L-alpha-glyceryl phosphoryl choline crystal preparation
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Solution Overview
Problem
Conventional L-alpha-glyceryl phosphoryl choline is produced in a liquid state, limiting its use to soft capsules that are inconvenient and require complex manufacturing, with poor storage stability due to high hygroscopicity.
Innovation Solution
Development of Type I and Type II crystals through a method involving seed crystal addition and optimized crystallization conditions, reducing water content and using alcohol solutions to produce crystals with specific diffraction patterns and thermal properties, resulting in higher purity and lower hygroscopicity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If L-alpha-glyceryl phosphoryl choline is produced in liquid state by conventional methods, then the manufacturing process is simple, but the storage stability is poor due to high hygroscopicity and the formulation options are limited
Solution Approach 1:
The patent applies parameter changes by controlling crystallization temperature (5-20°C), solvent composition (alcohol type and ratio), and water content (6-12%) to transform L-alpha-glyceryl phosphoryl choline from liquid state to solid crystal state, achieving Type I and Type II crystals with different properties and improved storage stability
Solution Approach 2:
The patent utilizes phase transitions by inducing crystallization from liquid solution to solid crystal through controlled cooling and solvent evaporation, creating stable solid forms (Type I anhydrous crystal and Type II monohydrate crystal) that replace the unstable liquid form
2Manufacturing precision
If L-alpha-glyceryl phosphoryl choline is crystallized using conventional methods, then the purity is improved, but the crystals are very hygroscopic and fine in structure
Solution Approach 1:
The patent controls the water content parameter at 6-12% during crystallization and adjusts alcohol solvent composition to prevent excessive hygroscopicity while maintaining high purity, producing crystals with controlled crystal size and reduced harmful hygroscopic properties
Solution Approach 2:
The patent creates different local crystal structures (Type I anhydrous and Type II monohydrate) with distinct properties by controlling local crystallization conditions, achieving areas of high purity with reduced hygroscopicity through specific crystal lattice arrangements
3Ease of operation
If liquid L-alpha-glyceryl phosphoryl choline is used for formulation, then the manufacturing is simple, but the drug compliance is poor and complex manufacturing facilities are required
Solution Approach 1:
The patent transforms the liquid active ingredient into solid crystal forms (Type I and Type II), enabling diverse pharmaceutical formulations such as tablets and capsules that are easier to manufacture and administer, replacing the limited soft capsule format required for liquid forms
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 crystals offer improved drug compliance, easier manufacturing, and enhanced storage stability, replacing conventional liquid forms with powder-type formulations that are more patient-friendly and stable.
Implementation Method 1
the above-mentioned GPC was dissolved in methanol and n-butanol whose amount was 20 times the methanol solution was added to the methanol solution. Finally, the total solution was concentrated in vacuum, cooled, and filtered to recover an anhydrous form of crystal
Data Source
AI summary
The present invention relates to I- and II-type crystals of L-α-glyceryl phosphoryl choline, and to a method for preparing same. More particularly, the present invention relates to noble I- and II-type anhydride crystals of L-α-glyceryl phosphoryl choline, which have a higher purity than conventional liquid L-α-glyceryl phosphoryl choline, and one advantage of which is that formulations and dosages of pharmaceuticals are easily modified, and another advantage of which is that the hygroscopicity of the crystals are much lower than that of conventional polymorphic crystals, providing excellent stability during storage. The present invention also relates to a method for preparing the I- and II-type crystals of L-α-glyceryl phosphoryl choline.