Abuse resistant drug formulation

• US 9,572,803 B2
• Filed: 12/27/2012
• Issued: 02/21/2017
• Est. Priority Date: 09/15/2006
• Status: Expired due to Fees

• Current Assignee: Cima Labs Incorporated (Teva Pharmaceutical Industries Limited)
• Original Assignee: Cima Labs Incorporated (Teva Pharmaceutical Industries Limited)
• Inventors: Habib, Walid A., Hamed, Ehab, Vega Zepeda, Manuel A.
• Primary Examiner(s): Berrios, Jennifer A
• Application Number:
  US13/728,801
• Publication Number:
  US 20130122101A1
• Time in Patent Office: 1,517 Days
• Field of Search: None
• US Class Current: 1/1
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• CPC Class Codes: A61K 9/14 Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51
• CPC Class Codes: A61K 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61K 9/1694 resulting in granules or microspheres of the matrix type containing more than 5% of excipient
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61K 9/2081 with microcapsules or coated microparticles according to A61K9/50
• CPC Class Codes: A61K 9/5042 Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/5047 Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose

Abstract

A pharmaceutical composition may include a coated particulate which may include at least one active pharmaceutical ingredient, particularly one susceptible to abuse by an individual. The coated particles may include a fat/wax and have improved controlled release and/or crush resistance. Method of making these coated particulate and dosage forms therewith are also described.

Claims

1. A coated granulate, comprising:

a granulate consisting of

at least one opioid in an amount between about 0.1 to about 90 percent by weight of the granulate mixed with two materials, wherein said first material is ethyl cellulose and is present in an amount between 5 and 75 percent by weight of the granulate and a second material that is selected from the group consisting of hydroxypropylmethylcellulose, methylcellulose, hydroxyethylmethylcellulose, and hydroxyethylcellulose and is present in an amount between 15 and 50 percent by weight of the granulate; and

a coating on said granulate provided in an amount of between about 20 and about 7 5 percent by weight of the coated granulate exhibiting crush resistance, wherein the coating comprises ethylcellulose.

2. The coated granulate of claim 1 wherein the second material is hydroxypropylmethylcellulose.

3. The coated granulate of claim 1 wherein the at least one opioid is selected from the group consisting of oxycodone, codeine, hydrocodone, morphine, hydromorphone, oxymorphone, methadone, propoxyphene, meperidine, fentanyl, buprenorphine, butorphanol, dezocine, levomethadyl acetate, levorphanol, nalbuphine, pentazocine, remifentanil, sufentanil, and tramadol.

4. The coated granulate of claim 2 wherein the at least one opioid is selected from the group consisting of oxycodone, codeine, hydrocodone, morphine, hydromorphone, oxymorphone, methadone, propoxyphene, meperidine, fentanyl, buprenorphine, butorphanol, dezocine, levomethadyl acetate, levorphanol, nalbuphine, pentazocine, remifentanil, sufentanil, and tramadol.