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Published on: February 3, 2023
Effect of amorphization method on telmisartan solubility and the tableting process.
P Lepek1, W Sawicki, K Wlodarski
1Department of Physical Chemistry, Medical University of Gdansk, Gdansk, Poland.
Summary
Amorphous telmisartan (TLM) significantly enhances solubility and dissolution compared to its crystalline form. This improved physicochemical property is crucial for developing effective amorphous TLM tablet formulations.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Chemical Engineering
Background:
- Telmisartan (TLM), an angiotensin II receptor antagonist, exhibits poor water solubility in its crystalline form.
- Improving the physicochemical properties of poorly soluble drugs is essential for enhanced bioavailability and therapeutic efficacy.
Purpose of the Study:
- To transform crystalline telmisartan (TLM) into its amorphous state using melt quench and cryogenic grinding techniques.
- To evaluate the impact of amorphization on TLM's solubility, chemical stability, and tableting properties.
- To compare the performance of amorphous TLM formulations with crystalline TLM tablets.
Main Methods:
- Amorphous TLM was prepared using melt quench and cryogenic grinding.
- Chemical stability was assessed via high-performance liquid chromatography.
- Amorphous state confirmation utilized differential scanning calorimetry and X-ray powder diffraction.
- Solubility studies were conducted in various media (0.1M HCl, phosphate buffer pH 6.8, water) at different temperatures.
- Tablet formulations were prepared and evaluated for physical properties and dissolution.
Main Results:
- Both melt quench and cryogrinded amorphous TLM exhibited significantly higher solubility than crystalline TLM.
- The amorphous forms demonstrated good chemical stability during preparation.
- Differential scanning calorimetry indicated a glass transition at T(g)=401K for amorphous TLM.
- Dissolution tests showed improved performance for amorphous TLM formulations.
Conclusions:
- Amorphization effectively enhances the solubility and dissolution rate of telmisartan.
- Amorphous TLM is suitable for developing improved tablet formulations with better therapeutic potential.
- The study highlights the importance of solid-state transformation for optimizing drug delivery systems.
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