Film preparation for biphasic release of pharmacologically active or other substances

• US 7,037,526 B1
• Filed: 11/03/2000
• Issued: 05/02/2006
• Est. Priority Date: 11/12/1999
• Status: Expired due to Term

• Current Assignee: LTS Lohmann Therapie-Systeme AG
• Original Assignee: LTS Lohmann Therapie-Systeme AG
• Inventors: Ludwig, Karin, Krumme, Markus
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): HOWARD, SHARON LEE
• Application Number:
  US10/129,837
• Time in Patent Office: 2,006 Days
• Field of Search: 424/472, 424/484
• US Class Current: 424/484
• CPC Class Codes: A61K 9/2072 characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms A61K9/0004, A61K9/0056, A61K9/0065 take precedence
• CPC Class Codes: A61K 9/209 containing drug in at least two layers or in the core and in at least one outer layer
• CPC Class Codes: A61K 9/7007 Drug-containing films, membranes or sheets A61K9/0041, A61K9/0043, A61K9/006, A61K9/0063 take precedence

Abstract

A polymer-based preparation in film form for biphasic release of substances present therein to liquid surroundings, is characterized in that the preparation comprises at least two polymer matrix layers which differ in terms of their construction from polymers, with release taking place rapidly from one of the layers, and release taking place slowly from at least one other layer.

Claims

1. A process for the production of a polymer-based preparation in film form, for biphasic release of substances contained therein to liquid surroundings, the preparation comprising at least two polymer matrix layers which differ in terms of their construction from polymers, with release taking place rapidly from one of the layers, and release taking place slowly from at least one other layer, said matrix of the rapidly releasing layer comprising a polyvinyl alcohol or a polyvinyl alcohol-containing polymer mixture, and said matrix of the slowly releasing layer(s) comprising at least one polymer selected from the group consisting of cellulose ethers, polyurethane, polymethacrylates, poly(methyl methacrylates) and derivatives or copolymers thereof,

said process comprising the following steps:

a) providing a polymer solution suitable for the rapidly releasing layer, comprising the substances to be released;

b) coating of the polymer solution onto an inert substrate by knife or roller application or spraying processes and subsequent drying to form the rapidly releasing film layer;

c) providing a polymer solution suitable for the slowly releasing layer, comprising the substances to be released; and

d) coating of this solution onto the rapidly releasing film layer by knife or roller application or spraying processes or printing and subsequent drying to form the slowly releasing film layer.

3. The process according to claim 1, wherein production of the first film layer starts from a polymer melt which is applied by knife or roller application, spraying or extrusion processes to an inert substrate and is then dried and/or cooled, and the further layers are coated from polymer solutions.

4. The process according to claim 1, wherein the release of the substance(s) from the slowly releasing layer(s) is further delayed by increasing the size of the substance particles, by coating or by microencapsulation of the substance or of the active ingredient, or by pharmaceutical technology measures having similar effects.

2. A process for the production of a polymer-based preparation in film form, for biphasic release of substances contained therein to liquid surroundings, the preparation comprising at least two polymer matrix layers which differ in terms of their construction from polymers, with release taking place rapidly from one of the layers, and release taking place slowly from at least one other layer, said matrix of the rapidly releasing layer comprising a polyvinyl alcohol or a polyvinyl alcohol-containing polymer mixture, and said matrix of the slowly releasing layer(s) comprising at least one polymer selected from the group consisting of cellulose ethers, polyurethane, polymethacrylates, poly(methyl methacrylates) and derivatives or copolymers thereof,

said process comprising the following steps:

a) providing a polymer solution suitable for the slowly releasing layer, comprising the substances to be released;

b) coating of the polymer solution onto an inert substrate by knife or roller application or spraying processes and subsequent drying to form the rapidly releasing film layer;

c) providing a polymer solution suitable for the rapidly releasing layer, comprising the substances to be released; and

d) coating of this solution onto the slowly releasing film layer by knife or roller application or spraying processes or printing and subsequent drying to form the slowly releasing film layer.

5. A method for the release of substances or active pharmaceutical ingredients into human or animal body fluids or artificial simulations of such body fluids, which comprises:

applying to a subject in need thereof a polymer-based preparation in film form for biphasic release of substances contained therein to liquid surroundings, the preparation comprising at least two polymer matrix layers which differ in terms of their construction from polymers, with release taking place rapidly from one of the layers, and release taking place slowly from at least one other layer, said matrix of the rapidly releasing layer comprising a polyvinyl alcohol or a polyvinyl alcohol-containing polymer mixture, and said matrix of the slowly releasing layer(s) comprising at least one polymer selected from the group consisting of cellulose ethers, polyurethane, polymethacrylates, poly(methyl methacrylates) and derivatives or copolymers thereof.

6. A method for producing pharmaceutical preparations for medical therapeutic treatment of diseases in humans or animals, which comprises:

incorporating a pharmaceutically active substance into a polymer-based preparation in film form for biphasic release of substances contained therein to liquid surroundings, the preparation comprising at least two polymer matrix layers which differ in terms of their construction from polymers, with release taking place rapidly from one of the layers, and release taking place slowly from at least one other layer, said matrix of the rapidly releasing layer comprising a polyvinyl alcohol or a polyvinyl alcohol-containing polymer mixture, and said matrix of the slowly releasing layer(s) comprising at least one polymer selected from the group consisting of cellulose ethers, polyurethane, polymethacrylates, poly(methyl methacrylates) and derivatives or copolymers thereof.