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
  • A61K9/282—Organic compounds, e.g. fats
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
  • A61J3/00—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
  • A61J3/005—Coating of tablets or the like
• • 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
  • A61K9/2853—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)
• • 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
  • A61J2205/00—General identification or selection means
  • A61J2205/20—Colour codes
• • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
  • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
  • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
  • Y10S424/00—Drug, bio-affecting and body treating compositions
  • Y10S424/07—Microporous membranes

Definitions

• This invention relates to tablets and other individual dosage forms which are characterized by a thin film coating of a water permeable plastic composition, and to the method of making such tablets and dosage forms.
• the invention also relates to a thin water permeable tablet coating film, and to a liquid composition useful for laying down the aforementioned film.
• a tablet coating composition which is comprised of a portion of a hard, water soluble or water dispersible waxlike substance and a portion of a film forming resinous substance.
• additional materials are coloring materials, water insoluble waxes, plasticizing agents, and possibly wetting agents and drying agents.
• the hard, water soluble wax-like substances to which the invention pertains are materials of the polyethylene glycol type having a melting point of at least 50 C.
• Water dispersible waxes which may also be used either alone or in addition to the water soluble polyethylene glycol are glyceryl monostearate and diglycol stearate.
• the cellulose acetate phthalate resins are suitable for use.
• the cellulose acetate phthalate plastics are those described in United States Patents Nos. 2,093,- 462, 2,093,464, and 2,126,460.
• polycarboxycylic acid partial esters of cellulose esters of lower aliphatic monocarboxycylic acids such as, cellulose acetate phthalate, cellulose propionate phthalate and cellulose butyrate phthalate.
• coloring agents which may be used in the practice of this invention are any of the non-toxic dyes, lakes and pigments which have been certified for use in the food, drug and cosmetic industries.
• dyes of the type represented by red D. and C. #37, green F. D. and S. #1, yellow D. and C. #11, red D. and C. #21, orange D. and C. #4, red D. and C. #18, and red D. and C. #39 are suitable for use as colorants in the coating composition.
• the pigments which we have found suitable are yellow hydrated iron oxide, brown hydrated iron oxide, red iron oxide, black iron oxide, titanium dioxide, and the ultramarine blues.
• Many lakes are found suitable in the practice of this invention and D. and C.
• a lake is a dye which has been precipitated on an insoluble metal compound.
• D. and C. dyes which means those suitable for use in the drug and cosmetic industry, it is necessary to deposit the dye on a pharmaceutically acceptable carrier such as aluminum hydroxide.
• water insoluble waxes which we have found suitable are beeswax, lanolin, stearic acid, onesta wax, cocoa butter and cetyl alcohol.
• Onesta wax is the trade name for a high melting point hydrogenated vegetable oil fraction which resembles beeswax in consistency.
• plasticizing agents We may use castor oil, mineral oil, corn oil, sesame oil and propylene glycol. If desired we may also substitute a portion of a drying oil such as soy bean oil or the like and we also may use surface active agents such as the polyoxyethylene sorbitan derivatives and the sulfated fatty alcohols of the Duponol type.
• a highly important advantage of this invention is that the coating composition described herein can be applied from solvent solution such as acetone, alcohol or a combination thereof and as a result the drying time between coats is reduced from approximately an hour or two in the case of water down to about 5 minutes in the case of the solvent solution. Hence, it is possible to completely coat a tablet in a matter of minutes where prior practices have example, if desired.
• the invention is most highly suit-;
• a tablet coated according to the practice of this invention is considerably smaller in size than one coated by the initially described standard procedure and the smaller tablet is more acceptable because it can be swallowed more easily.
• the film of this invention very effectively coats the tablets so that no unpleasant taste can be perceived but at the same time distinctive markings punched into the tablet core will show through very clearly and be readily discernible on the surface.
• a sweetening dor flavoring agent may be added of course, if desire We prefer to use between about 14% and 20% weight by volume of the hard, water soluble or water dispersible wax-like substance in making up the fluid coating composition for application to tablets. Likewise, we may use between about 4% and about 7% weight by volume of the film-forming resinous substance.
• the waxy adjuvant is not used in a concentration greater than weight by volume and the plasticizing agent is used in a concentration of from 1% to 5% weight by volume.
• weight by volume weight per volume and w./v. are used herein for their customary meaning as understood in the pharmaceutical industry. All three expressions mean the same thing, that is, the weight of ingredient per unit volume of suspension or solution.
• the expression is used for convenience in designating the amount of a solid that is to be dissolved or suspended in a liquid to give a definite ultimate volume of solution or suspension.
• 10% weight per volume means, for example, 10 grams of solid dissolved or suspended in a liquid and the liquid made up to a total volume of 100 ml.
• the amount of cellulose acetate phthalate plastic in the solution is 10% weight by volume and in the examples when it is stated that, for instance, 300 cc .of cellulose acetate phthalate solution is used, it is to be understood that. there will be. 30 g. of cellulose acetate phthalate in the solution, or 10% w./v.
• Example I A tablet coating solution is made up according to the followingformula:
• the polyethylene glycol is dissolved in a portion of warm acetone and is then added to the C.A.P. solution. The remainder of the acetone is added and the mixture is thoroughly stirred.
• the solution is applied to a moving bed of tablets or granules by pouring small portions onto the tablets. As the tablets rotate the material is distributed evenly over the surface thereof and in a few minutes time the solvents will have evaporated leaving a dry hard film. Thereafter a second coat is applied in the same manner and subsequent coats are applied until a film of the desired thickness is obtained. Tablets coated in this manner are pleasing in appearance and will disintegrate without delay either in water or in gastric secretions.
• the disintegration of the tablet may be speeded up somewhat by incorporating into the tablet one of the well-known disintegrators.
• the polyethylene glycol is present in about 14% and the cellulose acetate phthalate is present in an amount of about 6% weight by volume.
• Example II A solution suitable for coating tablets was prepared according to the following formula:
• a solution suitable for use in coating tablets is prepared according to the following formula:
• This solution is made up in the same manner as previously described and is applied to tablets in the same way.
• the film applies to the tablet quite evenly with a suitable distribution of film on the sides, edges and faces of the tablet.
• a few coats of the foregoing solution will give a film of approximately 0.005 inch in thickness and provides a suitable and pleasing film about the tablet core.
• Example IV A solution for use in coating tablets or the like is prepared according to the following formula:
• This solution is prepared similarly to the preceding solutions except that the beeswax is dissolved in acetone by heating the acetone to a fairly high temperature. When the acetone cools, beeswax may come out in a very fine suspension but does not alter the characteristics of the film. The film obtained is quite smooth and even and deposits uniformly on the sides, edges and faces of the tablet.
• Example 'V A preferred solution suitable for application to tablets to form a thin film thereon was made up according to the following formula:
• the polyethylene glycol and the stearic acid are added to warm acetone and when the acetone has cooled somewhat the yellow dye and castor oil are also added.
• the entire solution is mixed with the cellulose acetate phthalate solution and thereafter applied to tumbling tablets in customary tablet coating procedures. For instance about 10 cc. of the solution may be applied to about '2000 tablets in a rotating pan and after about minutes the coat will be evenly distributed on all of the tablets and will be substantially dry. Thereafter another cc. portion may be applied and the procedure repeated a number of times until a coating of suitable thickness has been established.
• Example VI A solution suitable for application to tablets and the like to form a thin film thereon is made up according to the following formula:
• the solution was prepared in the manner previously set forth in Example V and was applied to tumbling tablets in the same way.
• 20% w./v. of Waxlike substances and 7% w./v. of cellulose acetate phthalate plastic, in solution is employed.
• Example VII A solution suitable for application to tablets and the like to form a thin film thereonwas'made up according to the following formula: Polyethylene glycol-6000 g. w./v' -100.0 Cellulose acetate phthalate, 10% w./v. solution cc 200 Green dye, D. and C. #1 g. w./v 4.0 Mineral oil 'g. w./v 1.25 Lanolin g. w./v 5.0
• This solution is prepared in the same manner as set forth in the preceding examples and differs therefromin containing 20% w./v. of the water soluble wax-like material and 4% w./v. of cellulose acetate phthalate resin, in solution.
• Example VIII A solution suitable for application to tablets and the like to form a thin film thereon was made up according to the following formula:
• the solution is made up in the same manner as set forth in the previous examples. It differs therefrom in containing 14% w./v. of polyethylene glycol-6000 and 4% w./v. of cellulose acetate phthalate in solution. It also ditfers'in that a portion of orange lake is substituted for a portion of dye in order to provide greater depth of color and superior covering power forthe colorant in the solution.
• the solution is prepared in the same manner as set forth in the previous examples and is applied to tablets inthe same way.
• 14% w./v. of polyethylene glycol-6000 is employed and 7% w./v. of cellulose acetate phthalate, in solution, is used.
• the lake employed in this example gives a brilliant color and has excellent covering qualities for the tablet core. Lakes are quite useful in covering up tablets which have an off color or a mottled appearance.
• Example X V A solution suitable for application to tablets to form a thin film thereon was made up according to the following formula:
• the solution is made up in the same manner as set forth in the previous examples and when applied to tablets is found to provide a pleasing red color which has strong covering properties.
• Example XI The formula in Example X was duplicated substituting 3 g. of red iron oxide pigment for the lake of theprevious example; In this example a dull red color is obtained when" the solution is applied to the tablets and the covering power of the solution is very good.
• Example XII A solutionsuitable for application to tablets and the like to form a thin film thereon was made up according to the following formula:
• Example XIII Example V is repeated with the substitution of a 50% acetone, 50% anhydrous ethanol solution for the acetone of Example V.
• a fluid composition adapted "for application to tablets and .the like which :consists essentially :of about 14% to w./v. of a polyethylene glycol .having a monoearboxylic acid.
• a coated solid medicament having as the coating material a film of a physiologically acceptable composition consisting essentially of the water permeable combination of about 14 'to 20 parts by weight of a water soluble wax and about 4 to '7 parts by weight of apolycarboxylic acid partial ester of a cellulose .ester of-a lower aliphatic monocarboxylic acid.
• a coated tablet having as the coating material a thin film of a physiologically acceptable composition consisting essentially of the water permeable combination of about 14 to 20 parts by weight of a normally solid polyethyleneglycol and about 4 to '7 parts by weight of a polycarboxylic acid partial ester of a cellulose ester of a lower aliphatic monocarboxylic acid.
• a coated tablet having as the coating material a thin film of a physiologically acceptable composition con sisting essentially of the water permeable -.combination of about .14 to 20 parts by weight of a mormallyasolid polyethylene glycol .and about 4 to 7 parts by weight of cellfilose acetate phthalate.
• the method of coating tablets and the like which comprises applying to said tablets a film coating of a physiologically acceptable coating composition consisting essentiallyof the water vpermeablecombination or awater soluble wax and a polycarboxylic acid partial-ester of a cellulose ester of a lower aliphatic monocarboxylic acid.
• the method of coating a solid medicament which comprises applying to said medicament a film coating of a physiologically acceptable coating composition consisting essentially of the water permeable combination of about 14 to 20 parts by weight of a water soluble wax and about 4 to 7 parts by weight of a polycarboxylic acid partial ester of a cellulose ester .of a lower aliphatic monocarboxylic acid.
• a film coating of a physiologically acceptable coating composition consisting essentially .of the water permeable combination of about 14 to 20 parts by weight of a normally solid polyethylene v.glycol and about 4 to 7 parts by weight of a polycarboxylic acid partial ester .of .a cellulose .ester .of
• the method .of coating tablets and the like which comprises applying to said .tablets a .film .coating of a physiologically .acceptable coating composition consistng essentially of the water permeable combination of about 1.4.to 20 parts by weight of anormally solid polyethylene glycol and about -4 to 7 parts .by weight of cellulose acetate phthalate.
• a fluid composition adapted for application to tablets and the like as a film coating thereon which consists essentially of about 14% to 20% w/v. of a water soluble wax and about 4% t0 7% w./v. of a polycarboxylic acid partial ester of a cellulose .ester of a lower aliphatic monoearboxylic acid, and a non-aqueous solvent for said wax and said ester.

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Cited By (38)

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Citations (14)

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• 1953
  • 1953-11-09 US US391123A patent/US2881085A/en not_active Expired - Lifetime
• 1954
  • 1954-05-12 GB GB13892/54A patent/GB762229A/en not_active Expired
  • 1954-11-08 DE DEA21477A patent/DE1056786B/de active Pending
  • 1954-11-09 FR FR1115981D patent/FR1115981A/fr not_active Expired

Patent Citations (14)

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