Table 1.
Optimization of CBZ-β-CD complexes using HLE process
| Batch | Drug:β-CD molar ratio | Screw speed (rpm) | Solvent composition | Temperature of barrel (°C) | Solubility (mg/mL) | ||
|---|---|---|---|---|---|---|---|
| B2 | B3 | B4 | |||||
| Optimization of screw speed | |||||||
| CBS-1 | 1:1 | 25 | Water | 32 | 30 | 30 | 1.72 ± 0.04 |
| CBS-2 | 1:1 | 35 | Water | 32 | 30 | 30 | 1.47 ± 0.01 |
| CBS-3 | 1:1 | 50 | Water | 32 | 30 | 30 | 1.67 ± 0.03 |
| CBS-4 | 1:1 | 65 | Water | 32 | 30 | 30 | 1.74 ± 0.04 |
| CBS-5 | 1:1 | 80 | Water | 32 | 30 | 30 | 1.87 ± 0.03 |
| CBS-6 | 1:1 | 100 | Water | 32 | 30 | 30 | 1.78 ± 0.01 |
| CBS-7 | 1:1 | 150 | Water | 32 | 30 | 30 | 1.71 ± 0.01 |
| CBS-8 | 1:1 | 200 | Water | 32 | 30 | 30 | 1.65 ± 0.01 |
| CBS-9 | 1:1 | 250 | Water | 32 | 30 | 30 | 2.11 ± 0.01 |
| Optimization of solvent composition | |||||||
| CBS-5 | 1:1 | 80 | Water | 32 | 30 | 30 | 1.87 ± 0.03 |
| CBP-1 | 1:1 | 80 | Hydrochloric acid buffer pH 1.2 | 32 | 30 | 30 | 2.00 ± 0.01 |
| CBP-2 | 1:1 | 80 | Alkaline phosphate buffer pH 4.0 | 32 | 30 | 30 | 1.73 ± 0.008 |
| CBP-3 | 1:1 | 80 | Acetate buffer pH 4.6 | 32 | 30 | 30 | 2.18 ± 0.05 |
| CBP-4 | 1:1 | 80 | Neutralized phthalate buffer pH 5.0 | 32 | 30 | 30 | 4.27 ± 0.09 |
| CBP-5 | 1:1 | 80 | Phosphate buffer pH 5.8 | 32 | 30 | 30 | 1.84 ± 0.01 |
| CBP-6 | 1:1 | 80 | Phosphate buffer pH 6.8 | 32 | 30 | 30 | 1.87 ± 0.004 |
| CBP-7 | 1:1 | 80 | Phosphate buffer pH 7.4 | 32 | 30 | 30 | 1.75 ± 0.007 |
| CBP-8 | 1:1 | 80 | Alkaline borate buffer pH 9.2 | 32 | 30 | 30 | 1.84 ± 0.03 |
| Optimization of temperature | |||||||
| CBP-4 | 1:1 | 80 | Neutralized phthalate buffer pH 5.0 | 32 | 30 | 30 | 4.27 ± 0.09 |
| CBT-1 | 1:1 | 80 | Neutralized phthalate buffer pH 5.0 | 40 | 40 | 40 | 2.24 ± 0.01 |
| CBT-2 | 1:1 | 80 | Neutralized phthalate buffer pH 5.0 | 50 | 50 | 50 | 2.06 ± 0.01 |
| CBT-3 | 1:1 | 80 | Neutralized phthalate buffer pH 5.0 | 60 | 60 | 60 | 1.94 ± 0.01 |
| CBT-4 | 1:1 | 80 | Neutralized phthalate buffer pH 5.0 | 70 | 70 | 70 | 2.15 ± 0.01 |
| CBT-5 | 1:1 | 80 | Neutralized phthalate buffer pH 5.0 | 80 | 80 | 80 | 2.01 ± 0.01 |
| CBT-6 | 1:1 | 80 | Neutralized phthalate buffer pH 5.0 | 90 | 90 | 90 | 2.31 ± 0.016 |
| CBT-7 | 1:1 | 80 | Neutralized phthalate buffer pH 5.0 | 100 | 100 | 100 | 2.15 ± 0.007 |
| Optimization of molar ratio | |||||||
| CBP-4 | 1:1 | 80 | Neutralized phthalate buffer pH 5.0 | 32 | 30 | 30 | 4.27 ± 0.09 |
| CBR-1 | 1:0.5 | 80 | Neutralized phthalate buffer pH 5.0 | 32 | 30 | 30 | 2.10 ± 0.007 |
| CBR-2 | 1:2 | 80 | Neutralized phthalate buffer pH 5.0 | 32 | 30 | 30 | 2.24 ± 0.03 |