| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 227083 | Journal of Industrial and Engineering Chemistry | 2015 | 4 Pages |
•A new SMX–l-malic acid cocrystal was successfully synthesized by GAS.•SMX in the cocrystals obtained from GAS could dissolve 90% within 4.2 min.•SMX–l-malic acid cocrystal can dissolve faster than the commercial micronized SMX.
The objective of this work was to enhance the dissolution rate of a poorly water-soluble antibiotic drug, sulfamethoxazole (SMX), by forming cocrystal with l-malic acid (MA) using gas anti-solvent (GAS) process. The effect of SMX to MA mass ratio (2:1, 1.5:1 and 1:1) on drug content and dissolution rate was investigated. The GAS cocrystallization was carried out at 45 °C using the drug concentration of 50% saturation in acetone. It was found that cocrystals produced from SMX to MA ratio of 2:1 had higher drug content than those produced from the ratios 1.5:1 and 1:1. In the dissolution studies, it was found that 90% of SMX in the cocrystals could be dissolved within 4.2 min, whereas the times required to dissolve 90% of the drug in the physical mixtures were 8.2 min (ratio 1:1) and 25 min (ratio 2:1), and up to 28 min for the micronized SMX.
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