Sm-153 Chelate Formulation for Extended Shelf Life

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Solution Overview

Problem

Current radiopharmaceuticals, such as Quadramet, have a short shelf life and high radionuclidic impurity levels, particularly Eu-154, which limits their availability and increases production costs due to stringent licensing requirements and waste disposal challenges, necessitating a product with a longer shelf life and improved impurity profile.

Innovation Solution

A process for preparing a pharmaceutically-acceptable formulation of Sm-153 and DOTMP chelate composition with a clinically relevant dosage of at least 35 mCi Sm-153, allowing for an extended expiration date of greater than 5 days by using Sm-153 produced in a lower flux portion of the nuclear reactor, resulting in a lower specific activity and reduced impurity profile, and can be administered as a pre-mixed drug or kit with separate components.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If Sm-153 is produced in a nuclear reactor by bombarding Sm-152 targets, then Sm-153 is generated for therapeutic use, but radionuclidic impurities such as Eu-154 are formed with long half-lives causing extended waste disposal requirements and licensing complexity

Engineering Contradiction:
ImproveSm-153 production quantityVSAvoidradionuclidic impurity levels
Core Design Contradiction:
Quantity of substanceVSObject-generated harmful factors

Solution Approach 1:

The patent extracts and removes radionuclidic impurities (Eu-154, Eu-155, Gd-153) from the Sm-153 product through a multi-step purification process involving ion exchange chromatography and extraction chromatography, thereby separating the desired product from harmful contaminants

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent changes the chemical parameters of the Sm-153 solution by adjusting pH levels and using complexing agents to selectively bind and remove impurities while maintaining Sm-153 in a pharmaceutically acceptable form

Inventive Principle:
Principle #35Parameter changes

2Duration of action of moving object

If current radiopharmaceutical formulations are used, then therapeutic treatment is provided, but the shelf life is limited to approximately 1 week due to Sm-153 decay and impurity accumulation

Engineering Contradiction:
Improveshelf lifeVSAvoidimpurity profile
Core Design Contradiction:
Duration of action of moving objectVSReliability

Solution Approach 1:

The patent performs preliminary purification and formulation of Sm-153 at the time of production, removing impurities before they can accumulate to problematic levels, thereby extending the usable shelf life of the product

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent creates a composite pharmaceutical formulation combining Sm-153 with DOTMP chelating agent and other excipients that stabilize the radionuclide and prevent impurity formation during storage

Inventive Principle:
Principle #40Composite materials

3Quantity of substance

If high levels of Eu-154 impurity are present in the formulation, then waste disposal becomes complex and expensive requiring collection of radioactive urine and extended decay storage, but this increases institutional costs and licensing requirements

Engineering Contradiction:
Improvetherapeutic dosageVSAvoidwaste disposal complexity
Core Design Contradiction:
Quantity of substanceVSEase of manufacture

Solution Approach 1:

The patent converts the potentially harmful long-lived Eu-154 impurity into a manageable situation by reducing its concentration to below detectable levels, thereby transforming a waste disposal problem into a routine pharmaceutical process

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

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 formulation provides a therapeutically effective, cost-reduced, and more frequently available treatment option with reduced radionuclidic impurities, extending the shelf life and reducing production costs while meeting regulatory standards.

Implementation Method 1

Radionuclides such as Sm-153 are prepared in a nuclear reactor by bombarding purified targets of the element containing one less neutron

Methodology Applied
Scientific EffectNuclear transmutation: Nuclear Fission

Implementation Method 2

When Sm-153 decays, Eu-153 is formed and an unwanted impurity, radioactive Eu-154 is formed from neutron capture by Eu-153

Methodology Applied
Scientific EffectRadioactive decay: Radioactive Decay

Implementation Method 3

an unwanted impurity, radioactive Eu-154 is formed from neutron capture by Eu-153

Methodology Applied
Scientific EffectNeutron capture: Nuclear Fission

Data Source

PatentEP3054996B1Process for preparing high purity therapeutic bone agents
Publication Date: 2023.06.21 IGL PHARMA INC

AI summary

This invention relates to radioactive, bone-seeking, pharmaceutical methods, compositions and formulations that have a lower impurity profile, a longer shelf life, improved availability and are less expensive to prepare. The compositions of this invention can be conveniently prepared in a timely manner resulting in improved availability and delivery of the drugs to patients.