Lyophilized Saccharide-Degrading Enzyme Unit Dose Formulation

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Solution Overview

Problem

Lyophilization of saccharide-degrading enzymes often results in significant reduction of enzyme titer, leading to wastage of expensive enzymes as only a portion is used for administration, while the remaining excess is discarded.

Innovation Solution

A pharmaceutical composition is developed as a unit dose formulation containing a lyophilized saccharide-degrading enzyme with a titer of not less than 0.3 unit/μg, and an amount of not less than 2 μg and not more than 8 μg, which is produced by lyophilizing a solution containing the enzyme in a container.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Loss of energy

If lyophilization is used to prepare enzyme preparations, then distribution cost is reduced, but enzyme titer is significantly reduced

Engineering Contradiction:
Improvedistribution costVSAvoidenzyme titer
Core Design Contradiction:
Loss of energyVSQuantity of substance

Solution Approach 1:

The patent applies parameter changes by optimizing the lyophilization process parameters (temperature, pressure, time) and formulation composition (protective agents, buffer systems) to minimize enzyme titer loss while maintaining the cost benefits of lyophilized preparation

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces protective agents and excipients as intermediaries during lyophilization to protect the enzyme from denaturation and aggregation, thereby preserving enzyme titer while still achieving the cost reduction benefits of frozen drying

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of operation

If a lyophilized preparation in large excess is prepared first and then separated for single dose, then unit dose formulation is achieved, but large remaining amount of expensive enzyme is wasted

Engineering Contradiction:
Improveunit dose formulationVSAvoidenzyme wastage
Core Design Contradiction:
Ease of operationVSLoss of substance

Solution Approach 1:

The patent applies segmentation by dividing the enzyme preparation into precise unit doses during the lyophilization process itself, rather than preparing large excess and separating later. This ensures each container receives exactly the required amount, eliminating waste from discarded excess enzyme while maintaining convenient unit dose formulation

Inventive Principle:
Principle #1Segmentation

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

This approach significantly suppresses the reduction in titer due to lyophilization and storage, allowing for a stable and effective enzyme dosage, while minimizing enzyme wastage.

Implementation Method 1

a step of putting a solution comprising not less than 2 μg and not more than 8 μg of a saccharide-degrading enzyme into the container, and a step of lyophilizing the solution

Methodology Applied
Scientific EffectLyophilization: Freeze Drying

Implementation Method 2

lyophilizing the solution SO that a unit dose of the pharmaceutical composition can be provided

Methodology Applied
Scientific EffectSublimation: Sublimation

Data Source

PatentUS20250177499A1Pharmaceutical composition, package and method for producing the same
Publication Date: 2025.06.05 SEIKAGAKU KOGYO CO LTD

AI summary

A pharmaceutical composition containing a lyophilized saccharide-degrading enzyme having excellent titer, and a package containing the pharmaceutical composition. The pharmaceutical composition is a unit dose formulation containing a lyophilized saccharide-degrading enzyme with a titer of not less than 0.3 unit/μg as an active ingredient, and contains the saccharide-degrading enzyme in an amount of not less than 2 μg and not more than 6 μg.