Pharmaceutical compositions

Claim 2

Stable, microcrystalline cisplatin having a particle size distribution of at least about 80% in the range of 0 to 5 micrometers, less than about 20% in the range of 5 to 20 micrometers and essentially no particles larger than 20 micrometers; the crystalline form of said microcrystalline cisplatin being different from that of lyophilized cisplatin as demonstrable by x-ray powder diffraction patterns; and said microcrystalline cisplatin being completely soluble in water within about three minutes at a concentration of 1 mg. per ml.

Claim 3

The microcrystalline cisplatin of claim 1 having an x-ray powder diffraction pattern substantially as follows: ______________________________________ Interplanar Two Theta Relative Spacings (Degrees) Intensity (Angstroms) ______________________________________ 13.81 100 6.407 14.93 84 5.929 16.26 71 5.447 24.05 27 3.697 26.57 22 3.352 28.37 16 3.143 30.35 13 2.943 33.14 15 2.701 ______________________________________

Claim 4

The microcrystalline cisplatin of claim 1 or 2 wherein said microcrystalline cisplatin is sterile.

Claim 5

Sterile, stable, microcrystalline cisplatin in a sealed container in unit dosage form, reconstitutable with sterile water within about three minutes at a concentration of 1 mg. of microcrystalline cisplatin per ml. of sterile water, and suitable for intravenous administration to man; said microcrystalline cisplatin having a particle size distribution of at least about 80% in the range of 0 to 5 micrometers, less than about 20% in the range of 5 to 20 micrometers and essentially no particles larger than 20 micrometers; the crystalline form of said microcrystalline cisplatin being different from that of lyophilized cisplatin as demonstrable by x-ray powder diffraction patterns.

Claim 6

Sterile, stable, microcrystalline cisplatin in a sealed container in unit dosage form, reconstitutable with sterile water within about three minutes at a concentration of 1 mg. of microcrystalline cisplatin per ml. of sterile water, and suitable for intravenous administration to man; said microcrystalline cisplatin having a particle size distribution of at least about 80% in the range of 0 to 5 micrometers, less than about 20% in the range of 5 to 20 micrometers and essentially no particles larger than 20 micrometers; the crystalline form of said microcrystalline cisplatin being different from that of lyophilized cisplatin as demonstrable by x-ray powder diffraction patterns.

Claim 7

The sterile unit dosage form of microcrystalline cisplatin of claim 4 wherein said microcrystalline cisplatin has an x-ray powder diffraction pattern substantially as follows: ______________________________________ Interplanar Two Theta Relative Spacings (Degrees) Intensity (Angstroms) ______________________________________ 13.81 100 6.407 14.93 84 5.929 16.26 71 5.447 24.05 27 3.697 26.57 22 3.352 28.37 16 3.143 30.35 13 2.943 33.14 15 2.701 ______________________________________

Claim 8

A sterile, stable, dry-mix of microcrystalline cisplatin in a sealed container in unit dosage form, reconstitutable with sterile water within about three minutes at a concentration of 1 mg. of microcrystalline cisplatin per ml. of sterile water, and suitable for intravenous administration to man; said dry-mix also containing a sterile, nontoxic, pharmaceutically acceptable, inorganic source of chloride ions in an amount equivalent to that produced by the presence of sodium chloride in a concentration of from about 1 to about 20 mgs. per mg. of microcrystalline cisplatin; said microcrystalline cisplatin having a particle size distribution of at least about 80% in the range of 0 to 5 micrometers, less than about 20% in the range of 5 to 20 micrometers and essentially no particles larger than 20 micrometers; the crystalline form of said microcrystalline cisplatin being different from that of lyophilized cisplatin as demonstrable by x-ray powder diffraction patterns.

Claim 9

A sterile, stable, dry-mix of microcrystalline cisplatin in a sealed container in unit dosage form, reconstitutable with sterile water within about three minutes at a concentration of 1 mg. of microcrystalline cisplatin per ml. of sterile water, and suitable for intravenous administration to man; said dry-mix also containing a sterile, nontoxic, pharmaceutically acceptable, inorganic source of chloride ions in an amount equivalent to that produced by the presence of sodium chloride in a concentration of from about 1 to about 20 mgs. per mg. of microcrystalline cisplatin; said microcrystalline cisplatin having a particle size distribution of at least about 80% in the range of 0 to 5 micrometers, less than about 20% in the range of 5 to 20 micrometers and essentially no particles larger than 20 micrometers; the crystalline form of said microcrystalline cisplatin being different from that of lyophilized cisplatin as demonstrable by x-ray powder diffraction patterns.

Claim 10

The dry-mix of claim 6 wherein the inorganic source of chloride ions is sodium chloride.

Claim 11

The dry-mix of claim 7 wherein the sodium chloride is present at a concentration of about 9 mg. per mg. of microcrystalline cisplatin.

Claim 12

A sterile, stable, dry-mix of microcrystalline cisplatin in a sealed container in unit dosage form, reconstitutable with sterile water within about three minutes at a concentration of 1 mg. of microcrystalline cisplatin per ml. of sterile water, and suitable for intravenous administration to man; said dry-mix also containing a customary, harmless, physiologically acceptable excipient in a concentration of from about 2 mgs. to about 150 mgs. per mg. of microcrystalline cisplatin; said microcrystalline cisplatin having a particle size distribution of at least about 80% in the range of 0 to 5 micrometers, less than about 20% in the range of 5 to 20 micrometers and essentially no particles larger than 20 micrometers; the crystalline form of said microcrystalline cisplatin being different from that of lyophilized cisplatin as demonstrable by x-ray powder diffraction patterns.

Claim 13

A sterile, stable, dry-mix of microcrystalline cisplatin in a sealed container in unit dosage form, reconstitutable with sterile water within about three minutes at a concentration of 1 mg. of microcrystalline cisplatin per ml. of sterile water, and suitable for intravenous administration to man; said dry-mix also containing a customary, harmless, physiologically acceptable excipient in a concentration of from about 2 mgs. to about 150 mgs. per mg. of microcrystalline cisplatin; said microcrystalline cisplatin having a particle size distribution of at least about 80% in the range of 0 to 5 micrometers, less than about 20% in the range of 5 to 20 micrometers and essentially no particles larger than 20 micrometers; the crystalline form of said microcrystalline cisplatin being different from that of lyophilized cisplatin as demonstrable by x-ray powder diffraction patterns.

Claim 14

The dry-mix of claim 9 wherein the excipient is mannitol.

Claim 15

The dry-mix of claim 10 wherein the mannitol is present at a concentration of about 10 mg. per mg. of microcrystalline cisplatin.

Claim 16

A sterile, stable dry-mix of microcrystalline cisplatin in a sealed container in unit dosage form, reconstitutable with sterile water within about three minutes at a concentration of 1 mg. of microcrystalline cisplatin per ml. of sterile water, and suitable for intravenous administration to man; said dry-mix also containing both a sterile, nontoxic, pharmaceutically acceptable, inorganic source of chloride ions in an amount equivalent to that produced by the presence of sodium chloride in a concentration of from about 1 to about 20 mgs. per mg. of microcrystalline cisplatin and a customary, harmless, physiologically acceptable excipient in a concentration of from about 2 mgs. to about 150 mgs. per mg. of microcrystalline cisplatin; said microcrystalline cisplatin having a particle size distribution of at least about 80% in the range of 0 to 5 micrometers, less than about 20% in the range of 5 to 20 micrometers and essentially no particles larger than 20 micrometers; the crystalline form of said microcrystalline cisplatin being different from that of lyophilized cisplatin as demonstrable by x-ray powder diffraction patterns.

Claim 17

A sterile, stable dry-mix of microcrystalline cisplatin in a sealed container in unit dosage form, reconstitutable with sterile water within about three minutes at a concentration of 1 mg. of microcrystalline cisplatin per ml. of sterile water, and suitable for intravenous administration to man; said dry-mix also containing both a sterile, nontoxic, pharmaceutically acceptable, inorganic source of chloride ions in an amount equivalent to that produced by the presence of sodium chloride in a concentration of from about 1 to about 20 mgs. per mg. of microcrystalline cisplatin and a customary, harmless, physiologically acceptable excipient in a concentration of from about 2 mgs. to about 150 mgs. per mg. of microcrystalline cisplatin; said microcrystalline cisplatin having a particle size distribution of at least about 80% in the range of 0 to 5 micrometers, less than about 20% in the range of 5 to 20 micrometers and essentially no particles larger than 20 micrometers; the crystalline form of said microcrystalline cisplatin being different from that of lyophilized cisplatin as demonstrable by x-ray powder diffraction patterns.

Claim 18

The dry-mix of claim 12 wherein the inorganic source of chloride ions is sodium chloride and the excipient is mannitol.

Claim 19

The dry-mix of claim 13 wherein the sodium chloride is present at a concentration of about 9 mgs. per mg. of microcrystalline cisplatin and the mannitol is present at a concentration of about 10 mgs. per mg. of microcrystalline cisplatin.

Claim 20

The dry-mix of claim 6, 7, 8, 9, 10, 11, 12, 13 or 14 wherein the microcrystalline cisplatin has an x-ray powder diffraction pattern substantially as follows: ______________________________________ Interplanar Two Theta Relative Spacings (Degrees) Intensity (Angstroms) ______________________________________ 13.81 100 6.407 14.93 84 5.929 16.26 71 5.447 24.05 27 3.697 26.57 22 3.352 28.37 16 3.143 30.35 13 2.943 33.14 15 2.701 ______________________________________