Go to the main menu
Skip to content
Go to bottom
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 26, Issue 4 - Dec 1996
Volume 26, Issue 3 - Sep 1996
Volume 26, Issue 2 - Jun 1996
Volume 26, Issue 1 - Mar 1996
Selecting the target year
A Model for the Active Site of Cyclooxygenase
Kim, Yang-Bae ; Chung, Uoo-Tae ; Park, Il-Yeong ;
Journal of Pharmaceutical Investigation, volume 26, issue 3, 1996, Pages 155~168
The active site of cyclooxygenase was modeled by complementary receptor-cavity mapping procedure using 3D structures of the non-steroidal antiinflammatory drugs (NSAIDs). A total of 50 NSAIDs were chosen as data ligands which compete the same site on the enzyme. Partial atomic charges were estimated, and the energetic differences for various conformations were calculated so as to meet the need for a most efficient overlapping of the probably-equivalent functional groups of the ligand molecules. The structure activity relationships of the NSAIDs, if available, were fully considered throughout the modeling. The overall shape of the model obtained is similar to a boot-without-bottom. Most of inner surface of the cavity appeared as hydrophobic; two polar counterparts except the carboxyl-binding position were found. By this model, some clear explanations could be given on the experimental observations which were not satisfiably understood yet.
Solubility and In vivo Absorption Enhancement of Diclofenac Sodium by
Lee, Kyung-Tae ; Kim, Jong-Hwan ; Kim, Joo-Il ; Kim, Seung-Jo ; Seo, Hee-Kyoung ; Seo, Seong-Hoon ;
Journal of Pharmaceutical Investigation, volume 26, issue 3, 1996, Pages 169~174
Inclusion complexes of diclofenac sodium with
were prepared in aqueous solution, alkaline solution and solid phase. The interaction of diclofenac sodium with
in pH 9.0 alkaline solution was evaluated by the solubility method and the instrumental analysis such as thermal analysis, infrared spectroscopy, X-ray diffractometry. The solubility of diclofenac sodium was increased linearly with the increase in the concentration of
up to 0.15 mol and showed that the aqueous solubility rate of diclofenac sodium was significantly increased by complex with
. The optimum composition of this complex was one molecule of
included 1.59 molecular weight of diclofenac sodium as a guest molecule. The pharmacokinetic parameters of the diclofenac sodium and the complex with
were studied in rats by oral route.
between drug alone and inclusion complex showed significant difference to be 120 minute and 20 minute respectively. Both of
and AUC of inclusion complex was about 40% higher than drug alone. It is estimated from the data in this study that complexation of diclofenac sodium with
increased the absorption rate and improved the bioavalability of the diclofenac sodium by the formation of a water-soluble complexes.
Inhibition of Enzymatic Degradation of Leucine Enkephalin and
-Leucine Enkephalinamide in Various Rabbit Mucosal Extracts by Inhibitors
Chun, In-Koo ; Park, In-Sook ; Hyun, Jeen ;
Journal of Pharmaceutical Investigation, volume 26, issue 3, 1996, Pages 175~185
To inhibit the enzymatic degradation of leucine enkephalin (Leu-Enk) and its synthetic analog.
-leucine enkephalinamide (YAGFL), in the nasal, rectal and vaginal mucosal and serosal extracts of rabbits, effects of enzyme inhibitors such as amastatin (AM), puromycin (PM), thiorphan (TP), thimerosal (TM), EDTA, N-carboxymethyl-Phe-Leu (CPL), phenylethyl alcohol (PEA), phenylmercuric acetate (PMA), benzalkonium chloride (BC) and modified cyclodextrins, alone or in combination, were observed by assaying the pentapeptides staying intact during incubation. Mucosa extracts were prepared by exposing freshly-excised mucosal specimens mounted on Valia-Chien cells to isotonic phosphate buffer while stirring. The degradation of Leu-Enk and YAGFL followed the apparent first-order kinetics. The half-lives (mean) in the nasal, rectal and vaginal mucosal extracts were found to be 1.07, 0.33 and 1.14 hr for Leu-Enk, and 16.9, 6.2 and 6.8 hr for YAGFL, respectively. AM or PM, which is an aminopeptidase inhibitor, did not show a sufficient inhibition of Leu-Enk
degradation in all kinds of extracts.
decreased the degradation rate constants of Leu-Enk about 2 or 3 times, comparing with no additive. However, the use of mixed inhibitors of AM
/TM (0.25 mM)/EDTA (5 mM) resulted in a full stabilization of Leu-Enk by decreasing the degradation rate constants 67.3, 161.3 and 113.8 times far the nasal, rectal and vaginal mucosal extracts, respectively, comparing with no inhibitor. With mixed inhibitors, Leu-Enk remained intact more than 90% after 6 hr-incubation. In the stabilization of YAGFL, hM, TP or CPL alone showed little efffct, and some additives demonstrated a considerable inhibition of YAGFL degradation in the rank order of TM > BC > EDTA. However, the addition of mixed inhibitors such as TM (0.5 mM) and EDTA (5 mM) into the extracts protected YAGFL from the degradation by more than 85% even after 24 hr-incubation, suggesting almost complete inhibition of YAGFL degradation in the extract. On the other hand,
(10%) were also found to retard enzymatic degradation rates of YAGFL markedly, and resulted in staying intact more than 80% of YAGFL in the nasal and vaginal mucosal extracts, and more than 60% in the rectal mucosal extract after 16 hr-incubation.
Sustained Release Matrix Tablet Containing Sodium Alginate and Excipients
Shin, Sung-I ; Lee, Beom-Jin ; Lee, Tae-Sub ; Heo, Bo-Uk ; Ryu, Seung-Goo ;
Journal of Pharmaceutical Investigation, volume 26, issue 3, 1996, Pages 187~192
The matrix tablet containing sodium alginate and
can release drugs in a controlled fashion from hydrogel with gelling and swelling due to their interaction as water penetrates the matrices of the tablet. The purpose of this study was to evaluate release characteristics of the matrix tablet varying the amount of sodium alginate,
and other excipients such as chitosan, hydroxypropyl methylcellulose (HPMC) and
RS100 in the simulated gastric and intestinal fluid. The practically soluble ibuprofen was used as a model drug. The release profiles of matrix tablet in the gastric fluid as a function of sodium alginate/
ratio was not pronounced because of low solubility of drug and stability of alginate matrices. However, release rate of drug from the matrix tablet in the intestinal fluid was largely changed when sodium alginate/
ratio was increased, suggesting that the ratio of sodium alginate/
was an important factor to control the gelling and swelling of the matrix tablet. The incorporation of other excipients into the matrix tablet also influenced the release rate of drug. The chitosan and HPMC decreased the release rate of drug. No release of drug was occurred when
RS100 was added into the tablet. The retarded release of matrix tablet when excipients were added resulted from the hindrance of swelling and gelling of the matrix tablet containing sodium alginate and
. The hardness and bulk density of the matrix tablet was not correlated with release rate of drug in the study. From these findings, the ratio of sodium alginate and
in the matrix tablet in addition to incorporation of excipients could be very important to control the release rate of drug in dosage form design.
Polymorphism of Biphenyl Dimethyl Dicarboxylate
Sohn, Young-Taek ; Park, Myung-Sook ; Kwon, Soon-Kyoung ;
Journal of Pharmaceutical Investigation, volume 26, issue 3, 1996, Pages 193~199
The polymorphism of biphenyl dimethyl dicarboxylate was investigated by DSC. From product five crystal forms. Form 1, Form 2, Form 3, Form 4, and Form 5, were characterized and three crystal forms. Form 6, Form 7, and Form 8, were prepared with the recrystallization method. The dissolution patterns of these eight crystal farms were also studied, but there was practically no difference in dissolution rate.
Characteristics and Drug Release Control of Crosslinked Poloxamer Hydrogel
Byun, Eun-Jung ; Lee, Seung-Jin ; Kim, Kil-Soo ;
Journal of Pharmaceutical Investigation, volume 26, issue 3, 1996, Pages 201~205
Poloxamer, block copolymers of ethylene oxide and propylene oxide was crosslinked by diisocyanates and triisocyanates to form water-swellable, physically strong, rubber-like elastic, high biocompatible polyurethanes. The isocyanate-hydroxyl stoichiometry was kept 1:1, but the crosslinking density was varied. The variations examined were the ratio of diisocyanate and triisocyanate. The delivery of two drugs of different water solubilities from hydrogel matrices was studied. It appeared that the drug nature greatly influenced its release kinetics possibly due to drug-polymer interactions. The release profiles, however, could be modified to a great extent by adjusting the polymer network structure Generally the high crosslinking density was required for prolonged drug delivery.
Theoretical Model for the Electrical Resistance of Skin
Oh, Seaung-Youl ;
Journal of Pharmaceutical Investigation, volume 26, issue 3, 1996, Pages 207~213
The kinetic change of electrical resistance of hairless mouse skin as a function of ionic strength of the bathing medium was determined from impedance measurements. After increasing (decreasing) the ionic strength of the bathing medium, resistance decreased (increased) continuously with time, finally reaching an equilibrium value. We have modelled this process, using nonsteady-state diffusion kinetics. The results show semi-quantitative correlation between theoretically derived and experimentally obtained values. Overall, this work provides further mechanistic insight into ion-conduction through the skin.
Antihyperlipidemic Activity of Scutellaris baicalensis Georg., Coptidis japonica Makino and Rhei koreanum Nakai on Experimental Hyperlipidemia in Rats
Ro, Hwan-Seong ; Ko, Woo-Kyoung ; Kim, Oon-Ja ; Park, Kun-Koo ; Cho, Young-Whan ; Park, Hyoung-Sup ;
Journal of Pharmaceutical Investigation, volume 26, issue 3, 1996, Pages 215~219
Active component was sought among three herb medicines, which are used in combination as a traditional medicine prescribed for patients with hyperlipidemia related diseases. Antihyperlipidemic effect of this remedy has previously been shown model by the authors on the animal model. Hyperlipidemia was induced on male Wistar rats by keeping them on high lipid diet for one week, as previously described by the authors. Blood lipid profile was verified on these rats by measuring total cholesterol (TC), triglyceride (TG), high density lipoprotein (HDL) and low density lipoprotein (LDL). Then, the diet was changed to normal. At the same time, methanol extracts of Scutellaris baicalensis Georg.(radix), Coptidis japonica Makino(rhizoma) or Rhei koreanum Nakai(rhizoma) were given on daily basis, and changes in the blood lipid profile were monitored for 4 weeks. Methanol extract of Scutellaris baicalensis Georg. significantly reduced the TC value, implying the in vivo antihyperlipidemic effect.
A Study on the Optimum Conditions for Preparation of Calcium hydrogenphosphate Dihydrate by Box-Wilson Experimental Design
Rhee, Gye-Ju ; Kwak, Son-Hyuk ; Suh, Sung-Su ;
Journal of Pharmaceutical Investigation, volume 26, issue 3, 1996, Pages 221~232
An abrasive, calcium hydrogen phosphate dihydrate (DCPD), was synthesized in a Box-wilson experimental design by reactions between phosphoric acid and milk of lime, and calcium chloride and sodium phosphate solutions, and stabilized with TSPP and TMP. The optimum conditions for preparation of DCPD from phosphoric acid with milk of lime were such as; reaction temp.;
, conc. of lime; 25.9%, conc. of phosphoric acd; 77.9%, drying temp.;
and final pH; 6.46. The physico-chemical and pharmaceutical properties of DCPD were showed as follows: glycerin absorption value(68 ml/100g), whiteness(99.5%), particle size(10.9 nm), pH(7.8), and set test(pass). XRD and SEM of DCPD indicated a monoclinic system crystallographically.
adsorption isotherm curve by BET showed non porous type II form. The micromeritic parameters of DCPD showed that surface area was
and pore volume, pore area and pore radius were negligible. The rheogram of the toothpaste containing DCPD showed pseudoplastic flow with yield value of 321, and thixotropic behavior forming hysteresis loop. These results meet the requirements as abrasive standard, and sythesized DCPD is expected as a good dental abrasive such as a high quality grade in practice.