximum of 88% by weight, relative to the ready-to-use composition.
3. The pharmaceutical composition according to claim 1 or 2, characterized in that the composition contains water as a pharmaceutically innocuous solvent.
4. The pharmaceutical composition according to one of the preceding claims, characterized in that the composition contains between 12% by weight and 35% by weight of water, relative to the ready-to-use composition.
5. The pharmaceutical composition according to one of the preceding claims, characterized in that the composition contains between 5% by weight and 43% by weight, preferably between 12% by weight and 30% by weight of the antacid active ingredient, relative to the composition of ready to be used.
6. The pharmaceutical composition according to one of the preceding claims, characterized in that the composition contains aluminum hydroxide, magnesium hydroxide, magnesium trisilicate, magnesium carbonate, magnesium phosphate, calcium carbonate, calcium phosphate, sodium citrate, oxide of magnesium, magaldrate, hydrotalcite, sodium acid carbonate and / or bismuth subcarbonate as an antacid active substance.
7. The pharmaceutical composition according to one of the preceding claims, characterized in that the composition contains sugar and / or cane alcohol in a concentration between 45% by weight and 80% by weight, preferably between 48% by weight and 70% by weight. % by weight, each relative to the list composition to be used.
8. The pharmaceutical composition according to one of the preceding claims, characterized in that the composition contains sorbitol and / or maltitol as cane alcohol.
9. The pharmaceutical composition according to one of the preceding claims, characterized in that the composition contains sucrose as sugar.
10. The pharmaceutical composition according to one of the preceding claims, characterized in that the composition has a gelatinous consistency.
11. The pharmaceutical composition according to one of the preceding claims, characterized in that the composition also contains as ingredients between 2% by weight and 8% by weight of glycerol, between 0.2% by weight and 2% by weight of a thickening agent, particularly rubber xanthan, guar gum and / or a cellulose derivative, preferably microcrystalline cellulose, methylcellulose, hydroxyethylcellulose, rnethylhydroxypropylcellulose and / or hydroxypropylcellulose and between 0.05% by weight and 0.7% by weight of an aromatic substance.
12. The pharmaceutical composition according to one of the preceding claims, characterized in that the composition contains as main components 12% by weight - 28% by weight of the active substance antacid, respectively the mixture of the active substance, 46% by weight - 58% by weight of sugar and / or cane alcohol, as well as 18% by weight - 30% by weight of water.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19529862.4 | 1995-08-14 | ||
| DE19529862A DE19529862A1 (en) | 1995-08-14 | 1995-08-14 | Pharmaceutical preparation for oral use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX9602270A MX9602270A (en) | 1997-10-31 |
| MXPA96002270A true MXPA96002270A (en) | 1998-07-03 |
Family
ID=
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