Compositions comprising short-acting benzodiazepines

A lyophilized or spray-dried composition comprising at least one benzodiazepine according to formula (I)

• with
• W is H;
• X is CH2;
• n is 1;
• Y is CH2;
• m is 1;
• Z is O;
• p is 0 or 1;
• R1 is CH3, CH2CH3, CH2CH2CH3, CH(CH3)2 or CH2CH(CH3)2;
• R2 is 2-fluorophenyl, 2-chlorophenyl or 2-pyridyl;
• R3 is Cl or Br;
• R4, R5 and R6 form the group-CR8═U—V═ wherein R8 is hydrogen, C1-4 alkyl or C1-3 hydroxyalkyl, U is N or CR9 wherein R9 is H, C1-4 alkyl, C1-3 hydroxyalkyl or C1-4 alkoxy, V is N or CH and p is zero
• or a pharmaceutically acceptable salt thereof, wherein the composition
• comprises at least one pharmaceutically acceptable hygroscopic excipient, wherein the hygroscopic excipient is a carbohydrate selected from the group consisting of disaccharides and dextran.

A stable lyophilized or stable freeze-dried composition comprising at least one benzodiazepine according to formula (I)

• with
• W is H;
• X is CH2;
• n is 1;
• Y is CH2;
• m is 1;
• Z is O;
• p is 0 or 1;
• R1 is CH3, CH2CH3, CH2CH2CH3, CH(CH3)2 or CH2CH(CH3)2;
• R2 is 2-fluorophenyl, 2-chlorophenyl or 2-pyridyl;
• R3 is Cl or Br;
• R4, R5 and R6 form the group-CR8═U—V═ wherein R8 is hydrogen, C1-4 alkyl or C1-3 hydroxyalkyl, U is N or CR9 wherein R9 is H, C1-4 alkyl, C1-3 hydroxyalkyl or C1-4 alkoxy, V is N or CH and p is zero.
• or a pharmaceutically acceptable salt thereof, wherein the composition comprises at least one pharmaceutically acceptable hygroscopic excipient, wherein the hygroscopic excipient is a carbohydrate.

A composition comprising at least one benzodiazepine according to formula (I)

• with
• W is H;
• X is CH2;
• n is 1;
• Y is CH2;
• m is 1;
• Z is O;
• p is 0 or 1;
• R1 is CH3, CH2CH3, CH2CH2CH3, CH(CH3)2 or CH2CH(CH3)2;
• R2 is 2-fluorophenyl, 2-chlorophenyl or 2-pyridyl;
• R3 is Cl or Br;
• R4, R5 and R6 form the group-CR8═U—V═ wherein R8 is hydrogen, C1-4 alkyl or C1-3 hydroxyalkyl, U is N or CR9 wherein R9 is H, C1-4 alkyl, C1-3 hydroxyalkyl or C1-4 alkoxy, V is N or CH and p is zero.
• or a pharmaceutically acceptable salt thereof, wherein the composition comprises at least one pharmaceutically acceptable hygroscopic excipient, wherein the hygroscopic excipient is a carbohydrate.