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Synergistic effect of PEG-400 and cyclodextrin to enhance solubility of progesterone

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Conclusion

PEG-400, polysorbate 80, and 2 CDs (Trappsol HPB and Captisol) were used in an attempt to improve the aqueous solubility of a model hydrophobic drug, progesterone. The aqueous solubility of progesterone improved significantly from 0.007 mg/mL by the addition of PEG-400, CDs, and polysorbate 80. In systems containing various amounts of PEG-400 and 3% Trappsol HPB in water (% wt/wt), the theoretical solubility was calculated by adding the solubilities in the individual systems. The observed solubility values were up to 96% higher than the theoretical values. The effect of synergism was significant in 5% to 50% PEG-400/water systems containing Trappsol HPB. Systems containing Captisol did not show such synergistic effects. In general, the addition of polysorbate 80 to the PEG-400/water systems containing CDs affected synergism negatively.

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Correspondence to Hemant N. Joshi.

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Nandi, I., Bateson, M., Bari, M. et al. Synergistic effect of PEG-400 and cyclodextrin to enhance solubility of progesterone. AAPS PharmSciTech 4, 1 (2003). https://doi.org/10.1208/pt040101

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