Opioid agonist in a fast dispersing dosage form

• US 6,680,071 B1
• Filed: 01/14/2002
• Issued: 01/20/2004
• Est. Priority Date: 03/03/1999
• Status: Expired due to Term

• Current Assignee: Catalent Pharma Solutions Incorporated (Catalent, Inc.), Catalent Pharma Solutions Limited (Catalent, Inc.), Catalent USA Packaging LLC (Catalent, Inc.), Catalent USA Paintball, Inc. (Catalent, Inc.), Catalent USA Woodstock, Inc. (Catalent, Inc.)
• Original Assignee: RP Scherer Technologies Incorporated (Catalent, Inc.)
• Inventors: Johnson, Edward Stewart, Lacy, Jon
• Primary Examiner(s): KRASS, FREDERICK F
• Application Number:
  US09/936,060
• Time in Patent Office: 736 Days
• Field of Search: 424/484, 424/485, 424/486, 424/487, 424/488, 424/439, 424/441, 424/465, 424/466, 514/329, 514/816, 514/817, 514/818
• US Class Current: 424/484
• CPC Class Codes: A61K 31/4468 having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61K 9/2095 Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing mechanical aspects A61J3/00

Abstract

This invention relates to a pharmaceutical composition for oral administration comprising a carrier and, as active ingredient, an opioid (μreceptor) agonist, such as fentanyl, or a salt thereof, characterized in that the composition is in the form of a fast-dispersing dosage form designed to release the active ingredient rapidly in the oral cavity. A process for preparing such a composition and the use of such a composition as an analgesic, for the treatment of chronic pain and/or breakthrough pain, as an anesthetic premedication, for the induction of anesthesia, as a sedative and/or for the treatment of anxiety are also provided.

Claims

1. A pharmaceutical composition for oral administration comprising a carrier and, as an active ingredient, an opioid agonist characterized in that said composition is in the form of a solid fast-dispersing dosage form comprising a network of said active ingredient and a water-soluble or water-dispersible carrier which is inert towards said active ingredient and wherein, said dosage form disintegrates within 1-30 seconds of being placed in the oral cavity.

2. The pharmaceutical composition of claim 1 in which the opioid agonist is fentanyl or a salt thereof.

3. The pharmaceutical composition of claim 1 wherein said network has been obtained by subliming solvent from a composition in the solid state, that composition comprising said active ingredient and a solution of the carrier in a solvent.

4. The pharmaceutical composition of claim 1 in which said active ingredient is present in an amount from 0.2 to 95% by weight of the composition.

5. The pharmaceutical composition of claim 2 which fentanyl or a salt thereof is present in an amount from 0.5 to 10% by weight of the composition.

6. The pharmaceutical composition of claim 2 in which the active ingredient is present in an amount from 0.1 to 200 mg per dosage form.

7. A method of providing anesthetic pre-medication, said method comprising the step of providing to a patient in need thereof the pharmaceutical composition according to claim 1.

8. A method of inducing anesthesia, said method comprising the step of administering a pharmaceutical composition according to claim 1 to a patient in need thereof.

9. A method of administering an opioid agonist to a patient which comprises introducing into the oral cavity of the patient a composition according to claim 1.

10. A method of treating pain which comprises introducing into the oral cavity of a patient a therapeutically effective amount of a composition according to claim 1.

11. The method according to claim 10 in which the pain is chronic pain.

12. The method according to claim 10 in which the patient is experiencing chronic and the pain to be treated is breakthrough pain.