WO1992019209A2 - Taste-masked medicaments and their preparation - Google Patents
Taste-masked medicaments and their preparation Download PDFInfo
- Publication number
- WO1992019209A2 WO1992019209A2 PCT/US1992/002692 US9202692W WO9219209A2 WO 1992019209 A2 WO1992019209 A2 WO 1992019209A2 US 9202692 W US9202692 W US 9202692W WO 9219209 A2 WO9219209 A2 WO 9219209A2
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- medicament
- taste
- film
- coating
- cellulose ester
- Prior art date
Links
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
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
Definitions
- This invention relates to taste-masking of solid medicaments, particularly by enveloping them in a tasta- masking polymer film coating.
- Therapeutic formulations designed for oral adminis ⁇ tration often contain active ingredients which have an unpleasant taste. For instance, many drugs produce a bitter or acrid sensation when taken by mouth.
- the proportion of PVP in the film coating is from about 12% to 20% by weight. If used alone, however, the patentees found that the cellulose ester coating would not provide adequate bioavailability of the active ingredient at the specified coating levels of 5% to 20% by weight. This is clearly evident from Figure 1 of the patent depicting in graphic form the dissolution rate of APAP in simulated gastric fluid at a coating level of 17.5% by weight and which the percent o-f PVP in the coating blend varied from 0% to 25% 'by weight. As will be noted, at 0% PVP in the film coating drug release amounted to only 40% after 40 minutes.
- solid medicaments can be effectively taste-masked with a film envelope consisting essentially of a cellulose ester applied from a latex dispersion of the ester, while maintaining rapid release of active ingredients.
- a film envelope consisting essentially of a cellulose ester applied from a latex dispersion of the ester, while maintaining rapid release of active ingredients.
- Figure 1 is a graph of percent dissolution versus time for aspirin tablets (acetylsalicylic acid - ASA) coated with the ultra-thin cellulose ester films made in accordance with the invention and the uncoated core control.
- Figure 2 is a graph of percent dissolution versus time for ASA tablets coated with the ultra-thin cellu ⁇ lose ester films of the invention, for ASA tablets simi ⁇ larly coated with the cellulose ester/PVP blend of U. S. Patent No. 4,851,226 to Julian et al., and for the.un- coated core control.
- aqueous plasticized cellulose ester dispersion used in the practice of the invention is a known chemi- cal entity. Commonly referred to as a cellulose ester latex, it is prepared by dissolving the polymer in a suitable organic solvent, dispersing the resulting solu ⁇ tion in an aqueous phase, homogenizing, and evaporating the solvent. To the resulting latex is added an appro- priate plasticizer.
- cellulose ester latexes suita ⁇ ble for producing the ultra-thin coatings of the in ⁇ vention are latexes made from cellulose acetate, cellu- lose acetate butyrate and cellulose acetate phthalate.
- Cellulose ester polymers are manufactured and sold com ⁇ surgeally by a number of suppliers of industrial chemi ⁇ cals, for example, the Eastman Kodak Company, Kingsport, Tenn.
- suitable plasticizers for cellulose aqueous dispersions include triacetin, diacetin and triethylcitrate.
- medicament can be, for ex ⁇ ample, granules, tablets including tablets of the co - pressed coated granules of drugs such as aspirin (ASA) , acetaminophen, and ibuprofen.
- drugs such as aspirin (ASA) , acetaminophen, and ibuprofen.
- the ultra-thin, taste-masking films of the in ⁇ vention are conveniently produced by coating the solid medicament substrate with an aqueous cellulose acetate dispersion in which the preferred plasticizer is tri ⁇ acetin.
- the triacetin is added to the dispersion and the mixture thoroughly mixed.
- the amount of plasticizer ranges by weight from about 50% to about 150%, preferably from about '30% to 120%, optimally about 100% of the solids content of the dispersion.
- a cellu ⁇ lose acetate aqueous dispersion having a solids content of by weight of from about 28% to 32% is available from the FMC Corporation under the designation CA398-10 latex dispersion.
- the ultra-thin, taste-masking cellulose films of the invention are applied to the solid medicament in a known manner and with standard pharmaceutical coating equipment. Coating is normally carried out by spraying in a pan or in a fluidized bed. Solids content of the aqueous cellulose ester coat ⁇ ing formulation plus plasticizer is in the neighborhood of from about by weight 10% to about 30%, preferably 15% to 20%. In the final dried coating, the amount of plas ⁇ ticizer present in the film coating ranges by weight from about 30% to about 60%.
- ultra-thin cellulose ester film coatings of the invention can be realized with the ultra-thin cellulose ester film coatings of the invention at coating levels of about 0.4% by weight based on total solid dosage form weight.
- Other types of solid dosage forms such as granules may require somewhat higher coating levels. So far as has been determined, overall coating levels will vary from about 0.3% to about 1.0% by weight for effective taste- masking.
- the amount of coating applied to the substrate can be controlled in known manner such as solids content of the coating dispersion and contact times.
- ASA release was more rapid for aspirin tablets coated solely with CA latex than with the CA latex/PVP blend.
Abstract
Description
Claims
Priority Applications (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
AU21673/92A AU651721B2 (en) | 1991-04-30 | 1992-04-03 | Taste-masked medicaments and their preparation |
NO933920A NO933920L (en) | 1991-04-30 | 1993-10-29 | Taste-camouflaged drugs and their preparation |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US693,732 | 1976-06-07 | ||
US69373291A | 1991-04-30 | 1991-04-30 |
Publications (2)
Publication Number | Publication Date |
---|---|
WO1992019209A2 true WO1992019209A2 (en) | 1992-11-12 |
WO1992019209A3 WO1992019209A3 (en) | 1993-01-07 |
Family
ID=24785870
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/US1992/002692 WO1992019209A2 (en) | 1991-04-30 | 1992-04-03 | Taste-masked medicaments and their preparation |
Country Status (6)
Country | Link |
---|---|
EP (1) | EP0583399A4 (en) |
JP (1) | JP2538491B2 (en) |
AU (1) | AU651721B2 (en) |
CA (1) | CA2107229C (en) |
NO (1) | NO933920L (en) |
WO (1) | WO1992019209A2 (en) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5654005A (en) * | 1995-06-07 | 1997-08-05 | Andrx Pharmaceuticals, Inc. | Controlled release formulation having a preformed passageway |
JP2007031281A (en) * | 2003-06-25 | 2007-02-08 | Kowa Co | Ibuprofen-containing film-coated tablet |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4302440A (en) * | 1980-07-31 | 1981-11-24 | Sterling Drug Inc. | Easily-swallowed, powder-free and gastric-disintegrable aspirin tablet thinly-coated with hydroxypropyl methylcellulose and aqueous spray-coating preparation thereof |
US4795641A (en) * | 1987-08-20 | 1989-01-03 | Eastman Kodak Company | Polymer blends having reverse phase morphology for controlled delivery of bioactive agents |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5075114A (en) * | 1990-05-23 | 1991-12-24 | Mcneil-Ppc, Inc. | Taste masking and sustained release coatings for pharmaceuticals |
-
1992
- 1992-04-03 WO PCT/US1992/002692 patent/WO1992019209A2/en not_active Application Discontinuation
- 1992-04-03 JP JP4511820A patent/JP2538491B2/en not_active Expired - Lifetime
- 1992-04-03 AU AU21673/92A patent/AU651721B2/en not_active Ceased
- 1992-04-03 EP EP92912798A patent/EP0583399A4/en not_active Withdrawn
- 1992-04-03 CA CA002107229A patent/CA2107229C/en not_active Expired - Fee Related
-
1993
- 1993-10-29 NO NO933920A patent/NO933920L/en unknown
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4302440A (en) * | 1980-07-31 | 1981-11-24 | Sterling Drug Inc. | Easily-swallowed, powder-free and gastric-disintegrable aspirin tablet thinly-coated with hydroxypropyl methylcellulose and aqueous spray-coating preparation thereof |
US4302440B1 (en) * | 1980-07-31 | 1986-08-05 | Easily-swallowed, powder-free and gastric-disintegrable aspirin tablet thinly-coated with hydroxypropyl methylcellulose and aqueous spray-coating preparation thereof | |
US4795641A (en) * | 1987-08-20 | 1989-01-03 | Eastman Kodak Company | Polymer blends having reverse phase morphology for controlled delivery of bioactive agents |
Non-Patent Citations (1)
Title |
---|
See also references of EP0583399A1 * |
Also Published As
Publication number | Publication date |
---|---|
EP0583399A4 (en) | 1997-04-23 |
EP0583399A1 (en) | 1994-02-23 |
NO933920D0 (en) | 1993-10-29 |
CA2107229A1 (en) | 1992-10-31 |
JPH06501027A (en) | 1994-01-27 |
JP2538491B2 (en) | 1996-09-25 |
NO933920L (en) | 1993-10-29 |
WO1992019209A3 (en) | 1993-01-07 |
CA2107229C (en) | 1997-07-22 |
AU2167392A (en) | 1992-12-21 |
AU651721B2 (en) | 1994-07-28 |
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