Tablets comprising 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde
Provided herein are high strength/high drug load tablets comprising 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde (“Compound 1”), dispersible tablets comprising Compound 1, processes of manufacturing such tablets, and methods for treating patients with the tablets. Compound 1 is useful for treating hematological disorders such as sickle cell disease, pulmonary disease such as idiopathic pulmonary fibrosis, and hypoxia and hypoxemia conditions.
1. A tablet comprising:
(i) about 50% to about 70% by weight of Compound 1 of formula:
(ii) about 30% to about 40% by weight of microcrystalline cellulose;
(iii) about 0.25% to about 3% by weight of croscarmellose sodium;
(iv) about 1% to about 5% by weight of magnesium stearate;
(v) about 0.5% to about 2.5% of sodium lauryl sulfate; and
(vi) about 0.25% to about 5% by weight of colloidal silicon dioxide;
wherein the percentage by weight is relative to the total weight of the tablet.
2. The tablet of claim 1 , comprising:
(i) about 35% by weight of microcrystalline cellulose;
(ii) about 1.25% by weight of croscarmellose sodium;
(iii) about 2% by weight of magnesium stearate; and
(iv) about 1.5% by weight of sodium lauryl sulfate.
3. The tablet of claim 1 , wherein the tablet comprises from about 300 to about 900 mg of Compound 1.
4. The tablet of claim 1 , comprising about 60% by weight of Compound 1.
5. The tablet of claim 1 , comprising about 35% by weight of microcrystalline cellulose.
6. The tablet of claim 1 , comprising about 1.25% by weight of croscarmellose sodium.
7. The tablet of claim 1 , comprising about 2% magnesium stearate.
8. The tablet of claim 1 , comprising about 1.5% of sodium lauryl sulfate.
9. The tablet of claim 1 , wherein the tablet comprises from about 100 to about 600 mg of Compound 1.