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US 10,869,876 B2Granted
Rocuronium preparation with improved stability
AssigneeMaruishi Pharmaceutical Co., Ltd.
InventorsYutaka Itsuji, Hironori Nagahara, Keisuke Jinbo
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AssigneeMaruishi Pharmaceutical Co., Ltd.
InventorsYutaka Itsuji, Hironori Nagahara, Keisuke Jinbo
Estimating the term…
The present invention provides a rocuronium preparation with an excellent stability. The rocuronium preparation contains rocuronium and a buffer solution and having an adjusted pH of 3.5 or less (for example, 2.5 to 3.5). The buffer solution may be a citric acid-sodium hydroxide buffer solution, a tartaric acid-sodium hydroxide buffer solution, a potassium hydrogen phthalate-hydrochloric acid buffer solution, a glycine-hydrochloric acid buffer solution, or the like. Such a rocuronium preparation has, for example, after 6-month storage at 40° C., a generation rate of rocuronium-related substance C of 5% or less.
A rocuronium preparation in a liquid form consisting of rocuronium and a buffer solution, and optionally a solvent and optionally an isotonizing agent, and having a pH of 1.8 to 3.5, wherein the buffer solution is at least one selected from the group consisting of a formate buffer solution, a citrate buffer solution, a tartrate buffer solution, a phthalate buffer solution, a phosphate buffer solution, a citric acid-phosphate buffer solution and a glycine buffer solution, and wherein the preparation is stable after 6 months of storage at 40° C. by generating 3% or less of a rocuronium-related substance C.
A liquid rocuronium injection preparation consisting of rocuronium and a buffer solution, and optionally a solvent and optionally an isotonizing agent, and having a pH of 1.8 to 3.5, wherein the buffer solution is at least one selected from the group consisting of a formate buffer solution, a citrate buffer solution, a tartrate buffer solution, a phthalate buffer solution, a phosphate buffer solution, a citric acid-phosphate buffer solution and a glycine buffer solution, and wherein a rate of generated rocuronium-related substance C after 6-months storage at 40° C. is 3% or less.
A method for increasing or improving the stability of a rocuronium preparation, comprising adjusting the pH of a rocuronium preparation in a liquid form consisting of rocuronium and a buffer solution, and optionally a solvent and optionally an isotonizing agent, to 1.8 to 3.5, wherein the buffer solution is at least one selected from the group consisting of a formate buffer solution, a citrate buffer solution, a tartrate buffer solution, a phthalate buffer solution, a phosphate buffer solution, a citric acid-phosphate buffer solution and a glycine buffer solution, so that the rate of generated rocuronium-related substance C after 6-months storage at 40° C. is 3% or less.
A method for preventing or reducing both injection pain and vascular irritation caused by a rocuronium injection preparation and for increasing or improving the stability of the rocuronium injection preparation so that the rate of generated rocuronium-related substance C after 6-months storage at 40° C. is 3% or less, comprising adjusting the pH of a rocuronium injection preparation in a liquid form consisting of rocuronium and a buffer solution, and optionally a solvent and optionally an isotonizing agent, to 1.8 to 3.5, wherein the buffer solution is at least one selected from the group consisting of a formate buffer solution, a citrate buffer solution, a tartrate buffer solution, a phthalate buffer solution, a phosphate buffer solution, a citric acid-phosphate buffer solution and a glycine buffer solution, so that the rate of generated rocuronium-related substance C after 6-months storage at 40° C. is 3% or less.
Dependencies are inferred from the claim text.