Capsule and powder formulations containing lanthanum compounds
View Patent ↗The present invention includes an oral pharmaceutical capsule comprising a shell, lanthanum carbonate or lanthanum carbonate hydrate, and a lubricant such as talc, wherein the shell encapsulates the lanthanum carbonate or its hydrate and the lubricant. Capsule shells comprise, for example, gelatin. The present invention also includes an oral pharmaceutical powder comprising lanthanum carbonate or lanthanum carbonate hydrate and a pharmaceutically acceptable excipient. The oral pharmaceutical capsules and powders of the present invention can be administered to treat a patient at risk of or suffering from hyperphosphatemia, at risk of or suffering from chronic kidney disease (CKD), at risk of or suffering from soft tissue calcification associated with CKD, or at risk of or suffering from secondary hyperparathyroidism.
1. An oral pharmaceutical powder comprising (1) lanthanum carbonate or lanthanum carbonate hydrate, (2) crospovidone, and (3) talc, wherein a plasma lanthanum concentration of a patient after administration of the powder is similar to a plasma lanthanum concentration of the patient after administration of a chewable tablet comprising lanthanum carbonate, dextrates, colloidal silicon dioxide, and magnesium stearate.
2. The powder of claim 1 , wherein the lanthanum carbonate or lanthanum carbonate hydrate has the formula:
La 2 (CO 3 ) 3 .n H 2 O
wherein n has a value from 0 to 10.
3. The powder of claim 2 , wherein n has a value from 3 to 6.
4. The powder of claim 1 , wherein the lanthanum carbonate or lanthanum carbonate hydrate is in an amount from about 50% to about 95% by weight of the powder.
5. The powder of claim 1 , wherein the crospovidone is in an amount from about 1.0% to about 15% by weight of the powder.
6. The powder of claim 1 , wherein the talc is in an amount from about 0.01% to about 0.05% by weight of the powder.
7. The powder of claim 1 , further comprising a diluent.
8. The powder of claim 7 , wherein the diluent is dextrates.
9. The powder of claim 7 , wherein the diluent is in an amount from about 5% to about 50% by weight of the powder.
10. The powder of claim 1 , further comprising a flow aid.
11. The powder of claim 10 , wherein the flow aid is colloidal silicon dioxide.
12. The powder of claim 10 , wherein the flow aid is in an amount from about 0.1% to about 4.0% by weight of the powder.
13. The powder of claim 1 comprising (1) 86.7 wt % lanthanum carbonate hydrate, (2) 8.2 wt % dextrates, (3) 1.0 wt % colloidal silicon dioxide, (4) 4.0 wt % crospovidone, and (5) 0.025 wt % talc.
14. A method of treating hyperphosphatemia in a patient comprising administering to the patient an oral pharmaceutical powder comprising (1) lanthanum carbonate or lanthanum carbonate hydrate, (2) crospovidone, and (3) talc, wherein a plasma lanthanum concentration of the patient after administration of the powder is similar to a plasma lanthanum concentration of the patient after administration of a chewable tablet comprising lanthanum carbonate, dextrates, colloidal silicon dioxide, and magnesium stearate.
15. A method of treating a patient (1) at risk of or suffering from chronic kidney disease (CKD), (2) at risk of or suffering from soft tissue calcification associated with chronic kidney disease (CKD), or (3) at risk of or suffering from secondary hyperparathyroidism comprising administering to the patient an oral pharmaceutical powder comprising (1) lanthanum carbonate or lanthanum carbonate hydrate, (2) crospovidone, and (3) talc, wherein a plasma lanthanum concentration of the patient after administration of the powder is similar to a plasma lanthanum concentration of the patient after administration of a chewable tablet comprising lanthanum carbonate, dextrates, colloidal silicon dioxide, and magnesium stearate.
16. The method of claim 14 , wherein the crospovidone is in an amount from about 1.0% to about 15% by weight of the powder.
17. The method of claim 14 , wherein the talc is in an amount from about 0.01% to about 0.05% by weight of the powder.
18. The method of claim 14 , wherein the powder further comprises a diluent.
19. The method of claim 14 , wherein the powder further comprises a flow aid.
20. The method of claim 14 , wherein the powder comprises (1) 86.7 wt % lanthanum carbonate hydrate, (2) 8.2 wt % dextrates, (3) 1.0 wt % colloidal silicon dioxide, (4) 4.0 wt % crospovidone, and (5) 0.025 wt % talc.