CA1042796A - Therapeutic composition containing a psychosedative and an antacid - Google Patents
Therapeutic composition containing a psychosedative and an antacidInfo
- Publication number
- CA1042796A CA1042796A CA226,816A CA226816A CA1042796A CA 1042796 A CA1042796 A CA 1042796A CA 226816 A CA226816 A CA 226816A CA 1042796 A CA1042796 A CA 1042796A
- Authority
- CA
- Canada
- Prior art keywords
- antacid
- psychosedative
- weight
- antiflatulent
- magnesium
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
Links
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical class [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 title claims abstract description 26
- 229940069428 antacid Drugs 0.000 title claims abstract description 26
- 239000003159 antacid agent Substances 0.000 title claims abstract description 26
- 230000001458 anti-acid effect Effects 0.000 title claims abstract description 22
- 230000001225 therapeutic effect Effects 0.000 title claims abstract description 6
- 239000000203 mixture Substances 0.000 title claims description 11
- 239000003814 drug Substances 0.000 claims abstract description 20
- 238000000034 method Methods 0.000 claims abstract description 15
- 239000002671 adjuvant Substances 0.000 claims abstract description 6
- 239000012876 carrier material Substances 0.000 claims abstract description 6
- 238000004519 manufacturing process Methods 0.000 claims abstract description 4
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 claims description 10
- 229910021502 aluminium hydroxide Inorganic materials 0.000 claims description 10
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 claims description 10
- 239000001095 magnesium carbonate Substances 0.000 claims description 10
- 229910000021 magnesium carbonate Inorganic materials 0.000 claims description 10
- 239000000395 magnesium oxide Substances 0.000 claims description 10
- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 claims description 10
- 235000012245 magnesium oxide Nutrition 0.000 claims description 10
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 claims description 10
- VMIYHDSEFNYJSL-UHFFFAOYSA-N Bromazepam Chemical compound C12=CC(Br)=CC=C2NC(=O)CN=C1C1=CC=CC=N1 VMIYHDSEFNYJSL-UHFFFAOYSA-N 0.000 claims description 8
- 229960002729 bromazepam Drugs 0.000 claims description 7
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims description 6
- 150000001557 benzodiazepines Chemical class 0.000 claims description 6
- 239000004205 dimethyl polysiloxane Substances 0.000 claims description 5
- 235000013870 dimethyl polysiloxane Nutrition 0.000 claims description 5
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 claims description 5
- MWQCHHACWWAQLJ-UHFFFAOYSA-N Prazepam Chemical compound O=C1CN=C(C=2C=CC=CC=2)C2=CC(Cl)=CC=C2N1CC1CC1 MWQCHHACWWAQLJ-UHFFFAOYSA-N 0.000 claims description 4
- SEQDDYPDSLOBDC-UHFFFAOYSA-N Temazepam Chemical compound N=1C(O)C(=O)N(C)C2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 SEQDDYPDSLOBDC-UHFFFAOYSA-N 0.000 claims description 4
- ADIMAYPTOBDMTL-UHFFFAOYSA-N oxazepam Chemical compound C12=CC(Cl)=CC=C2NC(=O)C(O)N=C1C1=CC=CC=C1 ADIMAYPTOBDMTL-UHFFFAOYSA-N 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- DIWRORZWFLOCLC-HNNXBMFYSA-N (3s)-7-chloro-5-(2-chlorophenyl)-3-hydroxy-1,3-dihydro-1,4-benzodiazepin-2-one Chemical compound N([C@H](C(NC1=CC=C(Cl)C=C11)=O)O)=C1C1=CC=CC=C1Cl DIWRORZWFLOCLC-HNNXBMFYSA-N 0.000 claims description 3
- 239000005995 Aluminium silicate Substances 0.000 claims description 3
- 239000004480 active ingredient Substances 0.000 claims description 3
- 229940001004 aluminium glycinate Drugs 0.000 claims description 3
- 235000012211 aluminium silicate Nutrition 0.000 claims description 3
- PZZYQPZGQPZBDN-UHFFFAOYSA-N aluminium silicate Chemical compound O=[Al]O[Si](=O)O[Al]=O PZZYQPZGQPZBDN-UHFFFAOYSA-N 0.000 claims description 3
- 229910000323 aluminium silicate Inorganic materials 0.000 claims description 3
- RUJUQAPQALJUPC-UHFFFAOYSA-K bis[(2-aminoacetyl)oxy]alumanyl 2-aminoacetate Chemical compound [Al+3].NCC([O-])=O.NCC([O-])=O.NCC([O-])=O RUJUQAPQALJUPC-UHFFFAOYSA-K 0.000 claims description 3
- 229960004782 chlordiazepoxide Drugs 0.000 claims description 3
- ANTSCNMPPGJYLG-UHFFFAOYSA-N chlordiazepoxide Chemical compound O=N=1CC(NC)=NC2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 ANTSCNMPPGJYLG-UHFFFAOYSA-N 0.000 claims description 3
- 229960003932 cloxazolam Drugs 0.000 claims description 3
- ZIXNZOBDFKSQTC-UHFFFAOYSA-N cloxazolam Chemical compound C12=CC(Cl)=CC=C2NC(=O)CN2CCOC21C1=CC=CC=C1Cl ZIXNZOBDFKSQTC-UHFFFAOYSA-N 0.000 claims description 3
- 229960003529 diazepam Drugs 0.000 claims description 3
- AAOVKJBEBIDNHE-UHFFFAOYSA-N diazepam Chemical compound N=1CC(=O)N(C)C2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 AAOVKJBEBIDNHE-UHFFFAOYSA-N 0.000 claims description 3
- 229960004391 lorazepam Drugs 0.000 claims description 3
- VTHJTEIRLNZDEV-UHFFFAOYSA-L magnesium dihydroxide Chemical compound [OH-].[OH-].[Mg+2] VTHJTEIRLNZDEV-UHFFFAOYSA-L 0.000 claims description 3
- 239000000347 magnesium hydroxide Substances 0.000 claims description 3
- 229910001862 magnesium hydroxide Inorganic materials 0.000 claims description 3
- 239000000391 magnesium silicate Substances 0.000 claims description 3
- 229910052919 magnesium silicate Inorganic materials 0.000 claims description 3
- 235000019792 magnesium silicate Nutrition 0.000 claims description 3
- ZADYMNAVLSWLEQ-UHFFFAOYSA-N magnesium;oxygen(2-);silicon(4+) Chemical compound [O-2].[O-2].[O-2].[Mg+2].[Si+4] ZADYMNAVLSWLEQ-UHFFFAOYSA-N 0.000 claims description 3
- 229960002225 medazepam Drugs 0.000 claims description 3
- 229910052751 metal Inorganic materials 0.000 claims description 3
- 239000002184 metal Substances 0.000 claims description 3
- 229960004535 oxazepam Drugs 0.000 claims description 3
- VCCZBYPHZRWKFY-XIKOKIGWSA-N oxazolam Chemical compound C1([C@]23C4=CC(Cl)=CC=C4NC(=O)CN2C[C@H](O3)C)=CC=CC=C1 VCCZBYPHZRWKFY-XIKOKIGWSA-N 0.000 claims description 3
- 229950006124 oxazolam Drugs 0.000 claims description 3
- 230000000737 periodic effect Effects 0.000 claims description 3
- 229960004856 prazepam Drugs 0.000 claims description 3
- 229910000030 sodium bicarbonate Inorganic materials 0.000 claims description 3
- 235000017557 sodium bicarbonate Nutrition 0.000 claims description 3
- 229960003188 temazepam Drugs 0.000 claims description 3
- 229910000019 calcium carbonate Inorganic materials 0.000 claims description 2
- 239000000378 calcium silicate Substances 0.000 claims description 2
- 229910052918 calcium silicate Inorganic materials 0.000 claims description 2
- OYACROKNLOSFPA-UHFFFAOYSA-N calcium;dioxido(oxo)silane Chemical compound [Ca+2].[O-][Si]([O-])=O OYACROKNLOSFPA-UHFFFAOYSA-N 0.000 claims description 2
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 claims 4
- XBWAZCLHZCFCGK-UHFFFAOYSA-N 7-chloro-1-methyl-5-phenyl-3,4-dihydro-2h-1,4-benzodiazepin-1-ium;chloride Chemical compound [Cl-].C12=CC(Cl)=CC=C2[NH+](C)CCN=C1C1=CC=CC=C1 XBWAZCLHZCFCGK-UHFFFAOYSA-N 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 claims 2
- 229910000027 potassium carbonate Inorganic materials 0.000 claims 2
- 235000014380 magnesium carbonate Nutrition 0.000 claims 1
- 235000012254 magnesium hydroxide Nutrition 0.000 claims 1
- 235000011181 potassium carbonates Nutrition 0.000 claims 1
- 125000003310 benzodiazepinyl group Chemical class N1N=C(C=CC2=C1C=CC=C2)* 0.000 abstract 1
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 6
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 4
- YLCXGBZIZBEVPZ-UHFFFAOYSA-N Medazepam Chemical compound C12=CC(Cl)=CC=C2N(C)CCN=C1C1=CC=CC=C1 YLCXGBZIZBEVPZ-UHFFFAOYSA-N 0.000 description 3
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 3
- 235000019359 magnesium stearate Nutrition 0.000 description 3
- 206010052813 Aerophagia Diseases 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 230000001055 chewing effect Effects 0.000 description 2
- AMTWCFIAVKBGOD-UHFFFAOYSA-N dioxosilane;methoxy-dimethyl-trimethylsilyloxysilane Chemical compound O=[Si]=O.CO[Si](C)(C)O[Si](C)(C)C AMTWCFIAVKBGOD-UHFFFAOYSA-N 0.000 description 2
- 206010016766 flatulence Diseases 0.000 description 2
- 235000010355 mannitol Nutrition 0.000 description 2
- 229940083037 simethicone Drugs 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- DBFLXAXACNTBEP-UHFFFAOYSA-N 5-phenyl-3h-1,4-benzodiazepine Chemical compound N=1CC=NC2=CC=CC=C2C=1C1=CC=CC=C1 DBFLXAXACNTBEP-UHFFFAOYSA-N 0.000 description 1
- UZKCXUDBQQFNIW-UHFFFAOYSA-N 7,8-dihydro-1,4-benzodiazepin-6-one Chemical compound N1=CC=NC=C2C(=O)CCC=C21 UZKCXUDBQQFNIW-UHFFFAOYSA-N 0.000 description 1
- 206010020601 Hyperchlorhydria Diseases 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- VCCZBYPHZRWKFY-UHFFFAOYSA-N Oxazolam Chemical compound O1C(C)CN2CC(=O)NC3=CC=C(Cl)C=C3C21C1=CC=CC=C1 VCCZBYPHZRWKFY-UHFFFAOYSA-N 0.000 description 1
- 102000057297 Pepsin A Human genes 0.000 description 1
- 108090000284 Pepsin A Proteins 0.000 description 1
- 208000008469 Peptic Ulcer Diseases 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 150000001447 alkali salts Chemical class 0.000 description 1
- 239000012736 aqueous medium Substances 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 201000006549 dyspepsia Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 230000004970 emotional disturbance Effects 0.000 description 1
- 230000002996 emotional effect Effects 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 208000024798 heartburn Diseases 0.000 description 1
- 150000004679 hydroxides Chemical class 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 150000002739 metals Chemical class 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 150000002894 organic compounds Chemical class 0.000 description 1
- 230000008506 pathogenesis Effects 0.000 description 1
- 229940111202 pepsin Drugs 0.000 description 1
- 208000011906 peptic ulcer disease Diseases 0.000 description 1
- 229920000191 poly(N-vinyl pyrrolidone) Polymers 0.000 description 1
- 229920001515 polyalkylene glycol Polymers 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 208000020016 psychiatric disease Diseases 0.000 description 1
- 230000003236 psychic effect Effects 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
ABSTRACT
A process for the manufacture of a medicament, which process comprises mixing together a psychosedative from the benzodiazepine series, an antacid and an antiflatulent and, if desired, a carrier material and/or adjuvant suitable for therapeutic administration.
A process for the manufacture of a medicament, which process comprises mixing together a psychosedative from the benzodiazepine series, an antacid and an antiflatulent and, if desired, a carrier material and/or adjuvant suitable for therapeutic administration.
Description
1~)4;~79f~
The present invention is concerned with medicaments and a process for the manufacture thereof.
The medicaments provided by the present invention contain as the active ingredients a psychosedative from the benzodiazepine series, from 50 to 1000 parts by weight of an antacid and from 10 to 150 parts by weight of an antiflatulent per part by weight of psychosedative and, optionally, a compatible carrier material or adjuvant or both suitable for therapeutic administration.
Of the customary antacids which can be present in the medicaments provided by the present invention, there may be mentioned, in particular, salts, hydroxides and oxides of metals of the first to third group of the periodic system as well as mixtures and coprecipitates thereof. Preferred antacids for the purpose of the present invention are aluminium hydroxide (especially colloidal), aluminium glycinate, aluminium silicate, calcium silicate, calcium carbonate, magnesium oxide, magnesium hydroxide, magnesium carbonate, magnesium silicate, sodium bicarbonate and potassium carbonateO
Especially preferred are aluminium hydroxide/magnesium carbonate coprecipitate - and magnesium oxide as well as, in particular, mixtures thereof, with a quantitative ratio of 5:1 being especially favourableO
2a Of the customary antiflatulents which can be present in the `;~ medicaments provided by the present invention, there may be mentioned, in particular, polysiloxanesO Especially ~ ' 1~34;~79~6 preferred is dimethylpolysiloxane, which is used, in particular, in the form of Medic.~l ~ntifoam (~imethicone).
Psychosedatives from the benzodiazepine series suitable for use in the present invention are, inter alia, 7-chloro-
The present invention is concerned with medicaments and a process for the manufacture thereof.
The medicaments provided by the present invention contain as the active ingredients a psychosedative from the benzodiazepine series, from 50 to 1000 parts by weight of an antacid and from 10 to 150 parts by weight of an antiflatulent per part by weight of psychosedative and, optionally, a compatible carrier material or adjuvant or both suitable for therapeutic administration.
Of the customary antacids which can be present in the medicaments provided by the present invention, there may be mentioned, in particular, salts, hydroxides and oxides of metals of the first to third group of the periodic system as well as mixtures and coprecipitates thereof. Preferred antacids for the purpose of the present invention are aluminium hydroxide (especially colloidal), aluminium glycinate, aluminium silicate, calcium silicate, calcium carbonate, magnesium oxide, magnesium hydroxide, magnesium carbonate, magnesium silicate, sodium bicarbonate and potassium carbonateO
Especially preferred are aluminium hydroxide/magnesium carbonate coprecipitate - and magnesium oxide as well as, in particular, mixtures thereof, with a quantitative ratio of 5:1 being especially favourableO
2a Of the customary antiflatulents which can be present in the `;~ medicaments provided by the present invention, there may be mentioned, in particular, polysiloxanesO Especially ~ ' 1~34;~79~6 preferred is dimethylpolysiloxane, which is used, in particular, in the form of Medic.~l ~ntifoam (~imethicone).
Psychosedatives from the benzodiazepine series suitable for use in the present invention are, inter alia, 7-chloro-
-2-methylamino~5-phenyl-3H-1,4-benzodiazepine 4-oxide (chlordiazepoxide), 7-chloro-1,3-dihydro-1-methyl-5-phenyl--2H-1,4-benzodiazepin-~-one (diazepam), 7-chloro-2,3-dihydro--l-methyl-5-phenyl-lH-1,4-benzodiazepine (medazepam), 7-bromo--1,3-dihydro-5-(2-pyridyl)-2H-1,4-benzodiazepin-2-one (bromazepam) 10-chloro-llb-(2-chlorophenyl)-2,3,5,1lb--tetrahydrooxazolo[3,2-d][1,4]benzodiazepin-6(7H)-one (cloxazolazepam), 7-chloro-5-(2-chlorophenyl)-1,3-dihydro-
-3-hydroxy-2H-1,4-benzodiazepin-2-one (lorazepam), 7-chloro--1,3-dihydro-3-hydroxy-5-phenyl-2H-1,4-benzodiazepin-2-one (oxazepam), 10-chloro-2,3,5,11b-tetrahydro-2-methyl-llb--phenyloxazolo [3,2-d][1,4]benzodiazepin-6(7H)-one (oxazolazepam), 7-chloro-1-cyclopropylmethyl-1,3-dihydro-5-phenyl-2H-1,4--benzodiazepin-2-one (prazepam) and 7-chloro-1,3-dihydro-3--hydroxy-l-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one (temazepam~ as well as analogues thereof. The said psychosedatives can also be present in the form of pharmaceutically acceptable salts.
The quantitative ratio of the active ingredients in the medicaments provided by the present invention can vary within ~9S' /~ C-:~eC( abDve, relatively wide limits.~ From about 50 to 1000 parts by weight of antacid and from 10 to 150 parts by weight of antiflatulent are oxpr~i ntll presert per part by weight of psychosedetive.
.'' .
~ 3 -,', . . .
. ~
., ~.
~34'~796 Preferably from lO0 to 700 parts by weight of antacid and from 15 to 125 parts by weight of antiflatulent are present per part by weight of p~ychosedative.
A preferred unit dosage for adults contains from 0.5 to 5 mg of psychosedative,from 500 to 700 mg of antacid and from 75 to 125 mg of antiflatulent.
~he medicaments provided by the present invention are intended for the treatment of gastric hyperacidity and its effects (heartburn, peptic ulcer) as well as of a feeling of repletion and flatulence resulting from aerophagia and meteorism.
~hese symptoms are very frequently an expression or concomitant symptom of an emotional disturbance. ~hus, a significant relation between emotional stress and increased production of hydrochloric acid and pepsin has been demonstrated by numerous researchers. Moreover, not only practical clinical experience but also objective studies substantiate the important role played by the "nervous element" in aerophagia.
From the causative role of psychic factors in the pathogenesis of the said disturbances, it is evident that their effective treatment should not be limited to the symptomatic influence on the local occurrence by the administration of antacids and antiflatulents but, rather, that suitable measures should also be taken for the elimination of the basic psychic disturbance.
~)4~:796 It is known, however, that the basic salts used as antacids have the capability in aqueous media of adsorbing various organic compounds.
Accordingly, having regard to the relatively low dosage of psychosedative in comparison to antacid in the present medicaments, an insufficient resorption of ~he psychosedative would have been expected. Surprisingly, it has been found that this is not the case with the medicaments provided by the present inventionO
According to the process provided by the present invention, the medicaments aforesaid are manufactured by mixing together a psychosedative from the benzodiazepine series, from 50 to 1000 parts by weight of an antacid and from 10 to 150 parts by weight of an antiflatulent per part by weight of psychosedative and, optionally, a compatible carrier material or adjuvant or both suitable for therapeutic administration.
The mixture obtained can be brought into suitable oral dosage forms (e.g. tablets, capsules, syrups or chewing tablets) according to well-known methods. Examples of carrier materials and adjuvants are water, lactose, starch, magnesium stearate, talc and polyalkyleneglycols as well as ; flavouring substances, preservatives, stabilisers, wetting agents and emulsifiers.
i~)4'~796 The following Example illustrates the present invention:
Example Chewing tablets containing the following ingredients are manufactured:
Bromazepam 1.0 mg Aluminium hydroxide/magnesium carbonate coprecipitate500.0 mg ; Magnesium oxide 100.0 mg ; Simethicone 100.0 mg Sugar 640.0 mg D-Mannitol 600.0 mg LUVISKOL K 90 20.0 mg Magnesium stearate 20.0 mg Aroma q.s.ad. 2000.0 m~
Simethicone and magnesium oxide are stirred into an aqueous-alcoholic solution of L W ISKOL K 90. Subsequently, a mixture consisting of aluminium hydroxide/magnesium carbonate coprecipitate, D-Mannitol and a premix of bromazepam and sugar i9 added thereto with stirring. ~he moist mass is granulated, dried and sieved. A mixture of magnesium stearate and aroma material i9 added to this granulate. The mixture i5 mixed and pressed to tablets.
ema~K
: `:
The quantitative ratio of the active ingredients in the medicaments provided by the present invention can vary within ~9S' /~ C-:~eC( abDve, relatively wide limits.~ From about 50 to 1000 parts by weight of antacid and from 10 to 150 parts by weight of antiflatulent are oxpr~i ntll presert per part by weight of psychosedetive.
.'' .
~ 3 -,', . . .
. ~
., ~.
~34'~796 Preferably from lO0 to 700 parts by weight of antacid and from 15 to 125 parts by weight of antiflatulent are present per part by weight of p~ychosedative.
A preferred unit dosage for adults contains from 0.5 to 5 mg of psychosedative,from 500 to 700 mg of antacid and from 75 to 125 mg of antiflatulent.
~he medicaments provided by the present invention are intended for the treatment of gastric hyperacidity and its effects (heartburn, peptic ulcer) as well as of a feeling of repletion and flatulence resulting from aerophagia and meteorism.
~hese symptoms are very frequently an expression or concomitant symptom of an emotional disturbance. ~hus, a significant relation between emotional stress and increased production of hydrochloric acid and pepsin has been demonstrated by numerous researchers. Moreover, not only practical clinical experience but also objective studies substantiate the important role played by the "nervous element" in aerophagia.
From the causative role of psychic factors in the pathogenesis of the said disturbances, it is evident that their effective treatment should not be limited to the symptomatic influence on the local occurrence by the administration of antacids and antiflatulents but, rather, that suitable measures should also be taken for the elimination of the basic psychic disturbance.
~)4~:796 It is known, however, that the basic salts used as antacids have the capability in aqueous media of adsorbing various organic compounds.
Accordingly, having regard to the relatively low dosage of psychosedative in comparison to antacid in the present medicaments, an insufficient resorption of ~he psychosedative would have been expected. Surprisingly, it has been found that this is not the case with the medicaments provided by the present inventionO
According to the process provided by the present invention, the medicaments aforesaid are manufactured by mixing together a psychosedative from the benzodiazepine series, from 50 to 1000 parts by weight of an antacid and from 10 to 150 parts by weight of an antiflatulent per part by weight of psychosedative and, optionally, a compatible carrier material or adjuvant or both suitable for therapeutic administration.
The mixture obtained can be brought into suitable oral dosage forms (e.g. tablets, capsules, syrups or chewing tablets) according to well-known methods. Examples of carrier materials and adjuvants are water, lactose, starch, magnesium stearate, talc and polyalkyleneglycols as well as ; flavouring substances, preservatives, stabilisers, wetting agents and emulsifiers.
i~)4'~796 The following Example illustrates the present invention:
Example Chewing tablets containing the following ingredients are manufactured:
Bromazepam 1.0 mg Aluminium hydroxide/magnesium carbonate coprecipitate500.0 mg ; Magnesium oxide 100.0 mg ; Simethicone 100.0 mg Sugar 640.0 mg D-Mannitol 600.0 mg LUVISKOL K 90 20.0 mg Magnesium stearate 20.0 mg Aroma q.s.ad. 2000.0 m~
Simethicone and magnesium oxide are stirred into an aqueous-alcoholic solution of L W ISKOL K 90. Subsequently, a mixture consisting of aluminium hydroxide/magnesium carbonate coprecipitate, D-Mannitol and a premix of bromazepam and sugar i9 added thereto with stirring. ~he moist mass is granulated, dried and sieved. A mixture of magnesium stearate and aroma material i9 added to this granulate. The mixture i5 mixed and pressed to tablets.
ema~K
: `:
Claims (18)
PROPERTY OR PRIVILEGE IS CLAIMED ARE DEFINED AS FOLLOWS:
1. A process for the manufacture of a medicament, which process comprises mixing together a psychosedative from the benzodiazepine series, from 50 to 1000 parts by weight of an antacid and from 10 to 15% parts by weight of an antiflatulent per part by weight of psychosedative and, optionally, a carrier material or adjuvant or both suitable for therapeutic administration.
2, A process according to claim 1, wherein chlordiazepoxide, diazepam, medazepam, bromazepam, cloxazolazepam, lorazepam, oxazepam, oxazolazepam, prazepam or temazepam is used as the psychosedative from the benzodiazepine series.
3. A process according to claim 1, wherein a salt, hydroxide or oxide of a metal of the first to third group of the periodic system or a mixture or coprecipitate thereof is used as the antacid.
4. A process according to claim 3, wherein aluminium hydroxide, aluminium glycinate, aluminium silicate, calcium silicate, calcium carbonate, magnesium oxide, magnesium hydroxide, magnesium carbonate, magnesium silicate, sodium bicarbonate or potassium carbonate is used as the antacid.
5. A process according to claim 3, wherein aluminium hydroxide/
magnesium carbonate coprecipitate or magnesium oxide or a mixture thereof is used as the antacid.
magnesium carbonate coprecipitate or magnesium oxide or a mixture thereof is used as the antacid.
6. A process according to any one of claims 1 to 3 inclusive, wherein dimethylpolysiloxane is used as the antiflatulent.
7. A process according to any one of claims 1 to 3 inclusive, wherein bromazepam is used as the psychosedative, aluminium hydroxide/magnesium carbonate coprecipitate and magnesium oxide is used as the antacid and dimethylpolysiloxane is used as the antiflatulent.
8. A process according to claim 1, wherein from 100 to 700 parts by weight of antacid and from 15 to 125 parts by weight of antiflatulent are used per part by weight of psychosedative.
9. A process according to claim 9, wherein a unit dosage form contain-ing from about 0.5 to 5 mg of psychosedative, from 500 to 700 mg of antacid and from 75 to 125 mg of antiflatulent is manufactured.
10. A medicament containing as the active ingredients a psychosedative from the benzodiazepine series, from 50 to 1000 parts by weight of an antacid and from 10 to 150 parts by weight of an antiflatulent per part by weight of psychosedative and, optionally, a compatible carrier material or adjuvant or both suitable for therapeutic administration.
11. A medicament according to claim 10, wherein said psychosedative is chlordiazepoxide, diazepam, medazepam, bromazepam, cloxazolazepam, lorazepam, oxazepam, oxazolazepam, prazepam or temazepam.
12. A medicament according to claim 10, wherein the antacid is a salt, hydroxide or oxide of a metal of the first to third group of the periodic system or a mixture or coprecipitate thereof.
13. A medicament according to claim 12, wherein the antacid is aluminium hydroxide, aluminium glycinate, aluminium silicate, magnesium carbonate, magnesium oxide, magnesium hydroxide, magnesium silicate, sodium bicarbonate or potassium carbonate.
14. A medicament according to claim 12, wherein the antacid is aluminium hydroxide/magnesium carbonate coprecipitate or magnesium oxide or a mixture thereof.
15. A medicament according to any one of claims 10 to 12 inclusive, wherein the antiflatulent is dimethylpolysiloxane.
16. A medicament according to any one of claims 10 to 12 inclusive, wherein the psychosedative is bromazepam, the antacid is aluminium hydroxide/
magnesium carbonate coprecipitate and magnesium oxide and the antiflatulent is dimethylpolysiloxane.
magnesium carbonate coprecipitate and magnesium oxide and the antiflatulent is dimethylpolysiloxane.
17. A medicament according to claim 10 containing from 100 to 700 parts by weight of antacid and from 15 to 125 parts by weight of antiflatulent per part by weight of psychosedative.
18. A medicament according to claim 12 in unit dosage form containing from about 0.5 to 5 mg of psychosedative, from 500 to 700 mg of antacid and from 75 to 125 mg of antiflatulent.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH672374 | 1974-05-16 | ||
| CH1095674 | 1974-08-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA1042796A true CA1042796A (en) | 1978-11-21 |
Family
ID=25700062
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA226,816A Expired CA1042796A (en) | 1974-05-16 | 1975-05-13 | Therapeutic composition containing a psychosedative and an antacid |
Country Status (6)
| Country | Link |
|---|---|
| AR (1) | AR212907A1 (en) |
| CA (1) | CA1042796A (en) |
| DE (1) | DE2517585A1 (en) |
| FR (1) | FR2270886A1 (en) |
| NL (1) | NL7504704A (en) |
| PH (1) | PH13370A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5599577A (en) * | 1992-05-21 | 1997-02-04 | Mcneil-Ppc, Inc. | Simethicone containing pharmaceutical compositions |
| US6038608A (en) * | 1996-11-25 | 2000-03-14 | Nec Corporation | Virtual LAN system |
| US7341742B2 (en) | 2002-09-30 | 2008-03-11 | L. Perrigo Company | Simethicone containing tablet composition and method |
-
1975
- 1975-04-21 NL NL7504704A patent/NL7504704A/en not_active Application Discontinuation
- 1975-04-21 DE DE19752517585 patent/DE2517585A1/en not_active Withdrawn
- 1975-05-05 PH PH17121A patent/PH13370A/en unknown
- 1975-05-09 AR AR25871475A patent/AR212907A1/en active
- 1975-05-13 CA CA226,816A patent/CA1042796A/en not_active Expired
- 1975-05-14 FR FR7514981A patent/FR2270886A1/en active Granted
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5599577A (en) * | 1992-05-21 | 1997-02-04 | Mcneil-Ppc, Inc. | Simethicone containing pharmaceutical compositions |
| US5679376A (en) * | 1992-05-21 | 1997-10-21 | Mcneil-Ppc, Inc. | Simethicone containing pharmaceutical compositions |
| US5716641A (en) * | 1992-05-21 | 1998-02-10 | Mcneil-Ppc, Inc. | Simethicone containing pharmaceutical compositions |
| US5980944A (en) * | 1992-05-21 | 1999-11-09 | Mcneil-Ppc, Inc. | Simethicone containing pharmaceutical compositions |
| US6038608A (en) * | 1996-11-25 | 2000-03-14 | Nec Corporation | Virtual LAN system |
| US7341742B2 (en) | 2002-09-30 | 2008-03-11 | L. Perrigo Company | Simethicone containing tablet composition and method |
Also Published As
| Publication number | Publication date |
|---|---|
| PH13370A (en) | 1980-03-20 |
| FR2270886A1 (en) | 1975-12-12 |
| DE2517585A1 (en) | 1975-11-27 |
| NL7504704A (en) | 1975-11-18 |
| AR212907A1 (en) | 1978-11-15 |
| FR2270886B1 (en) | 1979-08-17 |
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