Rocuronium formulation with improved stability

一种罗库溴铵、制剂的技术，应用在罗库溴铵制剂领域，能够解决没有考虑pH降低等问题，达到优异安全性、改进稳定性、减少注射痛的效果

Inactive Publication Date: 2017-08-18
MARUISHI PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In other words, in said document, the occurrence of painful injections is recognized in the pH range of 3.5 to 7.5, and no consideration is given to lowering the pH below 3.5

Method used

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  • Rocuronium formulation with improved stability
  • Rocuronium formulation with improved stability
  • Rocuronium formulation with improved stability

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0089] 0.06 g of glycine, 0.67 g of sodium chloride, 30 g of 0.1 M HCl, and 1.0 g of rocuronium bromide were dissolved in water for injection, and water for injection was further added to adjust the volume to 100 ml.

[0090] The pH of the formulation obtained was 2.0. After storing the formulations at 40° C. for 3 and 6 months, the pH and the formation rate of rocuronium bromide-related substance C were measured. In both cases (after 3 and 6 months of storage) at a pH of 2.0, the formation rates of rocuronium bromide-related substance C were 1.24% (after 3 months of storage) and 2.52% (after 6 months of storage). months later).

Embodiment 2

[0092] 0.55 g of glycine, 0.50 g of sodium chloride, 30 g of 0.1 M HCl, and 1.0 g of rocuronium bromide were dissolved in water for injection, and water for injection was further added to adjust the volume to 100 ml.

[0093] The pH of the formulation obtained was 3.0. After storing the formulations at 40° C. for 3 and 6 months, the pH and the formation rate of rocuronium bromide-related substance C were measured. In both cases (after 3 and 6 months of storage) at a pH of 3.0, the formation rates of rocuronium bromide-related substance C were 0.77% (after 3 months of storage) and 1.58% (after 6 months of storage). months later).

reference example 1

[0095] 4.58 g of glycine, 30 g of 0.1 M HCl, and 1.0 g of rocuronium bromide were dissolved in water for injection, and water for injection was further added to adjust the volume to 100 ml.

[0096] The pH of the formulation obtained was 4.0. After storing the preparation for 3 months and 6 months in the same manner as in Example 1, the pH and the formation rate of rocuronium bromide-related substance C were measured. In both cases at a pH of 4.0, the formation rates of rocuronium bromide-related substance C were 2.81% (after 3 months of storage) and 5.36% (after 6 months of storage).

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Abstract

The present invention provides a rocuronium formulation having excellent stability. This formulation includes rocuronium and a buffer solution, and has a pH adjusted to 3.5 or less (for example, 2.5-3.5). 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. This type of rocuronium formulation has a rocuronium analog C generation rate of 5% or less after being stored for six months at 40 DEG C, for example.

Description

technical field [0001] The present invention relates to a formulation of rocuronium bromide having improved stability, and a method for improving the stability of a formulation of rocuronium bromide. Background technique [0002] Rocuronium bromide (or rocuronium bromide) is known as an active ingredient of narcotic muscle relaxants and the like (Non-Patent Document 1). [0003] Rocuronium bromide is relatively thermally unstable in aqueous solution and, therefore, its storage and / or transportation is cumbersome and expensive. For example, ESLAX, which is known as a commercially available rocuronium bromide preparation, requires refrigeration at 2 to 8°C (Non-Patent Document 1). [0004] For this reason, attempts have been made to improve the stability of rocuronium bromide in aqueous solutions. For example, WO2008 / 065142 (Patent Document 1) discloses a method for stabilizing the rocuronium bromide by adding a sulfoalkyl ether-β-cyclodextrin derivative or a pharmaceuticall...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5355A61K9/08A61K47/12A61K47/18A61P23/00
CPCA61K47/12A61K47/18A61K9/08A61K31/5355A61K31/58A61P21/02A61P23/00C23C16/345C23C16/45546C23C16/45578H01L21/0217H01L21/02211H01L21/0228H01L21/67109H01L21/67248A61K9/0019A61K31/568A61K47/02A61K47/06C23C16/455C23C16/45561C23C16/45563H01L21/31
Inventor 井辻裕长原弘毅神保敬亮
Owner MARUISHI PHARMACEUTICAL CO LTD
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