Compacted L-tryptophan Bulk Density Roller Compaction

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Solution Overview

Problem

Current pharmaceutical formulations of L-tryptophan require high amounts of excipients and result in large dosage forms due to the low bulk density of conventional L-tryptophan, which affects bioavailability and volume.

Innovation Solution

A process using roller compaction to densify L-tryptophan without auxiliary excipients, increasing its bulk density and allowing for the preparation of compacted, high-density L-tryptophan with reduced excipient requirements.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Volume of stationary object

If conventional L-tryptophan formulations are used, then the dosage forms are easier to manufacture with standard excipients, but the bulk density is low resulting in large volume and high excipient requirements

Engineering Contradiction:
Improvevolume of dosage formVSAvoidamount of excipient
Core Design Contradiction:
Volume of stationary objectVSQuantity of substance

Solution Approach 1:

The invention changes the physical state of L-tryptophan from conventional low-density crystalline form to high-density compacted form through roller compaction, achieving bulk densities of 0.3-0.6 g/ml compared to conventional 0.1-0.2 g/ml. This parameter change in density directly reduces the volume and excipient requirements for pharmaceutical formulations.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If soft gelatin capsules with vegetable oils are used, then the bioavailability of L-tryptophan is improved, but the amount of excipients increases and the dosage form volume increases

Engineering Contradiction:
Improvebioavailability of L-tryptophanVSAvoidamount of excipient
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The invention uses compacted L-tryptophan as an intermediary form that maintains the therapeutic benefits of oil-based formulations while eliminating the need for large amounts of vegetable oil excipients. The compacted form itself serves as the vehicle for improved bioavailability without requiring high volumes of auxiliary substances.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If high-dosage pharmaceutical forms are formulated, then the therapeutic effect is achieved, but the dosage form size becomes large and less patient-compliant

Engineering Contradiction:
Improvetherapeutic effectVSAvoiddosage form size
Core Design Contradiction:
ReliabilityVSVolume of stationary object

Solution Approach 1:

By changing the bulk density parameter of L-tryptophan through compaction, the invention enables high-dosage formulations (500-1000 mg and above) to be delivered in compact forms that maintain patient compliance. The increased density allows more active ingredient to be packed into a smaller volume without increasing the physical size of the dosage form.

Inventive Principle:
Principle #35Parameter changes

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 process achieves a significant increase in bulk density of L-tryptophan, reducing the volume and excipient needs in pharmaceutical compositions, enhancing bioavailability and patient compliance while maintaining chemical integrity.

Implementation Method 1

roller compaction of L-tryptophan

Methodology Applied
Scientific EffectMechanical compression: Compression

Data Source

PatentEP3705475B1High-density l-tryptophan, its preparation and uses thereof
Publication Date: 2023.08.30 TRADICHEM IND SERVICES SL
  • EP3705475B1 patent drawingFigure 1~2
  • EP3705475B1 patent drawingFigure 3~4
  • EP3705475B1 patent drawingFigure 5~6

AI summary

The invention relates to a process for preparing substantially pure compacted L-tryptophan comprising roller compaction of L-tryptophan. It also relates to the compacted high-density L-tryptophan obtainable with such process, to the use of compacted L-tryptophan for preparing pharmaceutical compositions and to pharmaceutical compositions comprising compacted L-tryptophan as active ingredient. The process of the invention allows to remarkably increase the bulk density of L-tryptophan and, furthermore, by using compacted L-tryptophan, it is possible to considerably reduce the amount of excipients required to prepare pharmaceutical compositions comprising L-tryptophan as active ingredient.