Extended release of active ingredients

• US 20020176842A1
• Filed: 03/26/2002
• Published: 11/28/2002
• Est. Priority Date: 04/09/2001
• Status: Abandoned Application

• Current Assignee: Christina Hann, Lyn Hughes, Simon Andrew Bellamy
• Original Assignee: Christina Hann, Lyn Hughes, Simon Andrew Bellamy
• Inventors: Hughes, Lyn, Bellamy, Simon Andrew, Hann, Christina
• Application Number:
  US10/107,288
• Publication Number:
  US 20020176842A1
• Time in Patent Office: Days
• US Class Current: 424/78.12
• CPC Class Codes: A01N 25/10 Macromolecular compounds
• CPC Class Codes: A61K 31/196 the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
• CPC Class Codes: A61K 31/785 Polymers containing nitrogen
• CPC Class Codes: A61K 47/34 Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers A61K47/10 takes precedence
• CPC Class Codes: A61K 47/585 Ion exchange resins, e.g. polystyrene sulfonic acid resin
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: B01J 39/05 in the strongly acidic form
• CPC Class Codes: B01J 39/07 in the weakly acidic form
• CPC Class Codes: B01J 41/05 in the strongly basic form
• CPC Class Codes: B01J 41/07 in the weakly basic form

Abstract

A dosage form is described that gives an extended release of active ingredients using unloaded ion exchange resins, that does not require the manufacture of a resinate.

Claims

1. A dosage form comprising:

a. an ionizable active ingredient;

b. an unloaded ion exchange resin.

4. A dosage form according to claim 1, wherein said ionizable active ingredient is selected from the group consisting of diclofenac sodium, indomethacin, and pesticides containing carboxyl groups, and said unloaded ion exchange resin is selected from the group consisting of styrenic strongly basic anion exchange resins with a quaternary amine functionality having a weight capacity of 0.1 to 6 meq/g, and styrenic weakly basic anion exchange resins with a tertiary amine functionality having a weight capacity of 0.1 to 8.5 meq/g, acrylic or methacrylic strongly basic anion exchange resins with a quaternary amine functionality having a weight capacity of 0.1 to 8 meq/g, and acylic or methacrylic weakly basic anion exchange resins with tertiary amine functionality having a weight capacity of 0.1 to 12 meq/g, and allylic and vinylic weakly basic anion exchange resins with primary, secondary, or tertiary amine functionalities having a weight capacity of 0.1 to 24 meq/g.

5. A dosage form according to claim 1, wherein said ionizable active ingredient is selected from the group consisting of paroxetine, and quaternary nitrogen compounds, and said unloaded ion exchange resin is selected from the group consisting of styrenic strongly acidic cation exchange resins with a sulfonic acid functionality having a weight capacity of 0.1 to 8 meq/g;

and styrenic weakly acidic cation exchange resins with a phenolic acid functionality having a weight capacity of 0.1 to 8.5 meq/g; and

acrylic or methacrylic weakly acidic cation exchange resins with a carboxylic or phenolic acid functionality with a weight capacity of 0.1 to 14 meq/g.

2. A dosage form comprising:

a an ionizable active ingredient;

b. an unloaded ion exchange resin;

further provided that the release rate and absorption rate of said ionizable active ingredient from said dosage form into a release medium can be modified by changing the variables, selected from the group consisting of, degree of cross-linking of the unloaded ion exchange resin, the particle size of the unloaded ion exchange resin, the pK of the functional groups of the unloaded resin, the solubility of the ionizable active ingredient in the release medium, the ionic strength and pH of the release medium, the pK of the ionizable active ingredient, the molecular weight of the ionizable active ingredient, temperature, and coating the unloaded ion exchange resin with a permeable membrane.

3. A dosage form comprising:

a. an ionizable active ingredient;

b. an unloaded ion exchange resin;

further provided that the site at which release and absorption take place can be modified by coating the unloaded resin and/or active ingredient with a non-permeable membrane that is dissolved only at the site where absorption and release are desired.