LU87009A1 - Compositions pharmaceutiques a liberation prolongee - Google Patents
Compositions pharmaceutiques a liberation prolongee Download PDFInfo
- Publication number
- LU87009A1 LU87009A1 LU87009A LU87009A LU87009A1 LU 87009 A1 LU87009 A1 LU 87009A1 LU 87009 A LU87009 A LU 87009A LU 87009 A LU87009 A LU 87009A LU 87009 A1 LU87009 A1 LU 87009A1
- Authority
- LU
- Luxembourg
- Prior art keywords
- pharmaceutical composition
- composition according
- acetylsalicylic acid
- hydroxypropyl
- acid
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims description 45
- 239000012730 sustained-release form Substances 0.000 title claims description 8
- 238000013268 sustained release Methods 0.000 title claims description 6
- 229960001138 acetylsalicylic acid Drugs 0.000 claims description 45
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims description 43
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 claims description 40
- 239000000203 mixture Substances 0.000 claims description 27
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 claims description 20
- 229960004889 salicylic acid Drugs 0.000 claims description 20
- 239000013543 active substance Substances 0.000 claims description 17
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 16
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 16
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 16
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 16
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 16
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 15
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 15
- 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 claims description 15
- 229920000881 Modified starch Polymers 0.000 claims description 13
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims description 11
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 7
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 6
- -1 hydroxypropyl groups Chemical group 0.000 claims description 5
- 238000004090 dissolution Methods 0.000 claims description 4
- 239000007787 solid Substances 0.000 claims description 4
- 125000005273 2-acetoxybenzoic acid group Chemical group 0.000 claims description 3
- 239000002253 acid Substances 0.000 claims description 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 3
- 150000003839 salts Chemical class 0.000 claims description 3
- 238000007906 compression Methods 0.000 claims description 2
- 230000006835 compression Effects 0.000 claims description 2
- 238000006116 polymerization reaction Methods 0.000 claims description 2
- 229920000609 methyl cellulose Polymers 0.000 claims 1
- 239000001923 methylcellulose Substances 0.000 claims 1
- 229960002900 methylcellulose Drugs 0.000 claims 1
- 238000009472 formulation Methods 0.000 description 15
- 229960001860 salicylate Drugs 0.000 description 11
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 description 11
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 9
- 210000002381 plasma Anatomy 0.000 description 9
- 238000012360 testing method Methods 0.000 description 9
- 238000000034 method Methods 0.000 description 7
- BSYNRYMUTXBXSQ-FOQJRBATSA-N 59096-14-9 Chemical compound CC(=O)OC1=CC=CC=C1[14C](O)=O BSYNRYMUTXBXSQ-FOQJRBATSA-N 0.000 description 6
- 230000008030 elimination Effects 0.000 description 6
- 238000003379 elimination reaction Methods 0.000 description 6
- 210000002700 urine Anatomy 0.000 description 6
- 210000004369 blood Anatomy 0.000 description 5
- 239000008280 blood Substances 0.000 description 5
- 235000021355 Stearic acid Nutrition 0.000 description 4
- 230000003110 anti-inflammatory effect Effects 0.000 description 4
- 239000003795 chemical substances by application Substances 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 4
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 4
- 239000002245 particle Substances 0.000 description 4
- 238000010972 statistical evaluation Methods 0.000 description 4
- 239000008117 stearic acid Substances 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
- 229920000945 Amylopectin Polymers 0.000 description 3
- 229920000856 Amylose Polymers 0.000 description 3
- 229920002261 Corn starch Polymers 0.000 description 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- 229920002472 Starch Polymers 0.000 description 3
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 3
- 239000008119 colloidal silica Substances 0.000 description 3
- 239000008120 corn starch Substances 0.000 description 3
- 230000001186 cumulative effect Effects 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 238000004128 high performance liquid chromatography Methods 0.000 description 3
- 230000004060 metabolic process Effects 0.000 description 3
- 239000000377 silicon dioxide Substances 0.000 description 3
- 239000008107 starch Substances 0.000 description 3
- 235000019698 starch Nutrition 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 208000002193 Pain Diseases 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- 206010037660 Pyrexia Diseases 0.000 description 2
- 230000001754 anti-pyretic effect Effects 0.000 description 2
- 210000004556 brain Anatomy 0.000 description 2
- 239000013078 crystal Substances 0.000 description 2
- 238000001514 detection method Methods 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000008187 granular material Substances 0.000 description 2
- 229940031702 hydroxypropyl methylcellulose 2208 Drugs 0.000 description 2
- 230000000302 ischemic effect Effects 0.000 description 2
- 238000004811 liquid chromatography Methods 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 230000036470 plasma concentration Effects 0.000 description 2
- 102000004169 proteins and genes Human genes 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- 229920006395 saturated elastomer Polymers 0.000 description 2
- 229910001220 stainless steel Inorganic materials 0.000 description 2
- 239000010935 stainless steel Substances 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- DAUAQNGYDSHRET-UHFFFAOYSA-N 3,4-dimethoxybenzoic acid Chemical compound COC1=CC=C(C(O)=O)C=C1OC DAUAQNGYDSHRET-UHFFFAOYSA-N 0.000 description 1
- 229920003084 Avicel® PH-102 Polymers 0.000 description 1
- 208000008035 Back Pain Diseases 0.000 description 1
- 206010006811 Bursitis Diseases 0.000 description 1
- 241000052343 Dares Species 0.000 description 1
- 206010070840 Gastrointestinal tract irritation Diseases 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 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
- 208000008930 Low Back Pain Diseases 0.000 description 1
- 229920003095 Methocel™ K15M Polymers 0.000 description 1
- 206010029240 Neuritis Diseases 0.000 description 1
- 239000004743 Polypropylene Substances 0.000 description 1
- 208000025747 Rheumatic disease Diseases 0.000 description 1
- 208000008765 Sciatica Diseases 0.000 description 1
- 206010042674 Swelling Diseases 0.000 description 1
- GPVDHNVGGIAOQT-UHFFFAOYSA-N Veratric acid Natural products COC1=CC=C(C(O)=O)C(OC)=C1 GPVDHNVGGIAOQT-UHFFFAOYSA-N 0.000 description 1
- 238000010306 acid treatment Methods 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 206010002022 amyloidosis Diseases 0.000 description 1
- 230000000202 analgesic effect Effects 0.000 description 1
- 229940035676 analgesics Drugs 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 239000000730 antalgic agent Substances 0.000 description 1
- 230000001088 anti-asthma Effects 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 230000002921 anti-spasmodic effect Effects 0.000 description 1
- 239000000935 antidepressant agent Substances 0.000 description 1
- 229940005513 antidepressants Drugs 0.000 description 1
- 239000003831 antifriction material Substances 0.000 description 1
- 229940125715 antihistaminic agent Drugs 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 229940030600 antihypertensive agent Drugs 0.000 description 1
- 239000002220 antihypertensive agent Substances 0.000 description 1
- 239000002221 antipyretic Substances 0.000 description 1
- 229940125716 antipyretic agent Drugs 0.000 description 1
- 229940124575 antispasmodic agent Drugs 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 206010003246 arthritis Diseases 0.000 description 1
- 238000013475 authorization Methods 0.000 description 1
- 238000009534 blood test Methods 0.000 description 1
- 159000000007 calcium salts Chemical class 0.000 description 1
- 235000010980 cellulose Nutrition 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 238000004040 coloring Methods 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- QPADNTZLUBYNEN-UHFFFAOYSA-N etallobarbital Chemical compound C=CCC1(CC)C(=O)NC(=O)NC1=O QPADNTZLUBYNEN-UHFFFAOYSA-N 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 239000000284 extract Substances 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 150000004676 glycans Chemical class 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- YLGXILFCIXHCMC-JHGZEJCSSA-N methyl cellulose Chemical compound COC1C(OC)C(OC)C(COC)O[C@H]1O[C@H]1C(OC)C(OC)C(OC)OC1COC YLGXILFCIXHCMC-JHGZEJCSSA-N 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 208000004296 neuralgia Diseases 0.000 description 1
- 230000010355 oscillation Effects 0.000 description 1
- 238000012856 packing Methods 0.000 description 1
- 229920001155 polypropylene Polymers 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 description 1
- 125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 description 1
- 238000004366 reverse phase liquid chromatography Methods 0.000 description 1
- 230000000552 rheumatic effect Effects 0.000 description 1
- 201000003068 rheumatic fever Diseases 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 238000000528 statistical test Methods 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 230000029305 taxis Effects 0.000 description 1
- 239000003204 tranquilizing agent Substances 0.000 description 1
- 230000002936 tranquilizing effect Effects 0.000 description 1
- 238000000870 ultraviolet spectroscopy Methods 0.000 description 1
- 239000005526 vasoconstrictor agent Substances 0.000 description 1
- 229940124549 vasodilator Drugs 0.000 description 1
- 239000003071 vasodilator agent Substances 0.000 description 1
Classifications
-
- 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
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB8624213 | 1986-10-09 | ||
| GB868624213A GB8624213D0 (en) | 1986-10-09 | 1986-10-09 | Sustained release pharmaceutical compositions |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| LU87009A1 true LU87009A1 (fr) | 1988-05-03 |
Family
ID=10605478
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| LU87009A LU87009A1 (fr) | 1986-10-09 | 1987-10-06 | Compositions pharmaceutiques a liberation prolongee |
Country Status (24)
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5948437A (en) * | 1996-05-23 | 1999-09-07 | Zeneca Limited | Pharmaceutical compositions using thiazepine |
| US5895663A (en) * | 1997-07-31 | 1999-04-20 | L. Perrigo Company | Pseudoephedrine hydrochloride extended-release tablets |
| PL198797B1 (pl) | 1999-03-31 | 2008-07-31 | Janssen Pharmaceutica Nv | Zastosowanie wstępnie żelowanej skrobi |
| US6242003B1 (en) | 2000-04-13 | 2001-06-05 | Novartis Ag | Organic compounds |
| US20060127474A1 (en) | 2001-04-11 | 2006-06-15 | Oskar Kalb | Pharmaceutical compositions comprising fluvastatin |
| SE0102888D0 (sv) * | 2001-08-29 | 2001-08-29 | Astrazeneca Ab | New formulation |
| SE0102886D0 (sv) * | 2001-08-29 | 2001-08-29 | Astrazeneca Ab | New formulation |
| SE0102887D0 (sv) * | 2001-08-29 | 2001-08-29 | Astrazeneca Ab | New formulation |
| TWI338583B (en) | 2004-05-20 | 2011-03-11 | Otsuka Pharma Co Ltd | Solid pharmaceutical formulation |
| SI1803447T1 (sl) * | 2004-09-09 | 2010-01-29 | Psicofarma S A De C V | Farmacevtski sestavek za zadrĺ˝evano sproĺ äśanje hidralazina in njegova uporaba kot podrpora zdravljenju raka |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE795766A (fr) * | 1972-02-22 | 1973-08-22 | Lilly Co Eli | Particules de napsylate de propoxyphene retard et procede de fabrication de ces particules |
| US4389393A (en) * | 1982-03-26 | 1983-06-21 | Forest Laboratories, Inc. | Sustained release therapeutic compositions based on high molecular weight hydroxypropylmethylcellulose |
| US4520009A (en) * | 1983-11-28 | 1985-05-28 | Verex Laboratories, Inc. | Sustained released aspirin formulation |
| DE3346571A1 (de) * | 1983-12-23 | 1985-07-04 | Bayer Ag, 5090 Leverkusen | Oral retardierte acetylsalicylsaeureformulierungen |
| KR850700212A (ko) * | 1984-03-21 | 1985-12-26 | 죠지 드모트 | 서방성 약제학적 캼셀제 |
-
1986
- 1986-10-09 GB GB868624213A patent/GB8624213D0/en active Pending
-
1987
- 1987-09-25 HU HU874311A patent/HU201875B/hu not_active IP Right Cessation
- 1987-09-25 NL NL8702294A patent/NL8702294A/nl not_active Application Discontinuation
- 1987-10-02 FR FR878713759A patent/FR2604902B1/fr not_active Expired - Lifetime
- 1987-10-02 BE BE8701131A patent/BE1000732A5/fr not_active IP Right Cessation
- 1987-10-02 CH CH3838/87A patent/CH675831A5/de not_active IP Right Cessation
- 1987-10-03 DE DE19873733540 patent/DE3733540A1/de not_active Withdrawn
- 1987-10-06 LU LU87009A patent/LU87009A1/fr unknown
- 1987-10-06 KR KR870011168A patent/KR880004801A/ko not_active Withdrawn
- 1987-10-06 IL IL84104A patent/IL84104A0/xx unknown
- 1987-10-07 PT PT85880A patent/PT85880B/pt not_active IP Right Cessation
- 1987-10-07 NZ NZ222083A patent/NZ222083A/en unknown
- 1987-10-07 AU AU79420/87A patent/AU7942087A/en not_active Abandoned
- 1987-10-07 NO NO874200A patent/NO874200L/no unknown
- 1987-10-07 GR GR871550A patent/GR871550B/el unknown
- 1987-10-07 GB GB8723515A patent/GB2195893B/en not_active Expired - Lifetime
- 1987-10-07 FI FI874414A patent/FI874414A7/fi not_active IP Right Cessation
- 1987-10-08 CA CA000548872A patent/CA1332809C/en not_active Expired - Lifetime
- 1987-10-08 DK DK527487A patent/DK527487A/da not_active Application Discontinuation
- 1987-10-08 ES ES8702873A patent/ES2014518A6/es not_active Expired - Lifetime
- 1987-10-08 PH PH35906A patent/PH24227A/en unknown
- 1987-10-08 IT IT48469/87A patent/IT1221493B/it active
- 1987-10-08 SE SE8703889A patent/SE8703889L/ not_active Application Discontinuation
- 1987-10-08 JP JP62256149A patent/JPS63101334A/ja active Pending
- 1987-10-09 ZA ZA877617A patent/ZA877617B/xx unknown
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