Orosoluble SAMe Compositions Bypassing Hepatic Metabolism
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Solution Overview
Problem
Oral administration of S-adenosyl methionine (SAMe) results in low systemic bioavailability due to high presystemic metabolism in the liver, limiting its effectiveness in treating extrahepatic diseases such as depression and osteoarthrosis.
Innovation Solution
Development of non-gastro-resistant, orosoluble compositions containing SAMe salts, preferably with light magnesium oxide, which are easily absorbed in the oral cavity, bypassing the hepatic system and enhancing bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If gastro-resistant tablets are used for oral administration of SAMe, then the molecule is protected from gastric degradation, but systemic bioavailability remains low due to high presystemic metabolism in the liver
Solution Approach 1:
The patent divides the absorption pathway into two routes: oral absorption through the bloodstream (avoiding the liver) and traditional gastrointestinal absorption (through the liver via portal vein). By formulating SAMe in orosoluble form, the active ingredient is absorbed through the oral mucosa into the systemic circulation, segmenting the absorption route to bypass hepatic presystemic metabolism while maintaining gastric protection through the salt form.
Solution Approach 2:
The patent uses orosoluble salts of SAMe as an intermediary form that enables direct absorption through the oral mucosa. This intermediary form allows the molecule to enter systemic circulation without passing through the portal vein and liver, thus avoiding first-pass metabolism while maintaining stability.
2Stability of the object's composition
If stable salts of SAMe are used, then storage stability is improved, but absorption speed and bioavailability are reduced due to gastro-resistant formulation requirements
Solution Approach 1:
The patent changes the chemical form of SAMe from the free base to stable salts (such as tosylate, butanedisulfonate, or phytate salts). This parameter change enables both storage stability at room temperature and, when formulated as orosoluble compositions, rapid dissolution and absorption in the oral cavity, thus resolving the contradiction between stability and absorption speed.
3Ease of operation
If oral administration is used, then patient compliance is improved, but hepatic presystemic metabolism reduces effective dosage
Solution Approach 1:
The patent segments the absorption pathway to provide patients with an oral administration option (improving compliance) while creating a separate absorption route through the oral mucosa that bypasses the liver (maintaining effective dosage). This allows easy oral use without suffering from first-pass metabolism.
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 orosoluble compositions achieve significantly higher bioavailability and quicker absorption of SAMe, with plasma peak concentrations reaching 40-50% within 1-2 hours, compared to traditional gastro-resistant tablets, ensuring effective treatment of neuropsychiatric, osteoarticular, and hepatic diseases.
Implementation Method 1
orosoluble compositions containing at least a salt of S-adenosyl methionine (SAME)
Implementation Method 2
which are easily absorbed in the oral cavity, bypassing the hepatic system
Data Source
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AI summary
The present invention refers to pharmaceutical, dietary and/or nutraceutical orosoluble and/or effervescent compositions for oral use containing at least a salt of S-adenosyl methionine (SAMe), combined with physiologically acceptable excipients and optionally additional active ingredients. In particular the invention refers to compositions with high palatability formulated in tablet, capsule or granules. The present invention also refers to the use of at least a salt of SAMe combined with physiologically acceptable excipients and optionally further active ingredients for treating, human or veterinarian, neuropsychiatric, osteoarticular or hepatic diseases.