Comparison of the solubility and pharmacokinetics of sildenafil salts

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 c...

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Published in:Archives of pharmacal research 2011, 34(3), , pp.451-454
Main Authors: Jung, Si-Young, Seo, Youn-Gee, Kim, Gun Kook, Woo, Jong Soo, Yong, Chul Soon, Choi, Han-Gon
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Area Under Curve
Biological Availability
Drug Compounding
Erectile Dysfunction - drug therapy
Male
Medicine
Pharmacology/Toxicology
Pharmacy
Piperazines - blood
Piperazines - chemistry
Piperazines - pharmacokinetics
Piperazines - pharmacology
Purines - blood
Purines - chemistry
Purines - pharmacokinetics
Rabbits
Sildenafil Citrate
Solubility
Structure-Activity Relationship
Sulfones - blood
Sulfones - chemistry
Sulfones - pharmacokinetics
Sulfones - pharmacology
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Summary: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 max 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.
ISSN:0253-6269
1976-3786
DOI:10.1007/s12272-011-0313-y