Compositions and Methods for Mild Sedation, Anxiolysis and Analgesia in the Procedural Setting

• US 20110091544A1
• Filed: 10/16/2009
• Published: 04/21/2011
• Est. Priority Date: 10/16/2009
• Status: Abandoned Application

• Current Assignee: AcelRx Pharmaceuticals Incorporated
• Original Assignee: AcelRx Pharmaceuticals Incorporated
• Inventors: Palmer, Pamela
• Application Number:
  US12/580,930
• Publication Number:
  US 20110091544A1
• Time in Patent Office: Days
• US Class Current: 424/464
• CPC Class Codes: A61J 7/0076 Medicament distribution means with pill counting devices A61J7/02; with time indication A61J7/04; containers or packages with special means for dispensing contents B65D83/00
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 31/5517 condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61P 23/00 Anaesthetics
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: A61P 25/22 Anxiolytics

Abstract

Small tablets for use in procedural sedation, anxiolysis and analgesia comprising the combination sufentanil and triazolam administered via the oral transmucosal route and methods for using the same are provided.

Claims

1. A dosage form for oral transmucosal administration to an alert, awake, subject prior to a medical or dental procedure, comprising:

a single bioadhesive tablet having a mass of from about 5 mg to about 25 mg or a volume of from about 5 mcl to about 25mcl, said tablet comprising the combination of sufentanil and triazolam.

2. The bioadhesive tablet according to claim 1, wherein said tablet has a mass of from about 2 mg to about 10 mg or a volume of from about 2 mcl to about 10 mcl.

3. The bioadhesive tablet according to claim 1, wherein said tablet has a thickness of from about 0.7 mm to about 1.0 mm or from about 0.75 mm to about 0.95 mm.

4. The bioadhesive tablet according to claim 1, wherein said tablet has a diameter of from about 2.5 mm to about 4.0 mm, or from about 3.0 mm to about 3.5 mm.

5. The bioadhesive tablet according to claim 1, wherein said tablet comprises from about 4 mcg to about 50 mcg of sufentanil.

6. The bioadhesive tablet according to claim 5, wherein said tablet comprises from about 10 mcg to about 20 mcg of sufentanil.

7. The bioadhesive tablet according to claim 5, wherein said tablet comprises from about 100 mcg to about 500 mcg of triazolam.

8. The bioadhesive tablet according to claim 5, wherein said tablet comprises from about 150 mcg to about 300 mcg of triazolam.

9. The bioadhesive tablet according to claim 1, wherein said oral transmucosal administration is sublingual administration.

10. The bioadhesive tablet according to claim 1, wherein said oral transmucosal administration is buccal administration.

11. The bioadhesive tablet according to claim 1, wherein said tablet comprises a substantially homogeneous composition.

12. The bioadhesive tablet according to claim 1, wherein said tablet does not comprise an ordered mixture of microparticles of drug adhered to the surface of carrier particles where the carrier particles are substantially larger than the microparticles of drug.

13. A single dose applicator (SDA), comprising a bioadhesive tablet according to claim 1.

14. A single dose applicator (SDA), comprising a bioadhesive tablet according to claim 8.

15. A method for procedural sedation, anxiolysis and analgesia of a subject during a diagnostic or therapeutic medical or dental procedure, comprising:

administering a sufentanil/triazolam tablet according to claim 1 to a subject prior to a medical or dental procedure, wherein at a specific time following said administering, the cumulative RASS sedation score is significantly lower for subjects who were administered a sufentanil/triazolam tablet as compared to subjects who were administered a placebo tablet.

16. The method according to claim 15, wherein the onset of sedation is evident 30 minutes following said administering.

17. The method according to claim 15, wherein at a specific time following said administering, the cumulative NRS anxiety score is significantly lower for subjects who were administered a sufentanil/triazolam tablet as compared to subjects who were administered a placebo tablet.

18. The method according to claim 17, wherein the onset of anxiolysis is evident 15 minutes following said administering.

19. The method according to claim 15, wherein all patients have a modified Aldrete score of greater than or equal to 8 beginning 2 hours or less following said administering.

20. The method according to claim 19, wherein the duration of sedation is 4 hours or less following said administering.

21. A method for procedural sedation, anxiolysis and analgesia of a subject, comprising,

administering a tablet according to claim 8 to a subject using a handheld dispensing device for placement of said tablet in the sublingual space.

22. The method according to claim 21, wherein said a handheld dispensing device is a single dose applicator (SDA).