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Sibeum Lee,Kyungwan Nam,김민수,Seoung Wook Jun,박정숙,우종수,Sung-Joo Hwang 대한약학회 2005 Archives of Pharmacal Research Vol.28 No.7
The objective of this study was to elucidate the feasibility to improve the solubility and bioavailability of poorly water-soluble itraconazole via solid dispersions by using supercritical fluid (SCF). Solid dispersions of itraconazole with hydrophilic polymer, HPMC 2910, were prepared by the aerosol solvent extraction system (ASES) under different process conditions of temperature/ pressure. The particle size of solid dispersions ranged from 100 to 500 nm. The equilibrium solubility increased with decrease (15 to 10 MPa) in pressure and increase (40 to 60oC) in temperature. The solid dispersions prepared at 45oC/15 MPa showed a slight increase in equilibrium solubility (approximately 27-fold increase) when compared to pure itraconazole, while those prepared at 60oC/10 MPa showed approximately 610-fold increase and no endothermic peaks corresponding to pure itraconazole were observed, indicating that itraconazole might be molecularly dispersed in HPMC 2910 in the amorphous form. The amorphous state of itraconazole was confirmed by DSC/XRD data. The pharmacokinetic parameters of the ASES-processed solid dispersions, such as Tmax, Cmax, and AUC0-24h were almost similar to Sporanox capsule which shows high bioavailability. Hence, it was concluded that the ASES process could be a promising technique to reduce particle size and/or prepare amorphous solid dispersion of drugs in order to improve the solubility and bioavailability of poorly water-soluble drugs.
Sibeum Lee,황성주,김민수,Seoung Wook Jun,박정숙 대한약학회 2005 Archives of Pharmacal Research Vol.28 No.5
Beads loaded with the water-soluble drug, phenylpropanolamine HCl (PPA), were prepared using an extruder and double arm counter-rotating roller modified from a traditional pill machine. The mean diameter of the cylindrical rod-like extrudate from the ram extruder was 3 mm; that of the uncoated bead after cutting and spheronization by the modified double arm counter-rotating roller was 3.26~3.28 mm. Although the surface of the beads was moderately rough and irregular, some exhibited hump-shaped protrusions, the sphericity was acceptable (roundness 1.15) and adequate for the subsequent coating process. An increase in mean diameter of the coated beads and improvements in friability and sphericity were observed in proportion to the amount of coating material applied (ethylcellulose or Eudragit?? RS 100). It was also found that the release rate of PPA from the coated beads could be controlled by the amount and type of coating materials applied or with the incorporation of Eudragit?? RS 100 into the core matrix. Further modifications to the double arm counter-rotating roller, including adjustment of the rotation speed and distance between the rollers, would yield smaller uncoated beads with improved roundness and surface roughness. In conclusion, the present method could be potentially applied to prepare controlled release drug delivery beads or pellet dosage forms.
미세유화약물송달시스템을 이용한 로바스타틴의 생체이용률 향상
윤복영,강복기,정상영,이영원,이시범,황성주,육순홍,강길선,이해방,조선행 한국약제학회 2002 Journal of Pharmaceutical Investigation Vol.32 No.4
A self-microemulsifying drug delivery system (SMEDDS) was developed to increase the dissolution rate, solubility, and ultimately bioavailability of a poorly water soluble drug, lovastatin. SMEDDS was the mixtures of oils, surfactants, and cosurfactants, which emulsify under conditions of gentle agitation, similar to those which would be encountered in the gastro-intestinal (GI) tract. Various types of self-emulsifying formulations were prepared using four types of oil (Capryol 90, Lauroglycol 90, Labrafil M 1944 CS and Labrafil M 2125), two surfactants (Cremophor EL and Tween 80), and three cosurfactants (Carbitol, PEG 400 and propylene glycol). The efficiency of emulsification was studied using a laser diffraction size analyzer to determine particle size distributions of the resultant emulsions. Optimized formulations selected for bioavailability assessment were Carpryol 90 (40%), Cremophor EL (30%) and Carbitol (30%). SMEDDS containing lovastatin (20 mg and 5 mg) were compared to a conventional lovastatin tablet (Mevacor^? , 20 mg/tab) by the oral administration as prefilled hard gelatin capsules to fasted beagle dogs for in vivo study. The area under the serum concentration-time curve from time zero to the last measured time in serum, AUC_0→24h, was significantly greater in SMEDDS, suggesting that bioavailability increase 130% and 192% by the SMEDDS, respectively. The self-emulsifying formulations of lovastatin afforded the improvement in absolute oral bioavailability relative to previous data of lovastatin tablet formulation. These data indicate the utility of dispersed self-emulsifying formulations for the oral delivery of lovastatin and potentially other poorly absorbed drugs.
김민수,이시범,이태완,전재일,황성주 충남대학교 약학대학 의약품개발연구소 2004 藥學論文集 Vol.19 No.-
We have studied the dissolution kinetics of three extended release commercial tablets of acetaminoPhen in simulated gastric juice, and the dissolution profiles were compared. The applied methods for the comparison of in vitro dissolution profiles are model independent methods including difference factor (f₁) and similarity factor (f₂), and statistical methods based on the analysis of variance and in t-test. The comparison of the dissolution profile, using difference factor (f₁), and similarity factor (f₂), indicates that the three tablets are equivalent in their dissolution. But, statistical methods based on the analysis of variance and in t-test indicate that the three tablets are not equivalent in their dissolution. The results show that statistical methods are better indicator of discrimination than the f-factors.
듀리세프 캡슐(세파드록실 500 mg)에 대한 비드세프 캡슐의 생물학적 동등성
김혜진,유진희,이시범,이태완,황성주 충남대학교 약학대학 의약품개발연구소 2004 藥學論文集 Vol.19 No.-
The purpose of the present study was to evaluate the bioequivalence of two cefadroxil capsules, test drug(Vidcef capsule Yuyu Inc.) and reference drug(Duricef capsule Bo Ryung Pharmaceutical Co, Ltd.), according to the guidelines of Korea Food and Drug Administration(KFDA). Twenty four healthy male volunteers, 23.21±2.92 year in age and 67.46±5.47 kg in body weight, were divided into two groups and a randomized 2×2 cross-over study was employed. After two capsules containing 1000 mg of cefadroxil were orally administered, blood sample were taken at the scheduled time intervals and the scheduled time intervals and the concentrations of cefadroxil in plasma were determined using HPLC with UV detector. The dissolution profiles of two cefadroxil capsules were very similar at all dissolution media. Pharmacokinetic parameters such as AUC_(t), C_(max) and T_(max) were calculated and ANOVA test was used for the statistical analysis of the parameters using logarithmically transformed AUC_(t) and C_(max) and untransformed T_(max). These results showed that the differences between two formulations were 0.06%-2.26% and 8.17% for AUC_(t), C_(max) and T_(max), respectively. There were no sequence effects between the two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log0.8 to log1.25(log 0.94∼log1.09 and log0.90∼log.1.06 for AUC_(t) and C_(max) respectively). Thus, the criteria of the KFDA guidelines for the bioequivalence were satisfied, indicating Duricef capsule and Vidcef capsule are bioequivalent.
Ji Hye Yun,명자혜,Hye Jin Kim,Sibeum Lee,Jong-Sei Park,Won Kim,Eun-Hee Lee,문철진,황성주 대한약학회 2005 Archives of Pharmacal Research Vol.28 No.4
The purpose of the present study was to develop a standard protocol for imidapril hydrochloride bioequivalence testing. For this reason, a specific LC-MS method was developed and validated for the determination of imidapril in human plasma. A solid-phase extraction cartridge, Sep-pak?? C18, was used to extract imidapril and ramipril (an internal standard) from deproteinized plasma. The compounds were separated using a XTerra MS?? C18 column (3.5 µm, 2.1×150 mm) and acetonitrile-0.1% formic acid (67:33, v/v) adjusted to pH 2.4 by 2 mmol/L ammonium formic acid, as mobile phase at 0.3 mL/min. Imidapril was detected as m/z 406 at a retention time of ca. 2.3 min, and ramipril as m/z 417 at ca. 3.6 min. The described method showed acceptable specificity, linearity from 0.5 to 100 ng/mL, precision (expressed as a relative standard deviation of less than 15%), accuracy, and stability. The plasma concentrationversus- time curves of eight healthy male volunteers administered a single dose of imidapril (10 mg), gave an AUC12hr of imidapril of 121.48 ± 35.81 ng mL-1 h, and Cmax and Tmax values of 32.59 ± 9.76 ng/mL and 1.75 ± 0.27 h. The developed method should be useful for the determination of imidapril in plasma with sufficient sensitivity and specificity in bioequivalence study.
용매증발법에 의한 부피바카인 마이크로스피어의 제오 및 평가 (II)
곽손현(Son Hyok Kwak),이시범(Sibeum Lee),우종수(Jong Soo Woo),이병철(Byung Chul Lee),황성주(Sung Joo Hwang) 大韓藥學會 2001 약학회지 Vol.45 No.6
Various bupivacaine-loaded microspheres were prepared using poly(d,1-lactide) (PLA) and poly(d ,1-lactic-co-glycolide) (PLGA) by a solvent evaporation method for the sustained release of drug. The effects of process conditions such as drug loading, polymer type and solvent type on the characteristics of microspheres were investigated. The prepared microspheres were characterized for their drug loading, size distribution, surface morphology and release kinetics. Drug loading efficiency and yield of PLGA microspheres were higher than those of PLA microspheres. The prepared microspheres had an average particle size below 5mcm. The particle size range of microspheres was 1.65∼2.24mcm. As a result of SEM, the particle size of PLA microspheres was smaller than that of PLGA microspheres. In morphology studies, micro- spheres showed a spherical shape and smooth surface in all process conditions. In thermal analysis, bupivacaine-loaded microspheres showed no peaks originating from bupivacaine. This suggested that bupivacaine base was molecular-dispersed in the polymer matrix of microspheres. The release pattern of the drug from microspheres was evaluated for 96 hours. The initial burst release of bupivacaine base decreased with increasing the molecular weight of PLGA, and the drug from microspheres released slowly, In conclusion, bupivacaine-loaded microspheres were successfully prepared from poly(d,1-lactide) and poly (d,1-lactic-co-glycolide) polymers with different molecular weights allowing control of the release rate.