Enhanced Venglustat-Based Pharmaceutical Compositions for Improved Efficacy and Patient Compliance

Publication ID: 24-11857512_0006_PTD
Published: October 28, 2025
Category:Direct Improvements & Enhancements

Legal Citation

pr1or.art Inc., “Enhanced Venglustat-Based Pharmaceutical Compositions for Improved Efficacy and Patient Compliance,” Published Technical Disclosure No. 24-11857512_0006_PTD, Published October 28, 2025, available at https://archive.pr1or.art/24-11857512_0006_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. 11,857,512.

Summary of the Inventive Concept

The present disclosure relates to novel venglustat-based pharmaceutical compositions and systems that address the limitations of existing formulations, providing improved physical and chemical stability, enhanced bioavailability, and better patient compliance.

Background and Problem Solved

The original patent disclosed pharmaceutical compositions comprising venglustat, but these compositions have inherent limitations, such as poor physical and chemical stability, low bioavailability, and unpleasant taste. The present inventive concept solves these problems by introducing novel formulations, excipients, and delivery systems that improve the overall performance of venglustat-based pharmaceuticals.

Detailed Description of the Inventive Concept

The new inventive concept comprises five distinct aspects. Firstly, a chewable tablet formulation with improved physical and chemical stability and reduced chewing difficulty index. Secondly, a novel excipient blend that enhances the dissolution rate of venglustat. Thirdly, a pH-dependent coating that facilitates targeted release of the active ingredient in the gastrointestinal tract. Fourthly, a novel taste-masking agent that reduces the bitterness of venglustat. Lastly, a system for monitoring and controlling the release of venglustat from an oral pharmaceutical composition, comprising a sensor that detects the pH of the gastrointestinal tract and adjusts the release rate of the active ingredient accordingly.

Novelty and Inventive Step

The present inventive concept introduces novel and non-obvious solutions to the limitations of existing venglustat-based pharmaceutical compositions. The combination of a chewable tablet formulation, novel excipient blend, pH-dependent coating, taste-masking agent, and pH-sensing release control system provides a unique and innovative approach to improving the efficacy and patient compliance of venglustat-based treatments.

Alternative Embodiments and Variations

Alternative embodiments of the inventive concept may include different excipient blends, coating materials, or taste-masking agents. Additionally, the pH-sensing release control system could be adapted for use with other oral pharmaceutical compositions. Variations of the chewable tablet formulation may include different shapes, sizes, or flavors to improve patient compliance.

Potential Commercial Applications and Market

The present inventive concept has significant commercial potential in the treatment of Fabry disease and other lysosomal storage disorders. The improved efficacy, safety, and patient compliance of the novel venglustat-based pharmaceutical compositions could lead to increased market share and revenue growth in the pharmaceutical industry.

CPC Classifications

SectionClassGroup
A A61 A61K31/439
A A61 A61K9/0053
A A61 A61K9/2009
A A61 A61K9/2013
A A61 A61K9/2018
A A61 A61K9/2095
A A61 A61K9/485
A A61 A61K9/4833
A A61 A61K9/4858
A A61 A61K9/4866

Field of Art

Pharmaceutical formulation and drug delivery systems, specifically focusing on oral pharmaceutical compositions for enzyme inhibitors like venglustat, with expertise in tablet design, excipient selection, and controlled release technologies

Person of Ordinary Skill (PHOSITA) Profile

A pharmaceutical formulation scientist with advanced degree (PhD or equivalent) in pharmaceutical sciences, experienced in drug delivery system design, tablet manufacturing, and excipient optimization, with knowledge of oral drug formulation techniques and patient compliance strategies

Obviousness Rationale

A PHOSITA would recognize that the PTD's variations represent standard pharmaceutical formulation optimization techniques applied to the venglustat composition disclosed in the source patent. The proposed modifications such as chewable tablet design, excipient blend optimization, pH-dependent coating, and taste-masking are well-established pharmaceutical engineering approaches for improving drug delivery and patient acceptability. These variations would be considered predictable extensions of known pharmaceutical formulation strategies within the existing technological framework.

Obvious Combinations & Variations

Source Patent Element
Tablet formulation of venglustat with specified excipients like mannitol, crospovidone, and hydroxypropyl cellulose
PTD Variation
Novel excipient blend designed to enhance dissolution rate and improve bioavailability
Obviousness Reasoning
Excipient optimization is a routine practice in pharmaceutical formulation, and a PHOSITA would find it obvious to modify excipient ratios and selections to improve drug performance using known pharmaceutical engineering techniques
Source Patent Element
Oral pharmaceutical composition comprising venglustat in tablet form
PTD Variation
Chewable tablet formulation with reduced chewing difficulty index
Obviousness Reasoning
Developing alternative dosage forms to improve patient compliance is a predictable design choice for pharmaceutical formulations, particularly for medications targeting chronic conditions
Source Patent Element
Basic tablet composition of venglustat
PTD Variation
pH-dependent coating for targeted gastrointestinal tract release
Obviousness Reasoning
Controlled release technologies and pH-responsive coatings are well-known pharmaceutical engineering techniques for modifying drug absorption and bioavailability
Source Patent Element
Oral tablet formulation of venglustat
PTD Variation
Taste-masking agent to reduce active ingredient bitterness
Obviousness Reasoning
Addressing organoleptic properties through taste-masking is a standard pharmaceutical formulation strategy to improve patient acceptability, particularly for bitter compounds
Source Patent Element
Basic pharmaceutical composition of venglustat
PTD Variation
pH-sensing release control system for dynamic drug delivery
Obviousness Reasoning
Smart drug delivery systems utilizing environmental sensing are known in the art, and applying such technologies to existing pharmaceutical compositions represents an obvious technological progression
35 U.S.C. § 103 Summary: Based on the teachings of US Patent 11857512 and the comprehensive pharmaceutical formulation strategies disclosed herein, a person of ordinary skill in the art would find the claimed variations obvious and predictable extensions of existing pharmaceutical engineering knowledge. The proposed modifications represent standard optimization techniques within the established technological framework of oral drug delivery systems, thereby rendering potential patent claims obvious and anticipatable as a matter of law.

Original Patent Information

Patent NumberUS 11,857,512
TitlePharmaceutical compositions comprising venglustat
Assignee(s)Genzyme Corporation