NZ200248A - Pharmaceutical compositions containing benfluorex hydrochloride in digestible hydrophobic matrix - Google Patents
Pharmaceutical compositions containing benfluorex hydrochloride in digestible hydrophobic matrixInfo
- Publication number
- NZ200248A NZ200248A NZ200248A NZ20024882A NZ200248A NZ 200248 A NZ200248 A NZ 200248A NZ 200248 A NZ200248 A NZ 200248A NZ 20024882 A NZ20024882 A NZ 20024882A NZ 200248 A NZ200248 A NZ 200248A
- Authority
- NZ
- New Zealand
- Prior art keywords
- active ingredient
- pharmaceutical compositions
- benfluorex
- hydrophobic matrix
- release pellets
- Prior art date
Links
- CJAVTWRYCDNHSM-UHFFFAOYSA-N benzoic acid 2-[1-[3-(trifluoromethyl)phenyl]propan-2-ylamino]ethyl ester Chemical compound C=1C=CC=CC=1C(=O)OCCNC(C)CC1=CC=CC(C(F)(F)F)=C1 CJAVTWRYCDNHSM-UHFFFAOYSA-N 0.000 title claims description 25
- 229960001213 benfluorex hydrochloride Drugs 0.000 title claims description 20
- 239000008194 pharmaceutical composition Substances 0.000 title claims description 18
- 239000011159 matrix material Substances 0.000 title claims description 11
- 230000002209 hydrophobic effect Effects 0.000 title claims description 10
- 239000008188 pellet Substances 0.000 claims description 38
- 239000004480 active ingredient Substances 0.000 claims description 29
- 239000000203 mixture Substances 0.000 claims description 23
- DUXYWXYOBMKGIN-UHFFFAOYSA-N trimyristin Chemical compound CCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCC DUXYWXYOBMKGIN-UHFFFAOYSA-N 0.000 claims description 13
- 238000000034 method Methods 0.000 claims description 11
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 10
- 230000002035 prolonged effect Effects 0.000 claims description 9
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 8
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 8
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 8
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 8
- 239000003795 chemical substances by application Substances 0.000 claims description 7
- 239000011248 coating agent Substances 0.000 claims description 6
- 238000000576 coating method Methods 0.000 claims description 6
- 239000008119 colloidal silica Substances 0.000 claims description 6
- 206010012601 diabetes mellitus Diseases 0.000 claims description 6
- 125000005456 glyceride group Chemical group 0.000 claims description 5
- 235000019359 magnesium stearate Nutrition 0.000 claims description 5
- 239000000725 suspension Substances 0.000 claims description 5
- 238000004018 waxing Methods 0.000 claims description 5
- 229960001264 benfluorex Drugs 0.000 claims description 4
- 235000019438 castor oil Nutrition 0.000 claims description 4
- 239000004359 castor oil Substances 0.000 claims description 4
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims description 4
- 230000007119 pathological manifestation Effects 0.000 claims description 3
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 2
- 239000000194 fatty acid Substances 0.000 claims description 2
- 229930195729 fatty acid Natural products 0.000 claims description 2
- 150000004665 fatty acids Chemical class 0.000 claims description 2
- 239000002552 dosage form Substances 0.000 claims 2
- 230000001681 protective effect Effects 0.000 claims 2
- 238000001192 hot extrusion Methods 0.000 claims 1
- 238000010561 standard procedure Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 7
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 6
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 5
- 239000008280 blood Substances 0.000 description 4
- 210000004369 blood Anatomy 0.000 description 4
- 229920002678 cellulose Polymers 0.000 description 4
- 238000001125 extrusion Methods 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- 229920002472 Starch Polymers 0.000 description 3
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 description 3
- 239000001913 cellulose Substances 0.000 description 3
- 235000010980 cellulose Nutrition 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 239000000902 placebo Substances 0.000 description 3
- 229940068196 placebo Drugs 0.000 description 3
- 229910001220 stainless steel Inorganic materials 0.000 description 3
- 239000010935 stainless steel Substances 0.000 description 3
- 239000008107 starch Substances 0.000 description 3
- 235000019698 starch Nutrition 0.000 description 3
- 102000015779 HDL Lipoproteins Human genes 0.000 description 2
- 108010010234 HDL Lipoproteins Proteins 0.000 description 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 2
- 230000001476 alcoholic effect Effects 0.000 description 2
- 239000011230 binding agent Substances 0.000 description 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
- 239000006185 dispersion Substances 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 2
- 230000002218 hypoglycaemic effect Effects 0.000 description 2
- 229910052500 inorganic mineral Inorganic materials 0.000 description 2
- 238000002844 melting Methods 0.000 description 2
- 230000008018 melting Effects 0.000 description 2
- 239000011707 mineral Substances 0.000 description 2
- 238000010606 normalization Methods 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000000454 talc Substances 0.000 description 2
- 235000012222 talc Nutrition 0.000 description 2
- 229910052623 talc Inorganic materials 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- QHZLMUACJMDIAE-UHFFFAOYSA-N 1-monopalmitoylglycerol Chemical compound CCCCCCCCCCCCCCCC(=O)OCC(O)CO QHZLMUACJMDIAE-UHFFFAOYSA-N 0.000 description 1
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 1
- 229920003084 Avicel® PH-102 Polymers 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- 208000018522 Gastrointestinal disease Diseases 0.000 description 1
- 239000001828 Gelatine Substances 0.000 description 1
- 208000035150 Hypercholesterolemia Diseases 0.000 description 1
- 208000031226 Hyperlipidaemia Diseases 0.000 description 1
- 208000013016 Hypoglycemia Diseases 0.000 description 1
- 102000011782 Keratins Human genes 0.000 description 1
- 108010076876 Keratins Proteins 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
- 102000004882 Lipase Human genes 0.000 description 1
- 108090001060 Lipase Proteins 0.000 description 1
- 235000019759 Maize starch Nutrition 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 1
- -1 Polyoxyethylene Polymers 0.000 description 1
- 229920003110 Primojel Polymers 0.000 description 1
- BHYLRAPBCJJTBB-UHFFFAOYSA-M S(=O)(=O)(OCCCCCCCCCCCC)[O-].[Na+].[O-2].[Fe+2] Chemical compound S(=O)(=O)(OCCCCCCCCCCCC)[O-].[Na+].[O-2].[Fe+2] BHYLRAPBCJJTBB-UHFFFAOYSA-M 0.000 description 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
- 239000004141 Sodium laurylsulphate Substances 0.000 description 1
- 230000036765 blood level Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 235000013339 cereals Nutrition 0.000 description 1
- 235000012000 cholesterol Nutrition 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 230000001186 cumulative effect Effects 0.000 description 1
- 230000001079 digestive effect Effects 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 239000008298 dragée Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 229940093476 ethylene glycol Drugs 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 229940096898 glyceryl palmitate Drugs 0.000 description 1
- FETSQPAGYOVAQU-UHFFFAOYSA-N glyceryl palmitostearate Chemical compound OCC(O)CO.CCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O FETSQPAGYOVAQU-UHFFFAOYSA-N 0.000 description 1
- 229940046813 glyceryl palmitostearate Drugs 0.000 description 1
- 229940075529 glyceryl stearate Drugs 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- 230000000055 hyoplipidemic effect Effects 0.000 description 1
- 201000001421 hyperglycemia Diseases 0.000 description 1
- 208000006575 hypertriglyceridemia Diseases 0.000 description 1
- 239000002050 international nonproprietary name Substances 0.000 description 1
- 208000006443 lactic acidosis Diseases 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 208000020442 loss of weight Diseases 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- LZRNINVWCBOEBZ-UHFFFAOYSA-M magnesium octadecanoate oxygen(2-) titanium(4+) Chemical compound [O-2].[Ti+4].C(CCCCCCCCCCCCCCCCC)(=O)[O-].[Mg+2] LZRNINVWCBOEBZ-UHFFFAOYSA-M 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 239000002985 plastic film Substances 0.000 description 1
- 229920006255 plastic film Polymers 0.000 description 1
- 229940093429 polyethylene glycol 6000 Drugs 0.000 description 1
- 230000000750 progressive effect Effects 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 150000003626 triacylglycerols Chemical class 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Emergency Medicine (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR8106915A FR2502952A1 (fr) | 1981-04-07 | 1981-04-07 | Nouveau medicament a base de chlorhydrate de benfluorex pour le traitement du diabete |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NZ200248A true NZ200248A (en) | 1985-08-30 |
Family
ID=9257087
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ200248A NZ200248A (en) | 1981-04-07 | 1982-04-06 | Pharmaceutical compositions containing benfluorex hydrochloride in digestible hydrophobic matrix |
Country Status (12)
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4793999A (en) * | 1987-03-27 | 1988-12-27 | Sheth Prabhakar R | Method of manufacturing an antihypertensive, diuretic and antihypokalemic pharmaceutical composition with polyethylene glycol |
| AU4369589A (en) * | 1988-10-27 | 1990-05-03 | Abbott Laboratories | Controlled-release delivery device, method for producing device, and method of using device |
| FR2684552B1 (fr) * | 1991-12-06 | 1995-04-28 | Adir | Utilisation de la d-fenfluramine et de derives de la fenfluramine dans le traitement de l'hypertension chez des sujets insulino-resistants. |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3062720A (en) * | 1959-05-20 | 1962-11-06 | Philips Roxane | Sustained release pharmaceutical tablet |
| GB1175516A (en) * | 1966-04-15 | 1969-12-23 | Science Union & Cie | New Phenyl-Aminopropane Derivatives and Preparations Containing them |
-
1981
- 1981-04-07 FR FR8106915A patent/FR2502952A1/fr active Granted
-
1982
- 1982-03-30 ZA ZA822176A patent/ZA822176B/xx unknown
- 1982-03-31 CA CA000400086A patent/CA1186997A/fr not_active Expired
- 1982-04-05 LU LU84069A patent/LU84069A1/fr unknown
- 1982-04-06 AU AU82387/82A patent/AU551033B2/en not_active Ceased
- 1982-04-06 CH CH2125/82A patent/CH653551A5/fr not_active IP Right Cessation
- 1982-04-06 IE IE810/82A patent/IE52959B1/en not_active IP Right Cessation
- 1982-04-06 PH PH27095A patent/PH17582A/en unknown
- 1982-04-06 NZ NZ200248A patent/NZ200248A/en unknown
- 1982-04-06 IT IT48180/82A patent/IT1148161B/it active
- 1982-04-06 GB GB8210194A patent/GB2099299B/en not_active Expired
- 1982-04-06 BE BE0/207773A patent/BE892781A/fr not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| BE892781A (fr) | 1982-10-06 |
| CH653551A5 (fr) | 1986-01-15 |
| GB2099299A (en) | 1982-12-08 |
| AU551033B2 (en) | 1986-04-17 |
| IE820810L (en) | 1982-10-07 |
| FR2502952A1 (fr) | 1982-10-08 |
| ZA822176B (en) | 1983-02-23 |
| IT8248180A0 (it) | 1982-04-06 |
| PH17582A (en) | 1984-10-02 |
| CA1186997A (fr) | 1985-05-14 |
| GB2099299B (en) | 1985-04-03 |
| LU84069A1 (fr) | 1983-04-13 |
| FR2502952B1 (enrdf_load_stackoverflow) | 1983-10-07 |
| AU8238782A (en) | 1982-10-14 |
| IE52959B1 (en) | 1988-04-27 |
| IT1148161B (it) | 1986-11-26 |
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