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REFERENCE LINKING PLATFORM OF KOREA S&T JOURNALS
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Journal of Pharmaceutical Investigation
Journal Basic Information
Journal DOI :
The Korean Society of Pharmaceutical Sciences and Technology
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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
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Mechanistic Studies of Ketoprofen Absorption in Perfused Rat Intestine Model
Kim, Mi-Jeong ; Lane, Majella E. ;
Journal of Pharmaceutical Investigation, volume 37, issue 2, 2007, Pages 73~78
DOI : 10.4333/KPS.2007.37.2.073
The aim of this study was to investigate the absorption properties of ketoprofen. The in-situ perfusion model has advantages over in vitro models as it provides intact lymphatic and blood flow circulation. The absorption properties of six different concentrations of ketoprofen have been studied in single pass in-situ rat intestine model.
4000 was used as a permeability marker and the possibility of an energy dependent contribution to ketoprofen absorption was also Investigated using the metabolic inhibitor sodium azide. Three different concentrations of sodium azide were studied to examine its effect on absorption of ketoprofen from the rat intestine. The findings of this study suggest that mono-carboxylic type drugs like ketoprofen cause permeability changes in the intestine. This is shown by the increase in absorption of
4000 as the concentration of ketoprofen is increased. However, the trend for ketoprofen permeability is to decrease over the concentration ranges. It was observed that the Papp values for ketoprofen with sodium azide shows a trend towards reduction in the amount of ketoprofen absorbed from the rat intestine which was significantly different (p<0.05) from that of ketoprofen with sodium azide 3.0mM. This indicates that sodium azide has an affect on the absorption of ketoprofen. The pH of all the perfusion solutions was altered to
by the buffering capacity of the small intestine secretions. The results suggest that mechanisms other than passive diffusion may be involved in ketoprofen absorption. This would be consistent with the involvement of active transport or saturatable processes in the absorption of drugs containing monocarboxylic acid group, as has been previously suggested from in vitro data.
Bioavailability of Tripotassium Dicitrato Bismuthate by ICP-MS in Human Volunteers
Kwon, Oh-Seung ; Kwon, Jee-Young ; Yoon, Ae-Rin ; Park, Kyung-Soo ;
Journal of Pharmaceutical Investigation, volume 37, issue 2, 2007, Pages 79~84
DOI : 10.4333/KPS.2007.37.2.079
This study was aimed to establish analytical method of Bi to develop a guideline of the bioequivalence test of tripotassium dicitrato bismuthate (TDB). For this purpose, a simple, specific and sensitive inductively coupled plasma-mass spectrometry (ICP/MS) method were developed and validated in human plasma. Various concentrations of bismuth standard solution (0-25ng/mL) were prepared with distilled water and human blank plasma. To 10mL of the volumetric flasks, 2mL of blank plasma was added with 8ml of distilled water. Bi standard solution was added to prepare the calibration samples and injected into ICP-MS. The plasma samples obtained from volunteers given 3 tablets of bismuth (total 900mg as TDB) were analyzed as described above. As a result, the coefficients of variation were <20% in quantitation limit (0.2 ng/mL) and <15% at the rest of concentrations. The stability test by repeated freezing-thawing cycles showed that the samples were stable only for 24hr. The stability tested for samples with a short-term period of storage at room temperature and pre-treatment prior to the analysis showed very stable over 24hr. In 8 healthy Korean subjects received Denol tablets at the dose of 900mg bismuth, AUC,
were determined to be
, respectively, from the plasma bismuth concentration-time curves. In conclusion, the method was suitable for the determination of bismuth in human plasma samples and could be applied to bioequivalence test of bismuth tablet.
Preparation and Evaluation of Cubic Liquid Crystalline Phase Gel and Cubosome containing Polyethoxylated Retinamide
Kyong, Kee-Yeol ; Jee, Ung-Kil ; Cho, Wan-Goo ;
Journal of Pharmaceutical Investigation, volume 37, issue 2, 2007, Pages 85~94
DOI : 10.4333/KPS.2007.37.2.085
The objective of this study is to prepare a stable delivery systems containing polyethoxylated retinamide(PERA) - derivatives of retinoic acid, effective anti-wrinkle and anti-acne agent. Cubic liquid crystalline phase gel (CLCPG) and cubosomes containing various concentrations of PERA were prepared to investigate the physicochemical properties. Furthermore, stability and transdermal absorption efficacy of the CLCPG containing PERA were investigated in comparison with oil-in-water (O/W) emulsions which are predominantly used as a topical formulation. CLCPG increase the stability of PERA in comparison with O/W emulsion. For tropical application, CLCPG containing PERA shows higher moisturizing effect than that of O/W emulsion. In skin permeation test, CLCPG shows higher PERA deposit on epidermis. With its specific physicochemical property caused by the glyceryl oleate, CLCPG itself could be used for stabilizer of various actives and applied as an effective delivery system for topical application. Cubosome, nano-sized dispersed CLCPG, is also expected to be applied in a various field of industry like food, cosmetics and pharmaceuticals.
In vitro Release Characteristics of Nitroglycerin from Microemulsion-Based Hydrogel System for Anal Fissure Treatment
Lee, Sang-Kil ; Shin, Hyun-Woo ; Kang, Myung-Joo ; Cho, Seong-Wan ; Cho, Jae-Youl ; Lee, Jae-Hwi ; Choi, Young-Wook ;
Journal of Pharmaceutical Investigation, volume 37, issue 2, 2007, Pages 95~99
DOI : 10.4333/KPS.2007.37.2.095
To develop topical nitroglycerin (NTG) preparation far chronic anal fissure treatment, the release rate of NTG should be controlled carefully. For this, microemulsion was prepared from the phase diagram construction with Cremophor ELP, ethanol and Labrafil
and the topical gel was prepared by dispersing NTG containing microemulsion into hydrophilic polymers. in viかo release characteristics were evaluated with Franz diffusion cell using cellulose membrane and compared with control hydrogels. The release rate of NTG was followed
order kinetics and, when comparing the NTG release from control hydrogel with that from the microemulsion-based hydrogel, the NTG release rate was controlled by the content of polymers within continuous phase and the concentration of dispersed phase.
Formulation of Sustained Release Granule for Venlafaxine-HCl Using Water-Insoluble Polymer
Park, Ji-Seon ; Seo, Jin-A ; Jeong, Sang-Young ; Yuk, Soon-Hong ; Shin, Byung-Cheol ; Hwang, Sung-Joo ; Cho, Sun-Hang ;
Journal of Pharmaceutical Investigation, volume 37, issue 2, 2007, Pages 101~106
DOI : 10.4333/KPS.2007.37.2.101
Venlafaxine, 1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl] cyclohexanol hydrochloride is a novel, nontricyclic antidepressant. venlafaxine is a unique antidepressant that differs structurally from other currently available. The aim ot the study was to formulate sustained-release venlafaxine granules and assess their formulation variables. It consists of two layers, venlafaxine drug layer and sustained release coating layer and manufactured by fluidized bed process. The sustained release of drug could be increased by double-control rising various components in venlafaxine drug layer and sustained-release layer. The drug-containing granules were coated with cellulose acetate, cetyl alcohol and Eudragit RS along with plastisizer such as dibuthyl sebacate as an nano-pore former The release oi venlafaxine depended on the type of Eudragit such as RS, and RL used in the formulation of controlled release layer. These results obtained clearly suggest that the sustained release oral delivery system for venlafaxine could be designed with satisfying drug release profile approved.
The Effect of Long-term Administration of Epigallocatechin on the Pharmacokinetics of Verapamil in Rats
Yun, Jae-Kyung ; Choi, Jun-Shik ;
Journal of Pharmaceutical Investigation, volume 37, issue 2, 2007, Pages 107~111
DOI : 10.4333/KPS.2007.37.2.107
Epigallocatechin gallate (EGCC), a flavonoid, is the main component of green tea extracts. EGCG has been reported to be an inhibitor of P-glycoprotein (P-gp) and cytochrom P450 3A(CYP3A4). This study investigated the effect of long-term administration of EGCG on the pharmacokinetics of verapamil in rats. Pharmacokinetic parameters of verapamil were determined after oral administration of verapamil (9 mg/kg) in rats pretreated with EGCG (7.5 mg/hg) for 3 and 9 days. Compared to oral control group, the presence of EGCG significantly (p<0.01) increased the area under the plasma concentration-time curve (AUC) of verapamil by 102% (coad), 83.2% (3 days) and 52.3% (9 days), and the peak concentration
by 134% (coad), 120% (3 days) and 66.1% (9 days). The absolute bioavailability (A.B.%) of verapamil was significantly (p<0.01) higher by 8.4% (coad), 7.7% (3 days), 6.4% (9 days) compared to control (4.2%), and presence of EGCG was no significant change in the terminal half-life
and the time to reach the peak concentration
of verapamil. Our results indicate that EGCG significantly enhanced oral bioavailability of verapamil in rats, implying that presence of EGCG could be effective to inhibit the CYP3A4-mediated metabolism and P-gp efflux of verapamil in the intestine. Drug interactions should be considered in the clinical setting when verapamil is coadministrated with EGCG or EGCG-containing dietary.
Microencapsulation of Fish Oil by Spray Drying using Different Wall Materials
Cha, Kwang-Ho ; Yang, Jin-Su ; Yeon, Seung-Ho ; Hong, Jang-Hwan ; Kim, Min-Soo ; Kim, Jeong-Soo ; Hwang, Sung-Joo ;
Journal of Pharmaceutical Investigation, volume 37, issue 2, 2007, Pages 113~117
DOI : 10.4333/KPS.2007.37.2.113
The aim of this study was to investigate the effect of different wall material on the microencapsulation efficiency of microcapsules containing fish oil. The present work reports on the microencapsulation of fish oil by spray drying using hydroxypropyl methylcellulose (HPMC) 2910, maltodextrin, gelatin, sodium caseinate as wall materials. The emulsion stability was assessed by emulsion stability index value (ESI). The microstructural properties of microcapsules was evaluated by scanning electron microscopy (SEM) and microencapsulation efficiency (ME) was assessed by soxhlet method. The highest ESI and ME were observed in the case of a 1:1 gelatin/sodium caseinate ratio and 1:1 glycerin fatty acid ester/lecithin ratio, and ME of microcapsules was increased with increasing the ESI of emulsion. Thus, the stability of emulsion was a critical factor for the encapsulation of fish oil.
Analysis of Prescriptions for Oral Solid Dosage Forms Split at Primary Health Care Using National Health Insurance Database
Park, Se-Jung ; Lee, Suk-Hyang ; Lee, Eui-Kyung ;
Journal of Pharmaceutical Investigation, volume 37, issue 2, 2007, Pages 119~126
DOI : 10.4333/KPS.2007.37.2.119
Tablet splitting is used in pharmacy practice to adjust the dose to be administered. However, it also causes several problems such as undesirable effect for sustained release or enteric-coated dosage form, inaccuracy of dose, and pharmacist's safety by splitting hazardous drugs. This study investigated the current status of oral dosage form splitting for patients older than 19 years by analyzing Korea National Health Insurance Claims Database. Out of oral solid drugs prescribed (N=1,486,584) 9.8% of them included tablets (or capsules) split. There were some splitting cases even in sustained release (4.9%), enteric-coated forms (1.3%) and hazardous drugs (2.7%) that were selected by NIOSH (The National Institute for Occupational Safety and Health). The most frequently split drugs were antihistamines, neuropsychotics and steroids. In case of digoxin and warfarin, unit doses in a domestic market were not diverse compared to foreign markets. Guidelines for splitting oral solid dosage forms, approval of diverse doses and conducting dose-response studies for the commonly splitting ingredients on Korean people are needed for the saff and effective use of oral solid drugs.