Comparison of the Solubility and Pharmacokinetics of Sildenafil Salts

Title
Comparison of the Solubility and Pharmacokinetics of Sildenafil Salts
Author(s)
용철순정시영[정시영]서윤기[서윤기]김건국[김건국]우종수[우종수]최한곤[최한곤]
Keywords
PHOSPHODIESTERASE-5 INHIBITORS; ERECTILE DYSFUNCTION; BIOAVAILABILITY; CITRATE; ENHANCEMENT; IBUPROFEN; RATS
Issue Date
201103
Publisher
PHARMACEUTICAL SOC KOREA
Citation
ARCHIVES OF PHARMACAL RESEARCH, v.34, no.3, pp.451 - 454
Abstract
To develop sildenafil lactate, a salt form of sildenafil with improved solubility and bioavailability of poorly water-soluble sildenafil base, this salt form was prepared using a spray dryer. Its solubility and pharmacokinetics in rabbits were evaluated compared with sildenafil base and sildenafil citrate. Sildenafil lactate improved the solubility of sildenafil in various solvents including distilled water compared with sildenafil citrate. It provided higher AUC and C(max) and, shorter t(1/2) values than did the other materials, indicating that it improved the oral bioavailability of sildenafil in rabbits. Our results suggest that sildenafil lactate would be useful to deliver sildenafil in a pattern that allows fast absorption and late metabolism. Furthermore, the plasma concentration at 0.25 h in sildenafil lactate was similar to the C, value at T(max) (0.5 h) in sildenafil citrate. Thus, sildenafil lactate might provide a faster onset of action and immediate erection compared with sildenafil citrate, the conventional drug.
URI
http://hdl.handle.net/YU.REPOSITORY/25579http://dx.doi.org/10.1007/s12272-011-0313-y
ISSN
0253-6269
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약학대학 > 약학부 > Articles
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