Pharmaceutical formulations containing dopamine receptor ligands

Abstract

The present invention relates to stable and bioavailable immediate release formulations comprising dopamine receptor ligands. Methods of treating various disorders by administering the formulations are also described.

We claim: 
     
       1. A method of treating a condition selected from the group consisting of schizophrenia, bipolar disorder, acute mania, and depression comprising administering to a patient in need thereof a solid oral dosage form comprising between about 0.5% and about 15% of cariprazine or a pharmaceutically acceptable salt thereof, an excipient having low water activity selected from the group consisting of pregelatinized starch, mannitol, anhydrous calcium hydrogen phosphate, and mixtures thereof, and between about 0.1% and about 0.5% less than 0.5% of trans-4-[2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl]-cyclohexyl-amine or a pharmaceutically acceptable salt thereof; wherein the formulation has a pH in the range of about 9.0 to about 12.0. 
     
     
       2. The method of  claim 1 , wherein the solid oral dosage form comprises cariprazine or a pharmaceutically acceptable salt thereof in an amount from about 0.5 mg to about 15 mg. 
     
     
       3. The method of  claim 1 , wherein the solid oral dosage form comprises cariprazine or a pharmaceutically acceptable salt thereof in an amount from about 1 mg to about 12 mg. 
     
     
       4. The method of  claim 1 , wherein the solid oral dosage form comprises magnesium stearate. 
     
     
       5. The method of  claim 1 , wherein the excipient having a low water activity pregelatinized starch is present in an amount greater than 80% by weight of the solid oral dosage form. 
     
     
       6. The method of  claim 1 , wherein the solid oral dosage form comprises a compound that modulates the pH environment of the composition solid oral dosage form in an amount between about 1% by weight and 15% by weight of the composition solid oral dosage form. 
     
     
       7. The method of  claim 1 , wherein the solid oral dosage form has a dissolution rate of more than about 80% within about the first 60 minutes following administration of the solid oral dosage form to the patient. 
     
     
       8. The method of  claim 1 , wherein the excipient comprises pregelatinized starch. 
     
     
       9. The method of  claim 1 , wherein the excipient comprises mannitol. 
     
     
       10. The method of  claim 1 , wherein the excipient comprises anhydrous calcium hydrogen phosphate. 
     
     
       11. The method of claim 1, wherein the solid oral dosage form comprises less than 0.1% of trans-4-[2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl]-cyclohexyl-amine or a pharmaceutically acceptable salt thereof.