Formulations of 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione

Abstract

Pharmaceutical compositions and single unit dosage forms of 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione, or a pharmaceutically acceptable stereoisomer, prodrug, salt, solvate, hydrate, or clathrate, are provided herein. Also provided are methods of treating, managing, or preventing various disorders, such as cancer or an inflammatory disease.

What is claimed is: 
     
         1 . An oral dosage form which weighs about 62.5 mg and comprises: 1) pomolidomide, or a pharmaceutically acceptable salt or solvate thereof, at an amount that provides 0.5 mg potency of pomolidomide; and 2) a pharmaceutically acceptable carrier or excipient. 
     
     
         2 . The dosage form of  claim 1 , wherein the carrier or excipient comprises starch. 
     
     
         3 . The dosage form of  claim 2 , wherein the starch is pregelatinized starch. 
     
     
         4 . The dosage form of  claim 3 , wherein the pregelatinized starch is present at an amount of about 35 mg. 
     
     
         5 . The dosage form of  claim 1 , wherein the carrier or excipient comprises sodium stearyl fumarate. 
     
     
         6 . The dosage form of  claim 5 , wherein the sodium stearyl fumarate is present at an amount of about 0.16 mg. 
     
     
         7 . The dosage form of  claim 1 , wherein the carrier or excipient comprises mannitol. 
     
     
         8 . The dosage form of  claim 7 , wherein the mannitol is spray dried mannitol. 
     
     
         9 . The dosage form of  claim 8 , wherein the spray dried mannitol is present at an amount that brings the total weight of the composition to about 62.5 mg. 
     
     
         10 . The dosage form of  claim 1 , which is to be administered in the form of a size 4 or larger capsule. 
     
     
         11 . An oral dosage form which weighs about 125 mg and comprises: 1) pomolidomide, or a pharmaceutically acceptable salt or solvate thereof, at an amount that provides 1 mg potency of pomolidomide; and 2) a pharmaceutically acceptable carrier or excipient. 
     
     
         12 . The dosage form of  claim 11 , wherein the carrier or excipient comprises starch. 
     
     
         13 . The dosage form of  claim 12 , wherein the starch is pregelatinized starch. 
     
     
         14 . The dosage form of  claim 13 , wherein the pregelatinized starch is present at an amount of about 70 mg. 
     
     
         15 . The dosage form of  claim 11 , wherein the carrier or excipient comprises sodium stearyl fumarate. 
     
     
         16 . The dosage form of  claim 15 , wherein the sodium stearyl fumarate is present at an amount of about 0.32 mg. 
     
     
         17 . The dosage form of  claim 11 , wherein the carrier or excipient comprises mannitol. 
     
     
         18 . The dosage form of  claim 17 , wherein the mannitol is spray dried mannitol. 
     
     
         19 . The dosage form of  claim 18 , wherein the spray dried mannitol is present at an amount that brings the total weight of the composition to about 125 mg. 
     
     
         20 . The dosage form of  claim 11 , which is to be administered in the form of a size 4 or larger capsule. 
     
     
         21 . An oral dosage form which weighs about 250 mg and comprises: 1) pomolidomide, or a pharmaceutically acceptable salt or solvate thereof, at an amount that provides 2 mg potency of pomolidomide; and 2) a pharmaceutically acceptable carrier or excipient. 
     
     
         22 . The dosage form of  claim 21 , wherein the carrier or excipient comprises starch. 
     
     
         23 . The dosage form of  claim 22 , wherein the starch is pregelatinized starch. 
     
     
         24 . The dosage form of  claim 23 , wherein the pregelatinized starch is present at an amount of about 140 mg. 
     
     
         25 . The dosage form of  claim 21 , wherein the carrier or excipient comprises sodium stearyl fumarate. 
     
     
         26 . The dosage form of  claim 25 , wherein the sodium stearyl fumarate is present at an amount of about 0.64 mg. 
     
     
         27 . The dosage form of  claim 21 , wherein the carrier or excipient comprises mannitol. 
     
     
         28 . The dosage form of  claim 27 , wherein the mannitol is spray dried mannitol. 
     
     
         29 . The dosage form of  claim 28 , wherein the spray dried mannitol is present at an amount that brings the total weight of the composition to about 250 mg. 
     
     
         30 . The dosage form of  claim 21 , which is to be administered in the form of a size 2 or larger capsule. 
     
     
         31 . An oral dosage form which weighs about 180 mg and comprises: 1) pomolidomide, or a pharmaceutically acceptable salt or solvate thereof, at an amount that provides 3 mg potency of pomolidomide; and 2) a pharmaceutically acceptable carrier or excipient. 
     
     
         32 . The dosage form of  claim 31 , wherein the carrier or excipient comprises starch. 
     
     
         33 . The dosage form of  claim 32 , wherein the starch is pregelatinized starch. 
     
     
         34 . The dosage form of  claim 33 , wherein the pregelatinized starch is present at an amount of about 100 mg. 
     
     
         35 . The dosage form of  claim 31 , wherein the carrier or excipient comprises sodium stearyl fumarate. 
     
     
         36 . The dosage form of  claim 35 , wherein the sodium stearyl fumarate is present at an amount of about 0.45 mg. 
     
     
         37 . The dosage form of  claim 31 , wherein the carrier or excipient comprises mannitol. 
     
     
         38 . The dosage form of  claim 37 , wherein the mannitol is spray dried mannitol. 
     
     
         39 . The dosage form of  claim 38 , wherein the spray dried mannitol is present at an amount that brings the total weight of the composition to about 180 mg. 
     
     
         40 . The dosage form of  claim 31 , which is to be administered in the form of a size 2 or larger capsule. 
     
     
         41 . An oral dosage form which weighs about 240 mg and comprises: 1) pomolidomide, or a pharmaceutically acceptable salt or solvate thereof, at an amount that provides 4 mg potency of pomolidomide; and 2) a pharmaceutically acceptable carrier or excipient. 
     
     
         42 . The dosage form of  claim 41 , wherein the carrier or excipient comprises starch. 
     
     
         43 . The dosage form of  claim 42 , wherein the starch is pregelatinized starch. 
     
     
         44 . The dosage form of  claim 43 , wherein the pregelatinized starch is present at an amount of about 135 mg. 
     
     
         45 . The dosage form of  claim 41 , wherein the carrier or excipient comprises sodium stearyl fumarate. 
     
     
         46 . The dosage form of  claim 45 , wherein the sodium stearyl fumarate is present at an amount of about 0.6 mg. 
     
     
         47 . The dosage form of  claim 41 , wherein the carrier or excipient comprises mannitol. 
     
     
         48 . The dosage form of  claim 47 , wherein the mannitol is spray dried mannitol. 
     
     
         49 . The dosage form of  claim 48 , wherein the spray dried mannitol is present at an amount that brings the total weight of the composition to about 240 mg. 
     
     
         50 . The dosage form of  claim 41 , which is to be administered in the form of a size 2 or larger capsule. 
     
     
         51 . An oral dosage form which weighs about 300 mg and comprises: 1) pomolidomide, or a pharmaceutically acceptable salt or solvate thereof, at an amount that provides 5 mg potency of pomolidomide; and 2) a pharmaceutically acceptable carrier or excipient. 
     
     
         52 . The dosage form of  claim 51 , wherein the carrier or excipient comprises starch. 
     
     
         53 . The dosage form of  claim 52 , wherein the starch is pregelatinized starch. 
     
     
         54 . The dosage form of  claim 53 , wherein the pregelatinized starch is present at an amount of about 168 mg. 
     
     
         55 . The dosage form of  claim 51 , wherein the carrier or excipient comprises sodium stearyl fumarate. 
     
     
         56 . The dosage form of  claim 55 , wherein the sodium stearyl fumarate is present at an amount of about 0.75 mg. 
     
     
         57 . The dosage form of  claim 51 , wherein the carrier or excipient comprises mannitol. 
     
     
         58 . The dosage form of  claim 57 , wherein the mannitol is spray dried mannitol. 
     
     
         59 . The dosage form of  claim 58 , wherein the spray dried mannitol is present at an amount that brings the total weight of the composition to about 300 mg. 
     
     
         60 . The dosage form of  claim 51 , which is to be administered in the form of a size 1 or larger capsule.