Parenteral Nutrition Composition for Higher Choline Bioavailability

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Solution Overview

Problem

Existing parenteral nutrition formulations face challenges in providing adequate choline bioavailability due to intestinal bacterial degradation, leading to reduced effectiveness in managing cardiovascular and liver diseases and cognitive functions.

Innovation Solution

A parenteral nutrition composition comprising deoxycholic acid, cytidine diphosphate-choline, and choline alfoscerate, along with phosphatidylcholine, tocopherol, nicotinic acid, and adenosine triphosphate, which increases choline bioavailability by bypassing intestinal absorption and enhancing choline delivery to the liver and brain.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If choline is administered orally through tube feeding or dietary intake, then choline can be supplied to the body, but intestinal bacteria degrade choline to dimethylamines and trimethylamines, significantly lowering choline bioavailability

Engineering Contradiction:
Improvecholine bioavailabilityVSAvoidintestinal bacterial degradation
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent uses phosphatidylcholine as an intermediary carrier to deliver choline to the body. Instead of administering choline directly which gets degraded by intestinal bacteria, the choline is embedded within phosphatidylcholine molecules that can be administered parenterally (IV, IM, or SC), bypassing the intestinal bacterial degradation pathway and delivering choline directly into the bloodstream where it can be utilized by the body.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent extracts choline from its natural dietary form and incorporates it into phosphatidylcholine molecules for parenteral administration. This extraction and reformation allows choline to be delivered in a form that bypasses intestinal metabolism, eliminating the harmful bacterial degradation that occurs with oral administration.

Inventive Principle:
Principle #2Taking out (Extraction)

2Quantity of substance

If choline is degraded by intestinal bacteria to trimethylamine, then some choline absorption occurs, but elevated trimethylamine levels are associated with trimethylaminuria and cardiovascular diseases

Engineering Contradiction:
Improvecholine absorptionVSAvoidtrimethylamine production
Core Design Contradiction:
Quantity of substanceVSObject-generated harmful factors

Solution Approach 1:

Phosphatidylcholine serves as an intermediary that delivers choline directly to the bloodstream without requiring intestinal bacterial metabolism. This bypasses the entire metabolic pathway that converts choline to trimethylamine, thereby preventing trimethylamine production while still achieving choline absorption and utilization.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent converts the potential harm of choline metabolism by intestinal bacteria into a benefit by using parenteral phosphatidylcholine administration. This approach eliminates the harmful trimethylamine production pathway while preserving and enhancing the beneficial effects of choline for brain function, cardiovascular health, and liver disease management.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

3Quantity of substance

If parenteral nutrition formulation includes multiple choline compounds, then choline bioavailability increases for immediate onset of action, but formulation complexity increases

Engineering Contradiction:
Improvecholine bioavailabilityVSAvoidformulation complexity
Core Design Contradiction:
Quantity of substanceVSDevice complexity

Solution Approach 1:

The patent combines multiple choline-containing compounds (phosphatidylcholine, cytidine diphosphate-choline, and choline alfoscerate) into a single parenteral nutrition formulation. This merging of compounds works synergistically to provide immediate choline bioavailability while supporting brain function and managing cardiovascular and liver diseases, despite the increased formulation complexity.

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentUS12502397B2Parenteral nutrition formulation and methods of preparation thereof
Publication Date: 2025.12.23 STELLAR BIOMOLECULAR RES GMBH
  • US12502397B2 patent drawing

AI summary

An aqueous parenteral nutrition composition includes deoxycholic acid, cytidine diphosphate-choline and choline alfoscerate. The parenteral nutrition further includes 4.5-5.5% (w/v) phosphatidylcholine, in which combination of the phosphatidycholine with cytidine diphosphate-choline and choline alfoscerate increases choline bioavailability for immediate onset of action.