SAMe Formulation Pharmacokinetics via Controlled Release

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Solution Overview

Problem

Conventional SAMe formulations have low pharmacokinetic profiles, characterized by short half-life and low AUC values, leading to inadequate biological response and tolerability issues due to high pill count and side effects associated with frequent dosing.

Innovation Solution

Designing non-parenteral compositions that release SAMe within a specific 'window' of dissolution, combining with suitable excipients and processing parameters to achieve targeted drug release, particularly in the gastrointestinal tract, resulting in improved Cmax and AUC values, and reducing side effects through once-daily dosing.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional SAMe formulations are administered multiple times daily, then adequate pharmacokinetic coverage is achieved, but pill burden and side effects increase

Engineering Contradiction:

Improvepharmacokinetic coverageVSAvoidpill burden

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent segments the dosing frequency by designing formulations with different release characteristics (immediate release vs. extended release) to allow once-daily dosing while maintaining adequate pharmacokinetic coverage, thereby reducing pill burden while preserving reliability

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent applies dynamics by creating formulations with controlled release rates that extend the duration of action, allowing the dosing frequency to be reduced from multiple times daily to once daily while maintaining adequate plasma concentration levels throughout the dosing interval

Inventive Principle:

Principle #15Dynamics

2Reliability

If conventional SAMe formulations are administered twice daily, then therapeutic effect is maintained, but gastrointestinal side effects and insomnia occur

Engineering Contradiction:

Improvetherapeutic effectVSAvoidgastrointestinal side effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies preliminary action by designing formulations that control the timing and rate of SAMe release in the gastrointestinal tract, preventing premature degradation and optimizing absorption to reduce gastrointestinal side effects while maintaining therapeutic effect

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The patent changes parameters of the formulation (such as excipient composition, coating characteristics, and manufacturing conditions) to modify the release profile and bioavailability of SAMe, thereby reducing gastrointestinal side effects and insomnia while maintaining therapeutic effectiveness

Inventive Principle:

Principle #35Parameter changes

3Quantity of substance

If higher doses of SAMe are administered, then plasma concentrations increase, but tolerability decreases

Engineering Contradiction:

Improveplasma concentrationVSAvoidtolerability

Core Design Contradiction:

Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent changes formulation parameters (excipient selection, manufacturing conditions, dosage form characteristics) to optimize the bioavailability and pharmacokinetic profile of SAMe, achieving adequate plasma concentrations at lower doses and improving tolerability

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS9931356B2Pharmacokinetics of S-adenosylmethionine formulations

Publication Date: 2018.04.03 BONAFIDE HEALTH LLC

AI summary

Compositions and methods to improve the pharmacokinetic profile of S-Adenosylmethionine (SAMe) are provided, as are methods of treating various disorders using SAMe formulations with improved pharmacokinetic profiles. More specifically, the invention is directed to methods of treating a disease or disorder in a subject and/or improving the nutritional status of a subject by administering formulations exhibiting improved pharmacokinetic profiles of exogenous SAMe. The method also includes the step of orally administering compositions of the invention to the subject once per day after overnight fast; that is prior to food intake in the morning.