Dispersible compositions
The present invention is concerned with dispersible compositions comprising rilpivirine or a pharmaceutically acceptable acid addition salt thereof as an active ingredient. Such compositions are useful in the treatment of HIV infection and their dispersibility properties lend themselves to be useful in particular amongst the pediatric or geriatric population.
1. A composition having a granular fraction and an extragranular fraction, wherein the fractions comprise the following ingredients by weight based on the total weight of the composition:
Granular Fraction
2.75 mg of rilpivirine HCl;
1% to 8% of a diluent;
0.01 to 2.5% of a wetting agent;
0 to 10% of a binder; and
0.1% to 5% of a disintegrant; and
Extragranular Fraction
35% to 87% of microcrystalline cellulose;
1% to 5% of a disintegrant;
0.01 to 2.5% of a wetting agent; and
0 to 5% of a lubricant.
2. The composition according to claim 1 wherein the granular fraction comprises up to 50% by weight of the total weight of the composition.
3. The composition according to claim 2 wherein the granular fraction comprises between 5 and 20% by weight of the composition.
4. The composition according to claim 1 wherein the extragranular fraction comprises up to 95% by weight of the total weight of the composition.
5. The composition according to claim 4 wherein the extragranular fraction comprises between 50 and 95% by weight of the composition.
6. The composition according to claim 1 having the following composition:
Granular Fraction
2.75 mg rilpivirine HCl; and
lactose monohydrate; and
croscarmellose sodium; and
polyvinylpyrrolidone; and
Polysorbate 20;
Total: 8.73 mg; and
Extragranular Fraction
mannitol; and
microcrystalline cellulose; and
sodium lauryl sulfate; and
croscarmellose sodium;
sodium stearyl fumarate;
Total: 100 mg.