Cyclodextrin complexes for neuraxial administration of drugs
AssigneeThe Regents of the University of California
InventorsTony L. Yaksh, Harlan F. Hill
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Abstract
A method of delivering a drug to a patient, comprising administering said drug to the neuraxis of said patient in the form of a complex between said drug and a cyclodextrin, the cyclodextrin comprising at least one substituent to reduce crystallization of the complex or the cyclodextrin. Compositions suitable for carrying out the method are also disclosed.
Claims21
A method of delivering an analgesic drug to the neuraxis of a patient, comprising administering said analgesic drug to the neuraxis of said patient in the form of a solution of an inclusion complex between said analgesic drug and a .beta.-cyclodextrin substituted about 15% to about 80% with at least one substituent selected from the group consisting of --OCH.sub.3, --ROH, --RSO.sub.3 H, --CO.sub.2 R, --NHR, --NR.sub.2, --NROH, and --SiR.sub.3, wherein each R is independently selected from C.sub.1-10 alkyl groups that may be linear, branched, or cyclic, whereby said inclusion complex is effective to increase bioactivity of said drug, reduce redistribution of said drug from the neuraxis, and reduce systemic toxicity of the drug when compared to delivery of the drug alone to the neuraxis of said patient.
A composition for delivery of a drug to the neuraxis of a patient with increased bioactivity and decreased systemic toxicity, comprising a water soluble inclusion complex of an analgesic drug having a systemic toxicity, and a bioactivity when delivered into the neuraxis of a patient, complexed with a .beta.-cyclodextrin substituted about 15% to about 80% with at least one substituent selected from the group consisting of --OCH.sub.3, --ROH, --RSO.sub.3 H, --CO.sub.2 R, --NHR, --NR.sub.2, --NROH, and --SiR.sub.3, wherein each R is independently selected from C.sub.1-10 alkyl groups that may be linear, branched, or cyclic, wherein the amount of the drug and the substituted .beta.-cyclodextrin in the inclusion complex are effective to increase said bioactivity of said drug, reduce redistribution from the neuraxis, or to reduce said systemic toxicity when delivered into the neuraxis of said patient, as compared to delivery of the drug alone to the neuraxis of the patient.
Dependencies are inferred from the claim text.