IP Library Patent Application 14181041
Patent Application
App. No. 14/181,041

Tazobactam Arginine Compositions

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Patent No.
US None
App. No.
14/181,041
Abstract

This disclosure provides compositions containing solid forms of tazobactam arginine, and methods of manufacturing and using these compositions.

Claims (38)

1 - 6 . (canceled)

7 . A composition obtained by a process comprising the steps of:

a) combining L-arginine, tazobactam acid and acetone in an aqueous solution at a pH of 5.9+/−0.5;

b) allowing a solid tazobactam arginine composition to precipitate from the aqueous solution; and

c) obtaining the solid tazobactam arginine composition from the aqueous solution.

8 . The composition of claim 7 , wherein the tazobactam acid and L-arginine are combined in the aqueous solution before combination with the acetone.

9 . The composition of claim 8 , wherein the aqueous solution is at a temperature of about 22-30 degrees C.

10 . The composition of claim 9 , further comprising cooling the solution comprising L-arginine, tazobactam acid and acetone to a temperature of about 10-15 degrees C. prior to obtaining the solid tazobactam arginine composition from the aqueous solution.

11 . The composition of claim 7 , further comprising combining the solid tazobactam arginine composition with a beta lactam antibiotic in a pharmaceutical composition.

12 . The composition of claim 7 , wherein the solid tazobactam arginine composition has a differential scanning calorimetry (DSC) thermogram having a characteristic peak at about 209 degrees C.

13 . The composition of claim 7 , wherein the solid tazobactam arginine composition has a thermogravity (TG) curve with an onset temperature of about 201 degrees C.

14 . The composition of claim 7 , wherein the solid tazobactam arginine composition has a solubility in acetic acid of greater than about 100 mg/mL at about 22 degrees C.

15 . The composition of claim 7 , wherein the solid tazobactam arginine composition has a solubility in water of greater than about 100 mg/mL at about 22 degrees C.

16 . The composition of claim 8 , obtained by a method further comprising cooling the solution comprising L-arginine, tazobactam acid and acetone to a temperature of about 10-15 degrees C. prior to obtaining the solid tazobactam arginine composition from the aqueous solution, and combining the solid tazobactam arginine composition with a beta lactam antibiotic selected from the group consisting of the compounds in Table 2 in a pharmaceutical composition, wherein:

a) the aqueous solution is at a temperature of about 22-30 degrees C.;

b) the solid tazobactam arginine composition has a differential scanning calorimetry (DSC) thermogram having a characteristic peak at about 209 degrees C.; and

c) the solid tazobactam arginine composition has a thermogravity (TG) curve with an onset temperature of about 201 degrees C.

17 . A composition obtained by a method comprising the steps of:

a) combining L-arginine, tazobactam acid and isopropanol in an aqueous solution;

b) allowing a solid tazobactam arginine composition to precipitate from the aqueous solution; and

c) obtaining the solid tazobactam arginine composition from the aqueous solution.

18 . The composition of claim 17 , wherein the tazobactam acid and L-arginine are combined in the aqueous solution before combination with the isopropanol.

19 . The composition of claim 18 , wherein the aqueous solution is at a temperature of about 22-30 degrees C.

20 . The composition of claim 19 , further comprising combining the solid tazobactam arginine composition with a beta lactam antibiotic in a pharmaceutical composition.

21 . The composition of claim 20 , wherein the beta lactam antibiotic is selected from the group consisting of the beta lactam compounds of Table 2.

22 . The composition of claim 17 , wherein the solid tazobactam arginine composition has a differential scanning calorimetry (DSC) thermogram having a characteristic peak at about 209 degrees C.

23 . The composition of claim 17 , wherein the solid tazobactam arginine composition has a thermogravity (TG) curve with an onset temperature of about 201 degrees C.

24 . The composition of claim 17 , wherein the solid tazobactam arginine composition has a solubility in acetic acid of greater than about 100 mg/mL at about 22 degrees C.

25 . The composition of claim 17 , wherein the solid tazobactam arginine composition has a solubility in water of greater than about 100 mg/mL at about 22 degrees C.

26 . The composition of claim 18 , obtained by a method further comprising cooling the solution comprising L-arginine, tazobactam acid and isopropanol to a temperature of about 10 degrees C. prior to obtaining the solid tazobactam arginine composition from the aqueous solution, and combining the solid tazobactam arginine composition with a beta lactam antibiotic selected from the group consisting of the compounds in Table 2 in a pharmaceutical composition, wherein:

a) the aqueous solution is at a temperature of about 25 degrees C.;

b) the solid tazobactam arginine composition has a differential scanning calorimetry (DSC) thermogram having a characteristic peak at about 209 degrees C.; and

c) the solid tazobactam arginine composition has a thermogravity (TG) curve with an onset temperature of about 201 degrees C.

27 . A pharmaceutical composition obtained by a process comprising the steps of:

a) combining tazobactam, L-arginine in an aqueous solution with an antisolvent selected from the group consisting of acetone and isopropanol;

b) allowing a solid composition comprising tazobactam and L-arginine to precipitate from the aqueous solution;

c) obtaining the solid composition from the aqueous solution and

d) combining the solid composition with a beta lactam antibiotic in a pharmaceutical composition comprising tazobactam and L-arginine.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 3, 2015
From: CALIXA THERAPEUTICS, INC.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 037198/0658 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 18, 2014
From: CUBIST PHARMACEUTICALS, INC.
To: CALIXA THERAPEUTICS, INC.
Reel/Frame 034200/0860 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 25, 2014
From: LAI, JAN-JI; GU, JIAN-QIAO; PATHARE, PRADIP M.; JURKAUSKAS, VALDAS; TERRACCIANO, JOSEPH; DAMOUR, NICOLE MILLER
To: CUBIST PHARMACEUTICALS, INC.
Reel/Frame 032520/0553 →