Claims for Patent: 10,632,199

Summary for Patent: 10,632,199

Title:	Long-acting polymeric delivery systems
Abstract:	Compositions comprised of a delivery vehicle or delivery system and an active agent dispersed within the delivery vehicle or system, wherein the delivery vehicle or system contains a polyorthoester polymer and a polar aprotic solvent. Also disclosed are low viscosity delivery systems for administration of active agents. The low viscosity delivery systems have a polyorthoester polymer, a polar aprotic solvent and a solvent containing a triglyceride viscosity reducing agent. Compositions described include an amide- or anilide-type local anesthetic of the "caine" classification, and a non-steroidal anti-inflammatory drug (NSAID), along with related methods, e.g., for treatment of post-operative pain or for prophylactic treatment of pain. The compositions are suitable for delivery via, e.g., direct application and instillation, intradermal injection, subcutaneous injection, and nerve block (perineural).
Inventor(s):	Ottoboni; Thomas B. (Belmont, CA), Girotti; Lee Ann Lynn (San Bruno, CA)
Assignee:	Heron Therapeutics, Inc. (San Diego, CA)
Application Number:	16/107,965
Patent Claims:	1. A composition, consisting essentially of: a delivery vehicle, bupivacaine, and meloxicam, wherein the ratio of bupivacaine to meloxicam ranges from about 15:1 to 50:1, wherein meloxicam is present in the composition in an amount between about 0.005-0.75 wt % and wherein the composition contains no additional active agents. 2. The composition of claim 1, wherein bupivacaine is present in the composition in an amount ranging from about 0.1 to 8.0 wt % and meloxicam is present in the composition in an amount ranging from about 0.01-0.5 wt %. 3. The composition of claim 1, wherein the delivery vehicle is a sustained-release delivery vehicle. 4. The composition of claim 1, wherein the delivery vehicle is aqueous based. 5. The composition of claim 3, wherein the sustained-release delivery vehicle is a bioerodible or biodegradable polymer. 6. The composition of claim 5, wherein the polymer is a polyorthoester represented by the structure shown as Formula I: ##STR00033## where: R* is a C.sub.1-4 alkyl, n is an integer ranging from 5 to 400, and A is a diol, where A is R.sup.1 and/or R.sup.3, where the fraction of A units that are of formula R.sup.1 is between 0 and 25 mole percent, where when A is R.sup.3, R.sup.3 is ##STR00034## where x is 2; and when A is R.sup.1, R.sup.1 is ##STR00035## R.sup.5 is H, and R.sup.6 is ##STR00036## the sum of p and q is, on average, 2 and s is 2, where the resulting component of the polyorthoester comprises the subunit ##STR00037## 7. The composition of claim 6, wherein the delivery vehicle comprises the polyorthoester, a polar aprotic solvent and a triglyceride viscosity reducing agent. 8. The composition of claim 7, wherein the polar aprotic solvent is selected from dimethyl sulfoxide, N-methyl pyrrolidone and dimethyl acetamide. 9. The composition of claim 7, wherein bupivacaine is present in the composition at between about 0.01 wt % and about 7.5 wt % of the composition. 10. The composition of claim 9, wherein meloxicam is present in the composition at between about 0.005 wt % to 0.25 wt % of the composition. 11. The composition of claim 7, wherein the delivery vehicle comprises: 40 wt % to 75 wt % of the polyorthoester; 5 wt % to 12 wt % dimethyl sulfoxide; and 20 wt % to 40 wt % triacetin; and wherein bupivacaine is present in an amount of between about 1 wt % to 5 wt %. 12. The composition of claim 11, wherein the delivery vehicle further comprises 0.01 wt % to 0.3 wt % maleic acid. 13. The composition of claim 1, wherein meloxicam is present in the composition in an amount ranging from about 0.005-0.25 wt %. 14. The composition of claim 1, wherein meloxicam is present in the composition in an amount ranging from about 0.005-0.125 wt %. 15. The composition of claim 1, wherein the ratio of bupivacaine to meloxicam ranges from about 20:1 to 40:1. 16. The composition of claim 1, wherein the the ratio of bupivacaine to meloxicam ranges from about 30:1 to 35:1. 17. A method for producing analgesia or pain relief in a subject in need thereof, comprising: administering to the subject the composition according to claim 1. 18. A method for managing pain or for prophylactic treatment of pain in a subject, comprising administering to the subject the composition according to claim 1. 19. The method of claim 17, wherein the composition is administered perineural or to a surgical wound. 20. The method of claim 18, wherein the pain is postsurgical pain.