Overcoming Solubility Challenges: Micronization of Berberine Using the GAS Antisolvent Technique

克服溶解度难题:利用GAS反溶剂技术对小檗碱进行微粉化

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Abstract

Berberine is a compound widely used in Chinese herbal medicine. It can potentially treat diabetes, cholesterol, and mental illnesses and has antimicrobial effects. However, its application is limited due to its low solubility in water, thus limiting its bioavailability. Micronization techniques are used to increase the surface area and improve the dissolution rate. The micronized particles were produced using the antisolvent GAS technique at a temperature of 35 °C and 80 bar. A solubility study with acetone, dichloromethane, ethanol, methanol, 1-butanol, and 1-propanol was carried out. Fourier-transform infrared spectroscopy analysis confirmed the preservation of functional groups. Additionally, a reduction in particle size to 6.34 μm was achieved, which contributed to an increase of up to 18% in cumulative dissolution. Furthermore, an increase in melting temperature and dissolution rate was observed. Thus, the antisolvent GAS technique proves to be an efficient approach for particle micronization and the consequent enhancement of dissolution properties.

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