Claims for Patent: 9,694,079

Summary for Patent: 9,694,079

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. (Redwood City, CA)
Application Number:	15/260,820
Patent Claims:	1. A delivery system for administration to a subject, the delivery system comprising: 40 wt % to 75 wt % of a polyorthoester; 3 wt % to 25 wt % dimethyl sulfoxide; 10 wt % to 35 wt % triacetin; 2 wt % to 5 wt % bupivacaine; and 0.01 wt % to 1 wt % meloxicam; wherein the polyorthoester is represented by the structure shown as Formula I: ##STR00033## where R* is C.sub.1-4 alkyl, n ranges 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 R.sup.3 is ##STR00034## where x is 2; and when 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. 2. The delivery system of claim 1, wherein the delivery system has a viscosity less than 10000 mPa-s when measured at 37.degree. C. using a viscometer. 3. The delivery system of claim 1, wherein the fraction of A units that are of formula R.sup.1 is about 20 mole percent. 4. The delivery system of claim 1, wherein the polyorthoester has a weight average molecular weight between 2,500 daltons and 10,000 daltons. 5. The delivery system of claim 1, wherein the bupivacaine and the meloxicam are solubilized in a single phase. 6. The delivery system of claim 1, wherein the delivery system is an extended-release composition. 7. The delivery system of claim 1, further comprising maleic acid. 8. A method for providing analgesia or pain relief to a subject in need thereof, comprising: administering to the subject the delivery system according to claim 1. 9. The method of claim 8, wherein the delivery system is administered as a nerve block. 10. The method of claim 8, wherein the delivery system is administered as a peripheral nerve block. 11. The method of claim 8, wherein the delivery system is administered to a surgical wound. 12. The method according to claim 8, wherein the pain is post-operative pain. 13. A method for prophylactic treatment of pain in a subject, comprising: administering to the subject the delivery system according to claim 1. 14. The delivery system of claim 1, wherein the polyorthoester comprises the unit ##STR00037##