Electron Beam Sterilization of Hypercompressed Polymer Dosage Forms

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Hypercompressed biologically compatible polymers and copolymers used in pharmaceutical formulations are susceptible to degradation when sterilized with radiation, leading to reduced potency and stability issues, particularly when containing thermally unstable APIs like proteins or polypeptides, which fail to meet regulatory standards.

Innovation Solution

The use of electron beam sterilization for hypercompressed pharmaceutical formulations made with ester capped lactide, glycolide, or lactide-glycolide copolymers avoids the degradation issues associated with gamma radiation, allowing for the production of sterile, stable products without compromising the API's integrity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If gamma radiation is used to sterilize hypercompressed polymeric pharmaceutical formulations, then sterilization is achieved, but the polymeric material and API are degraded or denatured

Engineering Contradiction:
Improvesterilization effectivenessVSAvoidpolymer and API stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent changes the radiation parameter from gamma radiation to electron beam radiation. This parameter change allows sterilization to be achieved while avoiding the degradation and denaturation problems associated with gamma radiation, thereby maintaining both sterilization effectiveness and material stability.

Inventive Principle:
Principle #35Parameter changes

2Productivity

If hypercompression is applied to densify polymeric microspheres containing API, then controlled release formulation is formed, but radiation-induced degradation is facilitated due to closer proximity of reactive species

Engineering Contradiction:
Improveformulation densityVSAvoidradiation-induced degradation
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the radiation type parameter from gamma to electron beam, which resolves the contradiction by enabling sterilization of hypercompressed formulations without exacerbating degradation. The electron beam radiation achieves sterilization while minimizing the harmful effects on the densely packed reactive species in hypercompressed formulations.

Inventive Principle:
Principle #35Parameter changes

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

Electron beam sterilization effectively reduces radiation-induced degradation byproducts, ensuring the stability and potency of the API, meeting regulatory standards for pharmaceutical use and extending the shelf life of the product.

Implementation Method 1

The use of electron beam sterilization for hypercompressed pharmaceutical formulations made with ester capped lactide, glycolide, or lactide-glycolide copolymers avoids the degradation issues associated with gamma radiation

Methodology Applied
Scientific EffectElectron beam radiation: Electron Beam

Implementation Method 2

ionizing radiation interacts with the electrons of polymer molecules with a transfer of energy that results in ion formation and ejection of secondary electrons

Methodology Applied
Scientific EffectIonizing radiation: Ionisation

Implementation Method 3

when gamma radiation is applied to make a sterile product based on a polymeric material comprising a lactide polymer, glycolactide or lactide-glycolactide copolymer, these polymeric materials and any polypeptide or protein, which is present, may be degraded or denatured

Methodology Applied
Scientific EffectGamma radiation: Radiation

Implementation Method 4

The immediate outcome of the exposure to ionizing radiation, such as gamma radiation, is the formation of various energetic species such as trapped radicals, electrons and ions; the decays of these energetic species results in fragmentation and generates free radicals

Methodology Applied
Scientific EffectFree radical formation: Ionisation

Implementation Method 5

hypercompressed (densified) biologically compatible lactide polymer, glycolactide or lactide-glycolactide copolymers containing APIs

Methodology Applied
Scientific EffectHypercompression: Compression

Data Source

PatentEP3651771B1Radiation sterilization of hypercompressed polymer dosage forms
Publication Date: 2023.08.30 SUSTAINED NANO SYSTEMS LLC

AI summary

A sterile pharmaceutical dosage form which comprises an ester capped lactide polymer, glycolide polymer or a lactide-glycolide copolymer hypercompressed with an active pharmaceutical ingredient wherein said sterile pharmaceutical dosage form has been sterilized with an electron beam and a method of preparing said sterile pharmaceutical dosage form.