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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 22, Issue 4 - Dec 1992
Volume 22, Issue 3 - Sep 1992
Volume 22, Issue 3 - Sep 1992
Volume 22, Issue 2 - Jun 1992
Volume 22, Issue 1 - Mar 1992
Volume 22, Issue 1 - Mar 1992
Selecting the target year
Hydrogels for Drug Delivery System:-Colon-Specific Delivery-
Park, Ki-Dong ; Jeong, Seo-Young ; Kim, Young-Ha ;
Journal of Pharmaceutical Investigation, volume 22, issue 4, 1992, Pages 251~266
A major problem with the peptide-based drugs is that these drugs must generally be administered by injection. Therefore, there is considerable research interest in alternative routes of delivery, such as buccal, nasal, gastrointestinal route and etc. Site-specific drug delivery to the colon, as an alternative to parenteral drug delivery, is of interest for the delivery of peptide-based drugs as well as the delivery of low molecular weight drugs for the treatment of colonic disease, This review describes some considerations of colon-specific drug delivery using hydrogels.
Preparation and Evaluation of Sustained-Release
Han, Kun ; Shin, Do-Su ; Jee, Ung-Kil ; Chung, Youn-Bok ;
Journal of Pharmaceutical Investigation, volume 22, issue 4, 1992, Pages 267~279
Microencapsulations of amoxicillin and cephalexin, using Eudragit RS, RL, E, S and L were investigated. The microcapsules were prepared by the solvent evaporation process in liquid paraffin phase, which is based on dispersion of acetone/isopropanol containing the drug in liquid paraffin. Aluminium tristearate was used as an additive for the preparation of microcapsules. The size distribution, dissolution test and observation by SEM were examined. Good reproducibility in microcapsule preparation was observed. The microcapsules obtained were spherical and free-flowing particles. The dissolution rates of amoxicillin and cephalexin from the microcapsules were considerably decreased as compared with those from amoxicillin and cephalexin powder, respectively. As the dispersing agents (aluminium tristearate) increased, the particle size of microcapsules decreased and the dissolution rate increased. In order to control the release rate of drugs, microcapsules were prepared by mixing Eudragit RS/RL or Eudragit S/L. As Eudragit RL ratio in microcapsule of Eudragit RS/RL increased, the dissolution rate increased. As Eudragit L ratio in microcapsule of Eudragit S/L increased, the dissolution rate increased. Furthermore, the release rates of drugs from Eudragit RS/L or RS/polyelthylene glycol 1540 (PEG 1540) were examined. The dissolution rate of drugs increased with increasing of Eudragit L or PEG 1540 ratio. In conclusion, the release rates of drugs from Eudragit RS/RL or RS/PEG 1540 microcapsule could be controlled, and these microcapsules will be convenient for reducing frequency of administration.
Stability and Dissolution Enhancement of Omeprazole by Pharmacentical Formulation
Jee, Ung-Kil ; Lee, Gye-Won ; Jeon, Un-Jong ;
Journal of Pharmaceutical Investigation, volume 22, issue 4, 1992, Pages 281~287
Omeprazole (OMZ) is very unstable in acidic solution, which selectively inhibit the release of the gastric juice in the gastric mucosa, In order to stabilize (OMZ) in oral solid dosage form, the enteric-coated microcapsules and compression-coated OMZ tablets containing lysine or arginine as stabilizer were prepared and their dissolution and stability test were performed. The haif life of OMZ microcapsules containing arginine was 194 days at
and OMZ was completely released in 60 min. The half-lives of enteric coated and non-coated compression-coated OMZ tablets with lysine were 292 and 95 days at
, respectively. The half-lives of enteric coated and non-coated compression-coated tablets with arginine were 1752 and 293 days at
, respectively, and OMZ were released completely in 20 min in the 2nd fluid of K.P.VI. Consequently, the enteric-coated compression-coated OMZ tablets with arginine as stabilizer provided a good formulation for oral solid dosage form.
Kinetic Analysis of the Counter-transport Phenomenon in the Hepatic Transport of Organic Anionic Drugs
Chung, Youn-Bok ; Han, Kun ; No, Jung-Ryul ;
Journal of Pharmaceutical Investigation, volume 22, issue 4, 1992, Pages 289~300
The counter-transport phenomena in the hepatic transport of 1-anilino-8-naphthalene sulfonate (ANS) were kinetically investigated by analyzing the plasma disappearance-time profiles and the transport into the isolated hepatocytes. In vivo "counter transport phenomena" were simulated based on the perfusion model which incorporated the carrier-mediated transport and the saturable intracellular binding. The condition that the mobility of carrier-ligand complex is greater than that of free carrier is not essential for the occurrence of counter-transport phenomenon. To examine the inhibitory effects on the initial uptake of a ligand by the liver, it is necessary to judge whether the true counter-transport mechanism (trans-stimulation) is working or not. The initial plasma disappearance curves of ANS were then kinetically analyzed based on a two-compartment model, in which the ligand is eliminated only from the peripheral compartment (liver compartment). No effects on the initial plasma disappearance rates of ANS were observed after preloading of bromophenol blue (BPB) or rose bengal (RB) in the liver. Inhibitory effect of BPB or RB on the initial uptake (or efflux) rates of ANS by the isolated hepatocytes were not observed, suggesting that the true counter transport mechanism is not working. In conclusion, checking the preloading effects of transstimulation on the initial uptake of a ligand by the liver could be a useful criterion for carrier cycling and common use of the same carrier between two ligands. However, one cannot exclude those possibilities even if the preloading effects cannot be observed.
Effect of Phenobarbital on the Metabolite Kinetics of Diltiazem in Rats
Lee, Yong-Bok ; Koh, Ik-Bae ; Shim, Chang-Koo ; Kim, Shin-Keun ; Lee, Min-Hwa ;
Journal of Pharmaceutical Investigation, volume 22, issue 4, 1992, Pages 301~306
The influence of phenobarbital (PB) pretreatment (75 mg/kg/day, i.p. for 4 days) on the metabolite kinetics of diltiazem (DTZ) was studied in rats in order to elucidate the effect of esterase induced by PB on the formation of DTZ to desacetyldiltiazem (DAD), DAD was injected via portal vein (3 mg/kg) to the control and PB-pretreated rats, The intrinsic hepatic clearance of DAD was significantly increased by PB pretreatment and the absolute bioavailability of DAD was significantly decreased in the PB-pretreated rats. According to the hepatic biotransformation model of DTZ, the fraction of systemic clearance of DTZ which forms DAD
was different from that of DTZ which furnishes the available DAD to the systemic circulation
in control rats. This result shows that DTZ was suspected of the sequential hepatic first-pass metabolism. On the other hand, PB pretreatment enhanced the
value of DTZ by 44%. It may be concluded that the deacetylation of DTZ to DAD in rats is increased by the esterase induced by PB but the transfer rate of DAD immediately formed from DTZ into systemic circulation is not affected by PB due to the 27% decreased absolute bioavailability of DAD resulting from PB pretreatment.
Improvement of Dissolution Rate of Mefenamic Acid by Roll Mixing with Sodium Lauryl Sulfate
Park, Seong-Yeon ; Seo, Seong-Hoon ;
Journal of Pharmaceutical Investigation, volume 22, issue 4, 1992, Pages 307~315
Dissolution rate of practically insoluble mefenamic acid was improved by roll mixing with sodium lauryl sulfate (SLS) or polyvinylpyrrolidone (PVP). The dissolution rate of the drug roll mixtures with SLS was superior to that of roll mixtures with PVP. The maximal dissolution rate was found in the roll mixtures system with SLS content of 60%. The dissolution rate of mefenamic acid roll mixtures with SLS content of 60% reached to the maximum value after 10 min of roll mixing. The transport of roll mixtures with SLS across rat jejunum was studied by the perfusion method using everted rat jejunum in vitro. The absorption rate of roll mixtures was superior to that of mefanamic acid.
HPLC Determination of Diltiazem and Deacetyldiltiazem in Rat Plasma
Lee, Yong-Hee ; Shim, Chang-Koo ; Lee, Min-Hwa ; Kim, Shin-Keun ;
Journal of Pharmaceutical Investigation, volume 22, issue 4, 1992, Pages 317~321
A high-performance liquid chromatographic (HPLC) method was developed for the determination of diltiazem (DTZ) and its major metabolite, deacetyldiltiazem (DAD), in rat plasma. DTZ, DAD and imipramine, the internal standard, were selectively fractionated from plasma on a
. The composition of the mobile phase was methanol: acetonitrile: 0.04 M ammonium bromide: triethylamine (40:24:36:0.06 in volume). The pH of the mobile phase of their method was lowered to 6.4. The eluents from the column were detected for DTZ and DAD using a UV detector at 237 nm. The recovery was >85% for DTZ and DAD, and average intra-day and inter-day coefficients of variation were <6% for DTZ and DAD at the concentration ranges of 20-1000 ng/ml. Detection limit of DTZ and DAD in plasma was 20 ng/ml with signal-to-noise ratio of 3. This method would be applicable to practical pharmacokinetic studies without detriment to the HPLC column.
Release of Cytarabine from
Block Copolymer Microspheres
Cho, Chong-Su ; Kwon, Joong-Kuen ; Jo, Byung-Wook ; Lee, Kang-Choon ; Sung, Yong-Kiel ;
Journal of Pharmaceutical Investigation, volume 22, issue 4, 1992, Pages 323~326
(LEL) block copolymers containing
(PCLL) as the A component and poly(ethylene oxide) (PEO) as the B component were investigated as drug delivery matrix. PCLL homopolymer and LEL block copolymer microspheres containing anticancer drug, cytarabine, were prepared by a solvent evaporation process and the release patterns of cytarabine from the microspheres were investigated in vitro. The size of PCLL homopolymer and LEL block copolymer microspheres was ranged from
in diameter and the shape of the microspheres was almost round. The release pattern of cytarabine from the block copolymer microspheres was dependent on the mole % of PEO of the block copolymers.