Claims for Patent: 9,549,907

Summary for Patent: 9,549,907

Title:	Immediate release oral guaifenesin solution
Abstract:	Disclosed is an immediate release solution for oral administration of guaifenesin and at least one additional drug. In addition to water the solution comprises as solvents propylene glycol and glycerol in a concentration which significantly increases the bioavailability of guaifenesin in the human body.
Inventor(s):	Hafey; Paul (Keller, TX)
Assignee:	SOVEREIGN PHARMACEUTICALS, LLC (Fort Worth, TX)
Application Number:	14/940,455
Patent Claims:	1. An immediate release solution for the oral administration of guaifenesin, wherein the solution comprises hydrocodone and/or a pharmaceutically acceptable salt thereof as additional drug and as solvents water and a total of from 48% to 72% by weight, relative to a total weight of the solution, of propylene glycol and glycerol, and wherein the solution, when orally administered to an adult human subject as a single dose in an amount which affords 200 mg of guaifenesin, provides (i) a C.sub.max of at least 3600 ng/mL of guaifenesin and/or an AUC.sub.(0-inf) of guaifenesin of at least 3700 nghr/mL and (ii) a therapeutically effective plasma concentration of guaifenesin for at least 4 hours. 2. The solution of claim 1, wherein the solution comprises a total of from 54% to 66% by weight of propylene glycol and glycerol. 3. The solution of claim 1, wherein a weight ratio of glycerol to propylene glycol is from 1.7:1 to 2.5:1. 4. The solution of claim 1, wherein the solution comprises from 15% to 23% by of propylene glycol. 5. The solution of claim 1, wherein the solution comprises from 33% to 49% by weight of glycerol. 6. The solution of claim 1, wherein the solution provides a C.sub.max of at least 3800 ng/mL of guaifenesin. 7. The solution of claim 1, wherein the solution provides a C.sub.max of at least 4000 ng/mL of guaifenesin. 8. The solution of claim 6, wherein the solution provides an AUC.sub.(0-inf) of guaifenesin of at least 3900 nghr/mL. 9. The solution of claim 7, wherein the solution further provides an AUC.sub.(0-inf) of guaifenesin of at least 4100 nghr/mL. 10. The solution of claim 1, wherein the solution comprises hydrocodone bitartrate. 11. The solution of claim 10, wherein the solution comprises from 1.1 mg to 1.4 mg of hydrocodone bitartrate or an equivalent amount of hydrocodone and/or a different pharmaceutically acceptable salt of hydrocodone per 100 mg of guaifenesin. 12. The solution of claim 1, wherein the solution comprises from 30 mg/mL to 60 mg/mL of guaifenesin. 13. The solution of claim 12, wherein the solution comprises from 1.1 mg to 1.4 mg of hydrocodone bitartrate or an equivalent amount of hydrocodone and/or a different pharmaceutically acceptable salt of hydrocodone per 100 mg of guaifenesin. 14. The solution of claim 13, wherein the solution comprises from 15% to 23% by of propylene glycol and from 33% to 49% by weight of glycerol. 15. An immediate release solution for the oral administration of guaifenesin, wherein the solution comprises hydrocodone and/or a pharmaceutically acceptable salt thereof as additional drug and as solvents water and additionally propylene glycol and glycerol in a concentration which, when orally administered to an adult human subject as a single dose in an amount which affords 200 mg of guaifenesin, provides (i) a C.sub.max of guaifenesin which is higher than the C.sub.max of guaifenesin provided by an aqueous solution without propylene glycol and glycerol that comprises the same concentrations of guaifenesin and the at least one additional drug by a factor of at least 1.5 and/or an AUC.sub.(0-inf) of guaifenesin which is higher than the AUC.sub.(0-inf) of guaifenesin provided by the aqueous solution by a factor of at least 1.4 and (ii) a therapeutically effective plasma concentration of guaifenesin for at least 4 hours. 16. The solution of claim 15, wherein the solution provides a C.sub.max of guaifenesin which is higher than the C.sub.max of guaifenesin provided by an aqueous solution by a factor of at least 1.6 and an AUC.sub.(0-inf) of guaifenesin which is higher than the AUC.sub.(0-inf) of guaifenesin provided by the aqueous solution by a factor of at least 1.5. 17. The solution of claim 15, wherein the solution comprises a total of from 48% to 72% by weight of propylene glycol and glycerol, based on a total weight of the solution. 18. The solution of claim 17, wherein the solution comprises from 30 mg/mL to 60 mg/mL of guaifenesin. 19. The solution of claim 18, wherein the solution comprises from 1.1 mg to 1.4 mg of hydrocodone bitartrate or an equivalent amount of hydrocodone and/or a different pharmaceutically acceptable salt of hydrocodone per 100 mg of guaifenesin. 20. A method of increasing the bioavailability of guaifenesin in an aqueous solution for oral administration, wherein the method comprises including in the solution propylene glycol and glycerol in an amount which increases the C.sub.max of guaifenesin in an adult human subject by a factor of at least 1.5 and/or increases the AUC.sub.(0-inf) of guaifenesin by a factor of at least 1.4 when the solution is orally administered as a single dose in an amount which affords 200 mg of guaifenesin.