IL106253A - Controlled release oral solid pharmaceutical dosage form, its preparation and a pharmaceutical excipient for use therein - Google Patents
Controlled release oral solid pharmaceutical dosage form, its preparation and a pharmaceutical excipient for use thereinInfo
- Publication number
- IL106253A IL106253A IL106253A IL10625393A IL106253A IL 106253 A IL106253 A IL 106253A IL 106253 A IL106253 A IL 106253A IL 10625393 A IL10625393 A IL 10625393A IL 106253 A IL106253 A IL 106253A
- Authority
- IL
- Israel
- Prior art keywords
- gum
- surfactant
- dosage form
- wetting agent
- oral solid
- Prior art date
Links
- 238000013270 controlled release Methods 0.000 title claims abstract description 44
- 239000000546 pharmaceutical excipient Substances 0.000 title claims description 75
- 239000002552 dosage form Substances 0.000 title claims description 16
- 229940124531 pharmaceutical excipient Drugs 0.000 title claims description 7
- 239000007787 solid Substances 0.000 title claims description 4
- 238000002360 preparation method Methods 0.000 title description 4
- 239000000203 mixture Substances 0.000 claims abstract description 95
- 239000003814 drug Substances 0.000 claims abstract description 67
- 238000009472 formulation Methods 0.000 claims abstract description 32
- 239000000080 wetting agent Substances 0.000 claims abstract description 29
- 239000011159 matrix material Substances 0.000 claims abstract description 21
- 238000000034 method Methods 0.000 claims abstract description 19
- 239000008180 pharmaceutical surfactant Substances 0.000 claims abstract description 12
- 239000003085 diluting agent Substances 0.000 claims abstract description 4
- 239000004094 surface-active agent Substances 0.000 claims description 48
- 229920001285 xanthan gum Polymers 0.000 claims description 31
- 239000000230 xanthan gum Substances 0.000 claims description 30
- 235000010493 xanthan gum Nutrition 0.000 claims description 30
- 229940082509 xanthan gum Drugs 0.000 claims description 30
- 229920000869 Homopolysaccharide Polymers 0.000 claims description 26
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 26
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 26
- -1 alkyl ether carboxylates Chemical class 0.000 claims description 25
- 229920000161 Locust bean gum Polymers 0.000 claims description 24
- 239000000711 locust bean gum Substances 0.000 claims description 24
- 235000010420 locust bean gum Nutrition 0.000 claims description 24
- 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 claims description 18
- 239000008121 dextrose Substances 0.000 claims description 18
- 239000012530 fluid Substances 0.000 claims description 18
- 239000008184 oral solid dosage form Substances 0.000 claims description 17
- 238000004132 cross linking Methods 0.000 claims description 13
- 238000010521 absorption reaction Methods 0.000 claims description 9
- 239000007864 aqueous solution Substances 0.000 claims description 9
- 235000019329 dioctyl sodium sulphosuccinate Nutrition 0.000 claims description 9
- 150000002016 disaccharides Chemical class 0.000 claims description 9
- 229960000878 docusate sodium Drugs 0.000 claims description 9
- APSBXTVYXVQYAB-UHFFFAOYSA-M sodium docusate Chemical compound [Na+].CCCCC(CC)COC(=O)CC(S([O-])(=O)=O)C(=O)OCC(CC)CCCC APSBXTVYXVQYAB-UHFFFAOYSA-M 0.000 claims description 9
- 230000002496 gastric effect Effects 0.000 claims description 8
- 239000003701 inert diluent Substances 0.000 claims description 8
- 150000002772 monosaccharides Chemical class 0.000 claims description 8
- 239000008024 pharmaceutical diluent Substances 0.000 claims description 8
- 150000005846 sugar alcohols Polymers 0.000 claims description 8
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical class CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 7
- 150000001298 alcohols Chemical class 0.000 claims description 6
- 239000003945 anionic surfactant Substances 0.000 claims description 6
- 239000003093 cationic surfactant Substances 0.000 claims description 6
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 6
- 150000002148 esters Chemical class 0.000 claims description 6
- 239000000194 fatty acid Substances 0.000 claims description 6
- 229930195729 fatty acid Natural products 0.000 claims description 6
- 238000002156 mixing Methods 0.000 claims description 6
- 239000002736 nonionic surfactant Substances 0.000 claims description 6
- 229920000642 polymer Polymers 0.000 claims description 6
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 5
- 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 claims description 5
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 5
- 229930006000 Sucrose Natural products 0.000 claims description 5
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims description 5
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- 230000001225 therapeutic effect Effects 0.000 claims description 5
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical class OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 claims description 4
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 4
- 229920002584 Polyethylene Glycol 6000 Polymers 0.000 claims description 4
- 235000021355 Stearic acid Nutrition 0.000 claims description 4
- 150000008051 alkyl sulfates Chemical class 0.000 claims description 4
- 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 claims description 4
- 150000001875 compounds Chemical class 0.000 claims description 4
- 239000003172 expectorant agent Substances 0.000 claims description 4
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 4
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 4
- 239000008117 stearic acid Substances 0.000 claims description 4
- 150000003871 sulfonates Chemical class 0.000 claims description 4
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 3
- 210000001035 gastrointestinal tract Anatomy 0.000 claims description 3
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 3
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- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 3
- XDIYNQZUNSSENW-UUBOPVPUSA-N (2R,3S,4R,5R)-2,3,4,5,6-pentahydroxyhexanal Chemical class OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=O XDIYNQZUNSSENW-UUBOPVPUSA-N 0.000 claims description 2
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 claims description 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical class OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 2
- 239000005715 Fructose Substances 0.000 claims description 2
- 229930091371 Fructose Natural products 0.000 claims description 2
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 claims description 2
- 240000007472 Leucaena leucocephala Species 0.000 claims description 2
- 235000010643 Leucaena leucocephala Nutrition 0.000 claims description 2
- 239000008118 PEG 6000 Substances 0.000 claims description 2
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 2
- 239000002202 Polyethylene glycol Substances 0.000 claims description 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical class OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims description 2
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 claims description 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 2
- 125000002252 acyl group Chemical group 0.000 claims description 2
- 125000005910 alkyl carbonate group Chemical group 0.000 claims description 2
- 125000005599 alkyl carboxylate group Chemical group 0.000 claims description 2
- 150000001408 amides Chemical class 0.000 claims description 2
- 150000001412 amines Chemical class 0.000 claims description 2
- 229940035676 analgesics Drugs 0.000 claims description 2
- 229940069428 antacid Drugs 0.000 claims description 2
- 239000003159 antacid agent Substances 0.000 claims description 2
- 239000000730 antalgic agent Substances 0.000 claims description 2
- 239000003242 anti bacterial agent Substances 0.000 claims description 2
- 230000001088 anti-asthma Effects 0.000 claims description 2
- 230000001142 anti-diarrhea Effects 0.000 claims description 2
- 230000003474 anti-emetic effect Effects 0.000 claims description 2
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- 229940088710 antibiotic agent Drugs 0.000 claims description 2
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- 229940124572 antihypotensive agent Drugs 0.000 claims description 2
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- 229940124581 decongestants Drugs 0.000 claims description 2
- MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical class OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 claims description 2
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- 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 2
- 125000005908 glyceryl ester group Chemical group 0.000 claims description 2
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Classifications
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- 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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
-
- 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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Solid-Sorbent Or Filter-Aiding Compositions (AREA)
- Polysaccharides And Polysaccharide Derivatives (AREA)
- Lubricants (AREA)
- Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US07/922,312 US5472711A (en) | 1992-07-30 | 1992-07-30 | Agglomerated hydrophilic complexes with multi-phasic release characteristics |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL106253A0 IL106253A0 (en) | 1993-11-15 |
| IL106253A true IL106253A (en) | 1998-03-10 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL106253A IL106253A (en) | 1992-07-30 | 1993-07-06 | Controlled release oral solid pharmaceutical dosage form, its preparation and a pharmaceutical excipient for use therein |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US5472711A (de) |
| EP (2) | EP1582205A3 (de) |
| JP (1) | JP3967389B2 (de) |
| KR (1) | KR100342299B1 (de) |
| AT (1) | ATE311861T1 (de) |
| AU (1) | AU669531B2 (de) |
| CA (1) | CA2101189C (de) |
| DE (1) | DE69333927T2 (de) |
| ES (1) | ES2252731T3 (de) |
| FI (1) | FI117962B (de) |
| HU (1) | HUT67622A (de) |
| IL (1) | IL106253A (de) |
| MX (1) | MX9304485A (de) |
Families Citing this family (85)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5472711A (en) * | 1992-07-30 | 1995-12-05 | Edward Mendell Co., Inc. | Agglomerated hydrophilic complexes with multi-phasic release characteristics |
| US5773025A (en) * | 1993-09-09 | 1998-06-30 | Edward Mendell Co., Inc. | Sustained release heterodisperse hydrogel systems--amorphous drugs |
| US5455046A (en) * | 1993-09-09 | 1995-10-03 | Edward Mendell Co., Inc. | Sustained release heterodisperse hydrogel systems for insoluble drugs |
| US6726930B1 (en) | 1993-09-09 | 2004-04-27 | Penwest Pharmaceuticals Co. | Sustained release heterodisperse hydrogel systems for insoluble drugs |
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Also Published As
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| KR940005291A (ko) | 1994-03-21 |
| EP1582205A3 (de) | 2008-07-30 |
| US5472711A (en) | 1995-12-05 |
| ES2252731T3 (es) | 2006-05-16 |
| EP1582205A2 (de) | 2005-10-05 |
| US5670168A (en) | 1997-09-23 |
| IL106253A0 (en) | 1993-11-15 |
| EP0581676A3 (de) | 1995-06-07 |
| EP0581676B1 (de) | 2005-12-07 |
| FI933393L (fi) | 1994-01-31 |
| CA2101189C (en) | 1999-09-21 |
| US5478574A (en) | 1995-12-26 |
| JP3967389B2 (ja) | 2007-08-29 |
| AU669531B2 (en) | 1996-06-13 |
| JPH06172221A (ja) | 1994-06-21 |
| KR100342299B1 (ko) | 2002-11-18 |
| FI117962B (fi) | 2007-05-15 |
| CA2101189A1 (en) | 1994-01-31 |
| DE69333927D1 (de) | 2006-01-12 |
| AU4185593A (en) | 1994-02-03 |
| MX9304485A (es) | 1994-04-29 |
| EP0581676A2 (de) | 1994-02-02 |
| ATE311861T1 (de) | 2005-12-15 |
| HU9302104D0 (en) | 1993-10-28 |
| DE69333927T2 (de) | 2006-06-29 |
| HUT67622A (en) | 1995-04-28 |
| FI933393A0 (fi) | 1993-07-29 |
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