Controlled extended drug release technology

• US 20060003007A1
• Filed: 07/01/2004
• Published: 01/05/2006
• Est. Priority Date: 07/01/2004
• Status: Active Grant

• Current Assignee: Intellipharmaceutics Corporation (Intellipharmaceutics International, Inc.)
• Original Assignee: Intellipharmaceutics Corporation (Intellipharmaceutics International, Inc.)
• Inventors: Odidi, Amina, Odidi, Isa
• Granted Patent: US 8,394,409 B2
• Time in Patent Office: Days
• US Class Current: 424/472
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/284 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Abstract

A controlled extended drug release technology for the controlled extended release of hydrophobic or hydrophilic drugs or therapeutically active agents consisting of a homogeneous blend of one or more therapeutic agents, gas generators and surrounded by one or more layers of coat made of thermoplastic water insoluble cellulose derivatives, acrylic polymers, superdisintegrants and optionally an oil, antioxidants and electrolytes. The technology platform is capable of releasing therapeutic agents via zero, first or pseudo first order release.

Claims

1. A tablet, pellet or bead, comprising:

(a) a central compartment containing a homogeneous blend of one or more therapeutic agents, gas generators and optionally oils, antioxidants and surface active agents

(b) one or more tableting, extrusion and coating aids

(c) one or more layers of coat surrounding the central compartment

(d) wherein release of therapeutic agent from said tablet, pellet or bead is characterized by a dissolution profile in which at least 0.5% to 50% of the therapeutic agent is released within three hours, and greater than 50% is released in 24 hours.

2. The tablet, pellet, or bead according to claim 1 wherein the coat is made from one or more cellulose derivatives.

3. The tablet, pellet, or bead according to claim 1 wherein the coat is made from one or more thermoplastic water insoluble cellulose derivatives and one or more superdisintegrants.

4. The tablet, pellet, or bead according to claim 1 wherein the coat is made from a mixture of one or more thermoplastic water insoluble cellulose derivatives and one or more acrylic polymers

5. The tablet, pellet, or bead according to claim 1 wherein the coat is made from a mixture of one or more thermoplastic water insoluble cellulose derivatives and one or more acrylic polymers, and one or more superdisintegrants

6. The tablet, pellet, or bead according to claim 1 wherein the coat is made from a mixture of one or more thermoplastic water insoluble cellulose derivatives and one or more acrylic polymers, one or more superdisintegrants and optionally one or more electrolytes

7. The tablet, pellet, or bead according to claims 1, 2, 3 and 4 wherein the coat contains optionally one or more electrolytes

8. The tablet, pellet or bead according to claim 7 wherein the gas generator consist of a soluble or insoluble acid source and an alkali metal carbonate.

9. The tablet, pellet or bead according to claim 7 wherein the acrylic polymer is selected from one or a mixture of anionic polymers based on methacrylic acid esters, methacrylates copolymer and or copolymers of acrylate and methacrylates and or ethylacrylate methylmethacrylate copolymers

10. The tablet, pellet or bead according to claim 7 wherein the superdisintegrant is selected from one or a mixture of croscarmelose, sodium starch glycolate, and crospovidone.

11. The tablet, pellet or bead according to claim 7 wherein the cellulose derivative is ethylcellulose.

12. The tablet, pellet or bead according to claim 7 wherein the electrolyte is chosen from one or a mixture of salts capable of providing, sodium (Na⁺), potassium (K⁺), chloride (CI⁻

), calcium (Ca²⁺), magnesium (Mg²⁺), bicarbonate (HCO₃⁻

), phosphate (Po₄²⁻

), sulfate (SO₄²⁻

) ions.

13. The tablet, pellet or bead according to claim 7 wherein the oil is chosen from one or a mixture of animal, plant or synthetic origin

14. The tablet, pellet or bead according to claim 1 and 7 wherein the coat optionally includes shellac and or Zein.

15. The tablet, pellet or bead according to claim 7 wherein the coat contains one or more oils

16. The tablet, pellet or bead according to claim 7 wherein the acrylic polymer, is chosen from one or a mixture of, methyl methacrylate copolymers, ethoxyethyl methacrylates, cyanoethyl methacrylate, aminoalkyl methacrylate copolymer, poly(acrylic acid), poly(methacrylic acid), methacrylic acid alkylamide copolyer, poly(methyl methacrylate), poly(methyl methacrylate) copolymer, polyacrylamide, aminoalkyl methacrylate copolymer, poly(methacrylic acid anhydride), and glycidyl methacrylate copolymers.

17. The tablet, pellet or bead according to claims 1 and 7 wherein the final coating layer is made from cellulose esters or acrylic polymers or a mixture thereof.

18. The tablet, pellet or bead according to claims 1 and 17 wherein the final coat contains a loading dose.

19. The tablet, pellet or bead according to claims 1, 17 and 18 wherein there is present a surface active agent.

20. The tablet, pellet or bead according to claims 1,17 and 18 wherein the gas generator is an oxygen generator.