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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
Editor in Chief :
Volume & Issues
Volume 25, Issue 4 - Dec 1995
Volume 25, Issue 3 - Sep 1995
Volume 25, Issue 3 - Sep 1995
Volume 25, Issue 2 - Jun 1995
Volume 25, Issue 1 - Mar 1995
Selecting the target year
Effect of Exercise on the Physiological Changes of Korean Cyclists
Kim, Chong-Kook ; Lee, Beom-Jin ;
Journal of Pharmaceutical Investigation, volume 25, issue 2, 1995, Pages 95~100
Serum electrolyte concentration and body weight were determined before and after exercise for 2h in Korean cyclists. The serum concentration of electrolytes (Na, Ca, Zn, K, P and Cl) was increased but that of Mg was decreased as a result of exercise. The increase of serum K and P concentration was statistically significant after exercise. As the exercise time increased, the loss of body weight also increased due to dehydration and sweat. The loss of body weight ranged 1.0 to 2.3 Kg as a function of exercise time but cyclists showed the exhaustion and muscle fatigue 2h after exercise. As the ambient temperature increased, the loss of body weight was slightly increased. However, frequent drinking water was required because of dehydration and thirst. Although frequent drinking water may reduce weight loss and thirst during exercise, sports drinking beverages simultaneously containing electrolytes and nutrients are more useful to replenish loss of water and electrolytes in an exhausted condition, resulting in the improvement of physical performance.
Preparation and Characteristics of Surface-Modified Albumin Microspheres with Methotrexate
Hwang, Sung-Joo ; Jo, Hang-Bum ; Rhee, Gye-Ju ; Kim, Chong-Kook ;
Journal of Pharmaceutical Investigation, volume 25, issue 2, 1995, Pages 101~108
The surface of albumin microspheres could be modified with methotrexate (MTX) by using 1,3-dicyclohexylcarbodiimide (DCC). Surface-modified albumin microspheres entrapping no MTX (SAMS), free MTX (SAMSF) and MTX-bovine serum albumin (BSA) conjugates (SAMSC) were prepared. respectively, and their release characteristics were investigated in the presence of trypsin using a dissolution tester. The mean diameters of all the microspheres were
, and their shapes was small and uniform. MTX bound tn their surfaces was released slower than the entrapped free MTX, and laster than the entrapped MTX-BSA conjugates. Also, surface-modified MTX was scarcely released in the absence of a proteolytic enzyme. Therefore, the surface-modified MTX may be released rapidly from SAMSC at the target site, and thereafter MTX may be released slowly from the encapsulated MTX-BSA conjugates in SAMSC for a long period.
Controlled Release Dosage Form of Narcotic Antagonist(I): Synthesis of Biodegradable Polyphosphazenes and Preparation and Release Characteristics of Naloxone Implant
Park, Joo-Ae ; Lee, Seung-Jin ; Kim, Hyung-Kuk ; Kim, Kil-Soo ;
Journal of Pharmaceutical Investigation, volume 25, issue 2, 1995, Pages 109~116
For the administration of narcotic antagonist with short half-life and low patient compliance, the sustained release system using biodegradable matrix is effective. Polyphosphazenes are of considerable interest as biodegradable matrix systems for controlled release of drugs. In this study, biodegradable polyphosphazenes available for the sustained release implantable device were synthesized, and their application was examined. Poly[dichlorophosphazene] was synthesized by solution polymerization method and confirmed with IR spectrum. Poly[bis(ethyl glycinate) phosphazene] and poly[ (diethyl glutamate)-co-(ethyl glycinate)phosphazene] were then produced by substitution of amino acid alkyl esters for chloride side groups. Using these polymers, the implantable devices of 1 mm thickness and
size containing naloxone hydrochloride were prepared and their release and degradation profiles were measured. In the case of poly[bis(ethyl glycinate)phosphazene] with swelling characteristics, degradation rate was slower than the release rate, showing that the release rate is partly dependent on the swelling rate. In contrast, the degradation rate of polyl[(diethyl glutamate)-co-(ethyl glycinate)phosphazene] matrix was identical with release rate of naloxone hydrochloride. On the basis of these results, it is expected that these polymers can be applied to sustained release implantable systems delivering narcotic antagonist.
Controlled Release Dosage Form of Narcotic Antagonist(II) : Biocompatibility and Pharmacokinetics of Naloxone Implant
Moon, Mi-Ran ; Park, Joo-Ae ; Lee, Seung-Jin ; Kim, Hyung-Kuk ; Kim, Kil-Soo ;
Journal of Pharmaceutical Investigation, volume 25, issue 2, 1995, Pages 117~123
For the effective administration of narcotic antagonist, the application of sustained release implantable systems with biodegradable polyphosphazene was examined. Using poly[(diethyl glutamate)-co-(ethyl glycinate) phosphazene], the implantable devices containing naloxone hydrochloride were prepared and in vivo implantation studies were carried out subcutaneously in rat and rabbit with this preparation for the biocompatibility and pharmacokinetics. The histological finding in rats at initial time period was the inflammation that occurred focally around the implants, but they were showed subsequent mild and limited chronic inflammations and the irreversible changes such as necrosis and degeneration of the muscle or connective tissues were not observed. Therefore the placebo and naloxone implants are considered to be biocompatible formulations histologically. In pharmacokinetic studies, the release of naloxone from the naloxone implants into blood plasma was maintained in 192 hours, but the initial burst effect was observed. If this problem was solved, the application for the narcotic antagonist sustained release systems can be expected.
Effect of Fatty Alcohols on Skin Permeation of Flurbiprofen
Kim, Hyun ; Park, Eun-Seok ; Chi, Sang-Cheol ;
Journal of Pharmaceutical Investigation, volume 25, issue 2, 1995, Pages 125~128
To increase the skin permeation rate of flurbiprofen, fatty alcohols were added in propylene glycol vehicle containing 1% flurbiprofen. Their enhancing effect on the skin permeation of flurbiprofen was evaluated using Keshary-Chien diffusion cells fitted with excised rat skins. Lauryl alcohol and oleyl alcohol increased the skin permeation rate of flurbiprofen 11.3 and 8.5 fold, respectively, compared to the control vehicle.
Skin Permeation of Indomethacin from Gels
Kam, Sung-Hoon ; Park, Eun-Seok ; Chi, Sang-Cheol ;
Journal of Pharmaceutical Investigation, volume 25, issue 2, 1995, Pages 129~136
In order to reduce the systemic side effects and the gastrointestinal irritation of indomethacin following its oral administration, the drug was formulated as a transdermal gel using poloxamer 407. In vitro diffusion cells fitted with excised rat skins were used to evaluate the effects of formulation variables on skin permeation of indomethacin from poloxamer gels. The formulation variables were the concentrations of indomethacin, poloxamer 407 and ethanol, and the gel pH. The increase of the drug amount in the gel from 0.5% to 2.0% induced a direct but nonlinear increase in the skin permeation rate of indomethacin. The increase of poloxamer concentration from 17.5% to 25% in the gel resulted in a decrease of skin permeation rate of indomethacin, which was due to a reduction in the amount of free drug molecules available for permeation through skin by entrapping more drug molecules within the micelles formed by poloxamer. The increase of ethanol concentration from 10% to 20% in the gel resulted in a linear increase of permeation rate of indomethacin through skin, possibly due to the penetration enhancing effect of ethanol. The skin permeation of indomethacin was substantially influenced by the gel pH, exhibiting a maximum at pH 4.
Uptake of a Dipeptide by the Dipeptide Transporter in the HT-29 Intestinal Cells
Oh, Doo-Man ;
Journal of Pharmaceutical Investigation, volume 25, issue 2, 1995, Pages 137~143
The peptide transporter can be utilized for improving the bioavailability of compounds that are poorly absorbed. Characterization of the dipeptide uptake into the human intestinal epithelial cells, HT-29 was investigated. The uptake of tritiated glycylsarcosine
was measured in confluent or subconfluent HT-29, Caco-2, and Cos-7 cells. Uptake medium was the Dulbecco's Modified Eagle's Media (DMEM) adjusted to pH 6.0. Both HT-29 and Caco-2 cells expressed the dipeptide transporter significantly (p<0.005) but Cos-7 did not. Certain portions of passive uptake were observed in all three cell lines. Uptake of Gly-Sar was largest at 7 days after plating HT-29 cells with significant inhibition with 25 mM cold Gly-Sar (p<0.05). but expression ratio of the dipeptide transporter was 0.7, suggesting lower expression. The effect of pH on Gly-Sar uptake was not significant in the range of pH 6 to 8. Gly-Sar uptake was also inhibited with 50 mM carnosine, 25 mM Gly-Sar, and 35 mM cephalexin significantly (p<0.05). From above results the dipeptide transporter was expressed well in HT-29 cells and was similar to that in the small intestine, suggesting that large amounts of mRNA of the transporter from the cells can be obtained.
Comparison of Cu(II)-DIPS and Human Recombinant Superoxide Dismutase, an Antioxidant
Yong, Chul-Soon ; Nam, Doo-Hyun ; Huh, Keun ;
Journal of Pharmaceutical Investigation, volume 25, issue 2, 1995, Pages 145~152
The superoxide dismutase (SOD) mimetic activity of copper complex of 3,5-disopropylsalicylic acid (Cu(II)-DIPS) was tested and compared to those of human recombinant SOD (hrSOD) and its conjugate form with polyethyleneglycol (PEG) using fer- ricytochrome c reduction assay. Stability constant of Cu(II)-DIPS was measured po- tentiometrically using SCOGS2 program. In the presence of 10 g/L albumin, Cu(II)-DIPS lost most of its SOD mimetic activity. HrSOD was modified with polyethylene glycol (PEG) of M.W. 5000. These conjugates have markedly prolonged plasma half-lives of enzymatic activity (15.5 hr) compared to native hrSOD (5 min). In summary, efficient SOD mimetics should be stable enough not to dissociate in blood by serum protein. HrSOD could have longer half-life by conjugation with inert PEG for sustained SOD effect.
Sustained Release of Ibuprofen from Sodium Alginate Beads
Kwon, Sang-Keun ; Seo, Seong-Hoon ;
Journal of Pharmaceutical Investigation, volume 25, issue 2, 1995, Pages 153~161
Alginic acid is a hydrophilic , colloidal polysaccharide obtained from cell wall of seaweed or brown algae and has a broad range of applications. Alginlc acid becomes alginate gel bead due to its cation-induced gelation. Dried alginate beads can be reswollen according to environmental pH. The purpose of this paper is to explore the possible applicability of alginate beads as an oral controlled release system of ibuprofen. In this experiment ibuprofen was incorporated in alginate beads and alginate beads were treated with various methods. Ibuprofen release from alginate beads in phosphate buffer (pH 7.4) was laster than in distilled water and dilute HCl. The release of ibuprofen was more sustained in bead than simple mixture and coprecipitate of ibuprofen and sodium alginate. The dissolution rate of ibuprofen was decreased in using of bead that hardened with formaldehyde. The dissolution rate of the drug from the bead was the fastest in 12 hour dried beads, 1.5%-sodium alginate concentration and 1%-calcium chloride concentration. Sodium alginate bead can be used as a sustaind release drug delivery system of water-insoluble drugs.
에 대한 소고
Journal of Pharmaceutical Investigation, volume 25, issue 2, 1995, Pages 163~164