Novel pharmaceutical forms, and methods of making and using the same

Abstract

Crystalline salts, polymorphs, solvates, and hydrates of bicalutamide, 5-fluorouracil, donepezil, anastrozole, nelfinavir, mirtazapine, lansoprazole, and tamsulosin, or derivatives thereof are provided by the subject invention. Methods of making and using the same are also provided.

What is claimed is: 
     
         1 . A bicalutamide, donepezil, nelfinavir, or tamsulosin salt made by reacting bicalutamide, donepezil, nelfinavir, or tamsulosin with an organic or inorganic acid in a crystallization solvent, wherein the form has an aqueous solubility of approximately 5 micrograms/mL to approximately 100 mg/mL. 
     
     
         2 . The bicalutamide, donepezil, nelfinavir, or tamsulosin salt of  claim 1 , comprising an (R)-tamsulosin HCl salt that is crystallized in a crystallization solvent comprising methanol. 
     
     
         3 . The bicalutamide, donepezil, nelfinavir, or tamsulosin salt of  claim 1 , comprising a nelfinavir HCl salt that is crystallized in a crystallization solvent comprising propylene glycol. 
     
     
         4 . The bicalutamide, donepezil, nelfinavir, or tamsulosin salt of  claim 1 , wherein the mole ratio of bicalutamide, donepezil, nelfinavir, tamsulosin, or a derivative thereof to the salt forming component is about M:N, wherein M is an integer from 1 to 100 and N is an integer from 1 to 100. 
     
     
         5 . The bicalutamide, donepezil, nelfinavir, or tamsulosin salt of  claim 4 , wherein M is an integer from 1 to 20 and N is an integer from 1 to 20. 
     
     
         6 . The bicalutamide, donepezil, nelfinavir, or tamsulosin salt of  claim 1 , wherein the salt is crystalline. 
     
     
         7 . The bicalutamide, donepezil, nelfinavir, or tamsulosin salt of  claim 1 , wherein said tamsulosin salt is a (R)-tamsulosin salt comprising (R)-tamsulosin HCl. 
     
     
         8 . The (R)-tamsulosin salt of  claim 7 , wherein:
 (a) the salt exhibits crystal parameters that are approximately equal to the following:
 Monoclinic, P2(1), a=7.5499(13) Å, b=9.1496(15) Å, c=31.755(5) Å, β=93.158(3)°, V=2190.2(6) Å 3 , Z=4; or 
   (b) the salt is characterized by a melting point at about 228-230 degrees C.   
     
     
         9 . The (R)-tamsulosin salt of  claim 8 , wherein the form is crystallized in a crystallization solvent comprising methanol. 
     
     
         10 . The bicalutamide, donepezil, nelfinavir, or tamsulosin salt of  claim 1 , whereub saud bekfubavur salt is a nelfinavir salt comprising nelfinavir HCl. 
     
     
         11 . The nelfinavir salt of  claim 10 , wherein the salt exhibits crystal parameters that are approximately equal to the following: Orthorhombic, P212121, a=10.7998(11) Å, b=10.9951(11) Å, c=26.198(3) Å, alpha=90 degrees, beta=90 degrees, gamma=90 degrees, V=3110.9(5) Å 3 , Z=4. 
     
     
         12 . The nelfinavir salt of  claim 11 , wherein the form is crystallized in a crystallization solvent comprising propylene glycol. 
     
     
         13 . A bicalutamide, 5-fluorouracil, donepezil, nelfinavir, or tamsulosin polymorph formed by the crystallization of bicalutamide, 5-fluorouracil, donepezil, nelfinavir, or tamsulosin in an appropriate solvent, wherein the polymorph has an aqueous solubility of at least about 100 micro grams/mL. 
     
     
         14 . The bicalutamide, 5-fluorouracil, donepezil, nelfinavir, or tamsulosin polymorph of  claim 13 , wherein the polymorph is formed by the crystallization of bicalutamide, 5-fluorouracil, donepezil, nelfinavir, or tamsulosin in a crystallization solvent comprising an organic or inorganic solvent. 
     
     
         15 . The bicalutamide, 5-fluorouracil, donepezil, nelfinavir, or tamsulosin polymorph of  claim 13 , wherein the polymorph is formed by the crystallization of bicalutamide, 5-fluorouracil, donepezil, nelfinavir, or tamsulosin in a crystallization solvent comprising an one or more alcohols. 
     
     
         16 . The bicalutamide, 5-fluorouracil, donepezil, nelfinavir, or tamsulosin polymorph of  claim 13 , wherein the polymorph is formed by the crystallization of bicalutamide, 5-fluorouracil, donepezil, nelfinavir, or tamsulosin in a crystallization solvent comprising methanol. 
     
     
         17 . The bicalutamide, 5-fluorouracil, donepezil, nelfinavir, or tamsulosin polymorph of  claim 13 , wherein the polymorph is formed by the crystallization of bicalutamide, 5-fluorouracil, donepezil, nelfinavir, or tamsulosin in a crystallization solvent comprising dimethyl sulfoxide. 
     
     
         18 . The bicalutamide, 5-fluorouracil, donepezil, nelfinavir, or tamsulosin polymorph of  claim 13 , wherein the polymorph is formed by the crystallization of bicalutamide, 5-fluorouracil, donepezil, nelfinavir, or tamsulosin in a crystallization solvent comprising ethanol. 
     
     
         19 . The bicalutamide, 5-fluorouracil, donepezil, nelfinavir, or tamsulosin polymorph of  claim 13 , wherein the polymorph is formed by the crystallization of bicalutamide, 5-fluorouracil, donepezil, nelfinavir, or tamsulosin in a crystallization solvent comprising chloroform. 
     
     
         20 . The bicalutamide, 5-fluorouracil, donepezil, nelfinavir, or tamsulosin polymorph of  claim 13 , wherein the polymorph is formed by the crystallization of bicalutamide, 5-fluorouracil, donepezil, nelfinavir, or tamsulosin in a crystallization solvent comprising ethylenediamine.