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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 38, Issue 6 - Dec 2008
Volume 38, Issue 5 - Oct 2008
Volume 38, Issue 4 - Aug 2008
Volume 38, Issue 3 - Jun 2008
Volume 38, Issue 2 - Apr 2008
Volume 38, Issue 1 - Feb 2008
Selecting the target year
Effect of Enhancers and Pressure Sensitive Adhesives on the Transdermal Delivery of Fentanyl
Lee, Ji-Young ; Jang, Joon-Ho ; Choi, Hoo-Kyun ;
Journal of Pharmaceutical Investigation, volume 38, issue 4, 2008, Pages 223~228
DOI : 10.4333/KPS.2008.38.4.223
The purpose of this study was to investigate the feasibility of developing transdermal drug delivery system (TDDS) for fentanyl used for the management of chronic cancer pain. The effect of type of pressure sensitive adhesive on the permeation of fentanyl from polyisobutylene (PIB), silicone and acrylic adhesive was evaluated. Due to the good adhesive force and relatively steady flux for 3 days, both acrylic and PIB adhesives were chosen for further study. The permeation rate of fentanyl was the highest from acrylic adhesive with hydroxyl functional group. Permeation rate increased linearly as the concentration of fentanyl in acrylic adhesive was increased from 2.5% to 10%. In case of PIB adhesive, crystals of fentanyl were developed above 5% drug load.
PK40 and Plurol
provided higher flux of fentanyl.
Temperature-Sensitive Drug Delivery System of Acetaminophen Using Neutral Chitosan Solution
Kim, Ho-Jeong ; Lee, Hwa-Jeong ; Koo, Young-Soon ;
Journal of Pharmaceutical Investigation, volume 38, issue 4, 2008, Pages 229~234
DOI : 10.4333/KPS.2008.38.4.229
In the present study, chitosan-glycerophosphate sodium salt solution as a thermosensitive system (TSS) was used to formulate a temperature-sensitive drug delivery system (TSDDS) containing acetaminophen (AAP). The optimized TSS was prepared by measuring gelation temperature, gelation time and rheological properties of TSS. The optimized gelation temperature and time of TSS were
and 100 seconds, respectively. The viscosity of TSS was also suitable for maintaining gel structure at
. The release profiles of TSDDS in PBS/pH 7.4 with various apparatuses and mass loss of TSDDS were investigated. The time required to release 50% of AAP from TSDDS (
) was 120 min with the formation of pore on the surfaces, which was 2 times longer than that from AAP-chitosan gel. In addition, TSDDS was degraded approximately 80% within 4 hr and then degraded slowly for 20 hrs. In conclusion, AAP-TSS (TSDDS) formulated in this study might be suitable for some specific uses such as subcutaneous injection and rectal formulation.
Pharmacokinetic Analysis of Levofloxacin in Healthy Korean Volunteers
Kim, Seung-Yong ; Chung, Youn-Bok ; Pyo, Hee-Soo ; Kwon, Oh-Seung ;
Journal of Pharmaceutical Investigation, volume 38, issue 4, 2008, Pages 235~240
DOI : 10.4333/KPS.2008.38.4.235
A sensitive and simple method of determining the plasma levofloxacin (LFX, CAS 100986-85-4) concentrations in human volunteers by liquid-liquid extraction were developed and validated by using a high-performance liquid chromatography/diode array detector. The method was also applied to pharmacokinetic study of LFX. LFX was orally administered to 8 healthy male Korean volunteers at single lowest dose of 200 mg, compared to the published reports in which more than 500 mg of LFX was orally administered. LFX in human plasma was determined. The detection limit of LFX was
, respectively. The terminal half-life was
. Our pharmacokinetic parameters were very consistent with that previously reported, showing good correlation between LFX doses and AUC (
). This method can be useful for the pharmacokinetics and bioequivalence study with relatively low dose for reducing the main side effects of LFX.
Preparation and Evaluation of Paclitaxel Solid Dispersion by Supercritical Antisolvent Process
Park, Jae-Hyun ; Chi, Sang-Cheol ; Woo, Jong-Soo ;
Journal of Pharmaceutical Investigation, volume 38, issue 4, 2008, Pages 241~247
DOI : 10.4333/KPS.2008.38.4.241
Paclitaxel is a taxane diterpene amide, which was first extracted from the stem bark of the western yew, Taxus brevifolia. This natural product has proven to be useful in the treatment of a variety of human neoplastic disorders, including ovarian cancer, breast and lung cancer. Paclitaxel is a highly hydrophobic drug that is poorly soluble in water. It is mainly given by intravenous administration. Therefore, The pharmaceutical formulation of paclitaxel (
; Bristol-Myers Squibb) contains 50%
EL and 50% dehydrated ethanol. However the ethanol/Cremophor EL vehicle required to solubilize paclitaxel in
has a pharmacological and pharmaceutical problems. To overcome these problems, new formulations for paclitaxel that do not require solubilization by
EL are currently being developed. Therefore this study utilized a supercritical fluid antisolvent (SAS) process for cremophor-free formulation. To select hydrophilic polymers that require solubilization for paclitaxel, we evaluated polymers and the ratio of paclitaxel/polymers. HP-
-CD was used as a hydrophilic polymer in the preparation of the paclitaxel solid dispersion. Although solubility of paclitaxel by polymers was increased, physical stability of solution after paclitaxel/polymer powder soluble in saline was unstable. To overcome this problem, we investigated the use of surfactants. At 1/20/40 of paclitaxel/hydrophilic polymer/ surfactant weight ratio, about 10 mg/mL of paclitaxel can be solubilized in this system. Compared with the solubility of paclitaxel in water (
), the paclitaxel solid dispersion prepared by SAS process increased the solubility of paclitaxel by near 10,000 folds. The physicochemical properties was also evaluated. The particle size distribution, melting point and amophorization and shape of the powder particles were fully characterized by particle size distribution analyzer, DSC, SEM and XRD. In summary, through the SAS process, uniform nano-scale paclitaxel solid dispersion powders were obtained with excellent results compared with
for the physicochemical properties, solubility and pharmacokinetic behavior.
Improved Dissolution of Solid Dispersed Atorvastatin Using Spray-Dryer
Lee, Jun-Hee ; Kim, Dae-Sung ; Kim, Won ; Park, Jong-Hak ; Ahn, Sik-Il ; Kim, Yun-Tae ; Rhee, John-M. ; Khang, Gil-Son ;
Journal of Pharmaceutical Investigation, volume 38, issue 4, 2008, Pages 249~254
DOI : 10.4333/KPS.2008.38.4.249
Solid dispersions of poorly water-soluble drug, atorvastatin, were prepared with Eudragit L100 to improve the solubility by spray dryer. To investigate the correlation between physicochemical properties and dissolution rate of solid dispersions, the samples were characterized by scanning electron microscopy (SEM), differential scanning calorimeter (DSC) and fourier transform infrared spectroscopy (FT-IR). SEM and DSC were found that atorvastatin is amorphous in the Eudragit L100 solid dispersion. FT-IR was used to analyze the salt formation by interaction between atorvastatin and Eudragit L100. The dissolution rate of solid dispersed atorvastatin was markedly increased compared to drug powder in stimulated intestinal juice (pH 6.8). Thus, the solid dispersed atorvastatin using the spray drying method with Eudragit L100 may be effective for the bioavailability.
Synthesis and In-vitro Evaluation of N4-Amino Acid Derivatives of Cytarabine for Improving the Oral Delivery of Cytarabine
Jin, Ming-Ji ; Hong, Joon-Hee ; Han, Hyo-Kyung ;
Journal of Pharmaceutical Investigation, volume 38, issue 4, 2008, Pages 255~259
DOI : 10.4333/KPS.2008.38.4.255
The present study aimed to investigate the in-vitro characteristics of N4-amino acid derivatives of cytarabine for the oral delivery of cytarabine. After the synthesis of L-Ile-cytarabine, L-Leu-cytarabine and L-Arg-cytarabine, the gastrointestinal stability of each prodrug was examined using artificial gastric juice and intestinal fluids. The cellular uptake characteristics of prodrugs were also examined in Caco-2 cells. While L-Ile-cytarabine and L-Leu-cytarabine appeared to be stable in all the tested biological media during 4-hr incubation, L-Arg-cytarabine was rapidly disappeared within 5 min. Accordingly, the cellular uptake of L-Ile-cytarabine and L-Leu-cytarabine was significantly higher than that of its parent drug, cytarabine in Caco-2 cells but the cellular uptake of L-Arg-cytarabine was similar to that from its parent drug. The cellular uptake of L-Ile-cytarabine and L-Leu-cytarabine appeared to be saturable as drug concentration increased from 0.4 to 4 mM. Collectively, L-Ile-cytarabine and L-Leu-cytarabine could be promising candidates to improve the oral absorption of cytarabine via a saturable transport pathway.
Bioequivqlence of Gabarep Tablet to Neurotin Tablet (Gabapentin 800 mg)
Seo, Young-Hwan ; Jeong, Ju-Cheol ; Lee, Jae-Young ; Li, Zheng-Yi ; Yoon, Hyoung-Jong ; Sohn, Uy-Dong ; Bang, Joon-Seok ; Kim, Ho-Hyun ; Jeong, Ji-Hoon ;
Journal of Pharmaceutical Investigation, volume 38, issue 4, 2008, Pages 261~267
DOI : 10.4333/KPS.2008.38.4.261
The aim of the present study was to evaluate the bioequivalence of two gabapentin preparations. We used Neurontin tablet 800 mg (Pfizer Korea Inc.) as a reference drug for bioequivalence of Gabalep tablet 800 mg (Chong Kun Dang Pharmaceutical Co., Korea), and performed this whole study according to the guidelines of Korea Food and Drug Administration (KFDA). Twenty five healthy male volunteers were administered with each drug in a randomized
cross-over study with one week washout interval. After drug administration, blood was taken at predetermined time intervals (
hours) and the concentrations of gabapentin in serum were determined using an high performance liquid chromatography-tandem mass spectrometer (LC-MS/MS) employing electrospray ionization technique and operating in multiple reaction mornitoring (MRM). The analytical method was validated in specificity, accuracy, precision and linearity. The phar-macokinetic parameters such as AUCt and Cmax were calculated and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed AUCt and Cmax.
. of AUCt and Cmax value for reference drug and test drug were
, respectively. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log(0.8) to log(1.25) for AUCt and Cmax, respectively. These results indicate that Gabalep tablet 800 mg is bioequivalent to Neurontin tablet 800 mg.
Bioequivalence of Lesacin
Tablet to Jeil Cravit
Tablet (Levofloxacin 100 mg) by Liquid Chromatography- Electrospray Tandem Mass Spectrometry
Lee, Jin-Sung ; Choi, Sang-Jun ; Ryu, Ju-Hee ; Seo, Ji-Hyung ; Lee, Myung-Jae ; Kang, Jong-Min ; Tak, Sung-Kwon ; Kang, Jin-Yang ; Lee, Kyung-Tae ;
Journal of Pharmaceutical Investigation, volume 38, issue 4, 2008, Pages 269~275
DOI : 10.4333/KPS.2008.38.4.269
The purpose of the present study was to evaluate the bioequivalence of two levofloxacin tablets, Jeil
tablet (Jeil Pharm. Co., Ltd., Korea, reference drug) and
tablet (Ilhwa. Co., Ltd., Korea, test drug), according to the guidelines of Korea Food and Drug Administration (KFDA). Twenty-four healthy male Korean volunteers received two tablets containing levofloxacin 200 mg in a
crossover study. There was a one-week washout period between the doses. Plasma concentrations of levofloxacin were monitored for over a period of 24 hr after administration by using a high performance liquid chromatography-tandem mass spectrometry (LC-MS/MS). The area under the plasma concentration-time curve from time zero to 24 hr (
), maximum plasma drug concentration (
) and time to reach
were complied from the plasma concentration-time data. Analysis of variance (ANOVA) test was utilized for the statistical analysis of the parameters using logarithmically transformed
. The 90% confidence intervals of the
ratio and the
, respectively. These values were within the acceptable bioequivalence intervals of
, recommended by KFDA. In all of these results, we concluded that
tablet was bioequivalent to Jeil
tablet, in terms of rate and extent of absorption.
Bioequivalence of Topamin Tablet to Topamax Tablet (Topiramate 100 mg)
Seo, Ji-Hyung ; Lee, Myung-Jae ; Choi, Sang-Jun ; Kang, Jong-Min ; Lee, Jin-Sung ; Tak, Sung-Kwon ; Lee, Kyung-Tae ;
Journal of Pharmaceutical Investigation, volume 38, issue 4, 2008, Pages 277~282
DOI : 10.4333/KPS.2008.38.4.277
The purpose of the present study was to evaluate the bioequivalence of two topiramate tablets, Topamax tablet (Janssen Korea. Co., Ltd., Seoul, Korea, reference drug) and Topamin tablet (Myungmoon Pharm. Co., Ltd., Seoul, Korea, test drug), according to the guidelines of Korea Food and Drug Administration (KFDA). Twenty-four healthy male Korean volunteers received one tablet at the dose of 100 mg topiramate in a
crossover study. There were two-weeks washout period between the doses. Plasma concentrations of topiramate were monitored by an LC-MS/MS for over a period of 96 hr after administration.
(the area under the plasma concentration-time curve from time zero to 96 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 (ANOVA) was carried out using logarithmically transformed
. The 90% confidence intervals of the
, ratio and the
ratio for Topamin/Topamax were
, respectively. These values were within the acceptable bioequivalence intervals of
. Taken together, our study demonstrated the bioequivalence of Topamax and Topamin with respect to the rate and extent of absorption.