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( Yi Dong Yan ),( Jun Ho Sung ),( Dong Won Lee ),( Jung Su Kim ),( Eun Mi Jeon ),( Dae Duk Kim ),( Dong Wuk Kim ),( Jong Oh Kim ),( Ming Guan Piao ),( Dong Xun Li ),( Chul Soon Yong ),( Han Gon Choi ) 영남대학교 약품개발연구소 2012 영남대학교 약품개발연구소 연구업적집 Vol.22 No.0
Various amide prodrugs of salicylic acid were synthesised, and their physicochemical propertiesincluding lipophilicity, chemical stability and enzymatic hydrolysis were investigated. In vivo skinpermeation and accumulation profiles were also evaluated using a combination of common permeationenhancing techniques such as the use of a supersaturated solution of permeants in an enhancer vehicle, a lipophilic receptor solution, removal of the stratum corneum and delipidisation of skin. Their capacity factor values were proportional to the degree of carbon-carbon saturation in the side chain. All these amides were highly stable in acetonitrile and glycerine. Amide prodrugs were converted tosalicylic acid both in hairless mouse liver and skin homogenates. N-dodecyl salicylamide (C12SM) showed the lowest permeation of salicylic acid in skin compared to the other prodrugs, probably due to its low aqueous solubility. It had a high affinity for the stratum corneum and its accumulation was restricted to only the uppermost layer of skin. Thus, this amide prodrug could be a safer topicalsunscreen agent with minimum potential for systemic absorption.ⓒ2011 Elsevier B.V.All rights reserved.
Dong Xun Li,Myo Jeong Han,Prabagar Balakrishnan,Yi Dong Yan,Dong Hoon Oh,Jung Hyun Joe,Youngee Seo,김종오,Sang Man Park,Chul Soon Yong,최한곤 대한약학회 2010 Archives of Pharmacal Research Vol.33 No.1
The main purpose of this study was to evaluate the effect of a mixed drug solution containing a surfactant and β-cyclodextrin (β-CD) on the solubility and bioavailability of a poorly watersoluble drug, flurbiprofen. Solubility, dissolution and in vivo pharmacokinetics of flurbiprofen in the presence of surfactant, β-CD or mixture of surfactant and β-CD were investigated. Among the surfactants tested, Tween 80 produced the highest improvement in the aqueous solubility of flurbiprofen. The solubility of flurbiprofen increased linearly as a function of β-CD, resulting in B8 type that suggested a formation of inclusion complex in a molar ratio of 1:1. The solubility of flurbiprofen increased further when Tween 80 was included in addition to β-CD, suggesting that a micelle formation in the presence of Tween 80 was the likely reason for additional increase. Furthermore, the data suggested that Tween 80 did not interfere with the inclusion interaction between flurbiprofen and β-CD. The solubility of flurbiprofen was the highest in the mixed system containing 1.3 mM β-CD and 0.3% w/v Tween 80, and the maximum solubility of 160 μg/mL was achieved. Consistent with the enhanced solubility, the plasma exposure (both AUC and Cmax) of flurbiprofen when dosed as the mixed system was significantly higher (as much as 2 to 3-fold) than that without surfactant or β-CD, with surfactant alone, or with β-CD alone. Therefore, the mixed system consists of surfactant and β-CD could be used as an effective oral dosage form to improve bioavailability of poorly water soluble drugs such as flurbiprofen.
( Dong Hoon Oh ),( Yi Dong Yan ),( Dong Wuk Kim ),( Jong Oh Kim ),( Chul Soon Yong ),( Han Gon Choi ) 영남대학교 약품개발연구소 2014 영남대학교 약품개발연구소 연구업적집 Vol.24 No.0
Objective: A novel flurbiprofen-loaded nanoemulsion which gave uniform emulsion droplets with a narrow size distribution was previously reported to be prepared using membrane emulsification method. The purpose of this study is to develop a novel flurbiprofen-loaded nanoparticle with a narrow size distribution and improved bioavailability. Method: The nanoparticle was prepared by solidifying nanoemulsion using sucrose as a carrier via spray drying method. Its physicochemical properties were investigated using SEM, DSC and PXRD. Furthermore, dissolution and bioavailability in rats were evaluated compared to a flurbiprofen-loaded commercial product. Results: The flurbiprofen-loaded nanoparticles with flurbiprofen/sucrose/surfactant mixture (1/20/2, weight ratio) gave good solidification and no stickiness. They associated with about 70,000-fold improved drug solubility and had a mean size of about 300 nm with a narrow size distribution. Flurbiprofen was present in a changed amorphous state in these nanoparticles. Moreover, the nanoparticles gave significantly shorter Tmax, and higher AUC and Cmax of the drug compared to the commercial product (p<0.05). In particular, they showed about nine-fold higher AUC of the drug than did the commercial product. Conclusion: These flurbiprofen-loaded nanoparticles prepared with sucrose by the membrane emulsification and spray drying method would be a potential candidate for orally delivering poorly water-soluble flurbiprofen with enhanced bioavailability.
Preparation and Evaluation of Taste-Masked Donepezil Hydrochloride Orally Disintegrating Tablets
Yan, Yi-Dong,Woo, Jong Soo,Kang, Joon Heok,Yong, Chul Soon,Choi, Han-Gon Pharmaceutical Society of Japan 2010 Biological & pharmaceutical bulletin Vol.33 No.8
<P>The purpose of this research was to prepare and evaluate a non-bitter donepezil hydrochloride (DH) orally disintegrating tablet (ODT) for enhanced patient compliance. Taste masking was done by preparing microspheres with different ratios of drug and Eudragit<SUP>®</SUP> EPO using spray drying method. The entrapment of the drug into microspheres was confirmed by scanning electron microscope (SEM) and X-ray powder diffraction. It was found that microspheres with a drug–polymer ratio of 1 : 2 could mask the taste obviously by inhibiting the release of DH in simulated salivary fluid. Microspheres-loaded tablets containing Polyplasdone NF and Low substituted Hydroxypropyl Cellulose (L-HPC) both at a 10% level showed rapid disintegration, <I>in vitro</I> (15.5 s) and <I>in vivo</I> (19.8 s), which were faster than that of marketed tablets (36.7, 41.3 s, respectively). Results from taste evaluation in human volunteers revealed that the ODTs with taste-masked microspheres had significantly enhanced palatability. Dissolution <I>in vitro</I> and pharmacokinetics in rats were evaluated for the tested ODTs compared to the donepezil hydrochloride commercial product (ARICEPT<SUP>®</SUP>). Both tablets showed comparable dissolution patterns <I>in vitro</I> and similar area under curve from 0 to 24 h (<I>AUC</I><SUB>0—24</SUB>), <I>C</I><SUB>max</SUB> and <I>T</I><SUB>max</SUB> of DH <I>in vivo</I> to each other, suggesting that the tested ODTs might give the similar drug efficacy in rats compared to that of ARICEPT<SUP>®</SUP>. Thus, it was concluded that DH ODTs with masked taste were obtained by Eudragit<SUP>®</SUP> EPO-based microspheres, drug loaded microspheres neither decreased the bioavailability nor delayed the release of DH.</P>
Yan, Yi-Dong,Marasini, Nirmal,Choi, Young Keun,Kim, Jong Oh,Woo, Jong Soo,Yong, Chul Soon,Choi, Han Gon Edifor] 2012 European journal of drug metabolism and pharmacoki Vol.37 No.3
<P>The present study investigated the effects of a curcumin self-emulsifying drug delivery systems (SEDDS) on the pharmacokinetics of orally administered docetaxel in rats. A single dose of docetaxel was orally administered (30 mg/kg) alone or after oral curcumin SEDDS (25, 50, 100 and 150 mg/kg) administration with time intervals of 0, 15 and 30 min, respectively. After oral administration, the C (max) and the area under the plasma concentration-time curve (AUC) of docetaxel were significantly increased (0 min, p < 0.05; 15 and 30 min, p < 0.01) by 2.2, 4.7 and 4.6 times and 2.0, 3.8 and 4.1 times compared to that of control group, respectively, after treatment with curcumin SEDDS (100 mg/kg) for each interval. Moreover, The C (max) of docetaxel was increased by 2.6 and 4.4 times in response to 25 and 50 mg/kg curcumin SEDDS treatment, respectively, the corresponding AUC was increased by about 2.4 and 3.1 times, and consequently the absolute bioavailabilities of docetaxel in these two treatment groups were 7.9 and 10.4%, respectively, which showed a significant increase of about 2.4- and 3.2-fold in comparison to the control value (3.3%). However, no further increase in either AUC or C (max) values of docetaxel was observed as the curcumin SEDDS dose was increased from 50 to 150 mg/kg. It is worth noting that the presence of curcumin SEDDS did not significantly decrease the systemic clearance, which was shown by the almost unchanged terminal half-life (t (1/2)) of docetaxel in all treatment groups. Thus, the enhanced bioavailability of oral docetaxel by curcumin SEDDS seemed to be likely due to an inhibition function of cytochrome P450 (CYP) 3A and P-glycoprotein (Pgp) in the intestines of the rats. However, further in vivo studies are needed to verify these hypotheses.</P>
Hydrogels with diffusion-facilitated porous network for improved adsorption performance
Yan-yan Pei,Dong-mei Guo,Qing-da An,Zuo-yi Xiao,Shangru Zhai,Bin Zhai 한국화학공학회 2018 Korean Journal of Chemical Engineering Vol.35 No.12
Porous alginate-based hydrogel beads (porous ABH) have been prepared through a facile and sustainable template-assisted method using nano-calcium carbonate and nano-CaCO3 as pore-directing agent for the efficient capture of methylene blue (MB). The materials were characterized by various techniques. The sorption capacities of ABH towards MB were compared with pure sodium alginate (ABH-1:0) in batch and fixed-bed column adsorption studies. The obtained adsorbent (ABH-1:3) has a higher BET surface area and a smaller average pore diameter. The maximum adsorption capacity of ABH-1:3 obtained from Langmuir model was as high as 1,426.0mg g1. The kinetics strictly followed pseudo-second order rate equation and the adsorption reaction was effectively facilitated, approximately 50minutes to achieve adsorption equilibrium, which was significantly shorter than that of ABH-1:0. The thermodynamic parameters revealed that the adsorption was spontaneous and exothermic. Thomas model fitted well with the breakthrough curves and could describe the dynamic behavior of the column. More significantly, the uptake capacity of ABH-1:3 was still higher than 75% of the maximum adsorption capacity even after ten cycles, indicating that this novel adsorbent can be a promising adsorptive material for removal of MB from aqueous solution under batch and continuous systems.
Yan, Yi-Dong,Kim, Jung Ae,Kwak, Mi Kyung,Yoo, Bong Kyu,Yong, Chul Soon,Choi, Han-Gon Pharmaceutical Society of Japan 2011 Biological & pharmaceutical bulletin Vol.34 No.8
<P>In this study, a novel liquid self-emulsifying drug delivery system (SEDDS) containing curcumin was formulated and further developed into a solid form by a spray drying method using Aerosil 200 as the solid carrier. The optimum liquid SEDDS consisted of Lauroglycol Fcc, Labrasol and Transcutol HP as the oil phase, the surfactant and the co-surfactant at a weight ratio of 15.0 : 70.8 : 14.2 (w/w/w), respectively. There was no difference in droplet size between the emulsions obtained from the liquid and solid forms of SEDDS. Solid state characterization of the solid SEDDS was performed by scanning electron micrograph (SEM), differential scanning calorimetry (DSC), and X-ray powder diffraction (XRPD). The drug formulated in the solid SEDDS was quickly and completely dissolved within 5 min, both in 0.1 <SMALL>N</SMALL> HCl and phosphate buffer pH 6.8 dissolution media, whereas crude curcumin powder was significantly less dissoluble. The solid SEDDS formulation was stable for at least 3 months at 40°C with 75% relative humidity. After oral administration to rats, curcumin in the solid SEDDS resulted in significant improvement in <I>in vivo</I> absorption compared with that of curcumin powder. As the dose of curcumin formulated in solid SEDDS increased from 25 to 100 mg/kg, the <I>C</I><SUB>max</SUB> and area under the drug concentration time curve (<I>AUC</I>) of curcumin were increased by 4.6 and 7.6 times, respectively. However, the over-proportional increase in the <I>AUC</I> in the higher dose group might be due to underestimation of <I>AUC</I> in the lower dose group. In conclusion, this solid SEDDS is a promising solid dosage form for poorly water-soluble curcumin.</P>