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AssigneeCydex, Inc.
InventorsGerold L. Mosher, Karen T. Johnson, Atef A. Gayed
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The present invention provides aqueous parenteral formulations containing an antiarrhythmic agent, such as amiodarone, and a sulfoalkyl ether cyclodextrin. The liquid formulations are clear, sterilizable, and chemically and physically stable. The liquid formulations do not require a surfactant and do not precipitate upon dilution with distilled water or other pharmaceutically acceptable liquid carrier. The sulfoalkyl ether cyclodextrin-containing formulation provides significant advantages over other cyclodextrin-containing formulations of amiodarone. The formulation can be prepared in acidic, neutral and slightly basic medium while providing acceptable concentrations of amiodarone suitable for parenteral administration. An SAE-CD-containing formulation of amiodarone can be provided in liquid form or as a reconstitutable powder. Moreover, highly concentrated solutions exceeding 200 mg of amiodarone per mL can be prepared. Solutions can be made either dilutable or non-dilutable with water at room temperature or under conditions typically encountered in the clinic.
A dilutable clear liquid formulation comprising amiodarone and a sulfoalkyl ether cyclodextrin (SAE-CD), wherein the molar ratio of SAE-CD to amiodarone is greater than or equal to about 1.1±0.01, and the liquid formulation is dilutable with a pharmaceutically acceptable aqueous liquid carrier at ambient temperature with insignificant precipitation of amiodarone.
A dilutable clear liquid formulation comprising amiodarone and an SAE-CD, wherein
A dilatable clear liquid formulation comprising amiodarone and an SAE-CD, wherein
A clear liquid formulation comprising amiodarone, SAE-CD and an aqueous liquid carrier, wherein the molar ratio of SAE-CD to amiodarone is less than or equal to about 1.09±0.01.
A reconstitutable solid comprising SAE-CD and amiodarone, wherein the molar ratio of SAE-CD to amiodarone is greater than or equal to about 1.1±0.01, and the reconstitutable solid forms a dilutable clear reconstituted liquid formulation when mixed with water at a temperature of about 20° C. to about 28° C.
A reconstitutable solid comprising SAE-CD and amiodarone, wherein the molar ratio of SAE-CD to amiodarone is less than about 1.09±0.01, and the reconstitutable solid forms a clear reconstituted liquid formulation when mixed with a pharmaceutically acceptable liquid carrier at a temperature of greater than or equal to about 30° C.
A clear dilutable concentrated liquid formulation comprising SBE7-β-CD and amiodarone, wherein the amiodarone is present in amount of greater than about 2 mg/mL, and the SBE7-β-CD to amiodarone ratio is greater than or equal to about 1.1±0.01 wherein the liquid formulation can be diluted with water at about 20° C. to 30° C. to form a clear diluted liquid formulation.
A clear ready-to-inject sterile liquid formulation comprising SBE7-β-CD and amiodarone, wherein the SBE7-β-CD is present in an amount of at least about 0.3% wt. and the amiodarone is present in amount of 1-2 mg/mL.
A method of increasing the solubility of an acid-ionizable agent comprising the steps of:
A method of preparing a clear liquid formulation comprising the steps of:
Dependencies are inferred from the claim text.