Particulate materials
View Patent ↗A particulate coformulation, each particle comprising a core of an active substance surrounded by an excipient coating, the particles having a volume mean diameter of 10 μm or less, which on oral administration releases the active substance at a rate such that the time (T max ) taken to attain the maximum active concentration in the bloodstream is one hour or less. The coformulation may be made using a Nektar™ SCF particle formation process.
1. A particulate coformulation of an active substance and an excipient, each particle comprising a core of the active substance surrounded by a coating of the excipient, the particles having a volume mean particle diameter of 10 μm or less, wherein the active substance has an amorphous form and the particlulate coformulation, on oral administration to a human or animal patient, has an active substance release rate such that a maximum concentration of the active substance in the human or animal patient's bloodstream is attained in about one hour or less and wherein the active substance is stable, with respect to reversion to its crystalline form at least 12 months following its coformulation with the excipient.
2. The particulate coformulation according to claim 1 , wherein the volume mean particle diameter is about 5 μm or less.
3. The particulate coformulation according to claim 1 , wherein a volume mean diameter of any agglomerates present is less than about 40 μm.
4. The particulate coformulation according to claim 1 , wherein the excipient concentration is from about 30% w/w to about 70% w/w.
5. The particulate coformulation according to claim 1 , which contains less than about 1000 ppm residual solvent.
6. The particulate coformulation according to claim 1 , wherein the active substance is a non-steroidal anti-inflammatory drug.
7. The particulate coformulation according to claim 6 , wherein the active substance is diclofenac.
8. The particulate coformulation according to claims 1 , wherein the active substance is fexofenadine.
9. The particulate coformulation according to claim 1 , which has been made by co-precipitating the active substance and the excipient from a common solvent or solvent mixture using a compressed fluid anti-solvent.
10. The particulate coformulation according to claim 9 , which has been made by co-precipitating the active substance and the exciplent by contacting a solution or suspension comprising a fluid vehicle, the active substance, and the excipient with the compressed fluid anti-solvent under conditions which allow the anti-solvent to simultaneously disperse the solution or suspension and to extract the fluid vehicle from the solution or suspension so as to cause particles of the coformulated active substance and excipient to precipitate.
11. The particulate coformulation according to claim 9 , wherein after co-precipitating the active substance and the excipient, the particulate coformulation comprises about 2000 ppm or less of the common solvent or solvent mixture.
12. A pharmaceutical or nutraceutical composition comprising the particulate coformulation according to claim 1 .
13. The pharmaceutical composition according to claim 12 , wherein in the particulate coformulation the active substance is a non-steroidal anti-inflammatory drug, and wherein the composition further comprises a prostaglandin.
14. The pharmaceutical composition according to claim 13 , wherein the active substance in the particulate coformulation is diclofenac and wherein the prostaglandin is misoprostol.