EP0153104A2
Expired / Lapsed
EP
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Diffusion coated multiple-units dosage form
Assignee: Takeda Pharma AS
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Filing: 1985-02-08
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Granted: —
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Expires: 2005-02-08
Abstract
Abstract In an oral pharmaceutical controlled release multiple-units formulation, individual units containing an active substance are coated with a substantially water-insoluble, but water-diffusible controlled release coating which includes 1) an inner film layer comprising a homogeneous combination of a water-dispersible film-forming agent and a polymeric substance which imparts compressibility to the coating, and 2) optionally an outer film layer comprising a film-forming agent which prevents adhesion between the units at elevated temperatures and imparts flowability to the units. The coating possesses a sufficient plastic deformability to result in no significant changes in the release characteristics of compressed coated units relative to non-compressed coated units.
Inventors
- 👤 Kim Kjornaes
- 👤 Jorgen Linnemann
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-26 18:08
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5073; A61K9/20; A61K9/2072; A61K9/2077; A61K9/2081
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
78 words
An oral pharmaceutical controlled release multiple-units formulation in which individual units containing an active substance are coated with a substantially water-insoluble, but water-diffusible controlled release coating which includes 1) an inner film layer comprising a homogeneous combination of a water-dispersible film-forming agent and a polymeric substance which imparts compressibility to the coating, and 2) optionally an outer film layer comprising a film-forming agent which prevents adhesion between the units at elevated temperatures and imparts flowability to the units.
Claim 2
Dependent Claim
78 words
An oral pharmaceutical controlled release multiple-units formulation in which individual units containing an active substance are coated with a substantially water-insoluble, but water-diffusible controlled release coating which includes 1) an inner film layer comprising a homogeneous combination of a water-dispersible film-forming agent and a polymeric substance which imparts compressibility to the coating, and 2) optionally an outer film layer comprising a film-forming agent which prevents adhesion between the units at elevated temperatures and imparts flowability to the units.
Claim 3
Dependent Claim
50 words
A formulation according to claim 1 in which the film-forming agent of the inner film layer is selected from cellulose derivatives, silicone polymers and copolymers, vinyl polymers and copolymers, biodegradable polymers such as polyamino acids, polylactic acid and copolymers and derivatives thereof, and acrylic polymers and copolymers, or mixtures thereof.
Claim 4
Dependent Claim
30 words
A formulation according to claim 2 in which the film-forming agent is selected from ethyl cellulose and a copolymerisate of poly(meth)-acrylic acid esters, hydroxypropylmethylcellulosephthalate, celluloseacetatephthalate, polyvinylacetatephthalate and vinylacetate-crotonic acid copolymerisates.
Claim 5
Dependent Claim
47 words
A formulation according to any of claims 1-3 in which the polymeric substance in the inner film coating is selected from polyvinylpyrrolidone, polyalkylene glycols such as polyethylene glycol, and cellulose derivatives such as hydroxypropylcellulose, carboxymethylcellulose, methylcellulose, propylcellulose, hydroxyethylcellulose, carboxyethylcellulose, carboxymethylhydroxyethylcellulose, hydroxymethylcellulose, carboxymethylethylcellulose, methylhydroxypropylcellulose or hydro- xyp ropylmethylcellulose.
Claim 6
Dependent Claim
48 words
A formulation according to claim 4 in which the polymeric substance is present in an amount between 1 and 10%, such as an amount between 2% and 8%, especially an amount of about 4% by weight relative to the amount of film-forming agent in the inner film layer.
Claim 7
Dependent Claim
31 words
A formulation according to any of claims 2-5 in which the film-forming agent is a copolymerisate of acrylic acid ethylester and methacrylic acid methylester and the water-soluble polymeric substance is hydroxypropylmethylcellulose.
Claim 8
Dependent Claim
30 words
A formulation according to any of the preceding claims in which the inner film layer comprises an additional anti-adhesive which is a finely divided, substantially water-insoluble, pharmaceutically acceptable, non-wetting powder.
Claim 9
Dependent Claim
38 words
A formulation according to claim 7 in which the anti-adhesive is present in an amount of between about 1 and 50%, preferably between about 5 and 30%, such as about 15% by weight of the inner film layer.
Claim 10
Dependent Claim
43 words
A formulation according to any of claims 1-8 in which the film-forming agent of the outer film layer is one which is anti-adhesive at temperatures above about 40°C, especially temperatures above about 50°C, such as a temperature between about 60°C and about 120°C.
Claim 11
Dependent Claim
67 words
A formulation according to claim 9 in which the film-forming agent of the outer film layer is selected from diffusion coating materials such as ethylcellulose or enteric coating materials such as anionic poly(meth)acrylic acid esters, hydroxypropylmethylcellulosephthalate, celluloseacetatephthalate, polyvinylacetatephthalate, polyvinylacetatephthalate-crotonic acid copolymerisates, or mixtures thereof, or water-soluble coating materials such as water-soluble cellulose derivatives, e.g. hydroxypropylcellulose, carboxymethylcellulose, methylcellulose, propylcellulose, hydroxyethylcellulose, carboxyethylcellulose, carboxymethylhydroxyethylcellulose, hydroxymethylcellulose, carboxymethylethylcellulose, methylhydroxypropylcellulose or hydr- oxypropylmethylcellutose.
Claim 12
Dependent Claim
38 words
A formulation according to claim 9 or 10 in which the film-forming agent of the outer film layer is present in an amount of about 0.1-10%, especially 0.5-5%, in particular about 1% by weight of the uncoated unit.
Claim 13
Dependent Claim
26 words
A formulation according to any of claims 9-11 in which the outer film coating additionally comprises a lubricant which is a finely divided pharmaceutically acceptable powder.
Claim 14
Dependent Claim
23 words
A formulation according to any of the preceding claims in which the units are crystals of a size between 0.1 and 1.5 mm.
Claim 15
Dependent Claim
37 words
A formulation according to any of claims 1-12 in which the units are cross-sectionally substantially homogeneous cores of a size of about 0.1-1.5 mm, in particular about 0.4-1.0 mm, such as about 0.4-0.7 mm or 0.7-1.0 mm.
Claim 16
Dependent Claim
19 words
A formulation according to any of claims 1-14 in which the active substance in the units is potassium chloride.
Claim 17
Dependent Claim
21 words
A formulation according to claim 15 in which the units are potassium chloride crystals of a size of about 0.1-1.5 mm.
Claim 18
Independent Claim
138 words
A method of preparing an oral pharmaceutical controlled release multiple-units formulation as claimed in any of claims 1-16, in which a) individual units containing an active substance are coated with a film-coating mixture comprising an aqueous dispersion of a film-forming agent and a polymeric substance which prevents adhesion between the units and which imparts compressibility to the inner film layer, b) the thus coated units are optionally provided with an outer film layer of a film-forming agent which prevents adhesion between the units at elevated temperatures and imparts flowability to the coated units, and c) the coated units are subsequently heated to a temperature at which the film-forming agent forms a continuous phase in homogeneous admixture with the polymeric substance, whereby a coating which substantially does not change its diffusion characteristics in the course of time is formed.
Claim 19
Dependent Claim
35 words
A method according to claim 17, in which the coated units are heated to a temperature above about 40°C, especially a temperature above about 50°C, such as a temperature between about 60°C and about 120°C.
Claim 20
Dependent Claim
32 words
An oral pharmaceutical controlled release composition which comprises a multiplicity of units as specified in any of claims 1-16 admixed with one or more pharmaceutically acceptable fillers, diluents, binders, lubricants or disintegrants.
Claim 21
Dependent Claim
26 words
A pharmaceutical composition according to claim 19 which is a tablet which disintegrates substantially immediately upon ingestion in the stomach into a multiplicity of individual units.
References Cited (Backward Citations)
No citation records indexed.
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