IP Library Granted Patent US 11,759,459
Granted Patent B2
US 11,759,459 · App. 17/958,780 · Granted Sep 19, 2023

Treatment of pain by subarachnoid administration of sustained-release liposomal anesthetic compositions

Inventors: Roy Winston (Parsippany, NJ); Kathy Los (Parsippany, NJ); Vladimir Kharitonov (Parsippany, NJ)
Assignee: Pacira Pharmaceuticals, Inc.
A61K31/445A61K9/0019A61K9/0085A61K9/127A61K31/485A61P23/00A61P23/02
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Quick Facts
Patent No.
US 11,759,459
App. No.
17/958,780
Granted
Sep 19, 2023
Kind
B2
Abstract

In some embodiments provided herein is a method of treating pain, the method comprising injecting into the subarachnoid space of the subject a pharmaceutical composition comprising: a) a multivesicular liposome comprising: at least one amphipathic lipid, and at least one neutral lipid; and b) an aqueous phase comprising bupivacaine phosphate, wherein the aqueous phase is encapsulated within the multivesicular liposome.

Claims (19)

1. A method of treating pain in a subject, the method comprising injecting into the subarachnoid space at the L3 and L4 level of the subject a pharmaceutical composition comprising: a) a multivesicular liposome comprising: at least one amphipathic lipid, and at least one neutral lipid; and b) an aqueous phase comprising bupivacaine phosphate, wherein the aqueous phase is encapsulated within the multivesicular liposome.

2. The method of claim 1 , wherein the aqueous phase further comprises hydrochloric acid.

3. The method of claim 1 , wherein the amphipathic lipid is selected from the group consisting of phosphatidylcholines, phosphatidylethanolamines, sphingomyelins, lysophosphatidylcholines, lysophosphatidylethanolamines, phosphatidylglycerols, phosphatidylserines, phosphatidylinositols, phosphatidic acids, cardiolipins, diacyl dimethylammonium propanes, and stearylamines.

4. The method of claim 1 , wherein the neutral lipid is at least one triglyceride.

5. The method of claim 1 , wherein the pharmaceutical composition comprises a therapeutically effective amount of bupivacaine phosphate.

6. The method of claim 1 , wherein the pharmaceutical composition comprises from about 10 mg to about 60 mg of bupivacaine phosphate.

7. The method of claim 6 , wherein the pharmaceutical composition comprises from about 20 mg to about 60 mg of bupivacaine phosphate.

8. The method of claim 6 , wherein the pharmaceutical composition comprises from about 30 mg to about 60 mg of bupivacaine phosphate.

9. The method of claim 1 , wherein the method comprises administering the pharmaceutical composition by epidural injection.

10. The method of claim 1 , wherein the method does not comprise administering the pharmaceutical composition by epidural injection.

11. The method of claim 1 , wherein the method does not comprise administering an opioid to the subject following the injection of the pharmaceutical composition into the subarachnoid space of the subject.

12. The method of claim 1 , wherein the method comprises administering an opioid to the subject following the injection of the pharmaceutical composition into the subarachnoid space of the subject.

13. The method of claim 12 , wherein the opioid is oxycodone and the method comprises administering oxycodone in a total amount less than 15 mg in the first about 72 hours following the injection of the pharmaceutical composition into the subarachnoid space of the subject.

14. The method of claim 1 , wherein the method comprises administering a non-opioid analgesic to the subject following the injection of the pharmaceutical composition into the subarachnoid space of the subject.

15. The method of claim 1 , wherein the subject has an AUC for VAS pain intensity scores over the first 72 hours following the injection of the pharmaceutical composition into the subarachnoid space of the subject of from about 100 to about 200.

16. The method of claim 1 , wherein the subject has a pruritus score as determined by the 5-D itch scale of about 10 to about 20.

17. The method of claim 1 , wherein the plasma concentration of bupivacaine in the subject after about 120 hours following the injection of the pharmaceutical composition into the subarachnoid space of the subject is about is about 150 ng/mL to about 250 ng/mL.

18. The method of claim 1 , wherein the pain is abdomen pain.

19. The method of claim 1 , wherein the pain is pelvic pain.

Assignments (6)
RELEASE OF SECURITY INTEREST Recorded Dec 5, 2025
From: JPMORGAN CHASE BANK, N.A.
To: PACIRA CRYOTECH, INC.; PACIRA PHARMACEUTICALS, INC.; PACIRA THERAPEUTICS, INC. (F/K/A FLEXION THERAPEUTICS, INC.)
Reel/Frame 073779/0532 →
SECURITY INTEREST Recorded Jul 4, 2025
From: PACIRA PHARMACEUTICALS, INC.
To: WELLS FARGO BANK, NATIONAL ASSOCIATION, AS ADMINISTRATIVE AGENT
Reel/Frame 071814/0792 →
CONFIRMATORY GRANT OF SECURITY INTEREST IN UNITED STATES PATENTS Recorded Mar 31, 2023
From: PACIRA CRYOTECH, INC.; PACIRA PHARMACEUTICALS, INC.; PACIRA THERAPEUTICS, INC. (F/K/A FLEXION THERAPEUTICS, INC.)
To: JPMORGAN CHASE BANK, N.A.
Reel/Frame 063214/0108 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 6, 2022
From: WINSTON, ROY
To: PACIRA PHARMACEUTICALS, INC.
Reel/Frame 061332/0361 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 6, 2022
From: WINSTON, ROY
To: PACIRA PHARMACEUTICALS, INC.
Reel/Frame 061332/0394 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 6, 2022
From: LOS, KATHY; KHARITONOV, VLADIMIR
To: PACIRA PHARMACEUTICALS, INC.
Reel/Frame 061332/0724 →
Continuity (5)
Continuation 17790426
Provisional Application 63066477 · Aug 17, 2020
Provisional Application 63064760 · Aug 12, 2020
Provisional Application 62959550 · Jan 10, 2020
Related Publication 20230038098A1 · Feb 9, 2023
Cited By (1)
US 12,226,610