Compositions and kits for omeprazole suspension
Disclosed herein are liquid diluents, formulations, and kits for preparing reconstituted suspensions of a proton pump inhibitor (e.g., omeprazole). The present disclosure also provides formulations for liquid diluents that do not have a tendency for gel formation following exposure to freeze-thaw cycles.
1. A liquid diluent for reconstituting omeprazole, consisting essentially of:
1.0%-4.0% w/v poloxamer 188;
1.0%-2.0% w/v sodium carboxymethylcellulose (CMC);
8.0%-8.8% w/v sodium bicarbonate;
0.5%-1.5% w/v sodium citrate;
0.1%-0.3% w/v simethicone emulsion;
0.35%-3.5% w/v sweetener;
0.4%-0.6% w/v preservative, wherein the preservative is benzyl alcohol; and
water;
wherein the liquid diluent is stable for at least 30 days and is resistant to gel formation for at least one freeze-thaw cycle.
2. The liquid diluent of claim 1 , wherein the poloxamer 188 is present in the liquid diluent at 1% w/v.
3. The liquid diluent of claim 1 , wherein the poloxamer 188 is present in the liquid diluent at 2% w/v.
4. The liquid diluent of claim 1 , wherein the poloxamer 188 is present in the liquid diluent at 4% w/v.
5. The liquid diluent of claim 1 , wherein the sodium CMC is present in the liquid diluent at 1.2% w/v.
6. The liquid diluent of claim 1 , wherein the liquid diluent comprises a coloring agent, and wherein the coloring agent is 0.002%-0.005% w/v FD&C Red No. 40.
7. The liquid diluent of claim 6 , wherein the FD&C Red No. 40 is 0.003% w/v.
8. The liquid diluent of claim 1 , wherein the liquid diluent comprises a flavoring agent, and wherein the flavoring agent is 0.1%-0.2% w/v Strawberry Flavor CW08.
9. The liquid diluent of claim 8 , wherein the Strawberry Flavor CW08 is 0.15% w/v.
10. The liquid diluent of claim 1 , wherein the sodium bicarbonate is present in the liquid diluent at 8.4% w/v.
11. The liquid diluent of claim 1 , wherein the sodium citrate is present in the liquid diluent at 1% w/v.
12. The liquid diluent of claim 1 , wherein the simethicone emulsion is present in the liquid diluent at 0.15% w/v.
13. The liquid diluent of claim 1 , wherein the sweetener comprises 70% sorbitol solution and sucralose.
14. The liquid diluent of claim 13 , wherein the 70% sorbitol solution is present in the liquid diluent at 2.5% w/v.
15. The liquid diluent of claim 13 , wherein the sucralose is present in the liquid diluent at 0.4 w/v.
16. The liquid diluent of claim 1 , wherein the benzyl alcohol is present in the liquid diluent at 0.5% w/v.
17. A suspension of omeprazole consisting essentially of:
omeprazole, poloxamer 188, sodium carboxymethylcellulose (CMC), sodium bicarbonate, sodium citrate, simethicone emulsion, benzyl alcohol, a sweetener, and water;
wherein the suspension is homogenous and stable for at least 30 days at ambient conditions and at refrigerated temperature conditions.
18. The suspension of claim 17 , wherein the poloxamer 188 is present in the suspension at 1.0%-4.0% w/v.
19. The suspension of claim 17 , wherein the poloxamer 188 is present in the suspension at 1.0% w/v.
20. The suspension of claim 17 , wherein the sodium CMC is present in the suspension at 1.0%-2.0% w/v.
21. The suspension of claim 17 , wherein the sodium CMC is 1.2% w/v.
22. The suspension of claim 17 , wherein the poloxamer 188 is 1.0%-4.0% w/v and the Sodium CMC is 1.0%-2.0% w/v.
23. The suspension of claim 17 , consisting essentially of:
omeprazole;
1.0%-4.0% w/v poloxamer 188;
1.0%-2.0% w/v sodium CMC;
8.0%-8.8% w/v sodium bicarbonate;
0.5%-1.5% w/v sodium citrate;
0.1%-0.3% w/v simethicone emulsion;
0.35%-3.5% w/v sweetener;
0.4%-0.6% w/v benzyl alcohol; and
water.
24. A kit consisting essentially of:
a first container having a 100% w/w omeprazole powder;
a second container having a liquid diluent consisting essentially of poloxamer 188, sodium carboxymethylcellulose (CMC), sodium bicarbonate, sodium citrate, simethicone emulsion, benzyl alcohol, a sweetener, and water;
wherein the liquid diluent is stable for at least 30 days and is resistant to gel formation for at least one freeze-thaw cycle,
wherein the first and second containers are of a size such that the omeprazole powder and liquid diluent can be combined in either the first or second container to produce a reconstituted omeprazole suspension;
wherein the reconstituted omeprazole suspension is homogenous and stable for at least 30 days at ambient and refrigerated temperature conditions.
25. The kit of claim 24 , wherein the percent of omeprazole powder dissolved to make the reconstituted omeprazole suspension is >80% by dissolution assay after 5 minutes of mixing.
26. The kit of claim 24 , wherein the poloxamer 188 is present in the reconstituted omeprazole suspension at 1.0%-4.0% w/v and the sodium CMC is present in the reconstituted omeprazole suspension at 1.0%-2.0% w/v.
27. The kit of claim 24 , wherein the diluent consists essentially of:
1.0% w/v of poloxamer 188;
1.2% w/v sodium CMC;
8.4% w/v sodium bicarbonate;
1.0% w/v sodium citrate;
0.5% w/v benzyl alcohol; and
0.15% w/v simethicone emulsion.
28. The kit of claim 24 , wherein the sweetener comprises 2.5% w/v sorbitol solution (70%) and 0.4% w/v sucralose.