NMDA Receptor Antagonist Formulation With Reduced Neurotoxicity
The present invention is directed to pharmaceutical compositions of effective amounts of NMDA receptor antagonists and preservative for the administration to a patient in need of effective analgesia and anesthesia. The compositions of the invention advantageously do not cause any significant neurotoxicity. The preferred NMDA receptor antagonist is ketamine. The preferred preservative is benzalkonium chloride.
1 . A spray device for intranasal delivery of a pharmaceutical composition, wherein the spray device contains a pharmaceutical composition comprising an aqueous solution of about 10% ketamine hydrochloride and about 0.001% to about 0.2% benzalkonium chloride, wherein the composition does not cause any significant neurotoxicity, and wherein the level of neurotoxicity is comparable to sterile water when administered.
2 . The spray device of claim 1 , wherein the pharmaceutical composition further comprises a suitable carrier selected from the group consisting of water, saline, bicarbonate, sucrose and mixtures thereof.
3 . A spray device for intranasal delivery of a pharmaceutical composition, wherein the spray device contains a pharmaceutical composition comprising an aqueous solution of about 10% ketamine hydrochloride and about 0.002% benzalkonium chloride, wherein the composition does not cause any significant neurotoxicity, and wherein the level of neurotoxicity is comparable to sterile water when administered.
4 . A spray device for intranasal delivery of a pharmaceutical composition, wherein the spray device contains a pharmaceutical composition comprising an aqueous solution of about 0.01 mg/kg to about 1 mg/kg ketamine hydrochloride and about 0.001% to about 0.2% per unit dose benzalkonium chloride, wherein the composition does not cause any significant neurotoxicity, and wherein the level of neurotoxicity is comparable to sterile water when administered.
5 . The spray device of claim 4 , wherein the pharmaceutical composition further comprises a suitable carrier selected from the group consisting of water, saline, bicarbonate, sucrose and mixtures thereof.
6 . The spray device of claim 4 , wherein the pharmaceutical composition is administered nasally with 1 to 5 sprays of the device.
7 . The spray device of claim 6 , wherein the pharmaceutical composition is administered nasally with 2 sprays of the device.