Morphine Infusion Stability via Inert Gas Packaging

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Solution Overview

Problem

Morphine solutions are unstable during autoclaving, leading to the formation of high levels of impurities, which exceeds desired limits, and existing solutions require additional steps and risk deleterious effects from oxygen scavenger pouches.

Innovation Solution

A morphine infusion dosage form with an aqueous solution of morphine or its pharmaceutically acceptable salt in flexible containers, surrounded by an outer covering with an inert gas or vacuum in the space between the container and outer covering, is sterilized by autoclaving without an oxygen scavenger pouch, maintaining stability and impurity levels within desired limits.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If morphine solution is subjected to autoclaving for sterilization, then sterility is achieved, but impurity levels increase significantly beyond desired limits

Engineering Contradiction:
ImprovesterilityVSAvoidimpurity levels
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The morphine solution is prepared with low dissolved oxygen content (<2 ppm) before autoclaving, and the container is surrounded by an outer covering with inert gas or vacuum in the space between container and outer covering. This preliminary preparation prevents oxidation during autoclaving, allowing sterilization without significant impurity formation.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

An inert gas (such as nitrogen) or vacuum is placed in the space between the container and outer covering. This creates an inert atmosphere that prevents oxygen from reaching the morphine solution during autoclaving, thereby preventing oxidative degradation and impurity formation while maintaining sterility.

Inventive Principle:
Principle #39Inert atmosphere (Inert environment)

2Stability of the object's composition

If an oxygen scavenger pouch is added to prevent oxidation during autoclaving, then stability is improved, but device complexity and risk of deleterious effects increase

Engineering Contradiction:
Improvechemical stabilityVSAvoidpackaging complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The invention removes the oxygen scavenger pouch from the packaging system entirely. Instead, stability is achieved through the combination of low dissolved oxygen content in the solution and the inert gas or vacuum atmosphere in the space between container and outer covering, eliminating the need for additional oxygen scavenging components.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The inert gas or vacuum atmosphere replaces the function of oxygen scavenger pouches by creating an oxygen-free environment that prevents oxidation during autoclaving and storage, simplifying the packaging system while maintaining chemical stability.

Inventive Principle:
Principle #39Inert atmosphere (Inert environment)

3Ease of manufacture

If the infusion bag is not overwrapped with an outer covering, then ease of manufacture is improved, but chemical stability during autoclaving deteriorates

Engineering Contradiction:
Improvemanufacturing simplicityVSAvoidchemical stability
Core Design Contradiction:
Ease of manufactureVSStability of the object's composition

Solution Approach 1:

The outer covering filled with inert gas or vacuum creates a protective inert atmosphere around the morphine solution during autoclaving. This prevents oxidative degradation, enabling the solution to withstand terminal sterilization while maintaining chemical stability, with the added benefit that the outer covering can serve as both protection and sterilization barrier.

Inventive Principle:
Principle #39Inert atmosphere (Inert environment)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The solution remains chemically and physically stable upon autoclaving and storage, with impurity levels below 0.2% by weight of morphine, maintaining potency and stability for at least 6 months, similar to unautoclaved samples and lower than marketed preparations.

Implementation Method 1

an inert gas or vacuum in the space between the container and outer covering... remains chemically and physically stable upon autoclaving

Methodology Applied
Scientific EffectOxidation prevention: Oxidation

Implementation Method 2

sterilized by autoclaving... stable upon autoclaving

Methodology Applied
Scientific EffectMoist heat sterilization: Heating

Data Source

PatentEP3290025B1Stable infusion dosage form of morphine
Publication Date: 2020.02.12 SUN PHARMACEUTICAL INDUSTRIES LTD
  • EP3290025B1 patent drawingFigure 1~2
  • EP3290025B1 patent drawingFigure 3~4
  • EP3290025B1 patent drawingFigure 5~6

AI summary

The present invention relates to an infusion dosage form comprising (i) an aqueous solution of morphine or its pharmaceutically acceptable salt as a sole active ingredient in a concentration ranging from about 0.1 mg/ml to about 10.0 mg/ml, filled in containers in volumes ranging from about 50 ml to about 250 ml, and having dissolved oxygen content of less than 2 ppm, (ii) the container being surrounded by an outer covering, and (iii) an inert gas or vacuum is present in the space between the container and outer covering, wherein the infusion dosage form is sterilized by autoclaving and is stable upon autoclaving, and further wherein the space between the container and outer covering does not have an oxygen scavenger pouch before or during autoclaving.