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REFERENCE LINKING PLATFORM OF KOREA S&T JOURNALS
> Journal Vol & Issue
Journal of Pharmaceutical Investigation
Journal Basic Information
Journal DOI :
The Korean Society of Pharmaceutical Sciences and Technology
Editor in Chief :
Volume & Issues
Volume 37, Issue 6 - Dec 2007
Volume 37, Issue 5 - Oct 2007
Volume 37, Issue 4 - Aug 2007
Volume 37, Issue 3 - Jun 2007
Volume 37, Issue 2 - Apr 2007
Volume 37, Issue 1 - Feb 2007
Selecting the target year
Preparation and Characterization of Piroxicam/Poloxamer Solid Dispersion Prepared by Melting Method and Solvent Method
Yu, Hang ; Chun, Myung-Kwan ; Choi, Hoo-Kyun ;
Journal of Pharmaceutical Investigation, volume 37, issue 1, 2007, Pages 1~5
DOI : 10.4333/KPS.2007.37.1.001
Solid dispersions of piroxicam were prepared by melting method using poloxamer as a carrier. The results of DSC and XRD studies showed that the amorphous farm of piroxicam coexisted with the crystalline form in the solid dispersions. However, the ratio of crystalline form of piroxicam in the solid dispersion prepared by melting method decreased in comparison with the same ratio of the solid dispersion prepared by solvent method. As the ratio of poloxamer in the solid dispersion increased, the ratio of the amorphous form of piroxicam in the solid dispersion increased. The dissolution rate of piroxicam from the solid dispersions was significantly higher than that from piroxicam powder. In comparison to the solid dispersion prepared by solvent method, the dissolution rate of piroxicam from the solid dispersion prepared by melting method was higher. As the ratio of poloxamer in the solid dispersion prepared by melting method increased, the initial dissolution rate decreased, however, the total amount dissolved at the end of the study increased.
Development of Polymer Coating Method for Stable Stent Coating Using Chemical Bond Between Metal Surface and Polymer
Nam, Dae-Sik ; Lee, Woo-Kyoung ;
Journal of Pharmaceutical Investigation, volume 37, issue 1, 2007, Pages 7~13
DOI : 10.4333/KPS.2007.37.1.007
To produce stable polymer coating layer using the interaction between metal stent and polymer layer, Ahx-HSAB was synthesized by coupling 6-aminoheanoic acid (Ahx) with N-Hydroxy succinimidyl 4-azidobenzonate (HSAB) containing photo reactive group. Then, Ahx-HSAB was applied to self·assembled monolayer (SAM) on
-coated surface, since one end of Ahx-HSAB was carboxyl acid which was known to be able to interact with
surface. That SAM layer was incubated in 1% polycaprolacton (PCL) solution and photoreacted by ultraviolet light (254 nm) to produce the chemical bond between SAM and polymer layer, followed by PCL polymer coating (
) by the method of spray coating. The surface change was investigated by measuring of contact angle of the surface. The contact angle values of stainless steel (SS) surface,
-coated surface, SAM layer by Ahx-HSAB, photoreacted surface with PCL and PCL layer by spray coating were 70.48
2.70 and 56.47
2.12, respectively. The stability of polymer layers was tested by incubation of PCL-coated plates in 0.1M PBS buffer (pH 7.4, 0.05%, Tween 80) with vigorous shaking (200 rpm). While the poiymer layer prepared by these processes showed the intact surface morphology over 3 days, the polymer layers prepared by spray coating of PCL onto SS plate (control 1) and
-coated SS plate (control 2) were Peeled off in 3 days. Thus, the polymer coating method using SAM and photoreaction seems to be a effective method to obtain the stable polymer layer onto SS surface.
Preparation of Cyclosporin A-loaded Nanoparticles Containing Ethyl Myristate or Chitosan and Pharmacokinetics in Rats
Nam, Dae-Sik ; ; Lee, Woo-Kyoung ;
Journal of Pharmaceutical Investigation, volume 37, issue 1, 2007, Pages 15~22
DOI : 10.4333/KPS.2007.37.1.015
An oil-in-water solvent evaporation method was used to prepare the cyclosporin A (CyA)-loaded nanoparticles varying in poly (D,L-lactide-co-glycolide) (PLGA) polymer (RG 502H, RG 503H) and the amount of additive ethyl myristate (EM) or chitosan (CS). The particles were characterized for drug loading and entrapment efficiency by HPLC, surface morphology by scanning electron microscopy, particle size by dynamic light scattering and surface charge by Zetapotential. The results showed drug loadings ranging from 10.9% to 15.8% with high encapsulation efficiency (82.0-97.8%). SEM and DLS studies showed discrete and spherical particles with smooth surfaces and mean size ranging 257.6-721.7 nm. The additive EM or CS did not change the mean sizes of the nanoparticles, whereas by the coating effect of CS, the Zetapotential values of the CS-added nanoparticles were moved to the more positive direction as the amount of CS was increased. From the pharmacokinetic analysis, the nanoparticles formulations showed the higher bioavailability and MRT than
While little adding effect of EM or CS was detected in pharmacokinetic profile when RG 503H was used as polymer carrier, more noticeable different pharmacokinetic behaviors could be observed in case of RC 502H. EM incorporation was found to elevate the
, whereas CS coating resulted in the decrease of F and
, which seems to be due to the function of CS as a barrier and a mucoadhesive coating.
Crystal Form of Cefuroxime axetil
Kim, Bo-Yeon ; Sohn, Young-Taek ;
Journal of Pharmaceutical Investigation, volume 37, issue 1, 2007, Pages 23~26
DOI : 10.4333/KPS.2007.37.1.023
Two crystal forms of cefuroxime axetil were obtained by the recrystallization from different organic solvents and characterized by differential scanning calorimetry (DSC), X-ray powder diffraction (XRD). It was confirmed that two crystal forms are identical. The dissolution patterns of these two forms were also checked in 0.07 N HCl at
, 100 rpm for 180 minutes. The transformation during storage was also studied.
Statistical Analysis on the Sources of Variance in Proficiency Test of Quantitative Analysis of Medicines
Cho, Jung-Hwan ;
Journal of Pharmaceutical Investigation, volume 37, issue 1, 2007, Pages 27~37
DOI : 10.4333/KPS.2007.37.1.027
Proficiency test is an essential tool far ensuring analytical ability of analytical chemists and analytical institutes. Usually, the standard protocol for proficiency test is focused on acceptability of reported analytical results of participants by calculating z-scores and related diagnostic parameters. The ultimate goal of this process is to reveal the sources of variability of analytical results and to find the way to reduce their influence. In this study, the method of analysis of variance (ANOVA) was applied to the analytical data collected from qualify control departments of pharmaceutical companies in KyungIn province in Korea in the year of 2000. As influencing factors of variability of analytical results, the use of internal standards for liquid and gas chromatograpy, the educational and professional background of participants, geological locations and yearly production sizes of participating companies were evaluated. To evaluate the variability in accuracy of analytical results, absolute differences from sample mean and sample median were used and to evaluate variability in precision of individual participants, the reported standard deviation of each participant was used. As a result, the use of internal standards in gas chromatographic analysis, participants' academic background and the yearly production sizes of pharmaceutical companies showed statistically significant influence to the accuracy and the precision of the reported analytical results used in this study.
Encapsulation of Plasmid DNA in PLGA Nanoparticles: Effects of Poloxamer and Temperature
Kang, Hyun-Suk ; Ryu, Sang-Hwa ; Myung, Chang-Seon ; Hwang, Sung-Joo ; Park, Jeong-Sook ;
Journal of Pharmaceutical Investigation, volume 37, issue 1, 2007, Pages 39~43
DOI : 10.4333/KPS.2007.37.1.039
Previously, we have reported that PLGA nanoparticles were prepared for sustained release of water-soluble blue dextran and the particle size, in vitro release pattern and encapsulation were modulated by varying polymers. This study was designed to encapsulate plasmid DNA in PLGA nanoparticles and to investigate the effect of Polymers and temperatures. PLGA nanoparticles were fabricated with poloxamer 188 (P188) or poloxamer 407 (P407) by using spontaneous emulsification solvent diffusion method. As a model plasmid DNA, pCMV-Taq2B/1L-18 was encapsulated in PLGA nanoparticles. Then, the particle size, zeta potential and encapsulation efficiency of nanoparticles containing plasmid DNA were investigated. Particle sizes of PLGA nanoparticles prepared with P188 and P407 were in the range of 200-330 nm and 250-290 nm, respectively. Zeta potentials of nanoparticles were negative regardless of nanoparticle compositions. Encapsulation efficiency of P407 nanoparticles prepared at
was higher than those at other preparation condition. From the results, the PLGA nanoparticles prepared with poloxamers at different temperature, could modulate the particles size of nanoparticles, and encapsulation efficiency of plasmid DNA.
In vitro Evaluation of Dextran-5-aminosalicylic Acid Conjugate as a Polymeric Colon-specific Prodrug of 5-aminosalicylic Acid
Jung, Yun-Jin ; Jeon, Hyun-Chu ; Choi, Dea-Kyu ; Kim, Young-Mi ;
Journal of Pharmaceutical Investigation, volume 37, issue 1, 2007, Pages 45~49
DOI : 10.4333/KPS.2007.37.1.045
Dextran-5-aminosalicylic acid conjugate (dextran-5-ASA) was in vitro-evaluated as a polymeric colon-spe-cific prodrug of 5-aminosalicylic acid (5-ASA). Chemical stability of dextran-5-ASA in the pH 1.2 or 6.8 buffer solutions was investigated at 37 for 6 hrs. The dextran backbone was not degraded and no 5-ASA release was detected. Moreover, dextran-5-ASA neither liberated 5-ASA in the homogenates of the small intestine of rats nor was transported across Caco-2 cell monolayers, suggesting no significant loss of dextran-5-ASA during transit through the upper intestine. Furthermore, incubation of dextran-5-ASA in 10% cecal contents of rats released about 37% and 55% of 5-ASA bound to dextran in 8 hr and 24 hr, respectively. While that with either esterase or dextranase failed to liberate 5-ASA from the polymeric prodrug, incubation of dextran-5-ASA with both esterases and dextranse released 5-ASA up to about 24% of 5-ASA bound to dextran. These results suggest that, after oral administration of dextran-5-ASA, the polymeric prodrug is delivered specifically to and releases 5-ASA in the large intestine, and reveal that the 5-ASA release by cleavage of the ester bond requires precedent depolymerization of the dextran backbone.
Optimization of Preparation Variables for Trimyristin Solid Lipid Nanoparticles
Choi, Mi-Hee ; Lee, Mi-Kyung ;
Journal of Pharmaceutical Investigation, volume 37, issue 1, 2007, Pages 51~55
DOI : 10.4333/KPS.2007.37.1.051
Solid lipid nanoparticles (SLNs) have been regarded to behave similar to the vegetable oil emulsions because emulsions of lipid melts are formed before lipid droplets being solidified to turn into SLNs. Compared to lipid emulsion, however, it has been more difficult to obtain stable SLNs and needs more extensive considerations on stabilizer and manufacturing process. In the present study, we tried to prepare phosphatidylcholine-based trymyristin (TM) SLNs using high pressure homogenization method and optimize the manufacturing variables such as homogenization pressure, number of homogenization cycles, cooling temperature, co-stabilizer and freeze-drying with cryoprotectants. Nano-sized TM particles could be Prepared using egg Phosphatidylcholine and pegylated phospholipids (
PE) as stabilizers. Based on the optimization study, the dispersion was manufactured by homogenization under the pressure of 100 MPa for more than 5 cycles, and solidifying the intermediately formed lipid melt droplets by dipping in liquid nitrogen followed by thawing at room temperature. In addition, TM SLNs could be freeze-dried and then redispersed easily without significant particle size changes after freeze drying with 10% and 12.5% sucrose or trehalose. The TM SLNs established in this study can be used as delivery system for drugs and cosmetics.
Bioequivalence of Donpezil
Tablet to Aricept
Tablet (Donepezil Hydrochloride 10 mg)
Lee, Hyun-Su ; Seo, Ji-Hyung ; Kang, Il-Mo ; Lee, Heon-Woo ; Ryu, Ju-Hee ; Lee, Kyung-Tae ;
Journal of Pharmaceutical Investigation, volume 37, issue 1, 2007, Pages 57~62
DOI : 10.4333/KPS.2007.37.1.057
The purpose of the present study was to evaluate the bioequivalence of two donepezil tablets,
tablet (Dae Woong Pharm. Co., Ltd., Korea, reference drug) and
tablet (Dong Wha Pharm. Ind. Co., Ltd., Korea, test drug), according to the guidelines of Korea Food and Drug Administration (KFDA). Twenty-four healthy male Korean volunteers received one tablet containing donepezil hydorchloride 10 mg in a
crossover study. There was a three-week washout period between the doses. Plasma concentrations of donepezil were monitored by an LC-MS/MS far over a period of 240 hr after the administration.
, (the area under the plasma concentration-time curve from time zero to 240 hr) was calculated by the linear trapezoidal rule method.
(maximum plasma drug concentration) and
(time to reach
)were compiled from the plasma concentration-time data. Analysis of variance was carried out using logarithmically transformed
, No significant sequence effects were found for all of the bioavailability parameters indicating that the crossover design was properly performed. The 90% confidence intervals of the
were log 0.95
log 1.03 and log 0.94
log 1.08, respectively. These values were within the acceptable bioequivalence intervals of log 0.80
log 1.25. Taken together, our study demonstrated the bioequivalence of
with respect to the rate and extent of absorption.