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Kim, Dong Shik,Yang, Eun Su,Yong, Chul Soon,Youn, Yu Seok,Oh, Kyung Taek,Li, Dong Xun,Kim, Jong Oh,Jin, Sung Giu,Choi, Han-Gon Elsevier 2017 Colloids and Surfaces B Vol.160 No.-
<P><B>Abstract</B></P> <P>The purpose of this study was to assess the impact of inorganic mesoporous carriers on the physicochemical properties and oral bioavailability of 1-palmitoyl-2-linoleoyl-3-acetyl-<I>rac</I>-glycerol (PLAG)-loaded solid self-emulsifying drug delivery system (solid SEDDS). Numerous PLAG-loaded solid SEDDS formulations were prepared by spray drying technique with sodium laurylsulfate (SLS), butylated hydroxyanisole (BHA) and inorganic mesoporous materials as a surfactant, antioxidant and solid carrier, respectively. The mesoporous materials, such as calcium silicate, silicon dioxide and magnesium aluminosilicate were used as the solid carriers. Their physicochemical properties, solubility, dissolution and pharmacokinetic studies in rats were performed compared with drug alone. Three solid SEDDSs composed of PLAG/BHA/SLS/mesopous carrier at the weight ratio of 1:0.0002:0.25:0.5 resulted in a small emulsion droplet and excellent drug loading efficiency. The solid SEDDS formulations prepared with calcium silicate and silicon dioxide showed a rough-surfaced irregular shape and rough-surfaced spheres, respectively. Magnesium aluminosilicate generated a sticky powder, due to its relatively low specific surface area, resulting in insufficient adsorption of PLAG. These solid SEDDSs improved the solubility, dissolution and oral bioavailability of PLAG. Ultimately, the solid SEDDS prepared with silicon dioxide resulted in the best drug loading efficiency, shape, solubility, dissolution and oral bioavailability due to its great specific surface area. Therefore, mesoporous carriers with different specific surface areas markedly influenced the physicochemical properties, solubility, dissolution and oral bioavailability of PLAG-loaded solid SEDDS.</P> <P><B>Highlights</B></P> <P> <UL> <LI> The effect of mesoporous carriers on PLGA-loaded solid SEDDS were assessed. </LI> <LI> Numerous PLGA-loaded solid SNEDDS were prepared using spray drying technique. </LI> <LI> Calcium silicate, silicon dioxide and magnesium aluminosilicate were used as the mesoporous carriers. </LI> <LI> The solid SEDDS prepared with silicon dioxide gave most excellent loading efficiency and bioavailability. </LI> <LI> Mesoporous carriers markedly influenced the physicochemical properties and bioavailability of solid SEDDS. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Li, Dong Xun,Park, Jung-Gil,Han, Hong-Hee,Yang, Chan-Woo,Choi, Jun-Young,Oh, Dong-Hoon,Yong, Chul-Soon,Choi, Han-Gon The Korean Society of Pharmaceutical Sciences and 2007 Journal of Pharmaceutical Investigation Vol.37 No.5
Poorly water-soluble ibuprofen and ethanol can be encapsulated in gelatin microcapsule by spray drying technique. To select an optimal formula of ibuprofen-loaded gelatin microcapsule which increased the ethanol content and ibuprofen solubility with the decreased amount of gelatin in the microcapsules, in this study, the effect of gelatin, ibuprofen and sodium lauryl sulfate on the ibuprofen solubility and the amount of ethanol and ibuprofen encapsulated in the gelatin microcapsule were investigated. Ibuprofen solubility and the amount of ethanol encapsulated increased as gelatin and sodium lauryl sulfate increased, reached maximum at 4% and 0.6%, respectively and then followed a rapid decrease. Furthermore, the ibuprofen solubility and the encapsulated ibuprofen content increased as the amount of ibuprofen increased, reaching maximum at 0.5% and beyond that, there was no change in the solubility and ibuprofen content. However, the encapsulated ethanol content remained same irrespective of the amount of ibuprofen. On the basis of increased ibuprofen solubility, our results showed that the formula of ibuprofen-loaded gelatin microcapsule at the ratio of gelatin/ibuprofen/sodium lauryl sulfate/water/ethanol of 4/0.5/0.6/30/70 with ibuprofen solubility of about $290\;{\mu}g/mL$ and ethanol content of about $160\;{\mu}g/mg$ could be a potential oral delivery system for poorly water-soluble ibuprofen.
Li, Dong Xun,Jang, Ki-Young,Kang, Wonku,Bae, Kyoungjin,Lee, Mann Hyung,Oh, Yu-Kyoung,Jee, Jun-Pil,Park, Young-Joon,Oh, Dong Hoon,Seo, Youn Gee,Kim, Young Ran,Kim, Jong Oh,Woo, Jong Soo,Yong, Chul Soon Pharmaceutical Society of Japan 2010 Biological & pharmaceutical bulletin Vol.33 No.2
<P>To develop a novel sibutramine base-loaded solid dispersion with improved solubility bioavailability, various solid dispersions were prepared with water, hydroxypropylmethyl cellulose (HPMC), poloxamer and citric acid using spray-drying technique. The effect of HPMC, poloxamer and citric acid on the aqueous solubility of sibutramine was investigated. The physicochemical properties of solid dispersion were investigated using scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray powder diffraction. The dissolution and pharmacokinetics in rats of solid dispersion were evaluated compared to the sibutramine hydrochloride monohydrate-loaded commercial product (Reductil<SUP>®</SUP>). The sibutramine base-loaded solid dispersion gave two type forms. Like conventional solid dispersion system, one type appeared as a spherical shape with smooth surface, as the carriers and drug with relatively low melting point were soluble in water and formed it. The other appeared as an irregular form with relatively rough surface. Unlike conventional solid dispersion system, this type changed no crystalline form of drug. Our results suggested that this type was formed by attaching hydrophilic carriers to the surface of drug without crystal change, resulting from changing the hydrophobic drug to hydrophilic form. The sibutramine-loaded solid dispersion at the weight ratio of sibutramine base/HPMC/poloxamer/citric acid of 5/3/3/0.2 gave the maximum drug solubility of about 3 mg/ml. Furthermore, it showed the similar plasma concentration, area under the curve (<I>AUC</I>) and <I>C</I><SUB>max</SUB> of parent drug, metabolite I and II to the commercial product, indicating that it might give the similar drug efficacy compared to the sibutramine hydrochloride monohydrate-loaded commercial product in rats. Thus, this solid dispersion system would be useful to deliver poorly water-soluble sibutramine base with enhanced bioavailability.</P>
Li, Dong Xun,Park, Young-Joon,Oh, Dong Hoon,Joe, Kwan Hyung,Lee, Jung Hoon,Yeo, Woo Hyun,Yong, Chul Soon,Choi, Han-Gon Pharmaceutical Society of Great Britain 2010 Journal of pharmacy and pharmacology Vol.62 No.4
<P>OBJECTIVES: The aim of this study was to develop a novel itraconazole-loaded gelatin microcapsule without ethanol with enhanced oral bioavailability. METHODS: Various gelatin microcapsules were prepared using a spray-drying technique. Their physicochemical properties, dissolution, characteristics and pharmacokinetics in rats were evaluated and compared with those of a commercial product. KEY FINDINGS: The gelatin microcapsule at a weight ratio for itraconazole/gelatin/citric acid of 1 : 3 : 0.3 was spherical in shape with a smooth surface and inner hole, and gave a maximum drug solubility of about 700 microg/ml. The gelatin microcapsule dramatically increased the initial dissolution rate of itraconazole compared with a commercial product in simulated gastric fluids (pH 1.2). Moreover, at the same dose as the commercial product, it gave significantly higher initial plasma concentrations, C(max) and AUC of itraconazole in rats than did the commercial product, indicating that providing the drug in the gelatin microcapsule caused enhanced absorption in rats. At half dose, it gave similar AUC, C(max) and T(max) values to the commercial product, suggesting that it was bioequivalent to the commercial product in rats. CONCLUSIONS: The itraconazole-loaded gelatin microcapsule without ethanol developed using a spray-drying technique at half the dose of the commercial product can deliver itraconazole in a pattern that allows fast absorption in the initial phase, making it bioequivalent to the commercial product.</P>
Numerical simulation and experiments of magnetic flux leakage inspection in pipeline steel
Xun-Bo Li,Xiang Li,Liang Chen,Pei-Fu Feng,Hai-Dong Wang,Zuo-Ying Huang 대한기계학회 2009 JOURNAL OF MECHANICAL SCIENCE AND TECHNOLOGY Vol.23 No.1
The magnetic flux leakage (MFL) method is currently the most commonly used pipeline inspection technique. In this paper, numerical simulation and experimental investigation on defect inspection in pipeline steel using MFL were carried out. In theoretical analysis, typical three-dimensional (3D) defects were accurately modeled and detailed MFL signals in the test surface were calculated by 3D finite element method (FEM). To confirm the 3D FEM results, different artificial defects were made and the MFL experiments were performed. The experimental study demonstrated that the results were agreement with the 3D FEM result. The results show that the 3D FEM is an effective analysis method for pipeline steel MFL inspection.
Development of Nifedipine-loaded Coated Gelatin Microcapsule as a Long Acting Oral Delivery
Dong Xun Li,오동훈,강진양,최종서,우종수,용철순,최한곤,김종오,이원석,홍명자 대한약학회 2009 Archives of Pharmacal Research Vol.32 No.1
To develop the long acting nifedipine oral delivery with enhanced bioavailability, nifedipine-loaded gelatin microcapsule containing nifedipine and ethanol in gelatin shell was prepared using a spray-dryer, and then coated microcapsule was prepared by coating the gelatin microcapsule with Eudragit acrylic resin. The dissolution test and the bioavailability of the coated microcapsule in rats were evaluated compared to nifedipine powder. The amount of nifedipine dissolved from gelatin microcapsule for 30 min increased about 5-fold compared to nifedipine powder in pH 1.2 simulated gastric fluid. Nifedipine released from the coated microcapsule was retarded in pH 1.2 simulated gastric fluid compared with that from gelatin microcapsule. Furthermore, the coated gelatin microcapsule maintained the plasma level of nifedipine over 4 h and gave significantly higher AUC of nifedipine than nifedipine powder. Thus, the Eudragit-coated gelatin microcapsule, which could maintain the plasma level of nifedipine over a longer period without the initial burst-out plasma concentration, is a preferable delivery system for poorly water-soluble nifedipine.
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.