High Surface-Area Lyophilized Compositions Comprising Arsenic For Oral Administration In Patients

Abstract

The present invention relates to treating malignancies such as tumors or cancers by orally administering lyophilized compositions comprising arsenic to a subject in such need. Malignancies include various hematological malignancies, such as acute myeloid leukemia (AML) including acute promyelocytic leukemia (APL), myelodysplastic syndrome (MDS), multiple myeloma (MM) and lymphomas and solid tumors including glioblastoma multiforme and breast cancer. This invention relates to a novel formulation comprising a lyophilized compositions comprising arsenic. The present invention also relates to a method for lyophilizing the arsenic trioxide, preparing the oral formulation comprising lyophilized compositions comprising arsenic, and a method for treating a subject with malignancies using the oral formulation.

What is claimed: 
     
         1 . A method for preparing an oral pharmaceutical formulation comprising a lyophilized composition comprising arsenic or lyophilized arsenic trioxide (As 2 O 3 ), said method comprising:
 (A) solubilizing As 2 O 3  powder in an aqueous medium to form an As 2 O 3  solution;   (B) lyophilizing said As 2 O 3  solution to generate a lyopremix;   (C) sifting said lyopremix to generate lyophilized As 2 O 3  powder;   (D) optionally, adding at least one bulking agent to said lyophilized As 2 O 3  powder;   (E) optionally, adding one or more lubricants to said lyophilized As 2 O 3  powder to generate said oral formulation of As 2 O 3 .   
     
     
         2 . A pharmaceutical composition in a solid dosage form suitable for oral administration, said composition comprising lyophilized composition comprising arsenic. 
     
     
         3 . A method of treating a cancer in a patient in need thereof, comprising the step of administering to the patient a therapeutically effective amount of a pharmaceutical composition comprising lyophilized composition comprising arsenic.