NO313490B1 - Farmasöytisk preparat inneholdende en glukosidase- og/eller amylasehemmer og en lipasehemmer - Google Patents
Farmasöytisk preparat inneholdende en glukosidase- og/eller amylasehemmer og en lipasehemmer Download PDFInfo
- Publication number
- NO313490B1 NO313490B1 NO19942900A NO942900A NO313490B1 NO 313490 B1 NO313490 B1 NO 313490B1 NO 19942900 A NO19942900 A NO 19942900A NO 942900 A NO942900 A NO 942900A NO 313490 B1 NO313490 B1 NO 313490B1
- Authority
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- Norway
- Prior art keywords
- inhibitor
- glucosidase
- lipase
- amylase
- acarbose
- Prior art date
Links
- 239000003392 amylase inhibitor Substances 0.000 title claims abstract description 17
- 102000004366 Glucosidases Human genes 0.000 title claims abstract description 16
- 108010056771 Glucosidases Proteins 0.000 title claims abstract description 16
- 229940122816 Amylase inhibitor Drugs 0.000 title claims abstract description 14
- 229940086609 Lipase inhibitor Drugs 0.000 title claims abstract description 13
- 239000000825 pharmaceutical preparation Substances 0.000 title claims description 7
- 239000003937 drug carrier Substances 0.000 claims abstract description 3
- AHLBNYSZXLDEJQ-FWEHEUNISA-N orlistat Chemical group CCCCCCCCCCC[C@H](OC(=O)[C@H](CC(C)C)NC=O)C[C@@H]1OC(=O)[C@H]1CCCCCC AHLBNYSZXLDEJQ-FWEHEUNISA-N 0.000 claims description 10
- 229960001243 orlistat Drugs 0.000 claims description 10
- 208000008589 Obesity Diseases 0.000 claims description 9
- 238000002360 preparation method Methods 0.000 claims description 9
- XUFXOAAUWZOOIT-SXARVLRPSA-N (2R,3R,4R,5S,6R)-5-[[(2R,3R,4R,5S,6R)-5-[[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-1-cyclohex-2-enyl]amino]-2-oxanyl]oxy]-3,4-dihydroxy-6-(hydroxymethyl)-2-oxanyl]oxy]-6-(hydroxymethyl)oxane-2,3,4-triol Chemical group O([C@H]1O[C@H](CO)[C@H]([C@@H]([C@H]1O)O)O[C@H]1O[C@@H]([C@H]([C@H](O)[C@H]1O)N[C@@H]1[C@@H]([C@@H](O)[C@H](O)C(CO)=C1)O)C)[C@@H]1[C@@H](CO)O[C@@H](O)[C@H](O)[C@H]1O XUFXOAAUWZOOIT-SXARVLRPSA-N 0.000 claims description 8
- 229960002632 acarbose Drugs 0.000 claims description 8
- XUFXOAAUWZOOIT-UHFFFAOYSA-N acarviostatin I01 Natural products OC1C(O)C(NC2C(C(O)C(O)C(CO)=C2)O)C(C)OC1OC(C(C1O)O)C(CO)OC1OC1C(CO)OC(O)C(O)C1O XUFXOAAUWZOOIT-UHFFFAOYSA-N 0.000 claims description 8
- 239000013543 active substance Substances 0.000 claims description 7
- AHLBNYSZXLDEJQ-UHFFFAOYSA-N N-formyl-L-leucylester Natural products CCCCCCCCCCCC(OC(=O)C(CC(C)C)NC=O)CC1OC(=O)C1CCCCCC AHLBNYSZXLDEJQ-UHFFFAOYSA-N 0.000 claims description 6
- 208000012696 congenital leptin deficiency Diseases 0.000 claims description 6
- 208000001022 morbid obesity Diseases 0.000 claims description 6
- FOZFSEMFCIPOSZ-SPCKQMHLSA-N (2r,3r,4r,5s)-2-(hydroxymethyl)-1-[[(2r,3s,4s,5r,6s)-3,4,5-trihydroxy-6-methoxyoxan-2-yl]methyl]piperidine-3,4,5-triol;trihydrate Chemical compound O.O.O.O[C@H]1[C@H](O)[C@@H](O)[C@@H](OC)O[C@@H]1CN1[C@H](CO)[C@@H](O)[C@H](O)[C@@H](O)C1.O[C@H]1[C@H](O)[C@@H](O)[C@@H](OC)O[C@@H]1CN1[C@H](CO)[C@@H](O)[C@H](O)[C@@H](O)C1 FOZFSEMFCIPOSZ-SPCKQMHLSA-N 0.000 claims description 4
- -1 Bay-N-3176 Natural products 0.000 claims description 4
- IBAQFPQHRJAVAV-ULAWRXDQSA-N Miglitol Chemical compound OCCN1C[C@H](O)[C@@H](O)[C@H](O)[C@H]1CO IBAQFPQHRJAVAV-ULAWRXDQSA-N 0.000 claims description 4
- NWWORXYTJRPSMC-QKPAOTATSA-N ethyl 4-[2-[(2r,3r,4r,5s)-3,4,5-trihydroxy-2-(hydroxymethyl)piperidin-1-yl]ethoxy]benzoate Chemical compound C1=CC(C(=O)OCC)=CC=C1OCCN1[C@H](CO)[C@@H](O)[C@H](O)[C@@H](O)C1 NWWORXYTJRPSMC-QKPAOTATSA-N 0.000 claims description 4
- SIKWOTFNWURSAY-UHFFFAOYSA-N Lipstatin Natural products CCCCCCC1C(CC(CC=CCC=CCCCCC)C(=O)OC(CC(C)C)NC=O)OC1=O SIKWOTFNWURSAY-UHFFFAOYSA-N 0.000 claims description 3
- OQMAKWGYQLJJIA-CUOOPAIESA-N lipstatin Chemical compound CCCCCC[C@H]1[C@H](C[C@H](C\C=C/C\C=C/CCCCC)OC(=O)[C@H](CC(C)C)NC=O)OC1=O OQMAKWGYQLJJIA-CUOOPAIESA-N 0.000 claims description 3
- VCIPQQCYKMORDY-KBYFLBCBSA-N (2r,3r,4s,5s,6r)-2-(hydroxymethyl)-6-[[(2r,3r,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxymethyl]piperidine-3,4,5-triol Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)N[C@@H]1CO[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 VCIPQQCYKMORDY-KBYFLBCBSA-N 0.000 claims description 2
- QRGQONAZHIKMGC-UHFFFAOYSA-N (4-phenoxyphenyl) 4-methylpiperidine-1-carboxylate Chemical compound C1CC(C)CCN1C(=O)OC(C=C1)=CC=C1OC1=CC=CC=C1 QRGQONAZHIKMGC-UHFFFAOYSA-N 0.000 claims description 2
- QJLPWVUZFKETMK-LLVKDONJSA-N (5r)-1,5,7,9,11,14-hexahydroxy-3-methyl-8,13-dioxo-5,6-dihydrobenzo[a]tetracene-2-carboxylic acid Chemical compound O=C1C2=C(O)C=C(O)C=C2C(=O)C2=C1C(O)=C1C[C@@H](O)C(C=C(C(=C3O)C(O)=O)C)=C3C1=C2O QJLPWVUZFKETMK-LLVKDONJSA-N 0.000 claims description 2
- WOISDAHQBUYEAF-UHFFFAOYSA-N Ebelactone A Natural products CCC(C)C(O)C(C)C(=O)C(C)C=C(C)CC(C)C1OC(=O)C1C WOISDAHQBUYEAF-UHFFFAOYSA-N 0.000 claims description 2
- UNBMQQNYLCPCHS-UHFFFAOYSA-N Ebelactone B Natural products CCC(C)C(O)C(C)C(=O)C(C)C=C(C)CC(C)C1OC(=O)C1CC UNBMQQNYLCPCHS-UHFFFAOYSA-N 0.000 claims description 2
- VCIPQQCYKMORDY-UHFFFAOYSA-N MDL 25637 Natural products OC1C(O)C(O)C(CO)NC1COC1C(O)C(O)C(O)C(CO)O1 VCIPQQCYKMORDY-UHFFFAOYSA-N 0.000 claims description 2
- RXSVYGIGWRDVQC-UHFFFAOYSA-N N-[6-[[(cyclohexylideneamino)oxy-oxomethyl]amino]hexyl]carbamic acid (cyclohexylideneamino) ester Chemical compound C1CCCCC1=NOC(=O)NCCCCCCNC(=O)ON=C1CCCCC1 RXSVYGIGWRDVQC-UHFFFAOYSA-N 0.000 claims description 2
- QJLPWVUZFKETMK-UHFFFAOYSA-N Pradimicin Q Natural products O=C1C2=C(O)C=C(O)C=C2C(=O)C2=C1C(O)=C1CC(O)C(C=C(C(=C3O)C(O)=O)C)=C3C1=C2O QJLPWVUZFKETMK-UHFFFAOYSA-N 0.000 claims description 2
- OCTNNXHKAOLDJL-BMGYQPLYSA-N Salbostatin Chemical compound O[C@H]1[C@H](O)[C@@H](CO)OC[C@@H]1N[C@@H]1[C@H](O)[C@@H](O)[C@H](O)C(CO)=C1 OCTNNXHKAOLDJL-BMGYQPLYSA-N 0.000 claims description 2
- OCTNNXHKAOLDJL-UHFFFAOYSA-N Salbostatin Natural products OC1C(O)C(CO)OCC1NC1C(O)C(O)C(O)C(CO)=C1 OCTNNXHKAOLDJL-UHFFFAOYSA-N 0.000 claims description 2
- 229930186167 Trestatin Natural products 0.000 claims description 2
- WWGVIIVMPMBQFV-HAGHYFMRSA-N Valilactone Natural products CCCCCC[C@H]1[C@@H](C[C@H](CCCCC)OC(=O)[C@@H](NC=O)C(C)C)OC1=O WWGVIIVMPMBQFV-HAGHYFMRSA-N 0.000 claims description 2
- FZNCGRZWXLXZSZ-CIQUZCHMSA-N Voglibose Chemical compound OCC(CO)N[C@H]1C[C@](O)(CO)[C@@H](O)[C@H](O)[C@H]1O FZNCGRZWXLXZSZ-CIQUZCHMSA-N 0.000 claims description 2
- WWGVIIVMPMBQFV-MUGJNUQGSA-N [(2s)-1-[(2s,3s)-3-hexyl-4-oxooxetan-2-yl]heptan-2-yl] (2s)-2-formamido-3-methylbutanoate Chemical compound CCCCCC[C@H]1[C@H](C[C@H](CCCCC)OC(=O)[C@@H](NC=O)C(C)C)OC1=O WWGVIIVMPMBQFV-MUGJNUQGSA-N 0.000 claims description 2
- RLVLLBHWAQWLKL-UHFFFAOYSA-N [2-[4-(2-methylpropyl)cyclohexyl]-2-oxoethyl] benzenesulfonate Chemical compound C1CC(CC(C)C)CCC1C(=O)COS(=O)(=O)C1=CC=CC=C1 RLVLLBHWAQWLKL-UHFFFAOYSA-N 0.000 claims description 2
- 229950001261 camiglibose Drugs 0.000 claims description 2
- UNBMQQNYLCPCHS-VYNDPHDASA-N ebelactone b Chemical compound CC[C@@H](C)[C@@H](O)[C@H](C)C(=O)[C@H](C)\C=C(/C)C[C@H](C)[C@@H]1OC(=O)[C@H]1CC UNBMQQNYLCPCHS-VYNDPHDASA-N 0.000 claims description 2
- 229950000269 emiglitate Drugs 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 229960001110 miglitol Drugs 0.000 claims description 2
- 229950001790 tendamistat Drugs 0.000 claims description 2
- 108010037401 tendamistate Proteins 0.000 claims description 2
- 229960001729 voglibose Drugs 0.000 claims description 2
- 229940122069 Glycosidase inhibitor Drugs 0.000 claims 1
- 102000005744 Glycoside Hydrolases Human genes 0.000 claims 1
- 108010031186 Glycoside Hydrolases Proteins 0.000 claims 1
- 239000003316 glycosidase inhibitor Substances 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 abstract description 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229940127470 Lipase Inhibitors Drugs 0.000 description 7
- 208000016261 weight loss Diseases 0.000 description 5
- 230000004580 weight loss Effects 0.000 description 5
- 206010012601 diabetes mellitus Diseases 0.000 description 4
- 239000002775 capsule Substances 0.000 description 3
- 235000020824 obesity Nutrition 0.000 description 3
- 238000011125 single therapy Methods 0.000 description 3
- 240000004808 Saccharomyces cerevisiae Species 0.000 description 2
- 230000037213 diet Effects 0.000 description 2
- 235000005911 diet Nutrition 0.000 description 2
- 239000007903 gelatin capsule Substances 0.000 description 2
- 241000023308 Acca Species 0.000 description 1
- JKNGELGDDBUFHG-UHFFFAOYSA-N Esterastin Natural products CCCCCCC1C(CC(CC=CCC=CCCCCC)OC(=O)C(CC(N)=O)NC(C)=O)OC1=O JKNGELGDDBUFHG-UHFFFAOYSA-N 0.000 description 1
- 208000031226 Hyperlipidaemia Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 208000031773 Insulin resistance syndrome Diseases 0.000 description 1
- 102000004882 Lipase Human genes 0.000 description 1
- 108090001060 Lipase Proteins 0.000 description 1
- 239000004367 Lipase Substances 0.000 description 1
- JKNGELGDDBUFHG-JJPNXARGSA-N [(2S,4Z,7Z)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]trideca-4,7-dien-2-yl] (2S)-2-acetamido-4-amino-4-oxobutanoate Chemical compound CCCCCC[C@H]1[C@H](C[C@H](C\C=C/C\C=C/CCCCC)OC(=O)[C@H](CC(N)=O)NC(C)=O)OC1=O JKNGELGDDBUFHG-JJPNXARGSA-N 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 235000019577 caloric intake Nutrition 0.000 description 1
- 230000029087 digestion Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 230000006806 disease prevention Effects 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 238000012262 fermentative production Methods 0.000 description 1
- 229930195733 hydrocarbon Natural products 0.000 description 1
- 150000002430 hydrocarbons Chemical class 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 235000019421 lipase Nutrition 0.000 description 1
- 235000012054 meals Nutrition 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 230000037081 physical activity Effects 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 239000000902 placebo Substances 0.000 description 1
- 229940068196 placebo Drugs 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 239000003826 tablet 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Child & Adolescent Psychology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Epoxy Compounds (AREA)
- Saccharide Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
Description
Foreliggende oppfinnelse vedrører farmasøytiske preparater inneholdende en glukosidase- og/eller amylasehemmer og en lipasehemmer som de aktive substanser i kombinasjon med en farmasøytisk akseptabel bærer.
Det ble funnet at man kan anvende slike preparater for behandling av sykelig fedme.
Oppfinnelsen vedrører således også et produkt inneholdende en glukosidase- og/eller amylasehemmer og en lipasehemmer som et kombinasjonspreparat for, separat eller i tid krono-logisk del anvendelse ved behandling av sykelig fedme.
Videre vedrører oppfinnelsen anvendelse av en glukosidase-og/eller amylasehemmer i kombinasjon med en lipasehemmer for fremstilling av farmasøytiske preparater for behandling av sykelig fedme.
Eksempler på anvendelige glukosidase- og/eller amylasehemmere ifølge oppfinnelsen er acarbose, adiposine, voglibose (AO-128), miglitol (Bay-m-1099), emiglitate (Bay-o-1248), MDL-25637, camiglibose (MDL-73945), tendamistate, AI-3688, trestatin, pradimicin-Q og salbostatin.
Eksempler på lipasehemmere er tetrahydrolipstatin, lipstatin, FL-386, WAY-121898, Bay-N-3176, valilactone, esterastin, ebelactone A, ebelactone B og RHC 80267.
Som lipasehemmere kan man også anvende biomasser eller gjærkaker som fremkommer ved fermentativ fremstilling av lipasehemmere, såsom lipstatin eller esterastin. Gjærkaker er f.eks. beskrevet i EP-A 129748 og USP 4189438.
Om glukosidase- og/eller amylasehemmere, såsom acarbose, er det kjent at de forsinker fordøyelsen av hydrokarboner. Videre er det kjent lipasehemmere, såsom tetrahydrolipstatin (orlistat) fører til partiell hemming av lipase i tarmen.
Ved enkeltterapi fører dog vanligvis lipasehemmerne selv i kombinasjon med en reduksjonsdiett bare til et avmålt vekttap, og glukosidase- og/eller amylasehemmere til praktisk talt intet vekttap, (se William-Olsson, T.) Acca Med Scand Suppl. 1985 706 s.1-39; Hillebrand, I., et al., Tohoku J Exp Med 1983 141 Suppl. s. 683-6; Jenny, A., et al., Diabetes Care, 1993 16(2) s. 499-502; Tuomilehto, J., et al., Diabetes Res Clin Pract, 1994 26(3) s. 215-22; Hoffmann, J. og Spengler, M., Diabetes Care, 1994 17(6) s. 561-6. På overraskende måte ble det nå funnet at en kom-binert anvendelse av en glukosidase- og/eller amylasehemmer og en lipasehemmer fører til et vesentlig høyere vekttap enn ved enkeltterapi. Dette ble påvist i følgende test.
Testen ble utført i to forsøksperioder på to forsøksper-soner (A og B). I en 7 dager varig for-test, da forsøks-personene ikke inntok noen medikamenter, fikk A hhv. B gjennomsnittlige dagskalorimengder på 2560 hhv. 1850 kcal. I den påfølgende 14 dager varige hovedtest fikk forsøks-personene ved hvert måltid 12 0 mg orlistat og 100 mg acarbose. Ingen spesiell diett ble holdt, og de fysiske aktivi-teter ble redusert til et minimum. Liksom i for-testen ble det også her gitt en gjennomsnittlig dagskalorimengde på 2185 hhv. 2050 kcal til A hhv. B. Av nedenstående tabell fremgår vekttapet for begge forsøkspersoner.
Sammenlignet med dette var vekttapet hos pasienter ved enkeltterapi med orlistat (3 x 120 mg/dag) i en placebo-kontrollert 12 ukers test gjennomsnittlig 1,8 kg (dvs. 0,3 kg/14 dager) (Int. J. Obesity 1992, 16 (Suppl. 1):16, Abstr. 063) .
Ifølge oppfinnelsen kan det anvendes en glukosidase- og/eller amylasehemmer i form av farmasøytiske preparater, som også inneholder i lipasehemmere, eller som ad hoc-kombinasjon med lipasehemmerholdige preparater.
Foretrukket er anvendelsen av acarbose og orlistat.
For behandling av sykelig fedme administreres virkestoffene oralt.
Virkestoffene kan administreres daglig i doseringer på ca 0,003 mg til ca 20 mg, fortrinnsvis 0,015 mg til 10 mg glukosidase- og/eller amylasehemmer og 0,15 mg til 20 mg, fortrinnsvis 0,5 mg til10 mg, lipasehemmer pr. kg kropps-vekt .
De orale preparater ifølge oppfinnelsen kan foreligge i form av tabletter, kapsler, løsninger og emulsjoner.
Faste administrasjonsformer, såsom tabletter og kapsler inneholder pr. doseringsenhet med fordel ca 0,2 mg til ca 100 mg glukosidase- og/eller amylasehemmer og 10 mg til 200 mg lipasehemmer.
I tillegg til behandling av fedme kan preparatene hhv. virkestoffkombinasjonen ifølge oppfinnlesen anvendes for behandling og forebyggelse av sykdommer som ofte opptrer i forbindelse med overvekt, såsom diabetes, hypertensjon, hyperlipidemi og insulinresistens-syndrom.
Ved alle disse indikasjoner kan virkestoffene anvendes i de ovenfor angitte doseringsområder, og den individuelle dosering kan besstemmes av den behandlede sykdoms art samt avhengig av pasientens alder og tilstand og innenfor rammen av legens fagkunnskap. Oppfinnelsen illustreres ytterligere ved følgende eksempler.
På i og for seg kjent måte fremstilles farmasøytiske preparater av følgende sammensetning:
Eksempel A
Myke gelatinkapsler:
Eksempel B
Harde gelatinkapsler:
Kapselfyllingsvekt 153,0 mg Eksempel C
Tabletter:
Tablettvekt 225,0 mg Eksempel D
Tabletter med kontrollert virkestoffavgivelse og forlenget oppholdstid i maven:
Eksempel E
Rekonstituerbart pulver:
Claims (8)
1. Farmasøytisk prepart inneholdende en glukosidase-og/eller amylasehemmer og en lipasehemmer som de aktive substanser i kombinasjon med en farmasøytisk akseptabel bærer.
2. Preparat ifølge krav 1, hvori glukosidase- og/eller amylasehemmeren er acarbose, adiposine, voglibose (AO-128), miglitol (Bay-m-1099), emiglitate (Bay-o-1248), MDL-25637, camiglibose (MDL-73945), tendamistate, AI-3688, trestatin, pradimicin-Q eller salbostatin.
3. Preparat ifølge krav 1, hvori lipasehemmeren er tetrahydrolipstatin, lipstatin, FL-386, WAY-121898, Bay-N-3176, valilactone, esterastin, ebelactone A, ebelactone B eller RHC 80267.
4. Preparat ifølge krav 1, 2 eller 3, inneholdende acarbose og tetrahydrolipstatin som de aktive substanser.
5. Produkt inneholdende en glukosidase- og/eller amylasehemmer og en lipasehemmer som et kombinasj onspreparat for samtidig, separat eller i tid kronlogisk delt anvendelse ved behandling av sykelig fedme.
6. Produkt ifølge krav 5, inneholdende en glykosidase-og/eller amylasehemmere som angitt i krav 2 og en lipasehemmer som angitt i krav 3, spesielt acarbose og tetrahydrolipstatin .
7 . Anvendelse av en glukosidase- og/eller amylasehemmer i kombinasjon med en lipasehemmer for fremstillingen av et farmasøytisk preparat for behandling av sykelig fedme.
8. Anvendelse av acarbose i kombinasjon med tetrahydrolipstatin ifølge krav 7.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH233993 | 1993-08-05 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| NO942900D0 NO942900D0 (no) | 1994-08-04 |
| NO942900L NO942900L (no) | 1995-02-06 |
| NO313490B1 true NO313490B1 (no) | 2002-10-14 |
Family
ID=4231504
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO19942900A NO313490B1 (no) | 1993-08-05 | 1994-08-04 | Farmasöytisk preparat inneholdende en glukosidase- og/eller amylasehemmer og en lipasehemmer |
Country Status (24)
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|---|---|
| US (1) | US5643874A (no) |
| EP (1) | EP0638317B1 (no) |
| JP (1) | JP2780932B2 (no) |
| KR (1) | KR100342285B1 (no) |
| CN (1) | CN1076196C (no) |
| AT (1) | ATE190503T1 (no) |
| AU (1) | AU684793B2 (no) |
| BR (1) | BR9403170A (no) |
| CA (1) | CA2128044C (no) |
| CZ (1) | CZ286202B6 (no) |
| DE (1) | DE59409200D1 (no) |
| DK (1) | DK0638317T3 (no) |
| ES (1) | ES2144019T3 (no) |
| GR (1) | GR3033643T3 (no) |
| HU (1) | HU222346B1 (no) |
| IL (1) | IL110510A (no) |
| NO (1) | NO313490B1 (no) |
| NZ (1) | NZ264142A (no) |
| PL (1) | PL175997B1 (no) |
| PT (1) | PT638317E (no) |
| RU (1) | RU2141844C1 (no) |
| SA (1) | SA94150156B1 (no) |
| TW (1) | TW381025B (no) |
| ZA (1) | ZA945673B (no) |
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