Emulsion compostions for the parenteral administration of sparingly water soluble ionizable hydrophobic drugs

Claim 2

A composition of matter for delivery by hydrophobic drugs comprising: (a) a hydrophobic drug; (b) an oleaginous vehicle or oil phase said oleaginous vehicle or oil phase being substantially free of BHT or BHA; (c) a co-surfactant or emulsifier; (d) a co-surfactant or auxiliary emulsifier; and (e) benzyl alcohol as a co-solvent; wherein the hydrophobic drug may be a sparingly water liquid and may be a basic drug which has an ionization constant lower or nearer the physiological pH or an acid drug which has an ionization constant higher or nearer the physiological pH.

Claim 3

The composition of matter as recited in claim 1 comprising: ______________________________________ Percent Ingredient Range W/V ______________________________________ Hydrophobic drug .001-1.0 Triglycerol Pentaoleate 5.0-20.0 Benzyl Alcohol 0.2-4.0 Sesame Oil 1.6-10.0 Soy or Egg Lecithin 0.4-1.6 dl-α-Tocopherol 0.0-0.1 Glycerine U.S.P. 2.0-4.5 Water for injection qs ad 100. ______________________________________

Claim 4

The composition of matter as recited in claim 1 comprising: ______________________________________ Percent Ingredient Range W/V ______________________________________ Hydrophobic drug 0.001-1.0 Triglycerol Pentaoleate 0.0-10.0 Benzyl Alcohol 0.2-4.0 Sesame Oil 0.0-5.0 Soy or Egg Lecithin 0.4-1.6 Oleic Acid 0.4-1.2 Hexanoic Acid 0.0-1.0 Linolenic Acid 0.0-1.0 Soybean Oil 3.0-10.0 dl-α-Tocopherol 0.002-0.1 Polyvinylpyrrolidone 0.0-0.2 Glycerine U.S.P. 2.0-4.0 Water for injection qs ad 100. ______________________________________

Claim 5

The composition of matter as recited in claim 1 comprising: Percent ______________________________________ Ingredient Range W/V ______________________________________ Hydrophobic drug .001-1.0 Sorbitan Triisostearate or 10.0-20.0 Triglycerol Diisostearate Benzyl Alcohol 2.0-3.0 Sesame Oil 3.0-5.0 [Pluronic ® F-68] Polyethylene polypropylene 0.5-0.75 glycol Water for injection qs ad 100. ______________________________________

Claim 6

The composition of matter as recited in claim 1 comprising: ______________________________________ Ingredient Percent W/V ______________________________________ Hydrophobic drug 0.05-0.8 Triglycerol Pentaoleate 10.0-20.0 Benzyl Alcohol 2.0-4.0 Sesame Oil 5.0-10.0 Soy or Egg Lecithin 0.8-1.6 Glycerine U.S.P. 2.25 Water for injection qs ad 100. ______________________________________

Claim 7

The composition of matter as recited in claim 1 comprising: ______________________________________ Ingredient Percent W/V ______________________________________ Hydrophobic drug 0.8 Triglycerol Pentaoleate 20.0 Benzyl Alcohol 4.0 Sesame Oil 10.0 Soy Lecithin 1.6 dl-α-Tocopherol 0.1 Glycerine U.S.P. 4.5 Water for injection qs ad 100. ______________________________________

Claim 8

The composition of matter as recited in claim 1 comprising: ______________________________________ Ingredient Percent W/V ______________________________________ Hydrophobic drug 0.1 Triglycerol Pentaoleate 10.0 Benzyl Alcohol 2.0 Sesame Oil 5.0 Soy or Egg Lecithin 0.8 Oleic Acid 0.75 dl-α-Tocopherol 0.002 Glycerine U.S.P. 2.25 Water for injection qs ad 100. ______________________________________

Claim 9

The composition of matter as recited in claim 1 comprising: ______________________________________ Ingredient Percent W/V ______________________________________ Hydrophobic drug 0.2 Soybean Oil 5.0-7.0 Benzyl Alcohol 0.9 Soy Lecithin 1.0-1.2 Oleic Acid 0.4-0.7 Hexanoic Acid 0.1 Linolenic Acid 0.0-0.3 dl-α-Tocopherol 0.01 Glycerine U.S.P. 2.25 Polyvinylpyrrolidone 0.0-0.04 Water for injection qs ad 100. ______________________________________

Claim 10

The composition of matter as recited in claim 1 comprising: ______________________________________ Percent Ingredient Range W/V ______________________________________ Hydrophobic drug 0.05 Sorbitan Triisostearate or 10.0 Triglycerol Diisostearate Benzyl Alcohol 2.0-3.0 Sesame Oil 3.0-5.0 [Pluronic ® F-68] Polyethylene polypropylene 0.5-0.75 glycol Water for injection qs ad 100. ______________________________________

Claim 11

The composition of matter as recited in claim 5, in which the hydrophobic drug is bis(2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.

Claim 12

A composition in accordance with claim 4, in which the hydrophobic drug is 3-[4,6-bis[(1,1-2,2-tetramethylpropyl)amino]-s-triazin-2-yl]-3-azabicyclo[3.2.2]nonane.

Claim 13

The composition of matter as recited in claim 6, in which the hydrophobic drug is 3-[4,6-bis[(1,1-2,2-tetramethylpropyl)amino]-s-triazin-2-yl]-3-azabicyclo[3.2.2]nonane.

Claim 14

The composition of matter as recited in claim 7, in which the hydrophobic drug is bis(2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.

Claim 15

The composition of matter as recited in claim 8, in which the hydrophobic drug is bis(2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.

Claim 16

The composition of matter as recited in claim 9, in which the hydrophobic drug is bis(2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.

Claim 17

The composition of matter as recited in claim 1, which consists essentially of: ______________________________________ Percent Ingredient Range W/V ______________________________________ Hydrophobic Drug .001-1.0 Sorbitan Triisostearate or 10.0-20.0 Triglycerol Diisostearate Benzyl Alcohol 2.0-3.0 Sesame Oil 3.0-5.0 Poloxamer 0.5-0.75 Water for injection qs ad 100. ______________________________________

Claim 18

The composition of matter as recited in claim 1, which consists essentially of: ______________________________________ Ingredient Percent W/V ______________________________________ Hydrophobic Drug 0.05-0.8 Triglycerol Pentaoleate 10.0-20.0 Benzyl Alcohol 2.0-4.0 Sesame Oil 5.0-10.0 Soy or Egg Lecithin 0.8-1.6 Glycerine U.S.P. 2.25 Water for injection qs ad 100. ______________________________________

Claim 19

The composition of matter as recited in claim 1, which consists essentially of: ______________________________________ Ingredient Percent W/V ______________________________________ Hydrophobic Drug 0.8 Triglycerol Pentaoleate 20.0 Benzyl Alcohol 4.0 Sesame Oil 10.0 Soy Lecithin 1.6 dl-α-Tocopherol 0.1 Glycerine U.S.P. 4.5 Water for injection qs ad 100. ______________________________________

Claim 20

The composition of matter as recited in claim 1, which consists essentially of: ______________________________________ Ingredients Percent W/V ______________________________________ Hydrophobic Drug 0.1 Triglycerol Pentaoleate 10.0 Benzyl Alcohol 2.0 Sesame Oil 5.0 Soy or Egg Lecithin 0.8 Oleic Acid 0.75 dl-α-Tocopherol 0.002 Glycerine U.S.P. 2.25 Water for injection qs ad 100. ______________________________________

Claim 21

The composition of matter as recited in claim 1, which consits essentially of: ______________________________________ Ingredient Percent W/V ______________________________________ Hydrophobic drug 0.2 Soybean Oil 5.0-7.0 Benzyl Alcohol 0.9 Soy Lecithin 1.0-1.2 Oleic Acid 0.4-0.7 Hexanoic Acid 0.1 Linolenic Acid 0.0-0.3 dl-α-Tocopherol 0.01 Glycerine U.S.P. 2.25 Polyvinylpyrrolidone 0.0-0.04' Water for injection qs ad 100. ______________________________________

Claim 22

The composition of matter as recited in claim 1, which consists essentially of: ______________________________________ Ingredient Percent W/V ______________________________________ Hydrophobic drug 0.05 Sorbitan Triisostearate or 10.0 Triglycerol Diisostearate Benzyl Alcohol 2.0-3.0 Sesame Oil 3.0-5.0 Poloxamer 0.5-0.75 Water for injection qs ad 100. ______________________________________

Claim 23

The composition of matter as recited in claim 16, in which the hydrophobic drug is bis(2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.

Claim 24

A composition in accordance with claim 17, in which the hydrophobic drug is bis(2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.

Claim 25

The composition of matter as recited in claim 18, in which the hydrophobic drug is bis(2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.

Claim 26

The composition of matter as recited in claim 19, in which the hydrophobic drug is bis(2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.

Claim 27

The composition of matter as recited in claim 20, in which the hydrophobic drug is bis(2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.

Claim 28

The composition of matter as recited in claim 21, in which the hydrophobic drug is bis(2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.