Crystalline Polymorphs for Stable Growth Hormone Release
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current methods for increasing growth hormone levels in mammals are limited by the stability and manufacturing properties of existing compounds, which often require specialized storage and have exacting pharmaceutical regulations, and there is a need for more effective pharmaceutical compositions that can stimulate growth hormone release.
Innovation Solution
The development of crystalline forms of (3R)-1-(2-methylalanyl-D-tryptophyl)-3-(phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide with specific X-ray powder diffraction patterns, which are more stable, have advantageous manufacturing properties, and can be used to stimulate growth hormone release by administering a therapeutically effective amount.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If crystalline forms of the compound are developed, then stability and manufacturing properties are improved, but the complexity of characterizing and regulating different crystal forms increases
Solution Approach 1:
The patent applies parameter changes by developing multiple crystalline forms (polymorphs) of the same compound, each with distinct X-ray powder diffraction patterns characterized by specific 2θ values. This allows optimization of stability and manufacturing properties by selecting appropriate crystal forms while maintaining the same chemical composition.
Solution Approach 2:
The patent utilizes phase transitions by creating different crystalline phases of the compound. Each polymorph represents a distinct solid phase with unique physical properties, enabling improved stability and manufacturability while the compound maintains its chemical identity.
2Reliability
If existing compounds are used to increase growth hormone levels, then growth hormone release is stimulated, but specialized storage conditions and exacting pharmaceutical regulations are required
Solution Approach 1:
The patent changes the physical state parameters of the compound by developing crystalline forms with specific diffraction patterns. This transformation from amorphous or less stable forms to well-defined crystalline structures improves manufacturing ease and storage conditions while maintaining the compound's effectiveness in stimulating growth hormone release.
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
These crystalline forms are highly pure, stable for extended periods without specialized storage, and can be readily suspended and filtered, making them suitable for large-scale production and fulfilling pharmaceutical regulations, effectively stimulating growth hormone release.
Implementation Method 1
having an X-ray powder diffraction pattern wherein at least one or at least two 2θ values measured using Cu Kα radiation are selected from the group consisting of about: 10.1, 11.1, 17.6, 20.0 and 20.8
Data Source
AI summary
Crystalline polymorphs of (3R)-1-(2-methylalanyl-D-tryptophyl)-3-(phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide which are useful as pharmaceutical agents are disclosed. Methods of production and isolation of these polymorphs and pharmaceutical compositions which include these polymorphs and pharmaceutical methods of treatment are also disclosed. The crystalline polymorphs of the present invention are useful as they act directly on the pituitary gland cells to release growth hormone.