Emulsion compositions for administration of sparingly water soluble ionizable hydrophobic drugs

Claim 2

A composition of matter for delivery by intravenous, intramuscular or intraarticular routes of hydrophobic drugs comprising: (a) a hydrophobic drug; (b) a pharmaceutically acceptable oleaginous vehicle or oil selected from the group consisting of (i) naturally occurring vegetable oils and (ii) semisynthetic mono, di or triglycerides said oil or oleaginous vehicle being free of BHT or BHA; (c) a surfactant or emulsifier; (d) a co-surfactant or auxiliary emulsifier; (e) an ion-pair former selected from C 6 -C 20 saturated or unsaturated aliphatic or aromatic acids when the hydrophobic drug is basic and a pharamaceutically acceptable aliphatic or aromatic amine when the hydrophobic drug is acidic; and (f) water.

Claim 3

The composition of matter as recited in claim 1 comprising: ______________________________________ Percent Ingredient Range W/V ______________________________________ Basic Hydrophobic Drug 0.01-5.0 Soybean Oil 3.0-20.0 Sesame Oil (super-refined) 0.0-5.0 Oleic Acid N.F. 0.2-4.0 Hexanoic Acid ˜short or long chain fatty 0.0-0.50 acid to form an ion-pair Polyvinylpyrrolidone 0.0-0.2 Soy or Egg Lecithin-emulsifier 0.25-2.0 Polyoxyethylated hydrocarbon 0.0-1.0 dl-α-Tocopherol 0.0-0.05 Glycerine U.S.P. 0.5-2.25 Water qs ad 100 ______________________________________ wherein the hydrophobic drug comprises a sparingly water soluble ionizable solid or a water insoluble viscous oily liquid and/or comprises a basic drug which has a pK' lower or nearer the physiological pH or an acidic drug which has a pK' higher or nearer the physiological pH.

Claim 4

The composition of matter as recited in claim 1 comprising: ______________________________________ Percent Ingredient Range W/V ______________________________________ Acidic Hydrophobic Drug 0.01-5.0 .sub.--N--Methyl-D-glucamine or 0.1-5.0 R--NH--CH.sub.2 (CHOH).sub.4 CH.sub.2 OH where R is alkyl(C.sub.1 -C.sub.6) Soybean Oil 3.0-20.0 Soy or Egg Lecithin 0.2-2.0 Benzyl Alcohol 0.1-1.0 Glycerine U.S.P. 0.5-5.0 Water for Injection qs ______________________________________ wherein the hydrophobic drug may be a sparingly water soluble ionizable solid or a water insoluble viscous oily liquid and/or may be an acidic drug which has an ionization constant higher or nearer the physiological pH.

Claim 5

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

Claim 6

The composition of matter as recited in claim 2 where 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 7

The composition of matter as recited in claim 3 where the hydrophobic drug is 4-biphenyl acetic acid.

Claim 8

The composition of matter as recited in claim 1 comprising: ______________________________________ Ingredient Amount % W/V ______________________________________ Hydrophobic Drug 0.2 Soybean Oil 10.0 Oleic Acid N.F. 1.2 Soy Lecithin 95% P.C. 1.2 Polyoxyethylated hydrocarbon 1.0 dl-α-Tocopherol 0.01 Glycerine U.S.P. 2.25 Water qs ad 100 ______________________________________

Claim 9

The composition of matter as recited in claim 1 comprising: ______________________________________ Ingredient Amount % W/V ______________________________________ Hydrophobic Drug 0.2 Oleic Acid U.S.P. 0.8 Hexanoic Acid 0.1 Soybean Oil 10.0 Soy Lecithin 95% P.C. 1.2 dl-α-Tocopherol U.S.P. 0.01 Polyvinylpyrrolidone 0.1 Glycerine U.S.P. 2.25 Water qs ad 100 ______________________________________

Claim 10

The composition of matter as recited in claim 1 comprising: ______________________________________ Ingredient Percent W/V ______________________________________ Hydrophobic Drug 1.0 .sub.--N--Methyl-D-glucamine 0.92 Soybean Oil 7.00 Soy Lecithin 95% P.C. 1.00 Benzyl Alcohol 0.60 Glycerine U.S.P. 4.50 Water qs ad 100. ______________________________________

Claim 11

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

Claim 12

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

Claim 13

The composition of matter as recited in claim 9 where the hydrophobic drug is 4-biphenyl acetic acid.

Claim 14

The composition of matter as recited in claim 1 comprising: ______________________________________ Percent Ingredient Range W/V ______________________________________ Hydrophobic Drug 0.1-1.0 Soybean Oil 20.0 Oleic Acid N.F. 1.2 Soy Lecithin 95% P.C. 1.2 Polyoxyethylated hydrocarbon 1.0 dl-α-Tocopherol U.S.P. 0.01 Water qs ad 100 ______________________________________

Claim 15

The composition of matter as recited in claim 3 where 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 16

The composition of matter as recited in claim 1, which consists essentially of: ______________________________________ Ingredient Percent W/V ______________________________________ Hydrophobic Drug 0.2 Soybean Oil 10.0 Oleic Acid N.F. 1.2 Soy Lecithin 95% P.C. 1.2 Polyoxyethylated Hydrocarbon 1.0 dl-α-Tocopherol 0.01 Glycerine U.S.P. 2.25 Water qs ad 100. ______________________________________

Claim 17

The composition of matter as recited in claim 1, which consists essentially of: ______________________________________ Ingredient Amount % W/V ______________________________________ Hydrophobic Drug 0.2 Oleic Acid U.S.P. 0.8 Hexanoic Acid 0.1 Soybean Oil 10.0 Soy Lecithin 95% P.C. 1.2 dl-α-Tocopherol U.S.P. 0.01 Polyvinylpyrrolidone Type N.P.-K-30 0.1 Glycerine U.S.P. 2.25 Water qs ad 100. ______________________________________

Claim 18

The composition of matter as recited in claim 1, which consists essentially of: ______________________________________ Ingredient Percent W/V ______________________________________ Hydrophobic Drug 1.0 .sub.--N--Methyl-D-glucamine 0.92 Soybean Oil 7.00 Soy Lecithin 95% P.C. 1.00 Benzyl Alcohol 0.60 Glycerine U.S.P. 4.50 Water qs ad 100. ______________________________________

Claim 19

The composition of matter as recited in claim 1, which consists essentially of: ______________________________________ Percent Ingredient Range W/V ______________________________________ Hydrophobic Drug 0.1-1.0 Soybean Oil 20.0 Oleic Acid N.F. 1.2 Soy Lecithin 95% P.C. 1.2 Polyoxyethylated Hydrocarbon 1.0 dl-α-Tocopherol 0.01 Water qs ad 100. ______________________________________

Claim 20

A composition as defined in claim 15, wherein the hydrophobic drug is bis( 2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.

Claim 21

A composition ad defined in claim 16, wherein the hydrophobic drug is bis(2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.

Claim 22

A composition ad defined in claim 17, wherein the hydrophobic drug is bis(2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.

Claim 23

A composition ad defined in claim 18, wherein the hydrophobic drug is bis(2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.