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KMID : 0369820110410040249
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Jorunal of Korean Pharmaceutical Sciences
2011 Volume.41 No. 4 p.249 ~ p.253
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Preparation and in vivo Evaluation of a Sildenafil Lactate-loaded Solid Self-emulsifying Drug Delivery System
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Jung Si-Young
Kim Dong-Wuk
Lee Dong-Won
Woo Jong-Soo
Kim Jong-Oh
Yong Chul-Soon
Choi Han-Gon
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Abstract
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To develop a sildenafil lactate-loaded solid self-emulsifying drug delivery system (SEDDS) with a fast onset of action and immediate action of erection, sildenafil lactate (0.3 g), which was prepared using a spray dryer, was dissolved in 4.7 g of the mixture of glyceryl monooleate/Transcutol/ Tween 20 (3/0.5/1, g). Its emulsion droplet size and pharmacokinetics in rabbits were evaluated compared with sildenafil citrate-loaded commercial tablet. The sildenafil lactateloaded SEDDS showed an emulsion droplet size of about 300 nm. In pharmacokinetics study, it gave significantly faster Tmax than did the commercial tablet. Thus, the sildenafil lactate-loaded SEDDS at the one-third drug dose compared to sildenafil citrate-loaded conventional tablet might induce a fast onset of action and immediate erection without enhanced bioavailability compared with the sildenafil citrate-loaded commercial tablet.
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KEYWORD
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Sildenafil lactate, SEDDS, Immediate erection, Pharmacokinetics
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