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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
The effect on skin deposition and moisturizing of ursolic acid in hydrogel system containing wood vinegar
Lee, Gye-Won ; Lee, Ju-Yeon ;
Journal of Pharmaceutical Investigation, volume 38, issue 2, 2008, Pages 87~92
DOI : 10.4333/KPS.2008.38.2.087
Wood vinegar is well known as a softening agent affecting on the stratum corneum that is easy to penetrate into the skin. In this study, we prepared mixed ursolic acid hydrogel with wood vinegar(1, 2, 5%) as a penetration enhancer. The accumulation of ursolic acid in the skin from hydrogels was evaluated in vitro hairless mouse skin and skin moisturizing effect of them was evaluated using the corneometer and the tewermeter. And the role of stratum corneum as a protective barrier was evaluated as well. The hydrogels were retained about 40% of water retention capacity 2hrs and had better effect on the stripped skin than full-thickness skin. The accumulation of ursolic acid through stripped skin from hydrogels with wood vinegar was not change compared to normal skin, which indicated the action site of wood vinegar and the accumulation site of ursolic acid would be stratum corneum. From these result, we could find wood vinegar seems to be a good enhancer for active materials with anti-wrinkle and anti aging effect such as ursolic acid, and can be a developed topical delivery system maintaining excellent water retention capacity.
Anti-Proliferative Effect of Tetraphenylporphine (TPP) as an Iron Chelator on Vascular Smooth Muscle Cells and its Release Profiles from Polymer Coating Layer
Park, Min-Hee ; Kang, Soo-Yong ; Park, Hyun-Jeong ; Seo, Jin-Seon ; Park, Young-A ; Kim, Ji-Eun ; Kim, Yang-Geun ; Whang, Bae-Geon ; Munkhjargal, Odonchimeg ; Shim, Young-Key ; Kho, Weon-Gyu ; Lee, Woo-Kyoung ;
Journal of Pharmaceutical Investigation, volume 38, issue 2, 2008, Pages 93~98
DOI : 10.4333/KPS.2008.38.2.093
The drug-eluting stent (DES) implantation is a widely acceptable treatment for coronary heart disease. It was reported that iron chelator had anti-proliferative effect on human vascular smooth muscle cells (HA-VSMCs). In this study, tetraphenylporphine (TPP) was selected as an iron chelator and drug for DES. MTT assay showed that TPP had antiproliferative effect on HA-VSMCs. TPP and polycaprolactone (PCL) were coated onto stainless steel plate using a spraycoating method. From the surface morphology examination of the coated plate by SEM, smooth polymer coating layer could be observed. The thickness of coating layer could be controlled by changing repeating time of coating. From in vitro release test, sustained release of TPP was observed from plate during two weeks. Thus, TPP as iron chelator can be used as drug for stent coating because of its antiproliferative effect and sustain release profile.
PLGA particles and half-shells prepared by double emulsion method: characterization and release profiles of ranitidine
Nam, Dae-Sik ; Kim, Seong-Cheol ; Kang, Soo-Yong ; Odonchimeg, Munkhjargal ; Shim, Young-Key ; Lee, Woo-Kyoung ;
Journal of Pharmaceutical Investigation, volume 38, issue 2, 2008, Pages 99~104
DOI : 10.4333/KPS.2008.38.2.099
PLGA micro/nano particles encapsulating ranitidine as a hydrophilic model drug were prepared by the double-emulsion solvent evaporation method. Surface morphology investigation by scanning electron microscope (SEM) showed that the emulsification by sonication could produce nanoparticles, whereas microparticles were prepared using high speed homogenizer. Moreover, while nanohalf-shell structure instead of spherical nanoparticle could be produced by adding poloxamer into oil phase (MC) with PLGA 504H, the addition of poloxamer didn't change particle shape in case of PLGA 502H. On the other hand, microparticle with poloxamer had more surface pores than those without poloxamer. The size and polydispersity (PDI) of particles were determined by particle size analyzer. Effective diameters of particles were in the range of
in case of nanoparticles and microparticles, respectively. Encapsulation efficiencies were in the range of
. The addition of poloxamer produced the particles with higher encapsulation efficiency. In vitro release study in phosphate buffer (pH 7.4) at
showed common large initial burst release. However, the relative slower release profile could be observed in case of microparticles. Poloxamer addition increased the release rate, which was thought to be related to the increased surface area of particles.
Preparation and Dissolution Characteristics of Sustained Release Granules Containing Indapamide
Park, Ji-Seon ; Seo, Hui ; Kim, Byung-Jin ; Jeong, Sang-Young ; Shin, Byung-Cheol ; Yuk, Sun-Hong ; Hwang, Sung-Joo ; Cho, Sun-Hang ;
Journal of Pharmaceutical Investigation, volume 38, issue 2, 2008, Pages 105~110
DOI : 10.4333/KPS.2008.38.2.105
Indapamide (4-chloro-N-(2-methyl-1-indolinyl)-3-sulfamoyl-benz-amide) is an oral antihypertensive diuretic agent indicated for the treatment of hypertensive. The diuretic and natriuretic effects are mainly due to the structure of o-chlorobenzenesulfonamide. The objective of this study was to formulate sustained release indapamide granules and assess their formulation variables. Granules were prepared by fluid bed coating method and consist of drug layer and membrane layer. The granules were coated with HPC and ethyl cellulose along with plasticizer dibuthyl sebacate. The release of indapamide depended on the type of Eudragit such as RS and NE 30 D used in the formulation controlled release layer. These results obtained clearly suggest that the sustained release oral delivery system for indapamide could be designed with satisfying drug release profile approved.
Improved Dissolution and Characterization of Solid Dispersed Atorvastatin Calcium
Lee, Jun-Hee ; Ku, Jeong ; Park, Jung-Soo ; Park, Jong-Hak ; Ahn, Sik-Il ; Mo, Jong-Hyun ; Kim, Yun-Tae ; Rhee, John-M. ; Lee, Hai-Bang ; Khang, Gil-Son ;
Journal of Pharmaceutical Investigation, volume 38, issue 2, 2008, Pages 111~117
DOI : 10.4333/KPS.2008.38.2.111
To overcome the solubility of poorly water-soluble drug, the formation of solid dispersion using a spray-dryer with polymeric material, that can potentially enhance the dissolution rate extend of drug absorption was considered in this study.
E100 as carrier for solid dispersion is acrylate copolymer that soluble in acidic buffer solutions (below pH 5.0). It was used to increase dissolution of atorvastatin calcium as a water-insoluble drug in acidic environments. In this study, a spray-dryer was used to prepare solid dispersion of atorvastatin calcium and
E100 for purpose of improving the solubility of drug. Atorvastatin calcium and
E100 were dissolved in ethanol and spray-dryed. DSC and XRD were used to analyze the crystallinity of the sample. It was found that atorvastatin calcium is amorphous in the
E100 solid dispersion. FT-IR was used to analyze the salt formation by interaction between atorvastatin calcium and
E100. Comparative dissolution study exhibited better dissolution characteristics than the commercial drug (
) as control. The dissolution rate of atorvastatin calcium was markedly increased in solid dispersion system in simulated gastric juice (pH 1.2). This study proposed that this solid dispersion system improved the bioavailability of poorly water-soluble atorvastatin calcium.
Characterization and Controlled Release of Solid Dispersed Sibutramine
Park, Jung-Soo ; Ku, Jeong ; Lee, Jun-Hee ; Kim, Yun-Tae ; Park, Jong-Hak ; Ahn, Sik-Il ; Mo, Jong-Hyun ; Lee, Hai-Bang ; Khang, Gil-Son ;
Journal of Pharmaceutical Investigation, volume 38, issue 2, 2008, Pages 119~126
DOI : 10.4333/KPS.2008.38.2.119
Solid dispersions of poorly water-soluble drug, sibutramine, were prepared with hydrophilic polymer, poly-N-vinylpyrrolidone (PVP), hydroxypropylmethylcellulose (HPMC) and organic acid, citric acid, to improve the solubility of drug. Physicochemical variation and shape of microsphere were characterized by scanning electron microscopy (SEM), differential scanning calorimeter (DSC) and Fourier-transform infrared spectroscopy (FT-IR). Microspheres containing additives showed more spherical shape than non additive microspheres. In vitro release behavior of microspheres presented at simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8). The solid dispersion form transformed the drug into an amorphous state and dramatically improved its dissolution rate. These data suggest that the solid dispersion technique is an effective approach for developing the appetite depressant drug products and various pharmaceutical excipients are able to control the release behaviors.
Preparation of Lipid Nanoparticles Containing Paclitaxel and their in vitro Gastrointestinal Stability
Kim, Eun-Hye ; Lee, Jung-Eun ; Lim, Deok-Hwi ; Jung, Suk-Hyun ; Seong, Ha-Soo ; Park, Eun-Seok ; Shin, Byung-Cheol ;
Journal of Pharmaceutical Investigation, volume 38, issue 2, 2008, Pages 127~134
DOI : 10.4333/KPS.2008.38.2.127
Peroral administration is the most convenient one for the administration of pharmaceutically active compounds. Most of poorly water-soluble drugs administered via the oral route, however, remain poorly available due to their precipitation in the gastrointestinal (GI) tract and low permeability through intestinal mucosa. In this study, one of drug delivery carriers, lipid nanoparticles (LNPs) were designed in order to reduce side effects and improve solubility and stability in GI tract of the poorly water soluble drugs. However, plain LNPs are generally unstable in the GI tract and susceptible to the action of acids, bile salts and enzymes. Accordingly, the surface of LNPs was modified with polyethylene glycol (PEG) for the purpose of improving solubility and GI stability of paclitaxel (PTX) in vitro. PEG-modified LNPs containing PTX was prepared by spontaneous emulsification and solvent evaporation (SESE) method and characterized for mean particle diameter, entrapping efficiency, zeta potential value and in vitro GI stability. Mean particle diameter and zeta potential value of PEG-modified LNP containing PTX showed approximately 86.9 nm and -22.9 mV, respectively. PTX entrapping efficiency was about 70.5% determined by UV/VIS spectrophotometer. Futhermore, change of particle diameter of PTX-loaded PEG-LNPs in simulated GI fluids and bile fluid was evaluated as a criteria of GI stability. Particle diameter of PTX-loaded PEG-LNPs were preserved under 200 nm for 6 hrs in simulated GI fluids and bile fluid at
when DSPE-mPEG2000 was added to formulation of LNPs above 4 mole ratio. As a result, PEG-modified LNPs improved stability of plain LNPs that would aggregate in simulated GI fluids and bile solution. These results indicate that LNPs modified with biocompatible and nontoxic polymer such as PEG might be useful for enhancement of GI stability of poorly water-soluble drugs and they might affect PTX absorption affirmatively in gastrointestinal mucosa.
Bioequivalence of Atorva Tablet
to Lipitor Tablet
(Atorvastatin 20 mg)
Lim, Hyun-Kyun ; Lee, Tae-Ho ; Lee, Jae-Hyun ; Youm, Jeong-Rok ; Song, Jin-Ho ; Han, Sang-Beom ;
Journal of Pharmaceutical Investigation, volume 38, issue 2, 2008, Pages 135~142
DOI : 10.4333/KPS.2008.38.2.135
The present study describes the evaluation of the bioequivalence of two atorvastatin tablets, Lipitor
(Pfizer, reference drug) and Atorva
(Yuhan, test drug), according to the guidelines of Korea Food and Drug Administration (KFDA). Forty-nine healthy male Korean volunteers received each medicine at the atorvastatin dose of 40 mg in a
crossover study with a two weeks washout interval. After drug administration, serial blood samples were collected at a specific time interval from 0-48 hours. The plasma atorvastatin concentrations were monitored by an high performance liquid chromatography -tandem mass spectrometer (LC-MS/MS) employing electrospray ionization technique and operating in multiple reaction monitoring (MRM) and positive ion mode. The total chromatographic run time was 4.5 min and calibration curves were linear over the concentration range of 0.1-100 ng/mL for atorvastatin. The method was validated for selectivity, sensitivity, linearity, accuracy and precision.
(the area under the plasma concentration-time curve from time zero to 48hr) was calculated by the linear log trapezoidal rule method.
(maximum plasma drug concentration) and
(time to reach
) were complied trom the plasma concentration-time data. Analysis of variance was carried out using logarithmically transformed
. No significant sequence effect was found for all of the bioavailability parameters indicating that the crossover design was properly performed. The 90% confidence intervals of the
ratio and the
ratio for Atorva
, respectively. These values were within the acceptable bioequivalence intervals of
. Based on these statistical considerations, it was concluded that the test drug, Atorva
was bioequivalent to the reference drug, Lipitor