Compressed tablet formulation
View Patent ↗This invention relates to a 50% drug loaded compressed tablet formulation for efavirenz. Efavirenz is a non-nucleoside reverse trancriptase inhibitor being studied clinically for use in the treatment of HIV infections and AIDS.
1. A compressed tablet comprising: efavirenz, filler/disintegrant, superdisintegrant, binder, surfactant, filler/compression aid, lubricant, and solvent, wherein efavirenz is about 50% by weight of the total composition of the compressed tablet, the superdisintegrant has a concentration in the tablet between about 1% to about 5% by weight, and the superdisintegrant is croscarmellose sodium.
2. The compressed tablet as recited in claim 1 , wherein:
the solvent comprises water, ethanol or mixtures thereof;
the filler/disintegrant is microcrystalline cellulose;
the binder is hydroxypropyl cellulose;
the surfactant is sodium lauryl sulfate;
the filler/compression aid is lactose hydrous spray dried; and
the lubricant is magnesium stearate.
3. The compressed tablet as recited in claim 2 , wherein the efavirenz is crystalline.
4. The compressed tablet as recited in claim 2 , wherein the croscarmellose sodium is about 5% by weight of the total composition of the compressed tablet.
5. The compressed tablet as recited in claim 1 , comprising efavirenz, microcrystalline cellulose NF, hydroxypropyl cellulose LF NF, croscarmellose sodium, sodium lauryl sulfate, lactose hydrous spray dried (EG), and magnesium stearate (EG).
6. The compressed tablet, as recited in claim 5 , containing about 300 mg of efavirenz, about 120 mg microcrystalline cellulose NF, about 19.2 mg hydroxypropyl cellulose LF NF, about 30 mg croscarmellose sodium, about 6 mg sodium lauryl sulfate, about 118.8 mg lactose hydrous spray dried (EG), and about 6 mg magnesium stearate (EG).
7. A compressed tablet comprising: efavirenz, filler/disintegrant, superdisintegrant, binder, surfactant, filler/compression aid, lubricant, and solvent; wherein efavirenz is about 50% by weight of the total composition of the compressed tablet, and the superdisintegrant has a concentration in the tablet between about 1% to about 5% by weight; and wherein the compressed tablet is prepared via wet granulation in which efavirenz, filler/disintegrant, superdisintegrant, binder, and surfactant are blended intragranularly, and filler/compression aid and lubricant are added extragranularly; and wherein the superdisintegrant is croscarmellose sodium.
8. The compressed tablet as recited in claim 7 , wherein:
the solvent comprises water, ethanol or mixtures thereof;
the filler/disintegrant is microcrystalline cellulose;
the binder is hydroxypropyl cellulose;
the surfactant is sodium lauryl sulfate;
the filler/compression aid is lactose hydrous spray dried; and
the lubricant is magnesium stearate.
9. The compressed tablet as recited in claim 8 , wherein the efavirenz is crystalline.
10. The compressed tablet as recited in claim 8 , wherein the croscarmellose sodium is about 5% by weight of the total composition of the compressed tablet.
11. The compressed tablet as recited in claim 2 , wherein efavirenz is present in an amount of about 300 mg.
12. The compressed tablet as recited in claim 2 , wherein efavirenz is present in an amount of about 600 mg.
13. The compressed tablet as recited in claim 8 , wherein efavirenz is present in an amount of about 300 mg.
14. The compressed tablet as recited in claim 8 , wherein efavirenz is present in an amount of about 600 mg.