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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 39, Issue 6 - Dec 2009
Volume 39, Issue 5 - Oct 2009
Volume 39, Issue 4 - Aug 2009
Volume 39, Issue 3 - Jun 2009
Volume 39, Issue 2 - Apr 2009
Volume 39, Issue 1 - Feb 2009
Selecting the target year
Preparation and Cellular Uptake of Hydrophobic Quantum Dots Encapsulated in Poly-L-Lactic Acid Film
Lee, Ji-Sook ; Woo, Kyoung-Ja ; Chung, He-Sson ;
Journal of Pharmaceutical Investigation, volume 39, issue 1, 2009, Pages 1~6
DOI : 10.4333/KPS.2009.39.1.001
To overcome the stability problem of hydrophilic quantum dot (Q-dot), cellular uptake of hydrophobic instead of hydrophilic Q-dot was studied in the hope to find a simple method to use Q-dot as a cellular imaging probe. Hydrophobic Q-dot and poly-L-lactic acid (PLLA) were co-dissolved in chloroform to prepare stable films. Due to the cellular compatibility of PLLA, adherent cells were cultured on the film to observe the degree of Q-dot uptake and cytotoxicity of the prepared films. The results show that Q-dots were absorbed into NIH3T3 and EMT6 cells. Cellular uptake was also observed when hydrophobic Q-dots were coated directly on a glass plate. PLLA/Q-dot film and Q-dot coated on glass plate did not show major cytotoxicity. In vivo tumor model was also used to show the uptake of Q-dot from the PLLA/Q-dot film to the tumor site.
Dissolution Rate Improvement of Tinidazole Tablets using PEO and HPMC
Kim, Kyung-Joo ; Park, Jun-Bum ; Choi, Jong-Seo ; Hwan, Hwang-Chang ; Lee, Joeng-Sig ; Kang, Chin-Yang ;
Journal of Pharmaceutical Investigation, volume 39, issue 1, 2009, Pages 7~12
DOI : 10.4333/KPS.2009.39.1.007
A novel polymeric tablet of Tinidazole was formulated to treat Helicobacter pylori and Giardia lambria more efficiently, It was possible to reduce hepatotoxicity by controlling the release of Tinidazole after peroral administration. A gastric retentive formulation made of naturally occurring carbohydrate polymers and containing Tinidazole was tested in vitro for swelling and dissolution characteristics. Tinidazole tablets containing various concentration of either PEO or HPMC were prepared by the wet granulation method. In vitro release of Tinidazole at pH 1.2 and pH 6.8 buffer solutions was observed at
by using a KP dissolution method and an UV (313 nm) spectrophotometer. Compared to a commercial Tinidazole tablet, in vitro release of Tinidazole at both pH 1.2 and pH 6.8 buffer solutions significantly decreased as the concentration of PEO or HPMC in the tablet increased up. And the gastric retentive formulation hydrated and swelled back to about 50% of its original size in 30 min. Thus, it was possible to control the release of Tinidazole by changing the content of PEO or HPMC in the tablet, thereby manipulating the release rate and the retention of Tinidazole.
Parenteral Docetaxel Emulsion System and Its Stability
Kim, Hyun-Jo ;
Journal of Pharmaceutical Investigation, volume 39, issue 1, 2009, Pages 13~18
DOI : 10.4333/KPS.2009.39.1.013
Docetaxel is an anticancer agent with low aqueous solubility. More extensive clinical use of this drug is somewhat delayed due to lack of appropriate delivery vehicles. An attempt was made to adopt an o/w emulsion as the drug carrier which incorporated docetaxel in the propyleneglycerol stabilized by a mixed-emulsifier system. A suitable formulation was found in this study: 10 mg/mL docetaxel, 10% (w/v) oil blend, 4% (w/v) PG, 3% (w/v) Solutol HS 15 in 2.25% (w/v) glycerol solution. The formulated emulsion has very good stability when stored at
, and the docetaxel containment efficiency can be maintained above 95% and the mean emulsion diameter around
for at least 3 months. The formulated emulsion is a promising carrier for docetaxel and other lipophilic drugs.
Enhanced Transdermal Delivery of Furosemide from the EVA Matrix through the Rat Skin
Chang, Ik-Hyeon ; Cho, Hwa-Young ; Noh, Jin-Hyung ; Park, Jung-Chan ; Park, Yong-Sun ; Kim, Seong-Jin ; Shin, Sang-Chul ;
Journal of Pharmaceutical Investigation, volume 39, issue 1, 2009, Pages 19~21
DOI : 10.4333/KPS.2009.39.1.019
This study was performed to examine the possibility of increasing the level of furosemide permeation from the ethylene-vinyl acetate (EVA) matrix through the skin by incorporating various enhancers in the EVA matrix. The effects of the enhancers on the level of furosemide permeation through the skin were evaluated using Franz diffusion cells with intact excised rat skins. The enhancers examined were the fatty acids (saturated, unsaturated), the pyrrolidones, the propylene glycol derivatives, the glycerides and the non-ionic surfactants. Among the enhancers used, polyoxyethylene-2-oleyl ether (a non-ionic surfactant) showed the best enhancement. The polyoxyethylene 2-oleyl ether as a permeation enhancer could be used for development of furosemide-EVA transdermal matrix system.
Simultaneous Determination of Paeoniflorin and Glycyrrhizin in Sayuk-san by HPLC/DAD
Lee, Mi-Kyeong ; Lee, Ki-Yong ; Kim, Seung-Hyun ; Jeon, Min-Ji ; Cho, Jung-Hee ; Oh, Mi-Hyun ; Baek, Ju-Hyun ; Kim, Hyo-Jin ; Sung, Sang-Hyun ;
Journal of Pharmaceutical Investigation, volume 39, issue 1, 2009, Pages 23~27
DOI : 10.4333/KPS.2009.39.1.023
A high performance liquid chromatographic (HPLC) method for the simultaneous determination of marker constituents, paeoniflorin and glycyrrhizin was established for the quality control of traditional herbal medicinal preparation, Sayuk-san (SYS). Separation and quantification were successfully achieved with a Waters XTerra RP18 column (
) by gradient elution of a mixture of acetonitrile and water containing 0.03% phosphoric acid (pH 2.03) at a flow rate of 1.0 mL/min. The diode-array UV/vis detector (DAD) was used for the detection and the wavelength for quantification was set at 230 nm. The presence of paeoniflorin and glycyrrhizin in this decoction was ascertained by retention time, spiking with each authentic standard and UV spectrum. All two compounds showed good linearity (
>0.996) in a relatively wide concentration ranges. The R.S.D. for intra-day and inter-day precision was less than 7.3% and the limits of detection (LOD) were less than 55.7 ng. The mean recovery of each compound was
with R.S.D. values less than 4.6%. This method was successfully applied to the determination of contents of paeoniflorin and glycyrrhizin in three commercial products of SYS. These results suggest that the developed HPLC method is simple, effective and could be readily utilized as a quality control method for commercial SYS products.
In-line Monitoring of Fluid-Bed Blending Process for Pharmaceutical Powders using Fiber Optics Probe and NIR Spectroscopy
Park, Cho-Rong ; Kim, Ah-Young ; Lee, Min-Jeong ; Lee, Hea-Eun ; Seo, Da-Young ; Shin, Sang-Mun ; Choi, Yong-Sun ; Kwon, Byung-Soo ; Bang, Kyu-Ho ; Kang, Ho-Kyung ; Kim, Chong-Kook ; Lee, Sang-Kil ; Choi, Guang-Jin ;
Journal of Pharmaceutical Investigation, volume 39, issue 1, 2009, Pages 29~36
DOI : 10.4333/KPS.2009.39.1.029
Since the quality of final products is significantly affected by the homogeneity of powder mixture, the powder blending process has been regarded as one of the critical pharmaceutical unit processes, especially for solid dosage forms. Accordingly, the monitoring to determine a blending process' end-point based on a faster and more accurate in-line/on-line analysis has attracted enormous attentions recently. Among various analytical tools, NIR (near-infrared) spectroscopy has been extensively studied for PAT (process analytical technology) system due to its many advantages. In this study, NIR spectroscopy was employed with an optical fiber probe for the in-line monitoring of fluid-bed blending process. The position of the probe, the ratio of binary powder mixture, the powder size differential and the back-flush period of the shaking bag were examined as principal process parameters. During the blending process of lactose and mannitol powders, NIR spectra were collected, corrected, calibrated and analyzed using MSC and PLS method, respectively. The probe position was optimized. A reasonable end-point was predicted as 1,500 seconds based on 5% RSD value. As a consequence, it was demonstrated that the blending process using a fluid-bed processor has several advantages over other methods, and the application of NIRS with an optical fiber probe as PAT system for a fluid-bed blending process could be high feasible.
Efficacy Evaluation of a Leuprorelin Formulation (Lorelin Depot Injection
) by Determination of Serum Testosterone in Rats
Lee, Hye-Ju ; Hwang, Seong-Mee ; Shim, Won-Sik ; Jung, Goo-Young ; Son, Kyung-Chul ; Kim, Dae-Duk ; Chung, Suk-Jae ; Shim, Chang-Koo ;
Journal of Pharmaceutical Investigation, volume 39, issue 1, 2009, Pages 37~41
DOI : 10.4333/KPS.2009.39.1.037
The purpose of this study was to compare the efficacy of Lorelin Depot
(Dongkook Pharm. Co., LTD) with Lucrin Depot
(Abbott) by measuring serum testosterone level in rats. Leuprorelin (leuprolide acetate), which is an active compound for the two formulations, is an LHRH analogue that is used for the treatment of a wide range of sex hormone-related disorders including advanced prostatic cancer, endometriosis and precocious puberty. Lorelin Depot
is a micro-encapsulated formulation to suppress testosterone level by releasing leuprorelin continuously for four weeks with a single subcutaneous injection. The comparison study of the efficacy was performed during four weeks, and serum testosterone levels were monitored in the two formulations. The mean serum testosterone levels from the formulations were decreased to that of the castrate range (50 ng/dL or less) after three days after the initial depot injection, and the concentration were remained throughout four weeks' period. There were no significant differences in the
of testosterone and testosterone levels at 3, 7, 14, 21 and 28 days between the two formulations. These results indicate that the two formulations, Lorelin Depot
and Lucrin Depot
, are bioequivalent in terms of the serum testosterone level in rats.
Determination of Aspirin Tablet Manufacturers by an NMR-based Metabolomic Approach
Choi, Moon-Young ; Kang, Sun-Mi ; Park, Jeong-Hill ; Kwon, Sung-Won ;
Journal of Pharmaceutical Investigation, volume 39, issue 1, 2009, Pages 43~49
DOI : 10.4333/KPS.2009.39.1.043
Aspirin or acetylsalicylic acid, a member of the salicylate family, is frequently used as an analgesic, antipyretic, anti-inflammatory and antiplatelet drug. Because aspirin is chemically unstable in water and heat for tablet formulation, additives including lubricants are used in preparing aspirin tablets, using a dry-granulation process. Aspirin tablets are produced by a number of manufacturers which usually use their own unique combination of additives during the manufacturing process. In this study, we employed an NMR based metabolomics technique to identify the manufacturers of various aspirin tablets. Aspirin tablets from six different companies were analyzed by 1H 400 MHz NMR. The acquired data was then integrated and processed by principal component analysis (PCA). Based on the NMR data, we were able to identify peaks corresponding to acetylsalicylic acid in all of the six samples, whereas different NMR patterns were found in the aromatic and aliphatic regions depending on the unique additive used. These observations led to the conclusion that the differences in the NMR patterns among the different aspirin tablets were due to the presence of additives.
Effects of βig-h3/Chitosan Dressing on Dermal Fibroblast and Wound Healing
Cho, Ae-Ri ; Choi, Hee-Sun ;
Journal of Pharmaceutical Investigation, volume 39, issue 1, 2009, Pages 51~54
DOI : 10.4333/KPS.2009.39.1.051
-h3, is a TGF-
-induced gene product, extracellular matrix protein with 68 kDa MW(683 amino acids) and has been known for its possible roles in cell adhesion, spreading, migration and proliferation. To minimize a proteolytic degradation of
-h3 incorporated chitosan sponge was prepared and its effects on fibroblast adhesion and migration were investigated. And its wound healing efficacy was evaluated in deep 2nd degree burn rabbit ear wound model.
-h3 enhanced fibroblast adhesion and proliferation. In histological observation, a significant over-proliferation of epidermal regeneration was observed in
-h3/chitosan dressing applied wound while epidermal regeneration was not proceeded yet in chitosan only treated wound.
-h3/sponge dressing could enhance epidermal regeneration.
Efficacy of Hydrogel Patch in Wound Rat Model
Oh, Seung-Seok ; Kim, Chul-Jun ; Kim, Hee-Sook ; Shin, Young-Hee ;
Journal of Pharmaceutical Investigation, volume 39, issue 1, 2009, Pages 55~58
DOI : 10.4333/KPS.2009.39.1.055
Sodium polyacrylate based hydrogel patch was prepared and its wound healing efficacy in comparison with control groups was evaluated in thermal burn wound (
, 10 sec burn) and excision wound rat model. Cytotoxicity of gamma irradiated (25 kGy) hydrogel patch was investigated in human fibroblasts and showed no significant cytotoxicity. Wound closure rates (H50%) in hydrogel patch group and BAND-
treated group were faster than that of control group (uncovered open wound). Hydrogel patch showed an enhancement in wound healing process.
Effect of Tripolyphosphate (TPP) on the Controlled Release of Cyclosporin A from Chitosan-coated Lipid Microparticles
Cheon, Ji-Woong ; Shim, Chang-Koo ; Chung, Suk-Jae ; Kim, Dae-Duk ;
Journal of Pharmaceutical Investigation, volume 39, issue 1, 2009, Pages 59~63
DOI : 10.4333/KPS.2009.39.1.059
Soybean phosphatidylcholine microparticles loaded with cyclosporin A (CsA) were prepared by the modified emulsion solvent diffusion and ionic gelation method, in which chitosan on the surface of the microparticles was crosslinked with various concentrations of tripolyphosphate (TPP). The morphology of the particles was characterized by scanning electron microscopy (SEM). The change of particle size and zeta-potential by chitosan on the surface of the lipid microparticles were systematically observed. The encapsulation efficiency and loading capacity of CsA in the particles were determined by high performance liquid chromatography (HPLC). In vitro release kinetics was studied using the dialysis method. In the results, the mean particle size and the zeta-potential of lipid microparticles increased when the attached chitosan was cross-linked (from 2.5 to 6.2
and from -37.0 to +93.0 mV, respectively). The cyclosporin A-loaded lipid microparticles appeared discrete and spherical particles with smooth surfaces. The encapsulation efficiency of CsA was between 79% and 90% while the loading capacity was between 41% and 56%. In vitro release study showed that the crosslinkage of chitosan by TPP significantly delayed the release of CsA from the particles in a concentration-dependent manner. Thus, the release of CsA from the lipid microparticles could be controlled by tripolyphosphate used as a cross-linking agent.
Bioequivalence Study of Toriem
Tablet to Motilium-M
Tablet (Domperidone Maleate 12.72 mg) Evaluated by Liquid Chromatography/Tandem Mass Spectrometry
Ryu, Ju-Hee ; Choi, Sang-Jun ; Lee, Myung-Jae ; Lee, Jin-Sung ; Kang, Jong-Min ; Tak, Sung-Kwon ; Seo, Ji-Hyung ; Lee, Kyung-Tae ;
Journal of Pharmaceutical Investigation, volume 39, issue 1, 2009, Pages 65~71
DOI : 10.4333/KPS.2009.39.1.065
The aim of the present study was to evaluate the bioequivalence of two domperidone maleate tablets, Motilium-
Tablet (Janssen Korea Ltd., reference product) and
Tablet (Daewon Pharm. Co., Ltd., test product). Domperidone was extracted by liquid-liquid extraction using tert-butyl methyl ether and separated in less than 3 min on
reverse-phase column using an isocratic elution. A tandem mass spectrometer, as detector, was used for quantitative analysis in positive mode by a multiple reaction monitoring mode to monitor the m/z
and the m/z
transitions for domperidone and the internal standard (roxithromycin), respectively. Calibration curves, from
ng/mL of domperidone, showed correlation coefficients (r) higher than 0.9941. Intra day and inter day precision (C.V. %) for quality control were ranged from 10.04 to 16.09% and from 10.87 to 18.69%, respectively. The lower limit of quantification (LLOQ) of domperidone was 0.05 ng/mL. The method described is precise and sensitive and has been successfully applied to the study of bioequivalence of domperidone in 24 healthy Korean volunteers. Twenty-four healthy male Korean volunteers received a single dose of each medicine (
domperidone maleate) in a
crossover study. There was a one-week washout period between the doses. Plasma concentrations of domperidone were monitored for over a period of 24 hr after the administration.
(the area under the plasma concentration-time curve) was calculated by the linear trapezoidal rule.
(maximum plasma drug concentration) and
(time to reach
) were compiled from the plasma concentration-time data. The 90% confidence intervals for the log transformed data were within acceptable range of log 0.8 to log 1.25 (e.g.,
). The major parameters,
met the criteria of KFDA for bioequivalence indicating that
tablet is bioequivalent to Motilium-
Validation of LC-MS/MS Method for Determination of Rabeprazole in Human Plasma : Application of Pharmacokinetics Study
Tak, Sung-Kwon ; Seo, Ji-Hyung ; Ryu, Ju-Hee ; Choi, Sang-Joon ; Lee, Myung-Jae ; Kang, Jong-Min ; Lee, Jin-Sung ; Hong, Seung-Jae ; Yim, Sung-Vin ; Lee, Kyung-Tae ;
Journal of Pharmaceutical Investigation, volume 39, issue 1, 2009, Pages 73~78
DOI : 10.4333/KPS.2009.39.1.073
A simple LC-MS/MS method of rabeprazole in human plasma was developed and validated. Rabeprazole and Internal standard (I.S), omeprazole, were extracted from human plasma by liquid liquid extraction, chromatographic separation of rabaprazole in plasma was achieved at
with a Shiseido UG120
column and methanol-10 mM ammonium acetate buffer (pH 9.42 with ammonium water), as mobile phase. Rabeprazole produced a protonated precursor ion [
] at m/z 360.10 and corresponding product ion at m/z 242.21. Internal standard produced a protonated precursor ion [
] at 346.09 and corresponding product ion at m/z 198.09. This method showed linear response over the concentration range of
with correalation coefficient greater than 0.99. The lower limit of quantitation (LLOQ) using 0.2 mL plasma was 1 ng/mL, which was sensitive enough for pharmacokinetics studies. The method was specific and validated with a limit of quantitation of 1 ng/mL. The intra-day and inter-day precision and accuracy were acceptable for all samples including the LLOQ. The applicability of the method was demonstrated by analysis of plasma after administration of a single 10 mg dose to 36 healthy subject. From the plasma rabeprazole concentration versus time curves, the mean
(The area under the plasma concentration-time curve from time 0 to 12 hr ) was
(maximum plasma drug concentration) of
after adiministration. The mean biological half-life of rabeprazole was
. Based on the results, this simple method could readily be used in pharmacokinetics studies.