High-purity large-scale preparation of stannsoporfin

Patent metadata

Field	Value
Publication number	US-10662209-B2
Application number	US-201916298603-A
Country	US
Kind code	B2
Filing date	Mar 11, 2019
Priority date	Oct 4, 2006
Publication date	May 26, 2020
Grant date	May 26, 2020

Abstract

Large scale (bulk) compositions comprising high-purity stannsoporfin are disclosed, as well as methods of synthesizing such compositions.

First claim

What is claimed is:

1. A composition comprising stannsoporfin, wherein the stannsoporfin is at least about 97% pure, and wherein any individual impurity is present in an amount less than about 0.08%.

2. The composition of claim 1 , wherein the stannsoporfin is at least about 98.5% pure.

3. The composition of claim 1 , wherein the composition comprises palladium in an amount of less than about 20 ppm.

4. The composition of claim 1 , wherein the composition comprises palladium in an amount of less than about 10 ppm.

5. The composition of claim 1 , wherein any impurity present is present in an amount of about 0.07% or less.

6. The composition of claim 1 , wherein the composition has a pH of about 7.0 to about 8.0.

7. The composition of claim 1 , wherein the composition has a pH of about 7.2 to about 7.9.

8. The composition of claim 1 , comprising at least about 10 grams of stannsoporfin.

9. The composition of claim 1 , comprising at least about 100 grams of stannsoporfin.

10. The composition of claim 1 , comprising at least about 10 grams of stannsoporfin, wherein the composition contains palladium in an amount of less than about 20 ppm.

11. The composition of claim 10 , wherein the stannsoporfin is a single-batch preparation of stannsoporfin.

12. The composition of claim 1 , wherein the composition further comprises at least one impurity in an amount between about 0.05% and about 0.08%, the at least one impurity having a relative retention time of 0.72-0.73 in an HPLC analysis.

13. A pharmaceutical composition comprising stannsoporfin and a pharmaceutically acceptable carrier, wherein the stannsoporfin is at least about 97% pure, and wherein any individual impurity is present in an amount less than about 0.08%.

14. The pharmaceutical composition of claim 13 , wherein the stannsoporfin is present in an amount suitable for delivering up to a 4.5 mg/kg dose by birth weight.

15. The pharmaceutical composition of claim 13 , wherein the stannsoporfin is present in an amount suitable for delivering a dose of about 1.5 mg/kg to about 3.0 mg/kg by birth weight.

16. The pharmaceutical composition of claim 13 , wherein the pharmaceutical composition has a pH of about 7.0 to about 8.0.

17. The pharmaceutical composition of claim 13 , wherein the pharmaceutical composition has a pH of about 7.2 to about 7.9.

18. The pharmaceutical composition of claim 13 , wherein the stannsoporfin is at least about 98.5% pure.

19. The pharmaceutical composition of claim 13 , wherein the pharmaceutical composition comprises palladium in an amount of less than about 20 ppm.

20. The pharmaceutical composition of claim 13 , wherein the pharmaceutical composition comprises palladium in an amount of less than about 10 ppm.

Assignees

• Mallinckrodt Hospital Products Ip Ltd

Inventors

• Drummond George S
• Caroselli Robert
• Cooke Keith A
• Levin Daniel
• Roe David G
• Boucher Christopher P

Classifications

• A61K9/0019

  Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00) · CPC title

• C07D487/22

  in which the condensed system contains four or more hetero rings · CPC title

• C07F7/003

  without C-Metal linkages · CPC title

• A61K31/555 Primary

  containing heavy metals, e.g. hemin, hematin, melarsoprol · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title