Synergistic effect of PEG-400 and cyclodextrin to enhance solubility of progesterone |
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Authors: | Indranil Nandi Michelle Bateson Mohammad Bari Hemant N Joshi |
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Institution: | (1) Geneva Pharmaceutical Technology Corp, 2400 Route 130 North, 08810 Dayton, NJ;(2) Galen Limited, Millbrook, BT40 2SH Larne, Northern Ireland;(3) Forest Laboratories Inc, 330 Prospect Street, 11096 Inwood, NY;(4) Barr Laboratories, Pharmaceutical Research & Development, 2 Quaker Road, 10970 Pomona, NY |
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Abstract: | 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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Keywords: | cosolvent cyclodextrins PEG-400 progesterone solubilization synergism |
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