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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 18, Issue 4 - Dec 1988
Volume 18, Issue 3 - Sep 1988
Volume 18, Issue 2 - Jun 1988
Volume 18, Issue 1 - Mar 1988
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Dissolution Enhancement of Metoclopramide by Coprecipitation with Water-Soluble Carriers
Yong, Jae-Ick ; Jeong, Cha-Ok ;
Journal of Pharmaceutical Investigation, volume 18, issue 2, 1988, Pages 43~47
In order to increase the dissolution characteristics of relatively water-insoluble metoclopramide (MCP), coprecipitates of MCP with polyvinylpyrrolidone (PVP), polyethylene glycol (PEG) 1000, 4000 or 6000 were prepared in various drug to polymer ratios. The dissolution rate of MCP-PVP coprecipitate was greater than those of MCP alone, MCP-PVP physical mixture and MCP-PEG coprecipitates. The dissolution rate of MCP-PEG 6000 coprecipitate was greater than those of MCP-PEG 1000 and MCP-PEG 4000 coprecipitates. The dissolution half-lives
for MCP alone and 1:5 (w/w) MCP-PEG 6000 coprecipitate were determined by the log-probit method at
and found to be 4.17 and 0.98 min, respectively.
Studies on Oral Absorption of Piperacillin Pivaloyloxymethyl Ester
Kang, Sung-An ;
Journal of Pharmaceutical Investigation, volume 18, issue 2, 1988, Pages 49~53
Pivaloyloxymethyl ester of piperacillin was synthesized by reacting sodium piperacillin with chloromethyl pivalate, and its chemical structure was determined by infrared and
nuclear magnetic resonance spectroscopic methods. The pharmaceutical properties of the ester were investigated to assess its potential as a novel prodrug of piperacillin. The interface transfer of piperacillin and the ester was studied in a two-phase in vitro system composed of aqueous pH buffers and n-octanol. The ester was more lipophilic, and less water soluble above pH 4.0 than piperacillin. Significant antibacterial activity was not observed in the ester in vitro, but the ester was hydrolyzed into the parent drug in the rat liver homogenate. The serum levels of orally administered ester suspension containing 0.1% Tween 80 were measured in rabbits. It was found that the ester showed higher blood level, comparing with no observation of piperacillin in serum, but the time reaching the maximum serum concentration was 5 hr.
Enhancement of Dissolution Properties of Poorly Soluble Drugs(IV) -Micronization of Furosemide by Recrystallization Method-
Koh, Ik-Bae ; Shin, Sang-Chul ; Oh, In-Joon ;
Journal of Pharmaceutical Investigation, volume 18, issue 2, 1988, Pages 55~59
The size of furosemide was reduced by the recrystallization method in order to increase the dissolution rate of the drug. Surfactants or hydrophilic polymers were used to suppress the aggregation in the crystal formation-growth process of microparticles by dispersing action. Dissolution rate of microparticles increased remarkably due to the size reduction of microparticle. The particle size decreased with increasing the concentration of the drug and the dispersing agents, i.e., surfactants or hydrophilic polymers. No polymorphic transition occurred during the microcrystallization process, but the habit of crystal formation was altered in the case of anionic surfactant.
Effects of Suppository Bases on Bioavailability of Aspirin Suppositories
Kim, Yong-Hyun ; Lee, Jin-Hwan ; Choi, Jun-Shik ;
Journal of Pharmaceutical Investigation, volume 18, issue 2, 1988, Pages 61~67
The influence of different suppository bases on the dissolution, and the bioavailability of aspirin suppositories in rabbits and humans was investigated using Witepsol H15 (WIT), WIT-Tween 80 (TWE), WIT-sodium lauryl sulfate (SLS), polyethylene glycol (PEG), hollow WIT (WIT-HOLL) and capsule incorporated into WIT (WIT-CAP). The results obtained were as follows: 1) Dissolution rates of aspirin suppositories with different bases in distilled water were faster in the order of WIT-TWE >WIT-SLS >PEG >WIT-HOLL >WIT >WIT-CAP. 2) The maximum blood levels
of aspirin in rabbits and humans were highest in WIT-TWE and WIT-SLS bases, but
from WIT base was lower than that in oral administration of aspirin suspension. 3) The times reaching the maximum blood levels
in rabbits were 1 hr for oral administration, 1.5-2.5 hr for WIT-TWE, WIT-SLS, PEG, and WIT bases, and 2.5-4.0 hr for WIT-HOLL and WIT-CAP bases, but
in humans were 1 hr for oral administration and WIT-TWE base, and 2-4 hr for WIT and WIT-HOLL bases. 4) Relative bioavailability (RBA) of aspirin suppositories in rabbits was higher in WIT-SLS, WIT-TWE and PEG bases than that in oral administration, and RBA of aspirin suppositories in humans was higher in the order of WIT-TWE >PEG >WIT-HOLL >oral >WIT bases tested. 5) Good correlation between dissolution rates and
was obtained: y = 0.60x+32.23 (r = 0.96) for rabbits, and y = 0.60x+35.74 (r = 0.97) for humans.
Development of Optically Active Chelate Resin for Direct Resolution of Enantiomers (I) -Solvent Effects in Chloromethylation of Crosslinked Polystyrene Resin Matrix-
Kim, Kil-Soo ; Jeon, Dong-Won ; Park, Kyoung-Hae ;
Journal of Pharmaceutical Investigation, volume 18, issue 2, 1988, Pages 69~81
We studied on the synthesis of chloromethylated polystyrene as a precursor of optically active polymers for direct resolution of optical isomers. Changing the degree of crosslinking and the kind of crosslinking agents, several polystyrene resin matrices were synthesized. The matrices were chloromethylated with methylal and chlorosulfonic acid as chloromethylating agents. The effects of solvents of various dielectric constants on the chloromethylation were quantitavely examined. We also synthesized chloromethylated polystyrene of macroreticular type that retained large surface area and good physical stability. The differences between the macroreticular type and macroporous type were investigated.
Development of Optically Active Chelate Resin for Direct Resolution of Enantiomers (II) -Effect of Methylmethacrylate Content on Chloromethylation of Crosslinked Styrene-Methylmethacrylate Copolymer-
Kim, Kil-Soo ; Jeon, Dong-Won ; Park, Kyoung-Hae ;
Journal of Pharmaceutical Investigation, volume 18, issue 2, 1988, Pages 83~88
We examined effects of crosslinking agents, i.e., ethyleneglycol dimethacrylate (EGD) and butanediol dimethacrylate (BDD) containing ester groups on chloromethylation of crosslinked polystyrene resin matrices. It was proved that the ester group in methylmethacrylate (MMA) accelerates the chloromethylation of the divinylbenzene (DVB)-crosslinked styrene-MMA copolymer. As the MMA content increased in the styrene-MMA copolymers, the chloromethylation was enhanced. Complete chloromethylation was obtained at about 25% MMA content.
Interactions between Water-Soluble Polyparacyclophanes and Drugs (I) -Design and Synthesis of Water-Soluble Polyparacyclophanes Containing Diphenyl Ether Skeletons-
Chun, In-Koo ; Lee, Min-Hwa ; Kim, Shin-Keun ;
Journal of Pharmaceutical Investigation, volume 18, issue 2, 1988, Pages 89~97
A series of novel water-soluble paracyclophanes containing two diphenyl ether skeletons and two bridging aliphatic chains of various length were designed and prepared to develop artificial host compounds which might provide efficient hydrophobic field. They were 1,5,19,23-tetraaza-12,30-dioxa[5,1.5.1] paracyclophane (6), 1,6,20,25-tetraaza-13,32-dioxa[184.108.40.206]paracyclophane (7), 1,7,21,27-tetraaza-14,34-dioxa[220.127.116.11]paracyclophane (8) and 1,8,22,29-tetraaza-15,36-dioxa[18.104.22.168]paracyclophane (9). As the corresponding acyclic analogue, 4,4'-dimethylaminodiphenyl ether (11) was synthesized for the comparative study of further host-guest interaction.