Freeze-dried pantoprazole preparation and pantoprazole injection
View Patent ↗Lyophilized pantoprazole preparations which are obtainable by freeze-drying of an aqueous solution of pantoprazole, ethylenediamine tetraacetic acid and/or a suitable salt thereof, and sodium hydroxide and/or sodium carbonate are disclosed. The preparations have advantageous properties when reconstituted for injection.
1. A pantoprazole injectable solution for bolus administration obtainable by reconstitution consisting of:
(a) a lyophilized preparation consisting of:
i. 5-difluoromethoxy-2-[(3,4-dimethoxy-2-pyridinyl)methylsulfinyl]-1H-benzimidazole (pantoprazole) or a solvate, hydrate, salt, hydrate of a salt or solvate of a salt thereof;
ii. ethylenediamine tetraacetic acid and/or a suitable salt thereof, and
iii. sodium hydroxide and/or sodium carbonate; and
(b) an aqueous solvent selected from the group consisting of physiological saline, an aqueous solution of 5% glucose and distilled water.
2. The pantoprazole injectable solution according to claim 1 , wherein the solvent is physiological saline.
3. The pantoprazole injectable solution according to claim 1 , wherein the pantoprazole is pantoprazole sodium.
4. The pantoprazole injectable solution according to claim 1 , wherein the pantoprazole is pantoprazole sodium sesquihydrate.
5. The pantoprazole injectable solution according to claim 1 , wherein the pantoprazole is pantoprazole magnesium.
6. The pantoprazole injectable solution according to claim 1 , wherein the pantoprazole is pantoprazole magnesium dihydrate.
7. The pantoprazole injectable solution according to claim 1 , wherein the pantoprazole is (−)-pantoprazole or a solvate, hydrate, salt, hydrate of a salt or solvate of a salt thereof.
8. The pantoprazole injectable solution according to claim 1 , wherein the ethylenediamine tetraacetic acid is present as ethylenediamine tetraacetic acid disodium salt.
9. The pantoprazole injectable solution according to claim 2 , wherein the ethylenediamine tetraacetic acid is present as ethylenediamine tetraacetic acid disodium salt.
10. The pantoprazole injectable solution according to claim 3 , wherein the ethylenediamine tetraacetic acid is present as ethylenediamine tetraacetic acid disodium salt.
11. The pantoprazole injectable solution according to claim 4 , wherein the ethylenediamine tetraacetic acid is present as ethylenediamine tetraacetic acid disodium salt.
12. The pantoprazole injectable solution according to claim 5 , wherein the ethylenediamine tetraacetic acid is present as ethylenediamine tetraacetic acid disodium salt.
13. The pantoprazole injectable solution according to claim 6 , wherein the ethylenediamine tetraacetic acid is present as ethylenediamine tetraacetic acid disodium salt.
14. The pantoprazole injectable solution according to claim 7 , wherein the ethylenediamine tetraacetic acid is present as ethylenediamine tetraacetic acid disodium salt.
15. The pantoprazole injectable solution according to claim 1 , wherein the lyophilized preparation consists of
(a) Pantoprazole sodium;
(b) ethylenediamine tetraacetic acid disodium salt; and
(c) sodium hydroxide.
16. The pantoprazole injectable solution according to claim 1 , wherein the lyophilized preparation consists of
(a) Pantoprazole sodium sesquihydrate;
(b) ethylenediamine tetraacetic acid disodium salt; and
(c) sodium hydroxide.