Enhanced Opioid Antagonist Delivery Systems

Publication ID: 24-11857547_0001_PTD
Published: October 28, 2025
Category:Direct Improvements & Enhancements

Legal Citation

pr1or.art Inc., “Enhanced Opioid Antagonist Delivery Systems,” Published Technical Disclosure No. 24-11857547_0001_PTD, Published October 28, 2025, available at https://archive.pr1or.art/24-11857547_0001_PTD
This technical disclosure describes improvements that would be readily apparent to a Person Having Ordinary Skill In The Art (PHOSITA) when considered in combination with the foundational architecture disclosed in U.S. Patent No. 11,857,547.

Summary of the Inventive Concept

The present invention relates to improved compositions and methods for opioid antagonist delivery, providing enhanced efficacy, safety, and accessibility in rescuing subjects from opioid overdose.

Background and Problem Solved

The original patent disclosed parenteral formulations for opioid overdose rescue, but had limitations in terms of targeted delivery, sustained release, and accessibility. The present invention addresses these limitations by introducing nanocarriers, sustained release formulations, and easy-to-use devices, providing improved efficacy and reduced side effects.

Detailed Description of the Inventive Concept

The inventive concept comprises a system for opioid overdose rescue, featuring a parenteral formulation with an aqueous solution containing about 1.5 mg of nalmefene free base and a nanocarrier for targeted delivery to the brain. The formulation can be designed to release nalmefene in a sustained manner over a period of at least 2 hours, providing prolonged protection against opioid overdose. Additionally, the composition can be combined with a peripheral opioid receptor antagonist to reduce the risk of opioid-induced constipation. The inventive concept also includes a device for opioid overdose rescue, comprising a pre-filled syringe containing the parenteral formulation, designed for easy and safe administration by a non-medical person.

Novelty and Inventive Step

The new claims introduce the use of nanocarriers for targeted delivery, sustained release formulations, and easy-to-use devices, which are not disclosed in the original patent. These features provide improved efficacy, safety, and accessibility in rescuing subjects from opioid overdose, thereby representing a non-obvious improvement over the prior art.

Alternative Embodiments and Variations

Alternative embodiments of the inventive concept could include the use of different nanocarriers, sustained release mechanisms, or devices for administration. Variations of the composition could include different opioid antagonists or peripheral opioid receptor antagonists, or different ratios of these components.

Potential Commercial Applications and Market

The inventive concept has significant commercial potential in the pharmaceutical industry, particularly in the area of opioid overdose rescue. The improved efficacy, safety, and accessibility of the inventive concept could lead to increased adoption and market share, with potential applications in emergency medical services, hospitals, and community-based settings.

Field of Art

Pharmaceutical formulations, specifically opioid antagonist delivery systems, with expertise in parenteral drug delivery, pharmacokinetics, and medical device design

Person of Ordinary Skill (PHOSITA) Profile

A pharmaceutical scientist or pharmacological engineer with advanced degree, experience in drug formulation, knowledge of nanocarrier technologies, and understanding of controlled drug delivery mechanisms

Obviousness Rationale

A PHOSITA would recognize that the PTD's variations represent predictable extensions of the source patent's core technology by applying known pharmaceutical engineering techniques to enhance nalmefene delivery. The proposed nanocarrier targeting, sustained release mechanism, and combination with peripheral antagonists are logical incremental improvements that leverage existing knowledge in drug delivery systems. These modifications would be considered routine optimization within the pharmaceutical field, utilizing standard techniques to improve drug efficacy and patient accessibility.

Obvious Combinations & Variations

Source Patent Element
Parenteral formulation of nalmefene with specific concentration and adjuvant
PTD Variation
Addition of nanocarrier for targeted brain delivery
Obviousness Reasoning
Nanocarrier drug targeting is a well-established technique in pharmaceutical science, representing a predictable method to improve drug distribution and efficacy
Source Patent Element
Intramuscular injection formulation of nalmefene
PTD Variation
Pre-filled syringe design for non-medical person administration
Obviousness Reasoning
Designing user-friendly drug delivery devices is a known approach to improve medication accessibility, representing an obvious design choice for emergency overdose treatment
Source Patent Element
Opioid antagonist composition for overdose rescue
PTD Variation
Combination with peripheral opioid receptor antagonist to reduce constipation
Obviousness Reasoning
Combining complementary pharmaceutical agents to mitigate side effects is a standard practice in drug development, representing a predictable optimization strategy
Source Patent Element
Basic nalmefene parenteral formulation
PTD Variation
Sustained release mechanism providing protection for at least 2 hours
Obviousness Reasoning
Extending drug release duration through known formulation techniques is a routine pharmaceutical engineering approach with predictable outcomes
35 U.S.C. § 103 Summary: Based on the teachings of US Patent 11857547, a person having ordinary skill in the art would find the variations disclosed in the Published Technical Disclosure to be obvious extensions of the prior art. The incremental improvements in nalmefene delivery, including nanocarrier targeting, sustained release mechanisms, and enhanced administration devices, represent predictable variations that would be readily conceived by a skilled pharmaceutical scientist without requiring inventive insight.

Original Patent Information

Patent NumberUS 11,857,547
TitleCompositions and methods for opioid antagonist delivery
Assignee(s)Purdue Pharma L.P.