• Journal of Pharmaceutical Investigation
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• 제41권4호
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• pp.249-253
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• 2011

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.

• Journal of Pharmaceutical Investigation
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• 제29권2호
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• pp.99-103
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• 1999

Self-Emulsifying System(SES), an isotropic mixture of oil and surfactant which forms oil-in-water emulsion, is expected to improve in vitro drug dissolution and enhance in vivo drug absorption. A poorly water soluble drug, ibu-profen(IBP) was incorporated into the SES to improve absorption, and enhance bioavailability of drug. Medium chain triglyceride, glyceryl tricaprylate(GTC) as an oil, and Tween 85 as a surfactant were used to formulate SES. To characterize SESs with various concentrations of Tween 85, the phase separation and solubility of IBP-SEDDS containing IBP as a function of Tween 85 concentration were conducted, and the particle size was measured using photon correlation spectroscopic method. The SES with optimal concentration of Tween 85(35%(w/w)) was selected based on its high drug loading, small particle size and low surfactant concentration. After an oral administration of IBP-SEDDS and IBP suspension in methyl cellulose equivalent to 40.0 mg/kg to rats, the pharmacokinetic parameters were compared. The $C_{max}(163.17\;vs\;88.82\;{\mu}g/ml)$, $AUC(12897.01\;vs\;8751.13\;{\mu}g\;min/ml)$ and Bioavailability(86.44 vs 58.65%) significantly increased but $T_max(10\;vs\;20\;min)$ was significantly advanced. The current SEDDS containing IBP provide an alternative to improve an oral bio-availability of IBP.

• Preventive Nutrition and Food Science
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• 제2권3호
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• pp.255-258
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• 1997

Isoflavones are associated with prevention of chronic diseases such as cancer, osteoporosis, and hypercholesterolemia. The isoflavone contents at different development stages of soybean were anayzed to examine the period of their formation and reaching maximum level. Soybean sedds have been collected from 13th to 21st week after sowing. Total daidzein and genistein contents increased from 115 and 37mg/kg at 13th week, to 795 and 699mg/kg at 21st week, respectively. Total glycitein content showed less remarkable change during seed development than other isoflavones. Thus mature soybean may have maximum preventive effect from chronic diseases since it contains the highest level of isoflavones.