Fospropofol formulations

Abstract

The present disclosure provides pharmaceutical compositions for oral administration of fospropofol, or pharmaceutically acceptable salts of fospropofol, as well as methods of oral administration of fospropofol.

1 . A pharmaceutical dosage form for oral administration, comprising fospropofol, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable acid, wherein the mole ratio of fospropofol, or a pharmaceutically acceptable salt thereof, to the pharmaceutically acceptable acid is 3:1 or less; and wherein oral administration of the dosage form to a subject results in a plasma fospropofol Cmax (fed) that is at least 30% of the corresponding plasma fospropofol Cmax (fasted). 
     
     
         2 . The pharmaceutical dosage form for oral administration according to  claim 1 , wherein oral administration of the dosage form to a subject results in a plasma fospropofol Cmax (fed) that is at least 90% of the corresponding plasma fospropofol Cmax (fasted). 
     
     
         3 . The pharmaceutical dosage form according to  claim 1 , wherein the pharmaceutically acceptable acid is ascorbic acid, citric acid, malic acid, or tartaric acid. 
     
     
         4 . The pharmaceutical dosage form according to  claim 1 , wherein the pharmaceutically acceptable acid is ascorbic acid. 
     
     
         5 . The pharmaceutical dosage form according to  claim 1 , wherein the pharmaceutically acceptable acid is tartaric acid. 
     
     
         6 . The pharmaceutical dosage form according to  claim 1 , wherein the pharmaceutically acceptable acid is citric acid. 
     
     
         7 . The pharmaceutical dosage form according to  claim 1 , wherein the pharmaceutically acceptable acid is malic acid. 
     
     
         8 . The pharmaceutical dosage form according to  claim 1 , wherein said subject is a human. 
     
     
         9 . The pharmaceutical dosage form according to  claim 1 , wherein the mole ratio of fospropofol, or a pharmaceutically acceptable salt thereof, to the pharmaceutically acceptable acid is 2:1 or less. 
     
     
         10 . The pharmaceutical dosage form according to  claim 1 , wherein the mole ratio of fospropofol, or a pharmaceutically acceptable salt thereof, to the pharmaceutically acceptable acid is 1.5:1 or less. 
     
     
         11 . A pharmaceutical dosage form for oral administration, comprising fospropofol, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable acid, wherein the mole ratio of fospropofol, or a pharmaceutically acceptable salt thereof, to the pharmaceutically acceptable acid is 3:1 or less; and wherein oral administration of the dosage form to a subject results in a plasma total fospropofol AUC ∞  (fed) that is at least 40% of the corresponding plasma total fospropofol AUC ∞  (fasted). 
     
     
         12 . The pharmaceutical dosage form according to  claim 11 , wherein the administration results in a plasma total fospropofol AUC ∞  (fed) that is at least 70% of the corresponding plasma total fospropofol AUC ∞  (fasted). 
     
     
         13 . The pharmaceutical dosage form according to  claim 11 , wherein the pharmaceutically acceptable acid is ascorbic acid, citric acid, malic acid, or tartaric acid. 
     
     
         14 . The pharmaceutical dosage form according to  claim 11 , wherein the pharmaceutically acceptable acid is ascorbic acid. 
     
     
         15 . The pharmaceutical dosage form according to  claim 11 , wherein the pharmaceutically acceptable acid is tartaric acid. 
     
     
         16 . The pharmaceutical dosage form according to  claim 11 , wherein the pharmaceutically acceptable acid is citric acid. 
     
     
         17 . The pharmaceutical dosage form according to  claim 11 , wherein pharmaceutically acceptable acid is malic acid. 
     
     
         18 . The pharmaceutical dosage form according to  claim 11 , wherein said subject is a human. 
     
     
         19 . The pharmaceutical dosage form according to  claim 11 , wherein the mole ratio of fospropofol, or a pharmaceutically acceptable salt thereof, to the pharmaceutically acceptable acid is 2:1 or less. 
     
     
         20 . The pharmaceutical dosage form according to  claim 11 , wherein the mole ratio of fospropofol, or a pharmaceutically acceptable salt thereof, to the pharmaceutically acceptable acid is 1.5:1 or less.