IL42459A - Medicament formulations having controlled residence time in the gastric region - Google Patents
Medicament formulations having controlled residence time in the gastric regionInfo
- Publication number
- IL42459A IL42459A IL42459A IL4245973A IL42459A IL 42459 A IL42459 A IL 42459A IL 42459 A IL42459 A IL 42459A IL 4245973 A IL4245973 A IL 4245973A IL 42459 A IL42459 A IL 42459A
- Authority
- IL
- Israel
- Prior art keywords
- formulation according
- prepolymer
- cross
- weight
- parts
- Prior art date
Links
- 238000009472 formulation Methods 0.000 title claims 44
- 239000000203 mixture Substances 0.000 title claims 44
- 239000003814 drug Substances 0.000 title claims 22
- 230000002496 gastric effect Effects 0.000 title claims 9
- 238000000034 method Methods 0.000 claims 15
- 239000003431 cross linking reagent Substances 0.000 claims 13
- 125000004432 carbon atom Chemical group C* 0.000 claims 12
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 9
- 239000004014 plasticizer Substances 0.000 claims 9
- PPBRXRYQALVLMV-UHFFFAOYSA-N Styrene Chemical compound C=CC1=CC=CC=C1 PPBRXRYQALVLMV-UHFFFAOYSA-N 0.000 claims 6
- 239000011248 coating agent Substances 0.000 claims 6
- 238000000576 coating method Methods 0.000 claims 6
- -1 alkyl vinyl ether Chemical compound 0.000 claims 5
- UPBDXRPQPOWRKR-UHFFFAOYSA-N furan-2,5-dione;methoxyethene Chemical compound COC=C.O=C1OC(=O)C=C1 UPBDXRPQPOWRKR-UHFFFAOYSA-N 0.000 claims 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 4
- 229920001577 copolymer Polymers 0.000 claims 4
- 239000012530 fluid Substances 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 238000013268 sustained release Methods 0.000 claims 4
- 239000012730 sustained-release form Substances 0.000 claims 4
- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical group CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 claims 4
- GXGJIOMUZAGVEH-UHFFFAOYSA-N Chamazulene Chemical group CCC1=CC=C(C)C2=CC=C(C)C2=C1 GXGJIOMUZAGVEH-UHFFFAOYSA-N 0.000 claims 3
- 150000008065 acid anhydrides Chemical class 0.000 claims 3
- 150000001336 alkenes Chemical class 0.000 claims 3
- 150000001990 dicarboxylic acid derivatives Chemical class 0.000 claims 3
- MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical compound OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 claims 3
- 235000019439 ethyl acetate Nutrition 0.000 claims 3
- 229940093499 ethyl acetate Drugs 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 230000002035 prolonged effect Effects 0.000 claims 3
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical compound OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 claims 2
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- WERYXYBDKMZEQL-UHFFFAOYSA-N butane-1,4-diol Chemical compound OCCCCO WERYXYBDKMZEQL-UHFFFAOYSA-N 0.000 claims 2
- DOIRQSBPFJWKBE-UHFFFAOYSA-N dibutyl phthalate Chemical compound CCCCOC(=O)C1=CC=CC=C1C(=O)OCCCC DOIRQSBPFJWKBE-UHFFFAOYSA-N 0.000 claims 2
- FLKPEMZONWLCSK-UHFFFAOYSA-N diethyl phthalate Chemical compound CCOC(=O)C1=CC=CC=C1C(=O)OCC FLKPEMZONWLCSK-UHFFFAOYSA-N 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 235000013773 glyceryl triacetate Nutrition 0.000 claims 2
- 239000001087 glyceryl triacetate Substances 0.000 claims 2
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 claims 2
- 150000002431 hydrogen Chemical group 0.000 claims 2
- 239000000463 material Substances 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000006353 oxyethylene group Chemical group 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 229920000058 polyacrylate Polymers 0.000 claims 2
- 229920000642 polymer Polymers 0.000 claims 2
- YPFDHNVEDLHUCE-UHFFFAOYSA-N propane-1,3-diol Chemical group OCCCO YPFDHNVEDLHUCE-UHFFFAOYSA-N 0.000 claims 2
- 229960002622 triacetin Drugs 0.000 claims 2
- LDVVTQMJQSCDMK-UHFFFAOYSA-N 1,3-dihydroxypropan-2-yl formate Chemical compound OCC(CO)OC=O LDVVTQMJQSCDMK-UHFFFAOYSA-N 0.000 claims 1
- VILCJCGEZXAXTO-UHFFFAOYSA-N 2,2,2-tetramine Chemical compound NCCNCCNCCN VILCJCGEZXAXTO-UHFFFAOYSA-N 0.000 claims 1
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- PIICEJLVQHRZGT-UHFFFAOYSA-N Ethylenediamine Chemical compound NCCN PIICEJLVQHRZGT-UHFFFAOYSA-N 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 235000021355 Stearic acid Nutrition 0.000 claims 1
- 239000004098 Tetracycline Substances 0.000 claims 1
- XSTXAVWGXDQKEL-UHFFFAOYSA-N Trichloroethylene Chemical compound ClC=C(Cl)Cl XSTXAVWGXDQKEL-UHFFFAOYSA-N 0.000 claims 1
- 229960001138 acetylsalicylic acid Drugs 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 229960003022 amoxicillin Drugs 0.000 claims 1
- LSQZJLSUYDQPKJ-NJBDSQKTSA-N amoxicillin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C(O)=O)(C)C)=CC=C(O)C=C1 LSQZJLSUYDQPKJ-NJBDSQKTSA-N 0.000 claims 1
- AVKUERGKIZMTKX-NJBDSQKTSA-N ampicillin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C(O)=O)(C)C)=CC=CC=C1 AVKUERGKIZMTKX-NJBDSQKTSA-N 0.000 claims 1
- 229960000723 ampicillin Drugs 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 229910000019 calcium carbonate Inorganic materials 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 229960000541 cetyl alcohol Drugs 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 238000004132 cross linking Methods 0.000 claims 1
- 150000004985 diamines Chemical class 0.000 claims 1
- 229960002380 dibutyl phthalate Drugs 0.000 claims 1
- 150000002009 diols Chemical class 0.000 claims 1
- DLNKOYKMWOXYQA-UHFFFAOYSA-N dl-pseudophenylpropanolamine Natural products CC(N)C(O)C1=CC=CC=C1 DLNKOYKMWOXYQA-UHFFFAOYSA-N 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 235000011187 glycerol Nutrition 0.000 claims 1
- 229940075507 glyceryl monostearate Drugs 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims 1
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 claims 1
- LSHROXHEILXKHM-UHFFFAOYSA-N n'-[2-[2-[2-(2-aminoethylamino)ethylamino]ethylamino]ethyl]ethane-1,2-diamine Chemical compound NCCNCCNCCNCCNCCN LSHROXHEILXKHM-UHFFFAOYSA-N 0.000 claims 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 1
- 239000006186 oral dosage form Substances 0.000 claims 1
- LSQZJLSUYDQPKJ-UHFFFAOYSA-N p-Hydroxyampicillin Natural products O=C1N2C(C(O)=O)C(C)(C)SC2C1NC(=O)C(N)C1=CC=C(O)C=C1 LSQZJLSUYDQPKJ-UHFFFAOYSA-N 0.000 claims 1
- 229960002895 phenylbutazone Drugs 0.000 claims 1
- VYMDGNCVAMGZFE-UHFFFAOYSA-N phenylbutazonum Chemical compound O=C1C(CCCC)C(=O)N(C=2C=CC=CC=2)N1C1=CC=CC=C1 VYMDGNCVAMGZFE-UHFFFAOYSA-N 0.000 claims 1
- DLNKOYKMWOXYQA-APPZFPTMSA-N phenylpropanolamine Chemical compound C[C@@H](N)[C@H](O)C1=CC=CC=C1 DLNKOYKMWOXYQA-APPZFPTMSA-N 0.000 claims 1
- 229960000395 phenylpropanolamine Drugs 0.000 claims 1
- 229920001483 poly(ethyl methacrylate) polymer Polymers 0.000 claims 1
- 229920003229 poly(methyl methacrylate) Polymers 0.000 claims 1
- 229920001515 polyalkylene glycol Polymers 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 239000004926 polymethyl methacrylate Substances 0.000 claims 1
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 claims 1
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 claims 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims 1
- 239000001103 potassium chloride Substances 0.000 claims 1
- 235000011164 potassium chloride Nutrition 0.000 claims 1
- 229960002816 potassium chloride Drugs 0.000 claims 1
- 239000008117 stearic acid Substances 0.000 claims 1
- 229960002180 tetracycline Drugs 0.000 claims 1
- 229930101283 tetracycline Natural products 0.000 claims 1
- 235000019364 tetracycline Nutrition 0.000 claims 1
- 150000003522 tetracyclines Chemical class 0.000 claims 1
- 229960001124 trientine Drugs 0.000 claims 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
-
- 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
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
- A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Claims (52)
1. A sustained release medicament formulation with prolonged gastric residence comprising a) a medicament core or a core comprising a diagnostic aid, and b) a pharmaceutically acceptable coating on said core comprising. (1) a pharmaceutically acceptable cross-linked polymeric component which comprises a prepolymer cross-linked with a cross-linking agent at a ratio of 8 parts by weight of prepolymer to 0.15 to 4 parts by weight of cross-linking agent, the prepolymer being a copolymer of (1) 20-90 parts by weight of a substituted or unsubstituted unsaturated dicarboxylic acid or acid anhydride having 1 to 3 carbon atoms between the two carboxylic groups, and (ii) 10-80 parts by weight of an alkene of 2 to 6 carbon atoms, styrene or an alkyl vinyl ether in which the alkyl radical contains 1 to 16 carbon atoms , said polymeric film being water-hydratable , water-permeable and swellable in the presence of gastric fluids, ..424i£>"S- - 563-- 118-3324 r a d , optionally , (2) a pharmaceutically acceptable, substantially water-insoluble polymeric component.
2. A sustained release medicament formulation with prolonged gastric residence comprising a) a medicament core, and b) a pharmaceutically acceptable coating on said core comprising a cross-linked polymeric film which comprises a prepolymer cross-linked with a cross-linking agent at a ratio of 8 parts by weight of prepolymer to 0.15 to 4 parts by weight of cross-linking agent, the prepolymer being a copolymer of (i) 20-90 parts by weight of a substituted or unsubstituted unsaturated dicarboxylic acid or acid anhydride having 1 to 3 carbon atoms between the two carboxylic groups, and (ii) 10-80 parts by weight of an alkene of 2 to 6 carbon atoms, styrene or an alkyl vinyl ether in which the alkyl radical contains 1 to 16 carbon atoms , said polymeric film being water-hydratable, water- permeable and swellable in the presence of gastric fluids. - 57 - 118-3324
3. A formulation according to Claim 2, in which the polymeric film comprises a prepolymer cross-linked with a cross-linking agent at a ratio of 8 parts by weight of prepolymer to 0.15 to 1.5 parts by weight of cross-linking agent.
4. A formulation according to Claim 2 or 3"j in which the prepolymer contains repeating units of formula I , in which one of and R? is hydrogen and the other is hydrogen, chlorine, fluorine, hydroxy, alkyl of 1 to 16 carbon atoms, aryl, aralkyl or -SO^H, and R is dimethylene, optionally substituted by alkyl of 1 to 4 carbon atoms, phenyl,- or alkoxy of 1 to 12 carbon atoms , or is -CH -CH=CH-CH„-. - 58 - 118-3324
5. A formulation according to Claim 4, in which the prepolymer contains repeating units of formula I, in which each of and R2 is hydrogen, and R is dimethylene optionally substituted by phenyl or methoxy.
6. A formulation according to Claim 5, in which the prepolymer contains repeating units of formula I, in which each of ^ and R2 is hydrogen and R is dimethylene substituted by methoxy.
7. A formulation according to any one of Claims 2 to 6, in which the average molecular weight of the prepolymer is from 100,000 to 5,000,000.
8. A formulation according to Claim 7,. in which the average molecular weight is 250,000 to 2,000,000.
9. A formulation according to any one of Claims 2 to 7, in which the prepolymer is that knov/n under the trade name Gantrez AN-119, Gantrez AN-139, Gantrez AN-149, Gantrez AN-169 or Gantrez AN-179 , as hereinbefore defined.
10. A formulation according to any one of Claims 2 to 9, in which the cross-linking agent is an alk lene diol, a polyalkylene glycol, a long-chain dihydric compound, a diamine, or a triol.
11. A formulation according to Claim 10, in which the cross-linking agent is 1 , 3-propylene diol, 42459-2 - 59 - 118-3324 diethylene glycol, glycerine, polyethyleneglycol, poly-tetramethylene glycol, methoxypolyethylene glycol, a poly-oxyethylene sorbitan ether, ethylene diamine, triethylene tetramine, pentaethylene hexamine or 1,2 ,3-but.ane-triol.
12. A formulation according to Claim 11, in which the cross-linking agent is an alkylene diol or poly-oxyethylene sorbitan ether.
13. A formulation according to any one of Claims 10 to 12, in which the cross-linking agent is polyoxy-ethylene sorbitan monooleate or monolaurate.
14. A formulation according to any one of Claims 2 to 13, in which the polymeric film incorporates a plasticiser.
15. A formulation according to any one of Claims 2 to 14, in which the prepolymer is cross-linked in the presence of a plasticiser, which is present to the extent of 8 parts by weight of prepolymer to 1 to 10 parts by weight of plasticiser.
16. A formulation according to Claim 15, in which the plasticiser is present to the extent of 8 parts by weight of polymer to 1 to 7 parts by weight of plasticiser. - 60 - 118-3324
17. A formulation according to Claim 16, in which the plasticiser is present to the extent of 8 parts by weight of prepolymer to 4 to 5 parts by weight of plasticiser.
18. A formulation according to any one of claims 14 to 17, in which the plasticiser is glyceryltri-acetate, ethylacetate , diethyl phthalate or dibutyl-phthalate.
19. A formulation according to Claim 18, in which the plasticiser is glyceryl triacetate.
20. A formulation according to any one of Claims 2 to 19, in which the polymeric film incorporates a material which is soluble in gastric fluids to provide for film opening.
21. A formulation according to Claim 20, in which the material is finely divided calcium carbonate.
22. A sustained release medicament formulation with prolonged gastric residence, comprising a) a medicament core and b) a pharmaceutically acceptable coating on said core comprising a binary polymeric film including 1) a , harmaceutically acceptable, substantially water-insoluble, polymeric component 42459-2 - 61 - 118-3324 ·♦'· and 2) a pharmaceutically acceptable cross- linked polymeric component which comprises a prepolymer cross-linked with a cross-linking agent at a ratio of 8 parts by weight of prepolymer to 0.15 to 4 parts by weight of cross-linking agent, the prepolymer being a copolymer of i) 20 to 90 parts by weight of a substituted or unsubstituted unsaturated dicarboxylic acid or acid anhydride having 1 to 3 carbon atoms between the two carboxylic groups, and (ii) 10-80 parts by weight of an alkene of 2 to 6 carbon atoms, styrene or an alkyl vinyl ether in which the alkyl radical contains 1 to 16 carbon atoms, said polymeric component being water-hydratable , water-permeable and swellable in the presence of gastric fluids.
23. A formulation according to Claim 22, in which the substantially insoluble polymeric component is a carboxyl containing or carboxylate copolymer. 42459-2
24. A formulation according to claim 23, in which the substantially water-insoluble polymeric component is a polyacrylate.
25. A formulation according to claim 24, in which the polyacrylate is poly (methylmethacrylate) or poly (ethylmethacrylate) .
26. A formulation according to any one of claims 22 to 25, in which the second polymeric component is a prepolymer defined in any one of claims 3 to 8.
27. A formulation according to any one of claims 22 to 26, in which the binary polymeric film comprises the first and second polymeric components in a ratio of from 90:10 to 10:90 by weight.
28. A formulation according to claim 27, in which the ratio is 60:40 to 10:90.
29. A formulation according to any one of the preceding claims, in which the medicament core is in the form of a tablet or capsule.
30. A formulation according to any one .of the preceding claims, in which the medicament core is in the form of a tablet.
31. A formulation according to any one , of the preceding claims, in which only part of the medicament core is coated with the polymeric film. $ 2 59-2 - 63 - 118-3324
32. A formulation according to claim 31, in which the medicament core comprises a multilayer tablet having a first layer comprising a water-insoluble drug and a second layer comprising a water-soluble drug, the second layer but not the first layer being coated with the polymeric film.
33. A formulation according to Claim 32, in which the tablet has an intermediary film bonding layer, the film being coated on the second layer and the intermediary layer.
34. A formulation according to claim 33, in which the intermediary bonding layer comprises stearic acid, glyceryl monostearate , spermacetti , cetyl alcohol or an acetylated monoglyceride .
35. A formulation according to claim 34, in which the intermediary bonding layer, additionally comprises a polymeric component comprising a prepolymer according to any one of claims 3 to 8.
36. A formulation according to any one of the preceding claims, in which the medicament core comprises tetracycline, ampicillin, aspirin, potassium chloride phenylpropanolamine, phenyl butazone, amoxycillin or pehtaerythritol tetranitrate .
37. A sustained release medicament formulation A2459 -2 - 64 - 118-3324 substantially , as herein described with reference to any one of the preceding Examples.
38. A method of producing a formulation according to Claim 2, which comprises a) coating a medicament core with a solution comprising a prepolymer and a cross-linking agent, as defined in Claim 2, and b) subjecting the resulting coated medicament core to cross-linking conditions.
39. A method according to claim 38, for the production of a formulation according to any one of claims 2 to 21, and 29 to 36, (as appendant to claims 2 to 21).
40. A method according to claim 38 or 39, in which the solution is in ethylacetate .
41. A method according to claim 30, 39, or . 40., in which the resulting coated medicament core is subjected to a temperature of from 10° to 90 °C and a relative humidity of from 30 to 95%.
42. A method according to claim 30, 39, 40 or 41, in which the resulting coated medicament core is subjected to a temperature of from 20° to 60°C and a relative humidity of from 40 to 60%.
43. A method according to any one of claims 38 42459-2 - 65 - 118-3324 to 42, in which the resulting coated medicament core is cross-linked in its shipping container.
44. A method according to claim 38, substantially as herein described with reference ;to any one of the Examples 1 to 7.
45. A formulation according to claim 2, whenever produced by a process according to any one of claims 38 to 44. .
46. A process for the production of a formulation according to claim 22, comprising coating a medicament core with a solution of a binary polymer comprising components 1) and 2), defined in claim 22.
47. A process according to Claim 46, in which the solution is in ethyl acetate.
48. A method according to claim 46 or 47, for the production of a formulation according to any one of claims 22, 28, 29 or 48 (as appendent to claims 22 to 28).
49. A method according to claim 46, substantially as herein described with reference to Example 8.
50. • 50. A formulation according to claim 22, whenever produced by a method according to any one of claims 46 to 49.
51. A method of increasing the potential gastric residence time of an oral dosage form, which comprises 42459-2 - 66 - 118-3324 providing a medicament core with a coating comprising polymeric film defined in any one of claims 1 to 28.
52. A method according to claim 51, substan tially as herein described with reference to any one o the Examples. 3700/MO/HD For the Appl ¾aats
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26124272A | 1972-06-09 | 1972-06-09 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL42459A0 IL42459A0 (en) | 1973-08-29 |
| IL42459A true IL42459A (en) | 1976-12-31 |
Family
ID=22992462
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL42459A IL42459A (en) | 1972-06-09 | 1973-06-07 | Medicament formulations having controlled residence time in the gastric region |
Country Status (19)
| Country | Link |
|---|---|
| JP (1) | JPS4961323A (en) |
| AU (2) | AU5682673A (en) |
| BE (1) | BE800637A (en) |
| CA (1) | CA1040533A (en) |
| CH (1) | CH582002A5 (en) |
| DD (2) | DD109309A5 (en) |
| DE (1) | DE2328580A1 (en) |
| ES (1) | ES415624A3 (en) |
| FR (1) | FR2187290B1 (en) |
| GB (1) | GB1428426A (en) |
| HU (1) | HU167947B (en) |
| IE (1) | IE38151B1 (en) |
| IL (1) | IL42459A (en) |
| NL (1) | NL7307737A (en) |
| OA (1) | OA04931A (en) |
| PL (1) | PL90109B1 (en) |
| RO (1) | RO64146A (en) |
| SE (1) | SE395609B (en) |
| ZA (1) | ZA733897B (en) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4207890A (en) | 1977-01-04 | 1980-06-17 | Mcneilab, Inc. | Drug-dispensing device and method |
| JPS5911563B2 (en) * | 1980-02-27 | 1984-03-16 | 日本原子力研究所 | Method for manufacturing multilayer sustained release composites |
| US4518433A (en) * | 1982-11-08 | 1985-05-21 | Fmc Corporation | Enteric coating for pharmaceutical dosage forms |
| DE3314003A1 (en) * | 1983-04-18 | 1984-10-18 | Boehringer Ingelheim KG, 6507 Ingelheim | DIVISIBLE TABLET WITH DELAYED ACTIVE SUBSTANCE RELEASE AND METHOD FOR THE PRODUCTION THEREOF |
| US4657784A (en) * | 1986-03-10 | 1987-04-14 | Ecolab Inc. | Process for encapsulating particles with at least two coating layers having different melting points |
| GB2196252B (en) * | 1986-09-18 | 1990-10-17 | London Pharmacy Innovation | Gastric controlled-release dosage forms |
| US4837030A (en) * | 1987-10-06 | 1989-06-06 | American Cyanamid Company | Novel controlled release formulations of tetracycline compounds |
| AU614328B2 (en) * | 1988-02-01 | 1991-08-29 | Mayne Pharma International Pty Ltd | Tetracycline dosage form |
| EP0327295A3 (en) * | 1988-02-01 | 1989-09-06 | F.H. FAULDING & CO. LTD. | Tetracycline dosage form |
| US5007790A (en) * | 1989-04-11 | 1991-04-16 | Depomed Systems, Inc. | Sustained-release oral drug dosage form |
| ES2270982T3 (en) | 2000-02-04 | 2007-04-16 | Depomed, Inc. | DOSAGE FORM OF NUCLEO AND CARCASA THAT IS APPROXIMATE TO A RELEASE OF THE ZERO ORDER PHARMACO. |
| US20130143867A1 (en) | 2011-12-02 | 2013-06-06 | Sychroneuron Inc. | Acamprosate formulations, methods of using the same, and combinations comprising the same |
| EP3878445A3 (en) | 2013-06-05 | 2021-10-27 | Synchroneuron Inc. | Acamprosate formulations, methods of using the same, and combinations comprising the same |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1050353B (en) * | 1966-01-06 | 1981-03-10 | Ceskoslovenska Akademie Ved | SUPPORTS FOR BIOLOGICALLY ACTIVE SUBSTANCES |
| AU454482B2 (en) * | 1970-11-05 | 1974-10-15 | Alza Corporation | Drug-delivery system |
-
1973
- 1973-05-30 CH CH781473A patent/CH582002A5/xx not_active IP Right Cessation
- 1973-06-01 SE SE7307796A patent/SE395609B/en unknown
- 1973-06-04 NL NL7307737A patent/NL7307737A/xx not_active Application Discontinuation
- 1973-06-05 GB GB2666273A patent/GB1428426A/en not_active Expired
- 1973-06-05 DE DE2328580A patent/DE2328580A1/en active Pending
- 1973-06-06 RO RO7300075051A patent/RO64146A/en unknown
- 1973-06-06 CA CA173,291A patent/CA1040533A/en not_active Expired
- 1973-06-07 FR FR7320766A patent/FR2187290B1/fr not_active Expired
- 1973-06-07 IL IL42459A patent/IL42459A/en unknown
- 1973-06-07 IE IE925/73A patent/IE38151B1/en unknown
- 1973-06-07 BE BE132036A patent/BE800637A/en unknown
- 1973-06-07 HU HUPU185A patent/HU167947B/hu unknown
- 1973-06-07 ES ES415624A patent/ES415624A3/en not_active Expired
- 1973-06-08 ZA ZA00733897A patent/ZA733897B/en unknown
- 1973-06-08 DD DD171441A patent/DD109309A5/xx unknown
- 1973-06-08 DD DD179622*A patent/DD112354A5/xx unknown
- 1973-06-08 PL PL1973163192A patent/PL90109B1/pl unknown
- 1973-06-09 JP JP48065304A patent/JPS4961323A/ja active Pending
- 1973-06-12 AU AU56826/73A patent/AU5682673A/en not_active Expired
- 1973-06-13 OA OA54935A patent/OA04931A/en unknown
- 1973-08-17 AU AU59357/73A patent/AU5935773A/en not_active Expired
Also Published As
| Publication number | Publication date |
|---|---|
| DE2328580A1 (en) | 1974-01-10 |
| DD109309A5 (en) | 1974-11-05 |
| IE38151B1 (en) | 1978-01-04 |
| AU5682673A (en) | 1974-12-12 |
| IE38151L (en) | 1973-12-09 |
| GB1428426A (en) | 1976-03-17 |
| BE800637A (en) | 1973-12-07 |
| NL7307737A (en) | 1973-12-11 |
| FR2187290B1 (en) | 1977-04-15 |
| CH582002A5 (en) | 1976-11-30 |
| CA1040533A (en) | 1978-10-17 |
| DD112354A5 (en) | 1975-04-12 |
| JPS4961323A (en) | 1974-06-14 |
| RO64146A (en) | 1978-11-15 |
| FR2187290A1 (en) | 1974-01-18 |
| OA04931A (en) | 1980-10-31 |
| ES415624A3 (en) | 1976-10-16 |
| PL90109B1 (en) | 1977-01-31 |
| IL42459A0 (en) | 1973-08-29 |
| HU167947B (en) | 1976-01-28 |
| SE395609B (en) | 1977-08-22 |
| AU5935773A (en) | 1975-02-20 |
| ZA733897B (en) | 1975-01-29 |
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