US3420931A - Pharmaceutical dragee - Google Patents
Pharmaceutical dragee Download PDFInfo
- Publication number
- US3420931A US3420931A US449637A US3420931DA US3420931A US 3420931 A US3420931 A US 3420931A US 449637 A US449637 A US 449637A US 3420931D A US3420931D A US 3420931DA US 3420931 A US3420931 A US 3420931A
- Authority
- US
- United States
- Prior art keywords
- coating
- drage
- drages
- percent
- suspension
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 239000008298 dragée Substances 0.000 title description 2
- 238000000576 coating method Methods 0.000 description 48
- 239000011248 coating agent Substances 0.000 description 35
- 238000000034 method Methods 0.000 description 27
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 18
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 18
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 16
- 239000000725 suspension Substances 0.000 description 16
- 239000006185 dispersion Substances 0.000 description 14
- 238000004519 manufacturing process Methods 0.000 description 14
- 235000000346 sugar Nutrition 0.000 description 13
- 229920000642 polymer Polymers 0.000 description 12
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 12
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 12
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 12
- 239000000454 talc Substances 0.000 description 12
- 229910052623 talc Inorganic materials 0.000 description 12
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 10
- 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 description 9
- 229930006000 Sucrose Natural products 0.000 description 9
- 229910000019 calcium carbonate Inorganic materials 0.000 description 9
- 239000005720 sucrose Substances 0.000 description 9
- 239000004408 titanium dioxide Substances 0.000 description 9
- 229920002554 vinyl polymer Polymers 0.000 description 9
- 235000011187 glycerol Nutrition 0.000 description 8
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 7
- 238000001035 drying Methods 0.000 description 7
- 239000011343 solid material Substances 0.000 description 6
- 229920000609 methyl cellulose Polymers 0.000 description 5
- 239000001923 methylcellulose Substances 0.000 description 5
- 235000010981 methylcellulose Nutrition 0.000 description 5
- 239000000178 monomer Substances 0.000 description 5
- 238000005507 spraying Methods 0.000 description 5
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 4
- XTXRWKRVRITETP-UHFFFAOYSA-N Vinyl acetate Chemical compound CC(=O)OC=C XTXRWKRVRITETP-UHFFFAOYSA-N 0.000 description 4
- 229920001577 copolymer Polymers 0.000 description 4
- 229920001519 homopolymer Polymers 0.000 description 4
- 239000000463 material Substances 0.000 description 4
- 239000000203 mixture Substances 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 3
- IMROMDMJAWUWLK-UHFFFAOYSA-N Ethenol Chemical compound OC=C IMROMDMJAWUWLK-UHFFFAOYSA-N 0.000 description 3
- 239000001768 carboxy methyl cellulose Substances 0.000 description 3
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 3
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 3
- 229940105329 carboxymethylcellulose Drugs 0.000 description 3
- 229920002678 cellulose Polymers 0.000 description 3
- 239000001913 cellulose Substances 0.000 description 3
- 235000010980 cellulose Nutrition 0.000 description 3
- 239000008199 coating composition Substances 0.000 description 3
- 239000000049 pigment Substances 0.000 description 3
- 229920002451 polyvinyl alcohol Polymers 0.000 description 3
- 239000000377 silicon dioxide Substances 0.000 description 3
- 239000003826 tablet Substances 0.000 description 3
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- 229920002261 Corn starch Polymers 0.000 description 2
- 239000001856 Ethyl cellulose Substances 0.000 description 2
- 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 2
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 2
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 2
- 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 2
- 239000004372 Polyvinyl alcohol Substances 0.000 description 2
- 229920002472 Starch Polymers 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- HLKZFSVWBQSKKH-UHFFFAOYSA-N but-3-enoic acid;1-ethenylpyrrolidin-2-one Chemical compound OC(=O)CC=C.C=CN1CCCC1=O HLKZFSVWBQSKKH-UHFFFAOYSA-N 0.000 description 2
- 239000008120 corn starch Substances 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 235000019325 ethyl cellulose Nutrition 0.000 description 2
- 229920001249 ethyl cellulose Polymers 0.000 description 2
- 239000007941 film coated tablet Substances 0.000 description 2
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 2
- 235000013828 hydroxypropyl starch Nutrition 0.000 description 2
- -1 i.e. Substances 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 239000006187 pill Substances 0.000 description 2
- 238000005498 polishing Methods 0.000 description 2
- 229920002689 polyvinyl acetate Polymers 0.000 description 2
- 239000011118 polyvinyl acetate Substances 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
- VZGDMQKNWNREIO-UHFFFAOYSA-N tetrachloromethane Chemical compound ClC(Cl)(Cl)Cl VZGDMQKNWNREIO-UHFFFAOYSA-N 0.000 description 2
- UJMBCXLDXJUMFB-UHFFFAOYSA-K trisodium;5-oxo-1-(4-sulfonatophenyl)-4-[(4-sulfonatophenyl)diazenyl]-4h-pyrazole-3-carboxylate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)C1=NN(C=2C=CC(=CC=2)S([O-])(=O)=O)C(=O)C1N=NC1=CC=C(S([O-])(=O)=O)C=C1 UJMBCXLDXJUMFB-UHFFFAOYSA-K 0.000 description 2
- 229910002012 Aerosil® Inorganic materials 0.000 description 1
- 229920000856 Amylose Polymers 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- 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 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- 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 description 1
- 206010013911 Dysgeusia Diseases 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 241000233866 Fungi Species 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
- 229930195725 Mannitol Natural products 0.000 description 1
- 244000061456 Solanum tuberosum Species 0.000 description 1
- 235000002595 Solanum tuberosum Nutrition 0.000 description 1
- 244000299461 Theobroma cacao Species 0.000 description 1
- 241000209140 Triticum Species 0.000 description 1
- 235000021307 Triticum Nutrition 0.000 description 1
- 240000008042 Zea mays Species 0.000 description 1
- 235000005824 Zea mays ssp. parviglumis Nutrition 0.000 description 1
- 235000002017 Zea mays subsp mays Nutrition 0.000 description 1
- VJHCJDRQFCCTHL-UHFFFAOYSA-N acetic acid 2,3,4,5,6-pentahydroxyhexanal Chemical compound CC(O)=O.OCC(O)C(O)C(O)C(O)C=O VJHCJDRQFCCTHL-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 238000013019 agitation Methods 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 235000013871 bee wax Nutrition 0.000 description 1
- 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 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 235000019219 chocolate Nutrition 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 238000004040 coloring Methods 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 235000005822 corn Nutrition 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- CALWOYBZYFNRDN-UHFFFAOYSA-N ethenol;ethenyl acetate Chemical compound OC=C.CC(=O)OC=C CALWOYBZYFNRDN-UHFFFAOYSA-N 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 239000012467 final product Substances 0.000 description 1
- 235000013312 flour Nutrition 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 239000001341 hydroxy propyl starch Substances 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000004922 lacquer Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000004014 plasticizer Substances 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 238000003825 pressing Methods 0.000 description 1
- ZUFQODAHGAHPFQ-UHFFFAOYSA-N pyridoxine hydrochloride Chemical compound Cl.CC1=NC=C(CO)C(CO)=C1O ZUFQODAHGAHPFQ-UHFFFAOYSA-N 0.000 description 1
- 229960004172 pyridoxine hydrochloride Drugs 0.000 description 1
- 235000019171 pyridoxine hydrochloride Nutrition 0.000 description 1
- 239000011764 pyridoxine hydrochloride Substances 0.000 description 1
- 229940100486 rice starch Drugs 0.000 description 1
- 238000005096 rolling process Methods 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 238000009495 sugar coating Methods 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 239000004149 tartrazine Substances 0.000 description 1
- UJMBCXLDXJUMFB-GLCFPVLVSA-K tartrazine Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)C1=NN(C=2C=CC(=CC=2)S([O-])(=O)=O)C(=O)C1\N=N\C1=CC=C(S([O-])(=O)=O)C=C1 UJMBCXLDXJUMFB-GLCFPVLVSA-K 0.000 description 1
- 229960000943 tartrazine Drugs 0.000 description 1
- 235000012756 tartrazine Nutrition 0.000 description 1
- 230000009974 thixotropic effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 239000002966 varnish Substances 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 238000010626 work up procedure Methods 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G3/00—Sweetmeats; Confectionery; Marzipan; Coated or filled products
- A23G3/34—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof
- A23G3/50—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof characterised by shape, structure or physical form, e.g. products with supported structure
- A23G3/54—Composite products, e.g. layered, coated, filled
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G3/00—Sweetmeats; Confectionery; Marzipan; Coated or filled products
- A23G3/02—Apparatus specially adapted for manufacture or treatment of sweetmeats or confectionery; Accessories therefor
- A23G3/20—Apparatus for coating or filling sweetmeats or confectionery
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G3/00—Sweetmeats; Confectionery; Marzipan; Coated or filled products
- A23G3/02—Apparatus specially adapted for manufacture or treatment of sweetmeats or confectionery; Accessories therefor
- A23G3/20—Apparatus for coating or filling sweetmeats or confectionery
- A23G3/26—Apparatus for coating by tumbling with a liquid or powder, spraying device-associated, drum, rotating pan
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G3/00—Sweetmeats; Confectionery; Marzipan; Coated or filled products
- A23G3/34—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof
- A23G3/343—Products for covering, coating, finishing, decorating
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G4/00—Chewing gum
- A23G4/02—Apparatus specially adapted for manufacture or treatment of chewing gum
- A23G4/025—Apparatus specially adapted for manufacture or treatment of chewing gum for coating or surface-finishing
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G4/00—Chewing gum
- A23G4/18—Chewing gum characterised by shape, structure or physical form, e.g. aerated products
- A23G4/20—Composite products, e.g. centre-filled, multi-layer, laminated
-
- 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
- A61K9/282—Organic compounds, e.g. fats
- A61K9/2826—Sugars or sugar alcohols, e.g. sucrose; Derivatives thereof
-
- 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
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G2200/00—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF containing organic compounds, e.g. synthetic flavouring agents
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G2200/00—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF containing organic compounds, e.g. synthetic flavouring agents
- A23G2200/06—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF containing organic compounds, e.g. synthetic flavouring agents containing beet sugar or cane sugar if specifically mentioned or containing other carbohydrates, e.g. starches, gums, alcohol sugar, polysaccharides, dextrin or containing high or low amount of carbohydrate
Definitions
- This invention relates to the production of sugar containing coatings on shaped masses of ingestible solid material.
- this invention is broadly directed to the production of sugar-containing coatings on shaped masses of ingestible solid material, it has particular application to the production of drages.
- drage is meant a shaped mass of solid material having thereon a sugar-containing coating of substantial thickness.
- the shaped mass for example, a pill or tablet, is not limited to any particular geometrical shape. It contains a pharmaceutical composition, i.e., active ingredient and, if necessary, excipients.
- a shaped mass without a sugarcontaining coating will be referred to as a core.
- An object of this invention is to provide an improved process for the production of coated shaped masses of solid material, and in particular to an improved process for the production of drages.
- a process which basically comprises coating a core with an aqueous dispersion comprising, in percent by weight, 1 to 60, preferably 35 to 40% of a sugar and 0.5 to 10% of a vinyl polymer, preferably a polymer of vinyl pyrrolidone and/ or a polymer of vinyl acetate.
- the use of a vinyl polymer in ice the coloring of drages, that is drages which already have the actual drage coating has also been described in the literature Kohler et al., Deutsch Opotheker-Zeitung 102 (1):l-8, Jan. 4, 1962.
- the coating pigment suspension used contained 0.325% of polyvinyl pyrrolidone in addition to sugar and other substances and is used to color the drages by pigment dyes, that is only for the last stage of the drage process.
- the entire coating process can be carried out with this composition alone since it can be applied manually or by suitable apparatus, with or without spraying, without any inconvenient sticking of the drages. It has not been found necessary to additionally introduce pulverulent substances such as talc, into the rotating vessel during the time of the coating process. With rationalized operation, the entire coating process can be carried out in one or two days. It was particularly unexpected that such a substantial improvement can be achieved by increasing the polymer from 0.325% to at least 0.5%, preferably to about 2%.
- the preferred polymers include homopolymers of vinyl pyrrolidone, vinyl acetate, and vinyl alcohol, and copolymers of vinyl pyrrolidone-vinyl acetate, and vinyl alcohol. These polymers are characterized by their physiological compatibility.
- Another polymer which is used advantageously is a commercial copolymer of 60 percent vinyl pyrrolidone and 40 percent vinyl acetate with the following characteristics: dry content: at least 95 percent; maximal monomer conent: 0.8 percent; viscosity parameter K: 34:6; nitrogen content: about 7.6%.
- the molecular weight of the polymer can vary widely. In general, polymers of molecular weights between about 10,000 and 2,000,000 are applied. It is important, however, that the monomer content of the polymer is kept as low as possible because of the possibly toxic side effects of higher concentrations of some of the monomers. In general, monomer contents lower than 1 percent by weight are unobjectionable.
- the percent by weight of sugar in the aqueous suspension is 1 to 60, preferably 35 to 40.
- sugars such as sucrose, glucose, sorbitol, mannitol, etc.; it is preferable, however, to use sucrose.
- the suspension may contain pigments, such as titanium dioxide or calcium carbonate, lubricants (talc or finely divided silica), fillers such as flour, binders, plasticizers and/ or softeners, e.g. glycerine, and preservatives.
- pigments such as titanium dioxide or calcium carbonate
- lubricants talc or finely divided silica
- fillers such as flour, binders, plasticizers and/ or softeners, e.g. glycerine
- preservatives e.g. glycerine
- the viscosity of the final dispersion can vary widely, depending on the composition of it, furthermore on temperature, air content, thixotropic effects, previous agitation and even time. In general, the viscosity of the dispersion is between 500 and 15,000, preferably about 2000 centipoise.
- the dispersion of this invention By using the dispersion of this invention, it was surprisingly discovered that it is possible to conduct the entire coating process only with one coating composition. This is the case because the dispersion of this invention can be applied either manually or mechanically, with or without spraying, and without the drages sticking to one another. Of most importance is that it is possible to carry out the entire coating process within one to two days. In contrast thereto, the average working time for the manufacture of one batch according to the conventional process is approximately one week. Thus, compared with the usual process, the new process represents a considerable saving of time, resulting in substantial labor savings, as well as in substantially increased plant capacity.
- the dispersion of this invention is so stable that it is unnecessary during the course of drages manufacture to use mixing or stirring devices, pumps, or other homogenizing equipment to prevent settling.
- a still further advantage of the invention consists of the fact that during the course of the whole process, there is no requirement for organic solvents. Moreover, during the course of the process it is unnecessary to employ intermediate drying steps for which purpose, in the usual coating processes, the drages had to be removed temporarily from the coating vessel.
- the application of the coating dispersion can be adapted to different types of operation. It is possible to lay on the coating either manually, or semi-automatically or completely automatically.
- the suspension can be applied by spraying or it can be poured in liquid form directly onto the cores tumbling in an angularly oriented rotating kettle. The suspension is applied until the material to be coated is well moistened. The kettle is then allowed to rotate until the coated cores no longer adhere to one another but instread roll freely. Finally, the coated cores are dried under continuous rotation, preferably with the aid of a warm air stream, or an infrared lamp, or any other equivalent drying means. These steps can be conducted continuously; and it is possible in this connection, to shorten or even omit the rotating phase (second phase) during the first coating applications.
- each core is coated with 10 to 500, preferably 50 to separate thin coats, each coat having a thickness of 0.5 to 200 preferably 5 to 2011..
- a particularly economical mode of conducting the process comprises passing a predetermined volume of the suspension through -a relay-controlled solenoid valve into the drage coating vessel to cover the drages rolling around therein.
- a three-phase time relay is employed, such that in the first phase the suspension is passed through the solenoid valve; in the second phase the rotating operation is conducted, the duration of which can be varied; and in the third phase the heating device is actuated.
- the suspension can be applied onto cores whose surface is not pretreated.
- the drages produced in accordance with this invention cannot be distinguished by their exterior from those which are produced according to the classical method of coating drages. They likewise taste sweet, can be colored, exhibit a natural silky sheen, and can, if desired, be lacquered. Their elastic and mechanical strengths meet the highest requirements.
- the quantity of suspension depends on the weight and the shape of the drage cores. Normally, the quantity is 10 to of the weight of the core, on a dry basis.
- the ratio of the components in the drage coating is the same as that of the coating solution, the exception being, of course, that water and/or other solvents are absent in the final coatmg.
- Polyvinyl pyrrolidone is dissolved in water; then, the remaining components are added under constant stirring; thereafter, the mixture is passed through a fine sieve or a homogenizing device.
- Aerosil (particulate SiO 4.0 Titanium dioxide 4.5
- EXAMPLE 3 Percent Hydroxyethyl cellulose 0.5 Polyvinyl pyrrolidone-polyvinyl acetate copolymer (proportion 6:4) 2.0 Titanium dioxide 4.5 Calcium carbonate 4.5 Talc 18.5 Glycerine 2.0 Sucrose 38.0 Water 30.0
- EXAMPLE 6 Percent Methyl cellulose 0.5 Polyvinyl pyrrolidone (average molecular weight 650,000) 0.5 Titanium dioxide 4.5 Calcium carbonate 4.5 Talc 20.0 Glycerine 2.0 Sucrose 38.0 Water 30.0
- EXAMPLE 7 Percent Methyl cellulose 0.5 Polyvinyl pyrrolidone (average molecular weight Titanium dioxide 4.5 Calcium carbonate 4.5 Silicon dioxide 4.0 Talc 6.5 Glycerine 2.0 Sucrose 38.0 Water 30.0
- EXAMPLE 8 Percent Methyl cellulose 0.5 Polyvinyl pyrrolidone 2.0 Aerosil (particulate SiO 4.0 Titanium dioxide 6.5 Calcium carbonate 6.5 Magnesium stearate 2.5 Glycerine 3 .0 Sucrose 45.0 Water 30.0
- 35 mg. lactose, 20 mg. corn starch, and mg. talc are mixed manually in a conventional drage vessel having a diameter at the opening of cm., with 0.5 liter of a suspension (produced in accordance with Example 2), at a rate of rotation of 15 revolutions per minute. The rotation is continued for 10 minutes and then for a further 10 minutes with a forced hot air (temperature 30-40 C.; 4.5 m. /minute). This processcoating, rotating, dryingis repeated over again until a weight of the individual coated cores of mg. is reached.
- the drages are kept in motion for a while longer with air being blown in, for the purpose of obtaining a silky shine which is preserved by applying a solution of bee wax in carbon tetrachloride, or another suitable polishing agent, and subsequent rotating for 1 to 2 hours.
- Total duration of the drage production process 16 hours (2 working days).
- EXAMPLE 10 40 kg. of cores, each core weighing 420 mg. and consisting of 250 mg. pyridoxine hydrochloride, 100 mg. lactose, 50 mg. corn starch, and 20 mg. carboxymethyl cellulose, are placed into a drage coating vessel of a width of 90 cm. at its opening. 25 kg. of a suspension, produced according to Example 5 and mixed with 1% coloring agent (TartraZine, Hydrazine yellow, FD&C yellow No. 5), are added piecemeal at ambient temperature from a storage vessel with the aid of a solenoid valve controlled 'by means of a 3-phase timing relay.
- 1% coloring agent TritraZine, Hydrazine yellow, FD&C yellow No. 5
- the three phases of the relay are set as follows: 1st Phase (coating application): 5 seconds; 2nd Phase (rotating without hot air supply): 10 minutes; 3rd Phase (rotating with hot air blown in as in Example 8): 10 minutes.
- the drage coating process is continued until the individual weight of the resultant drages amounts to 600 mg., whereupon a polishing step is conducted as in Example 8.
- Total duration of drage manufacturing process 16 hours (2 working days).
- drages are obtained which have a drage coating that is colored in all layers. It is also possible to utilize first a colorless suspension and to apply a colored suspension only at the end of the drage producing process.
- this invention provides a substantial improvement in the sugar coating of shaped masses of solid material. Aside from coating drages, it is apparent that this invention can be employed for the coating of other orally ingestible products, such as variously-colored sugar coated candies, particularly sugar-coated chocolates.
- a drage as defined by claim 1 wherein said aqueous dispersion further comprises about 0.5% by weight of a member selected from the group consisting of methyl cellulose, ethyl cellulose, carboxymethyl cellulose, bydroxyethyl cellulose, hydroxypropyl cellulose, and starch.
- a process for the production of a drage as defined by claim 1 comprising the steps of pouring the aqueous dispersion directly on cores tumbling in an angularly oriented rotating kettle; continuing the rotating until the coated cores roll freely; and then drying the coated cores.
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- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Health & Medical Sciences (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Preparation (AREA)
- Graft Or Block Polymers (AREA)
- Confectionery (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DEM60752A DE1216486B (de) | 1964-04-23 | 1964-04-23 | Verfahren zur Herstellung von Dragees |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| US3420931A true US3420931A (en) | 1969-01-07 |
Family
ID=7309936
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| US449637A Expired - Lifetime US3420931A (en) | 1964-04-23 | 1965-04-20 | Pharmaceutical dragee |
| US802759*A Expired - Lifetime US3554767A (en) | 1964-04-23 | 1969-02-24 | Coated confectionery |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| US802759*A Expired - Lifetime US3554767A (en) | 1964-04-23 | 1969-02-24 | Coated confectionery |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US3420931A (de) |
| BE (1) | BE662884A (de) |
| BR (1) | BR6568739D0 (de) |
| CH (1) | CH457722A (de) |
| DE (1) | DE1216486B (de) |
| DK (1) | DK110217C (de) |
| ES (1) | ES312136A1 (de) |
| GB (1) | GB1025139A (de) |
| IL (1) | IL23149A (de) |
| NL (1) | NL6501476A (de) |
| SE (1) | SE336199B (de) |
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|---|---|---|---|---|
| US3524756A (en) * | 1967-05-29 | 1970-08-18 | Colorcon | Process of coating tablets with alternate tacky and non-tacky layers |
| US3753767A (en) * | 1971-08-02 | 1973-08-21 | Colgate Palmolive Co | Method of sugar-coating tablets |
| US3835221A (en) * | 1970-03-05 | 1974-09-10 | Hoechst Ag | Orally administrable drug dosage form having delayed action |
| US3935326A (en) * | 1967-06-28 | 1976-01-27 | Boehringer Mannheim G.M.B.H. | Process for coating tablets with aqueous resin dispersions |
| US4001390A (en) * | 1974-04-04 | 1977-01-04 | Shin-Etsu Chemical Co., Ltd. | Method of coating pharmaceutical solid dosage forms |
| US4017647A (en) * | 1974-06-11 | 1977-04-12 | Shin-Etsu Chemical Company Limited | Method for providing enteric coatings on solid dosage forms |
| US4060598A (en) * | 1967-06-28 | 1977-11-29 | Boehringer Mannheim G.M.B.H. | Tablets coated with aqueous resin dispersions |
| US4150111A (en) * | 1974-05-28 | 1979-04-17 | Allister Warren | Enteric coated magnesium chloride |
| US4432966A (en) * | 1979-12-10 | 1984-02-21 | Roussel-Uclaf | Compressed tablets for disintegration in the colon comprising an active ingredient containing nucleus coated with a first layer containing microcrystalline cellulose which is coated with an enteric organic polymer coating |
| US4693896A (en) * | 1985-10-07 | 1987-09-15 | Fmc Corporation | Ethylcellulose-coated, gastric-disintegrable aspirin tablet |
| US4851226A (en) * | 1987-11-16 | 1989-07-25 | Mcneil Consumer Products Company | Chewable medicament tablet containing means for taste masking |
| US4867984A (en) * | 1984-11-06 | 1989-09-19 | Nagin K. Patel | Drug in bead form and process for preparing same |
| US5334253A (en) * | 1990-11-13 | 1994-08-02 | Lloyd Berg | Solution of certain five and six carbon atom carbohydrates |
| US5494681A (en) * | 1992-11-30 | 1996-02-27 | Kv Pharmaceutical Company | Tastemasked pharmaceutical materials |
| US5800601A (en) * | 1995-11-06 | 1998-09-01 | Videojet Systems International, Inc. | Food grade jet inks |
| US6248391B1 (en) * | 1997-07-16 | 2001-06-19 | Bpsi Holdings, Inc. | Bright white film coatings and film coating compositions therefor |
| US20040081695A1 (en) * | 2002-09-28 | 2004-04-29 | Sowden Harry S | Dosage forms having an inner core and an outer shell |
| US6747072B1 (en) * | 1994-10-04 | 2004-06-08 | Marconi Data Systems Inc. | White ink for marking candy substrates |
| US20040146559A1 (en) * | 2002-09-28 | 2004-07-29 | Sowden Harry S. | Dosage forms having an inner core and outer shell with different shapes |
| US20070218129A1 (en) * | 2003-08-06 | 2007-09-20 | Sarl Galenix Innovations | Solid Dispersible and/or Orodispersible Non-Filmy Containing at Least One Type of Active Substance Pharmaceutical Composition and Method for the Preparation Thereof |
| US20220008344A1 (en) * | 2018-12-17 | 2022-01-13 | Roquette Freres | Sugar-coated solid forms having improved stability |
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| US3957966A (en) * | 1972-05-19 | 1976-05-18 | Gaf Corporation | Stabilized vitamin food coatings |
| FR2247206B1 (de) * | 1973-01-24 | 1978-02-03 | Sterwin Ag | |
| US4127677A (en) * | 1977-12-12 | 1978-11-28 | Life Savers, Inc. | Xylitol-coated chewing gum and method |
| US4238510A (en) * | 1979-02-21 | 1980-12-09 | Life Savers, Inc. | Sugarless coating for chewing gum and confections and method |
| US4317838A (en) * | 1979-09-24 | 1982-03-02 | Life Savers, Inc. | Method for applying sugarless coating to chewing gum and confections |
| HU183408B (en) | 1981-04-28 | 1984-05-28 | Chinoin Gyogyszer Es Vegyeszet | Process for producing oral ratard pharmaceutical compositions |
| US4569852A (en) * | 1983-08-23 | 1986-02-11 | Warner-Lambert Company | Maintenance of flavor intensity in pressed tablets |
| EP0147780A3 (de) * | 1984-01-03 | 1987-03-11 | Merck & Co. Inc. | Vorrichtung zur Freisetzung von Arzneistoffen |
| DE3437679C1 (de) * | 1984-10-15 | 1985-08-29 | Richardson GmbH, 6080 Groß-Gerau | Präparat gegen schlechten Mundgeruch |
| US4929447A (en) * | 1986-01-07 | 1990-05-29 | Warner-Lambert Company | Encapsulation composition for use with chewing gum and edible products |
| FR2607671B1 (fr) * | 1986-12-04 | 1991-02-08 | Gen Foods France | Procede de fabrication directe de gomme de base pour pate masticatoire et de chewing-gum |
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| US5006362A (en) * | 1988-05-09 | 1991-04-09 | Berwind Pharmaceutical Services, Inc. | Branding pharmaceutical dosage forms, food and confectionery products with aqueous ingestible inks |
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-
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- 1964-04-23 DE DEM60752A patent/DE1216486B/de active Pending
-
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- 1965-02-05 NL NL6501476A patent/NL6501476A/xx unknown
- 1965-03-08 GB GB9693/65A patent/GB1025139A/en not_active Expired
- 1965-03-12 IL IL23149A patent/IL23149A/en unknown
- 1965-03-12 CH CH350865A patent/CH457722A/de unknown
- 1965-04-07 BR BR168739/65A patent/BR6568739D0/pt unknown
- 1965-04-14 DK DK195765AA patent/DK110217C/da active
- 1965-04-20 US US449637A patent/US3420931A/en not_active Expired - Lifetime
- 1965-04-22 BE BE662884A patent/BE662884A/xx unknown
- 1965-04-22 ES ES0312136A patent/ES312136A1/es not_active Expired
- 1965-04-23 SE SE05310/65A patent/SE336199B/xx unknown
-
1969
- 1969-02-24 US US802759*A patent/US3554767A/en not_active Expired - Lifetime
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| US2991226A (en) * | 1958-02-03 | 1961-07-04 | Frosst & Co Charles E | Long-acting wax-like talc pillage of penicillin |
| US2954322A (en) * | 1958-09-04 | 1960-09-27 | Olin Mathieson | Pharmaceuticals |
| US3148123A (en) * | 1960-05-17 | 1964-09-08 | Gen Aniline & Film Corp | Granulating and coating tablets |
| US3097144A (en) * | 1960-10-14 | 1963-07-09 | Upjohn Co | Heat-cured, polymeric, medicinal dosage film coatings containing a polyvinylpyrrolidone copolymer, polyethenoid acid, and polyethylene glycol |
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Cited By (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3524756A (en) * | 1967-05-29 | 1970-08-18 | Colorcon | Process of coating tablets with alternate tacky and non-tacky layers |
| US3935326A (en) * | 1967-06-28 | 1976-01-27 | Boehringer Mannheim G.M.B.H. | Process for coating tablets with aqueous resin dispersions |
| US4060598A (en) * | 1967-06-28 | 1977-11-29 | Boehringer Mannheim G.M.B.H. | Tablets coated with aqueous resin dispersions |
| US3835221A (en) * | 1970-03-05 | 1974-09-10 | Hoechst Ag | Orally administrable drug dosage form having delayed action |
| US3753767A (en) * | 1971-08-02 | 1973-08-21 | Colgate Palmolive Co | Method of sugar-coating tablets |
| US4001390A (en) * | 1974-04-04 | 1977-01-04 | Shin-Etsu Chemical Co., Ltd. | Method of coating pharmaceutical solid dosage forms |
| US4150111A (en) * | 1974-05-28 | 1979-04-17 | Allister Warren | Enteric coated magnesium chloride |
| US4017647A (en) * | 1974-06-11 | 1977-04-12 | Shin-Etsu Chemical Company Limited | Method for providing enteric coatings on solid dosage forms |
| US4432966A (en) * | 1979-12-10 | 1984-02-21 | Roussel-Uclaf | Compressed tablets for disintegration in the colon comprising an active ingredient containing nucleus coated with a first layer containing microcrystalline cellulose which is coated with an enteric organic polymer coating |
| US4867984A (en) * | 1984-11-06 | 1989-09-19 | Nagin K. Patel | Drug in bead form and process for preparing same |
| US4693896A (en) * | 1985-10-07 | 1987-09-15 | Fmc Corporation | Ethylcellulose-coated, gastric-disintegrable aspirin tablet |
| US4851226A (en) * | 1987-11-16 | 1989-07-25 | Mcneil Consumer Products Company | Chewable medicament tablet containing means for taste masking |
| US5334253A (en) * | 1990-11-13 | 1994-08-02 | Lloyd Berg | Solution of certain five and six carbon atom carbohydrates |
| US5494681A (en) * | 1992-11-30 | 1996-02-27 | Kv Pharmaceutical Company | Tastemasked pharmaceutical materials |
| US6747072B1 (en) * | 1994-10-04 | 2004-06-08 | Marconi Data Systems Inc. | White ink for marking candy substrates |
| US5800601A (en) * | 1995-11-06 | 1998-09-01 | Videojet Systems International, Inc. | Food grade jet inks |
| US6248391B1 (en) * | 1997-07-16 | 2001-06-19 | Bpsi Holdings, Inc. | Bright white film coatings and film coating compositions therefor |
| US6267808B1 (en) * | 1997-07-16 | 2001-07-31 | Bpsi Holdings, Inc. | Bright white film coatings and film coating compositions therefor |
| US20040081695A1 (en) * | 2002-09-28 | 2004-04-29 | Sowden Harry S | Dosage forms having an inner core and an outer shell |
| US20040146559A1 (en) * | 2002-09-28 | 2004-07-29 | Sowden Harry S. | Dosage forms having an inner core and outer shell with different shapes |
| US20070218129A1 (en) * | 2003-08-06 | 2007-09-20 | Sarl Galenix Innovations | Solid Dispersible and/or Orodispersible Non-Filmy Containing at Least One Type of Active Substance Pharmaceutical Composition and Method for the Preparation Thereof |
| US20220008344A1 (en) * | 2018-12-17 | 2022-01-13 | Roquette Freres | Sugar-coated solid forms having improved stability |
Also Published As
| Publication number | Publication date |
|---|---|
| IL23149A (en) | 1968-09-26 |
| NL6501476A (de) | 1965-10-25 |
| BR6568739D0 (pt) | 1973-08-02 |
| US3554767A (en) | 1971-01-12 |
| DE1216486B (de) | 1966-05-12 |
| CH457722A (de) | 1968-06-15 |
| ES312136A1 (es) | 1966-01-01 |
| DK110217C (da) | 1971-02-08 |
| SE336199B (de) | 1971-06-28 |
| BE662884A (de) | 1965-10-22 |
| GB1025139A (en) | 1966-04-06 |
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