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[Polymorphism of the 5R-5-hydroxytriptolide].

Rui-li Liu¹, Ya-xi Yang, Dong-ying Chen

¹Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.

Yao Xue Xue Bao = Acta Pharmaceutica Sinica

|January 21, 2012

Summary

This summary is machine-generated.

This study characterized the solid-state polymorph of 5R-5-hydroxytriptolide (LLDT-8), a rheumatoid arthritis drug candidate. Consistent characterization across methods confirmed its stability, ensuring therapeutic efficacy during clinical trials.

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Published on: January 21, 2020

Area of Science:

Pharmaceutical Sciences
Solid-State Chemistry
Crystallography

Context:

5R-5-hydroxytriptolide (LLDT-8) is an investigational drug for rheumatoid arthritis undergoing clinical trials.
Understanding the solid-state properties, specifically polymorphism, is crucial for drug development and ensuring consistent efficacy.

Purpose:

To perform polymorph screening of 5R-5-hydroxytriptolide (LLDT-8).
To characterize the identified polymorph using various analytical techniques.
To confirm the stability of the LLDT-8 solid form.

Summary:

LLDT-8 was crystallized using evaporative and antisolvent methods. Characterization via p-XRD, IR, DSC, and TG revealed consistent results, indicating a stable solid form.
Key p-XRD peaks were observed at specific 2θ values, and IR spectra showed characteristic absorption bands. DSC and TG determined a decomposition temperature of 271.2°C.
Single crystal X-ray diffraction identified LLDT-8 as a monoclinic crystal (space group P2(1)) forming a hydrogen-bonded dimer. Slurry experiments further confirmed solid-state stability across different solvent polarities.

Impact:

The consistent characterization and confirmed stability of the LLDT-8 polymorph provide a solid foundation for its continued clinical development.
This research assures the consistency of LLDT-8's efficacy in clinical trials by establishing its reliable solid-state form.
The findings contribute to the understanding of triptolide derivatives' solid-state behavior, aiding future drug design and formulation.