WO2000056266A2 - Taste masking coating compositions - Google Patents
Taste masking coating compositions Download PDFInfo
- Publication number
- WO2000056266A2 WO2000056266A2 PCT/IB1999/001735 IB9901735W WO0056266A2 WO 2000056266 A2 WO2000056266 A2 WO 2000056266A2 IB 9901735 W IB9901735 W IB 9901735W WO 0056266 A2 WO0056266 A2 WO 0056266A2
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- composition
- dry weight
- film forming
- present
- polymers
- Prior art date
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- 239000008199 coating composition Substances 0.000 title claims abstract description 13
- 235000019640 taste Nutrition 0.000 title description 21
- 230000000873 masking effect Effects 0.000 title description 13
- 229920000642 polymer Polymers 0.000 claims abstract description 49
- 239000000203 mixture Substances 0.000 claims abstract description 37
- 229940079593 drug Drugs 0.000 claims abstract description 31
- 239000003814 drug Substances 0.000 claims abstract description 31
- 239000000463 material Substances 0.000 claims abstract description 6
- 239000007888 film coating Substances 0.000 claims abstract 2
- 238000009501 film coating Methods 0.000 claims abstract 2
- 238000000576 coating method Methods 0.000 claims description 19
- 239000011248 coating agent Substances 0.000 claims description 18
- 229920002125 Sokalan® Polymers 0.000 claims description 12
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 12
- 239000003795 chemical substances by application Substances 0.000 claims description 10
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 9
- -1 carragennan Polymers 0.000 claims description 8
- 230000005465 channeling Effects 0.000 claims description 8
- 239000000454 talc Substances 0.000 claims description 8
- 229910052623 talc Inorganic materials 0.000 claims description 8
- 239000000314 lubricant Substances 0.000 claims description 7
- 239000002245 particle Substances 0.000 claims description 7
- 239000004014 plasticizer Substances 0.000 claims description 7
- 235000019359 magnesium stearate Nutrition 0.000 claims description 6
- 229920001223 polyethylene glycol Polymers 0.000 claims description 6
- 239000000725 suspension Substances 0.000 claims description 6
- 239000002202 Polyethylene glycol Substances 0.000 claims description 5
- 229920002472 Starch Polymers 0.000 claims description 5
- DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 claims description 5
- 239000008107 starch Substances 0.000 claims description 5
- 235000019698 starch Nutrition 0.000 claims description 5
- 239000001069 triethyl citrate Substances 0.000 claims description 5
- 235000013769 triethyl citrate Nutrition 0.000 claims description 5
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 claims description 5
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 4
- 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 4
- DOIRQSBPFJWKBE-UHFFFAOYSA-N dibutyl phthalate Chemical compound CCCCOC(=O)C1=CC=CC=C1C(=O)OCCCC DOIRQSBPFJWKBE-UHFFFAOYSA-N 0.000 claims description 4
- 239000004615 ingredient Substances 0.000 claims description 4
- 239000008101 lactose Substances 0.000 claims description 4
- 239000007910 chewable tablet Substances 0.000 claims description 3
- 239000007919 dispersible tablet Substances 0.000 claims description 3
- PYGXAGIECVVIOZ-UHFFFAOYSA-N Dibutyl decanedioate Chemical compound CCCCOC(=O)CCCCCCCCC(=O)OCCCC PYGXAGIECVVIOZ-UHFFFAOYSA-N 0.000 claims description 2
- 229920013820 alkyl cellulose Polymers 0.000 claims description 2
- 239000008119 colloidal silica Substances 0.000 claims description 2
- 239000000839 emulsion Substances 0.000 claims description 2
- 229940075507 glyceryl monostearate Drugs 0.000 claims description 2
- 229920003145 methacrylic acid copolymer Polymers 0.000 claims description 2
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 claims description 2
- WEAPVABOECTMGR-UHFFFAOYSA-N triethyl 2-acetyloxypropane-1,2,3-tricarboxylate Chemical compound CCOC(=O)CC(C(=O)OCC)(OC(C)=O)CC(=O)OCC WEAPVABOECTMGR-UHFFFAOYSA-N 0.000 claims description 2
- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 claims 2
- 239000004372 Polyvinyl alcohol Substances 0.000 claims 1
- 229920001577 copolymer Polymers 0.000 claims 1
- 229940099371 diacetylated monoglycerides Drugs 0.000 claims 1
- 125000003976 glyceryl group Chemical group [H]C([*])([H])C(O[H])([H])C(O[H])([H])[H] 0.000 claims 1
- 239000001087 glyceryl triacetate Substances 0.000 claims 1
- 235000013773 glyceryl triacetate Nutrition 0.000 claims 1
- 239000006186 oral dosage form Substances 0.000 claims 1
- 229920002451 polyvinyl alcohol Polymers 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 229960002622 triacetin Drugs 0.000 claims 1
- 238000004090 dissolution Methods 0.000 description 11
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 11
- MYSWGUAQZAJSOK-UHFFFAOYSA-N ciprofloxacin Chemical compound C12=CC(N3CCNCC3)=C(F)C=C2C(=O)C(C(=O)O)=CN1C1CC1 MYSWGUAQZAJSOK-UHFFFAOYSA-N 0.000 description 10
- 239000000243 solution Substances 0.000 description 10
- 239000006185 dispersion Substances 0.000 description 9
- 235000019658 bitter taste Nutrition 0.000 description 8
- 239000008187 granular material Substances 0.000 description 8
- 238000000034 method Methods 0.000 description 8
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 7
- 239000007787 solid Substances 0.000 description 7
- 229910002016 Aerosil® 200 Inorganic materials 0.000 description 6
- ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 description 5
- 239000001856 Ethyl cellulose Substances 0.000 description 5
- 229960003405 ciprofloxacin Drugs 0.000 description 5
- 229920001249 ethyl cellulose Polymers 0.000 description 5
- 235000019325 ethyl cellulose Nutrition 0.000 description 5
- 238000003756 stirring Methods 0.000 description 5
- 239000003826 tablet Substances 0.000 description 5
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 4
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 4
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 description 4
- 239000002552 dosage form Substances 0.000 description 4
- 229960003276 erythromycin Drugs 0.000 description 4
- 229960001680 ibuprofen Drugs 0.000 description 4
- 229960005489 paracetamol Drugs 0.000 description 4
- KEJCWVGMRLCZQQ-YJBYXUATSA-N Cefuroxime axetil Chemical compound N([C@@H]1C(N2C(=C(COC(N)=O)CS[C@@H]21)C(=O)OC(C)OC(C)=O)=O)C(=O)\C(=N/OC)C1=CC=CO1 KEJCWVGMRLCZQQ-YJBYXUATSA-N 0.000 description 3
- 229960001631 carbomer Drugs 0.000 description 3
- 229960002620 cefuroxime axetil Drugs 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 229920000058 polyacrylate Polymers 0.000 description 3
- 230000008569 process Effects 0.000 description 3
- 229910002012 Aerosil® Inorganic materials 0.000 description 2
- 229920003084 Avicel® PH-102 Polymers 0.000 description 2
- 229920003134 Eudragit® polymer Polymers 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 229920002845 Poly(methacrylic acid) Polymers 0.000 description 2
- 238000013459 approach Methods 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 239000007931 coated granule Substances 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 239000012729 immediate-release (IR) formulation Substances 0.000 description 2
- 150000002632 lipids Chemical class 0.000 description 2
- 239000008297 liquid dosage form Substances 0.000 description 2
- 239000006194 liquid suspension Substances 0.000 description 2
- 230000007935 neutral effect Effects 0.000 description 2
- 239000008188 pellet Substances 0.000 description 2
- 229920002689 polyvinyl acetate Polymers 0.000 description 2
- 239000011118 polyvinyl acetate Substances 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 229920002554 vinyl polymer Polymers 0.000 description 2
- JKNCOURZONDCGV-UHFFFAOYSA-N 2-(dimethylamino)ethyl 2-methylprop-2-enoate Chemical compound CN(C)CCOC(=O)C(C)=C JKNCOURZONDCGV-UHFFFAOYSA-N 0.000 description 1
- 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 description 1
- 229920003136 Eudragit® L polymer Polymers 0.000 description 1
- 229920003153 Eudragit® NE polymer Polymers 0.000 description 1
- 229920003137 Eudragit® S polymer Polymers 0.000 description 1
- 229920003114 HPC-L Polymers 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 235000019886 MethocelTM Nutrition 0.000 description 1
- 229920003091 Methocel™ Polymers 0.000 description 1
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 229920002535 Polyethylene Glycol 1500 Polymers 0.000 description 1
- 229920006266 Vinyl film Polymers 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000003463 adsorbent Substances 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 239000012736 aqueous medium Substances 0.000 description 1
- 230000004888 barrier function Effects 0.000 description 1
- 239000011324 bead Substances 0.000 description 1
- 235000013361 beverage Nutrition 0.000 description 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 1
- 239000000679 carrageenan Substances 0.000 description 1
- 235000010418 carrageenan Nutrition 0.000 description 1
- 229920001525 carrageenan Polymers 0.000 description 1
- 229940113118 carrageenan Drugs 0.000 description 1
- 229920003118 cationic copolymer Polymers 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 229920001688 coating polymer Polymers 0.000 description 1
- 239000007771 core particle Substances 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 125000004494 ethyl ester group Chemical group 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- XFBVBWWRPKNWHW-UHFFFAOYSA-N etodolac Chemical compound C1COC(CC)(CC(O)=O)C2=N[C]3C(CC)=CC=CC3=C21 XFBVBWWRPKNWHW-UHFFFAOYSA-N 0.000 description 1
- 229960005293 etodolac Drugs 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 229920013821 hydroxy alkyl cellulose Polymers 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 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
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 150000004702 methyl esters Chemical class 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 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
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 239000000820 nonprescription drug Substances 0.000 description 1
- 229960001180 norfloxacin Drugs 0.000 description 1
- OGJPXUAPXNRGGI-UHFFFAOYSA-N norfloxacin Chemical compound C1=C2N(CC)C=C(C(O)=O)C(=O)C2=CC(F)=C1N1CCNCC1 OGJPXUAPXNRGGI-UHFFFAOYSA-N 0.000 description 1
- 230000008447 perception Effects 0.000 description 1
- 239000008200 pharmaceutical coating composition Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000000955 prescription drug Substances 0.000 description 1
- 235000019633 pungent taste Nutrition 0.000 description 1
- 150000003856 quaternary ammonium compounds Chemical class 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 230000009747 swallowing Effects 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 210000001779 taste bud Anatomy 0.000 description 1
- VUYXVWGKCKTUMF-UHFFFAOYSA-N tetratriacontaethylene glycol monomethyl ether Chemical compound COCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO VUYXVWGKCKTUMF-UHFFFAOYSA-N 0.000 description 1
- ILJSQTXMGCGYMG-UHFFFAOYSA-N triacetic acid Chemical compound CC(=O)CC(=O)CC(O)=O ILJSQTXMGCGYMG-UHFFFAOYSA-N 0.000 description 1
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 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
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5026—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
- A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
- A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/501—Inorganic compounds
-
- 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
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
- A61K9/5078—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings with drug-free core
Definitions
- drugs are administered orally as tablets or capsules.
- drugs can be provided either as chewable or dispersible tablets or, as liquid dosage forms such as solutions, emulsions and suspensions. These dosage forms permit perceptible exposure of the active drug to the taste buds.
- Some drugs are extremely bitter and therefore unpalatable when given in these dosage forms. As a consequence, measures need to be taken to mask the taste of these drugs in order to enhance patient compliance.
- US 4,865,851 describes a taste masked formulation of cefuroxime axetil where the drug particles are provided with integral coatings of a lipid or mixtures of lipids which are insoluble in water and which serve to mask the bitter taste of cefuroxime axetil upon oral administration.
- This coating however, results in a significant reduction in the dissolution and consequently the bioavailability of cefuroxime axetil suspension is significantly low as compared to tablet dosage form.
- the coating composition also contains lubricants which function as anti- sticking agents (e.g. talc, colloidal silica and magnesium stearate) and pharmaceutically acceptable plasticisers (e.g. triethyl citrate, polyethylene glycol, glyceryl monostearate, giyceryl triacetate, acetyl triethylcitrate, triethylcitrate, dibutyl phthalate and dibutyl sebacate).
- the lubricant quantity may be upto 200% of the dry weight of film-forming polymer, and more preferably, upto 100% of the dry weight of the film-forming polymer.
- the plasticiser quantity may be upto 40% the dry weight of the film forming polymer.
- the coated formulations may optionally be cured at elevated temperatures.
- a total polymer content in the coating of upto 30% by weight of pharmaceutical cores or, more preferably, 10% by weight of pharmaceutical cores is sufficient to mask the taste of bitter tasting, highly water soluble drugs.
- the total polymer content of the applied coat was 12.0% by weight of the core while the total solids applied was 26% by weight of the core.
- a total polymer coating of only 12% was sufficient to mask the bitter taste of Norfloxacin while giving optimum dissolution required for immediate release formulations. (Table 1.3).
- the total polymer content of the applied coat was 11.90% by weight of the core while the total solids application was 27% by weight of the core.
- the bitter taste of ciprofloxacin was masked with the applied coat without affecting dissolution, as shown in Table 5.3
- aqueous talc dispersion (30% w/w) was added to a 1% carbopol dispersion in water under stirring for 30 minutes.
- the carbopol - talc dispersion was finally added into plasticized (with triethyl citrate) ethyl cellulose dispersion with stirring for 30-40 minutes.
Landscapes
- Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU62246/99A AU6224699A (en) | 1999-03-19 | 1999-10-26 | Taste masking coating compositions |
| BR9917219-4A BR9917219A (pt) | 1999-03-19 | 1999-10-26 | Composições de revestimento para mascaramento de sabor |
| EP99949283A EP1235556A4 (en) | 1999-03-19 | 1999-10-26 | COATINGS FOR TASTE MASKING |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN454DE1999 IN191482B (enrdf_load_stackoverflow) | 1999-03-19 | 1999-03-19 | |
| IN454/DEL/99 | 1999-03-19 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO2000056266A2 true WO2000056266A2 (en) | 2000-09-28 |
| WO2000056266A3 WO2000056266A3 (en) | 2002-07-04 |
Family
ID=11089863
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/IB1999/001735 WO2000056266A2 (en) | 1999-03-19 | 1999-10-26 | Taste masking coating compositions |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP1235556A4 (enrdf_load_stackoverflow) |
| CN (1) | CN1615121A (enrdf_load_stackoverflow) |
| AU (1) | AU6224699A (enrdf_load_stackoverflow) |
| BR (1) | BR9917219A (enrdf_load_stackoverflow) |
| IN (1) | IN191482B (enrdf_load_stackoverflow) |
| WO (1) | WO2000056266A2 (enrdf_load_stackoverflow) |
| ZA (1) | ZA200007724B (enrdf_load_stackoverflow) |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1110544A3 (de) * | 1999-12-20 | 2003-01-22 | Basf Aktiengesellschaft | Verwendung eines Filmüberzuges als geschmacksmaskierendes Coating von oralen Darreichungsformen |
| US6565877B1 (en) | 1999-06-11 | 2003-05-20 | Ranbaxy Laboratories Limited | Taste masked compositions |
| EP1411899A4 (en) * | 2001-08-01 | 2006-06-07 | Novartis Ag | COMPOSITION FOR MASKING THE TASTE |
| US20060233873A1 (en) * | 2003-01-24 | 2006-10-19 | Julien Meissonnier | Dispersion of taste masked crystals or granules of active substances, chewable soft capsules filled with said dispersion, and process for preparing same |
| US20090142378A1 (en) | 2002-02-21 | 2009-06-04 | Biovail Laboratories International S.R.L. | Controlled release dosage forms |
| US7780987B2 (en) | 2002-02-21 | 2010-08-24 | Biovail Laboratories International Srl | Controlled release dosage forms |
| US8889184B2 (en) * | 2006-09-07 | 2014-11-18 | Losan Pharma Gmbh | Particulate form of a pharmaceutical composition which is easy to swallow |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4321253A (en) * | 1980-08-22 | 1982-03-23 | Beatty Morgan L | Suspension of microencapsulated bacampicillin acid addition salt for oral, especially pediatric, administration |
| CH666405A5 (de) * | 1985-06-24 | 1988-07-29 | Ciba Geigy Ag | Feste, haltbare darreichungsformen mit elastischem filmueberzug. |
| US4851226A (en) * | 1987-11-16 | 1989-07-25 | Mcneil Consumer Products Company | Chewable medicament tablet containing means for taste masking |
| IT1227899B (it) * | 1988-12-23 | 1991-05-14 | Poli Ind Chimica Spa | Rivestimento totale o parziale di principi attivi farmaceutici e relative composizioni |
| US5527545A (en) * | 1989-09-18 | 1996-06-18 | Recordati S.A. Chemical And Pharmaceutical Company | Liquid-suspension controlled-release pharmaceutical composition |
| IE65964B1 (en) * | 1990-07-20 | 1996-01-24 | Slagel David | Products and processes for the treatment of the alimentary canal |
| IT1250421B (it) * | 1991-05-30 | 1995-04-07 | Recordati Chem Pharm | Composizione farmaceutica a rilascio controllato con proprieta' bio-adesive. |
| US5958459A (en) * | 1991-12-24 | 1999-09-28 | Purdue Pharma L.P. | Opioid formulations having extended controlled released |
| US5578316A (en) * | 1992-06-04 | 1996-11-26 | Smithkline Beecham Corporation | Palatable pharmaceutical compositions |
| DE19709532A1 (de) * | 1997-03-10 | 1998-09-17 | Basf Ag | Verwendung von redispergierbaren Polymerpulvern oder Polymergranulaten zum Überziehen von pharmazeutischen oder agrochemischen Darreichungsformen |
-
1999
- 1999-03-19 IN IN454DE1999 patent/IN191482B/en unknown
- 1999-10-26 CN CNA998165883A patent/CN1615121A/zh active Pending
- 1999-10-26 AU AU62246/99A patent/AU6224699A/en not_active Abandoned
- 1999-10-26 WO PCT/IB1999/001735 patent/WO2000056266A2/en not_active Application Discontinuation
- 1999-10-26 EP EP99949283A patent/EP1235556A4/en not_active Withdrawn
- 1999-10-26 BR BR9917219-4A patent/BR9917219A/pt not_active Application Discontinuation
-
2001
- 2001-09-19 ZA ZA200007724A patent/ZA200007724B/xx unknown
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6565877B1 (en) | 1999-06-11 | 2003-05-20 | Ranbaxy Laboratories Limited | Taste masked compositions |
| EP1110544A3 (de) * | 1999-12-20 | 2003-01-22 | Basf Aktiengesellschaft | Verwendung eines Filmüberzuges als geschmacksmaskierendes Coating von oralen Darreichungsformen |
| EP1411899A4 (en) * | 2001-08-01 | 2006-06-07 | Novartis Ag | COMPOSITION FOR MASKING THE TASTE |
| US20090142378A1 (en) | 2002-02-21 | 2009-06-04 | Biovail Laboratories International S.R.L. | Controlled release dosage forms |
| US7780987B2 (en) | 2002-02-21 | 2010-08-24 | Biovail Laboratories International Srl | Controlled release dosage forms |
| US8323692B2 (en) | 2002-02-21 | 2012-12-04 | Valeant International Bermuda | Controlled release dosage forms |
| US20060233873A1 (en) * | 2003-01-24 | 2006-10-19 | Julien Meissonnier | Dispersion of taste masked crystals or granules of active substances, chewable soft capsules filled with said dispersion, and process for preparing same |
| US8889184B2 (en) * | 2006-09-07 | 2014-11-18 | Losan Pharma Gmbh | Particulate form of a pharmaceutical composition which is easy to swallow |
Also Published As
| Publication number | Publication date |
|---|---|
| AU6224699A (en) | 2000-10-09 |
| EP1235556A2 (en) | 2002-09-04 |
| IN191482B (enrdf_load_stackoverflow) | 2003-12-06 |
| BR9917219A (pt) | 2002-04-23 |
| WO2000056266A3 (en) | 2002-07-04 |
| EP1235556A4 (en) | 2003-07-16 |
| ZA200007724B (en) | 2002-06-12 |
| CN1615121A (zh) | 2005-05-11 |
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