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http://dx.doi.org/10.4333/KPS.2011.41.4.249

Preparation and in vivo Evaluation of a Sildenafil Lactate-loaded Solid Self-emulsifying Drug Delivery System  

Jung, Si-Young (College of Pharmacy, Yeungnam University)
Kim, Dong-Wuk (College of Pharmacy, Hanyang University)
Lee, Dong-Won (College of Pharmacy, Yeungnam University)
Woo, Jong-Soo (Pharmaceutical Research Center, Hanmi Pharm. Co.)
Kim, Jong-Oh (College of Pharmacy, Yeungnam University)
Yong, Chul-Soon (College of Pharmacy, Yeungnam University)
Choi, Han-Gon (College of Pharmacy, Hanyang University)
Publication Information
Journal of Pharmaceutical Investigation / v.41, no.4, 2011 , pp. 249-253 More about this Journal
Abstract
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.
Keywords
Sildenafil lactate; SEDDS; Immediate erection; Pharmacokinetics;
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1 Wang, Y., Chow, M.S., Zuo, Z., 2008. Mechanistic analysis of pHdependent solubility and trans-membrane permeability of amphoteric compounds: application to sildenafil. Int. J. Pharm. 352, 217-224.   DOI
2 Gratz, S.R., Flurer, C.L., Wolnik, K.A., 2004. Analysis of undeclared synthetic phosphodiesterase-5 inhibitors in dietary supplements and herbal matrices by LC-ESI-MS and LC-UV. J. Pharm. Biomed. Anal. 36(3), 525-533.   DOI
3 Jung, S.J., Seo, Y.G., Kim, G.K., Woo, J.S., Yong, C.S., Choi, H.G., 2011. Comparison of the solubility and pharmacokinetics of sildenafil salts, Arch. Pharm. Res. 34(3) 451-454.   DOI
4 Li, D.X., Han, M.J., Balakrishnan, P., Yan, Y.D., Oh, D.H., Joe, J.H., Seo, Y.G., Kim, J.O., Park, S.M., Yong, C.S., Choi, H.G., 2010. Enhanced oral bioavailability of flurbiprofen by combined use of micelle solution and inclusion compound. Arch. Pharm. Res. 33, 95-101.   과학기술학회마을   DOI
5 Nichols, D.J., Muirhead, G.J., Harness, J.A., 2002. Pharmacokinetics of sildenafil after single oral doses in healthy male subjects: absolute bioavailability, food effects and dose proportionality. Br. J. Clin. Pharmacol. 53 (Suppl 1), 5S-12S.   DOI
6 Quintero, A., Caldera, A., Milano, B., Odreman, I., Hurtado, A., Manzanares, L., Villamizar, J., 2009. Validation of an HPLC method for sildenafil citrate analysis in human plasma samples. Pharmazie 64(12), 796-799.
7 Shah, N.H., Carvajal, M.T., Patel, C.I., Infeld, M.H., Malick, A.W., 1994. Self-emulsifying drug delivery systems (SEDDS) with polyglycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs. Int. J. Pharm. 106, 15-23.   DOI
8 Shin, H.S., Bae, S.K., Lee, M.G., 2006. Pharmacokinetics of sildenafil after intravenous and oral administration in rats: Hepatic and intestinal first-pass effects. Int. J. Pharm. 320, 64-70.   DOI
9 Society of Toxicology (SOT), 2008. Guiding Principles in the Use of Animals in Toxicology. www.toxicology.org/AI/FA/guidingprinciples.pdf
10 Amidon, G.L., Lennernas, H., Shah, V.P., Crison, J.R., 1995. A theoretical basis for a biopharmaceutics drug classification : the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm. Res. 12, 413-420.   DOI
11 Balakrishnan, P., Lee, B.J., Oh, D.H., Kim, J.O., Lee, Y.I., Kim, D.D., Jee, J.P., Lee, Y.B., Woo, J.S., Yong, C.S., Choi, H.G., 2009. Enhanced oral bioavailability of Coenzyme Q10 by selfemulsifying drug delivery systems. Int. J. Pharm. 374, 66-72.   DOI   ScienceOn
12 Boolell, M., Gepi-Attee, S., Gingell, J.C., Allen, M.J., 1996. Sildenafil, a novel effective oral therapy for male erectile dysfunction. Br. J. Urol. 184, 63-72.
13 Choi, H.G., Oh, Y.K., Kim, C.K., 1998. In-situ gelling and mucoadhesive liquid suppository containing acetaminophen: enhanced bioavailability. Int. J. Pharm. 165, 23-32.   DOI
14 Eardly, I., Ellis, P., Boolell, M., Wulff, M., 2002. Onset and duration of action of sildenafil citrate treatment of erectile dysfunction. Br. J. Clin. Pharmacol. 53, 61S-65S.   DOI
15 Elshafeey, A.H., Bendas, E.R., Mohamed, O.H., 2009. Intranasal microemulsion of sildenafil citrate: in vitro evaluation and in vivo pharmacokinetic study in rabbits. AAPS PharmSciTech. 10(2), 361-367.   DOI