Oral osmotic controlled drug delivery system for a sparingly soluble drug

• US 6,534,090 B2
• Filed: 06/26/2001
• Issued: 03/18/2003
• Est. Priority Date: 02/02/2001
• Status: Expired due to Fees

• Current Assignee: Sun Pharmaceutical Advanced Research Centre Limited (Sun Pharmaceutical Industries Limited)
• Original Assignee: Sun Pharmaceutical Advanced Research Centre Limited (Sun Pharmaceutical Industries Limited)
• Inventors: Pilgaonkar, Pratibha S., Puthli, Shivanand P., Karajgi, Jayant S., Dharmadhikari, Nitin B., Shrivastava, Ratnesh H., Menon, Suma G.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): FUBARA, BLESSING M
• Application Number:
  US09/891,848
• Publication Number:
  US 20030008006A1
• Time in Patent Office: 630 Days
• Field of Search: 424/473, 424/489, 424/469, 424/488, 424/493, 424/485, 424/486, 424/484
• US Class Current: 424/473
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas

Abstract

The present invention is for an oral osmotic controlled drug delivery system for a sparingly soluble drug comprising:

a. a core comprising (i) finely particulate anhydrous carbamazepine (ii) a polymeric swelling agent consisting of one or more swellable hydrophilic polymers selected such that the polymeric swelling agent exhibits controlled swelling and the wall does not rupture or burst, (iii) a crystal habit modifier in whose presence, upon contact with an aqueous medium, the anhydrous carbamazepine being transformed into cuboidal or rod-shaped crystals of the dihydrate of carbamazepine, or mixtures thereof, and (iv) water-soluble compounds for inducing osmosis,

b. a wall made of acylated cellulose which is impermeable to the components of the core, but permeable to water, and

c. a passageway through the wall for releasing the components present in the core to the surrounding environment.

Claims

1. An oral osmotic controlled drug delivery system for a sparingly soluble drug comprising:

a. a wall made of acylated cellulose,

b. a core surrounded by the wall, the core comprising (i) finely particulate anhydrous carbamazepine, (ii) a mixture of xanthan gum and croscarmellose sodium as a polymeric swelling agent which exhibits controlled swelling and the wall does not rupture or burst, (iii) a crystal habit modifier in whose presence, upon contact with an aqueous medium, the anhydrous carbamazepine is transformed into cuboidal or rod-shaped crystals of the dihydrate of carbarnazepine, or mixtures thereof, and (iv) a water-soluble compound for inducing osmosis, the wall being impermeable to the components of the drug-containing core, but permeable to water, and

c. a passageway through the wall for releasing the components present in the core to the surrounding environment.

2. An oral osmotic controlled drug delivery system as claimed in claim 1, wherein the xanthan gum has a particle size such that about 100% of the particles pass through a sieve of ASTM 80# and a minimum of about 92% of the particles pass through a sieve of ASTM 200#.

3. An oral osmotic controlled drug delivery system as claimed in claim 1, wherein the xanthan gum is present in amounts in the range from about 3.5% to about 4%, and the croscarmellose sodium is present in amounts in the range from about 3% to about 4.5% by weight of the core.

4. An oral osmotic controlled drug delivery system as claimed in claim 1, wherein the xanthan gum and the croscarmellose sodium are present in a 1:

1 weight ratio.

5. An oral osmotic controlled drug delivery system as claimed in claim 1, wherein the crystal habit modifier is selected from a vinylpyrrolidone polymer, a vinylpyrrolidone/vinyl acetate polymer, a polyethylene oxide polymer, a polyethylene glycol, a polyoxyethylene-polyoxypropylene glycol copolymer, a polyoxyethylene castor oil derivative, a long chain C₁₂-C₁₈ fatty acid glyceride, and mixtures thereof.

6. An oral osmotic controlled drug delivery system as claimed in claim 1, wherein the crystal habit modifier comprises vinyl pyrrolidone/vinyl acetate copolymer having a monomer ratio of vinyl pyrrolidone to vinyl acetate of approximately 60:

40 in % by weight.

7. An oral osmotic controlled drug delivery system as claimed in claim 1, wherein the crystal habit modifier comprises vinyl pyrrolidone/vinyl acetate copolymer in an amount from about 2% to about 3% by weight of the core.

8. An oral osmotic controlled drug delivery system as claimed in claim 1, wherein the crystal habit modifier comprises polyvinyl pyrrolidone having an approximate molecular weight of 1,000,000 Daltons.

9. An oral osmotic controlled drug delivery system of claim 1, wherein the acylated cellulose comprises one or more cellulose acetates, and the wall further comprises hydroxypropyl methylcellulose and polyethylene glycol 8000.

10. An oral osmotic controlled drug delivery system as claimed in claim 9, wherein one or more of the cellulose acetates comprises from about 78% to about 82% by weight of the wall, the hydroxypropyl methylcellulose comprises from about 5% to about 10% by weight of the wall and the polyethylene glycol 8000 comprises from about 10% to about 14% by weight of the wall.

11. An oral osmotic controlled drug delivery system as claimed in claim 1 wherein the cuboidal or rod-shaped crystals have a length of about 10 μ

m to about 600 μ

m.