DOUBLE-LAYER PHARMACEUTICAL FORMULATIONS CONTAINING OPIOID AGONISTS AND ANTAGONISTS

• US 20130011479A1
• Filed: 03/23/2011
• Published: 01/10/2013
• Est. Priority Date: 03/24/2010
• Status: Abandoned Application

• Current Assignee: L Molteni & C DEI Fratelli Alitti Societa Di Esercizio SPA
• Original Assignee: L Molteni & C DEI Fratelli Alitti Societa Di Esercizio SPA
• Inventors: Angeli, Roberto, Raffaeli, William, Rigamonti, Maria Adele
• Application Number:
  US13/636,243
• Publication Number:
  US 20130011479A1
• Time in Patent Office: Days
• US Class Current: 424/480
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• 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: A61P 25/04 Centrally acting analgesics, e.g. opioids

Abstract

Immediate-release formulations are described, consisting of double-layer tablets wherein one layers contains an opioid agonist and the other an opioid antagonist.

Claims

1. Immediate-release formulations in the form of double-layer tablets containing as active ingredients an opioid agonist and an opioid antagonist, wherein said active ingredients are kept separate from each other, each of them in one of said two layers.

2. Formulations according to claim 1, wherein the amount of opioid antagonist is 500-4000 times lower than that of the opioid agonist.

3. Formulations according to claim 1, wherein said opioid agonists are chosen from among:

oxycodone, hydromorphone, morphine, codeine, buprenorphine, methadone.

4. Formulations according to claim 1, wherein said opioid antagonists are chosen from among:

naltrexone and naloxone.

5. Formulations according to claim 1, wherein the layer containing the agonist comprises:

SD lactose, pregelatinised corn starch, pigment, Macrogol 6000, Cutina®

HR, colloidal silica, magnesium stearate.

6. Formulations according to claim 5, wherein said components of the layer containing the opioid agonist are present in the following percentages by weight, calculated on the total weight of the components of the aforesaid layer:

SD lactose 40-60%, pregelatinised corn starch 10-20%, pigment 0.5-2%, Macrogol 6000 10-20%, Cutina®

HR 5-20%, colloidal silica 0-2%, magnesium stearate 0-2%.

7. Formulations according to claim 1, wherein the layer containing the opioid antagonist comprises:

Granulac 200 lactose, corn starch, croscarmellose sodium, polyvinylpyrrolidone K30, colloidal silica, magnesium stearate.

8. Formulations according to claim 7, wherein said components of the layer containing the opioid antagonist are present in the following percentages by weight, calculated on the total weight of the components of the aforesaid layer:

Granulac 200 lactose 30-80%, corn starch 5-10%, croscarmellose sodium 5-10%, polyvinylpyrrolidone K30 2-5%, colloidal silica 0-2%, magnesium stearate 0-2%.

9. Formulations according to claim 1, wherein the tablets are film-coated.

10. Formulations according to claim 1 consisting of:

(a)

Layer Containing the Opioid Agonist