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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 24, Issue 4 - Dec 1994
Volume 24, Issue 3 - Sep 1994
Volume 24, Issue 3 - Sep 1994
Volume 24, Issue 2 - Jun 1994
Volume 24, Issue 1 - Mar 1994
Selecting the target year
Liposome Immunoassay for Bioactive Substances
Kim, Chong-Kook ; Park, Kyung-Mi ;
Journal of Pharmaceutical Investigation, volume 24, issue 4, 1994, Pages 201~215
Recent development in the immunochemical technique has resulted in a new ultrasensitive analytical method known as liposome immunoassay (LIA). Liposome is a key element in performing liposome immunoassays, specifically designed to participate in immune reactions. A variety of markers can be encapsulated in liposomes and used as quantitative indicators of reactions. Liposome immunoassay based on agglutination, complement-mediated Iysis, cytolysin-mediated Iysis, detergent-mediated Iysis or destabilization of the liposomal membrane have been reviewed. The quantity of markers released from liposomes should be proportional to the concentration of the analytes. Therefore, liposomal agglutination and Iysis which are essential to liposomal Iysis are critically reviewed to provide a better understanding of liposome immunoassay. Based on the literature review of recent advances in liposome immunoassay for bioactive substances, this assay method may provide a convenient, specific and highly sensitive method for detecting and measuring trace amount of clinically relevant substances in the future.
Hepatic Targeting of Acyclovir Using Asialofetuin as a Drug Carrier
Yong, Chul-Soon ; Son, Sung-Ho ; Jun, Chul-Soo ; Oh, Doo-Man ;
Journal of Pharmaceutical Investigation, volume 24, issue 4, 1994, Pages 217~225
With the purpose of improving the therapeutic index of
acyclovir (ACV) in the treatment of chronic hepatitis B infection, asialofetuin (AF) which after selective interaction with Ashwell's receptor specifically enters into hepatocytes, was chosen as a carrier system for hepatic targeting. This drug was first converted to its monophosphate (ACVMP), which was subsequently activated by water soluble carbodiimide to conjugate with
groups of Iysine residues of AF. The molar ratio of ACVMP to AF in the conjugate was 3.9. In rats, elimination of ACVMP-AF conjugate after i.v. injection showed two phase elimination kinetics. Initial apparent elimination rate constant in rats was
which was greater than that of ACV. The elimination rate constant from terminal phase was
. Area under the total radioactivities versus time curve was found to be several times larger in liver than in other organs (spleen, intestine, lung and kidney) after i.v. administration of the conjugate labelled in the drug moiety. The above results suggested that ACVMP-AF conjugate was rapidly taken up by hepatocytes and could be a useful hepatic targeting system.
Stability of Red Ginseng Saponin in Aqueous Solution
Lee, Seung-Jin ; Kim, Shin-Il ; Kim, Kil-Soo ;
Journal of Pharmaceutical Investigation, volume 24, issue 4, 1994, Pages 227~231
The stability of red ginseng saponin in aqueous solution was studied with the acceleration test method. The degradation rate constant of ginsenoside Rb1, an index component of red ginseng saponin, was
, and the shelf-life was about 570 days. The pH-rate profile demonstrated that the most stable range was pH 6-8. Mannitol and benzyl alcohol, common excipients for injection, exerted no influence on the degradation reaction of ginsenoside Rb1.
Preparation and Bioavailability of Oriental Medicine Containing Baicalin (I) : Identification and Physicochemical Properties of Coprecipitated Product of Scutellariae Radix and Coptidis Rhizoma
Yang, Jae-Heon ; Kim, Dong-Su ; Park, Hyun-Goo ; Lee, Nam-Hee ;
Journal of Pharmaceutical Investigation, volume 24, issue 4, 1994, Pages 233~243
Precipitation was formed during the preparation of decoction from a mixture of Scutellariae Radix and Coptidis Rhizoma or Phellodendri Cortex according to the prescription of Hwang-ryean-hae-dog-tang. Baicalin and berberine were identified in coprecipitated product and these components were the active ingredients of two herbal medicine. The coprecipitated product was very slightly soluble in water and sparingly soluble in ethanol. The stoichiometric ratio of baicalin and berberine was found to be 1:1. The lipid-water partition coefficients of coprecipitated product were increased more than baicalin and berberine in chloroform, but were decreased in other organic solvents. The content of baicalin and berberine in coprecipitated product, determined by HPLC, were 23.08% and 26.75%, but the content of active ingredients in supernatant were 0.66% and 0.26%, respectively. The dissolution profile of baicalin of coprecipitated product was increased more than extract of Scutellariae Radix in artificial gastric juice, but was decreased in artificial intestinal juice. The dissolution rate of berberine of coprecipitated product was lower than extract of Coptidis Rhizoma in artificial gastric juice and intestinal juice commonly.
Synthesis and Antitumor Activity of Pt(ll) Complexes Containing Ethylenediamine
Lee, Kyung-Tae ; Jung, Jee-Chang ; Roh, Young-Soo ;
Journal of Pharmaceutical Investigation, volume 24, issue 4, 1994, Pages 245~250
An attempt was made to develop new water-soluble antitumor Pt(ll) complexes containing ethylenediamine, and their structures were determined by infrared spectroscopy,
nuclear magnetic resonance and elemental analysis. Their antitumor activities in vitro against L-1210, p-388 leukemia cells and M-14 melanoma cells were investigated and acceptable antitumor activity was found as compared with cisplatin.
Drug Release Characteristics from Chain-extended and Crosslinked Polypropylene Glycol Hydrogels
Lee, Seung-Jin ;
Journal of Pharmaceutical Investigation, volume 24, issue 4, 1994, Pages 251~256
Polypropylene glycol (M.W. 4000) was crosslinked and chain-extended by using triisocyanate and diisocyanate to synthesize rubbery and water swellable hydrogels. Model drugs, i.e., sodium salicylate and indomethacin were incorporated in the polymer matrices by swelling loading. The drug release rates of drugs could be regulated by varying the degrees of crosslinking and chain-extension. Whereas, no correlation was observed between the drug release profiles and the swelling behaviours of the matrices. The release of drugs from the matrices was considered to be governed by the mobility and mesh size of the polymer chains in the matrices.
Controlled Drug Release from Polyacrylic Acid-Polyethylene Glycol Interpenetrating Networks
Kim, Youn-Jung ; Kim, Kil-Soo ; Lee, Seung-Jin ;
Journal of Pharmaceutical Investigation, volume 24, issue 4, 1994, Pages 257~263
The interpenetrating polymer networks (IPNs) of polyacrylic acid (PAA)-polyethylene glycol (PEG) were synthesized via crosslinking of PEG and simultaneous free radical polymerization of PAA. The equilibrium swelling of the IPNs matrices, ranged from 40% to 95%, was varied to a great extent as compared with PAA homopolymer due to the interpolymer interaction between PAA and PEG. The drug release kinetics of drug loaded matrices was significantly affected by the charge of drugs as well as interpolymer complexation.
Development of Cefazolin Prodrug for Oral Administration -Synthesis, Partition Coefficient and Antibacterial Activity of Cefazolin Ethoxycarbonylethyl Ester-
Jung, Young-Guk ; Burm, Jin-Pil ; Choi, Jun-Shik ; Lee, Jin-Hwan ;
Journal of Pharmaceutical Investigation, volume 24, issue 4, 1994, Pages 265~271
Cefazolin ethoxycarbonylethyl ester (CFZ-ET) was synthesized to improve oral absorption and bioavailability of the parent drug by esterification of sodium cefazolin (CFZ-Na). The successful synthesis of CFZ-ET was identified with analysis of UV spectra, FT-lR spectra and NMR spectra. Partition coefficient studies showed that CFZ-ET was more lipophilic than CFZ-Na and the ester was hydrolyzed into the parent drug in vivo. Although CFZ-ET did not have antimicrobial activity in vitro, the plasma taken after the oral administration of CFZ-ET had antimicrobial activity. Based on above observations, CFZ-ET might be rapidly hydrolyzed to CFZ in the body. Therefore, it may be concluded that CFZ-ET could be a novel prodrug of CFZ which can improve the bioavailability of CFZ-Na.
Stability of Mono- and Bis-pyridinium Oximes in Aqueous Systems
Jung, Chang-Hee ; Choi, Seung-Ju ; Seo, Won-Jun ; Sok, Dai-Eun ;
Journal of Pharmaceutical Investigation, volume 24, issue 4, 1994, Pages 273~279
The stability of three oximes, Hl-6 [(4-carbamoyl-2'[(hydroxyimino)-methyl]- 1,1'-oxydimethylenedi-(pyridinium chloride)], Hl-CN [(4 cyano-2'-[(hydroxyimino)-methyl] -1,1'-oxydimethylene-di-(pyridinium chloride)], and 2-PAM [pralidoxime chloride] in aqueous solutions was evaluated by HPLC assay. The rate of degradation is dependent on the pH as well as the temperature at which the solution is stored. The optimum pH for the stability of these oximes was pH 2 to 3. The degradation rate constant for 2-PAM (
, 27.2 kcal/mol) was smaller than those for bis-pyridiniumoximes, Hl-6 (
) and Hl-CN (
, 20.7 kcal/mol). In mechanistic analyses, it was found that Hl-CN was decomposed through not only the hydrolysis of nitrile group but also the cleavage of methylene ether bridge, in contrast to Hl-6 which was degraded mainly through the cleavage of methylene ether bridge.
The Effect of Oleic Acid and Propylene Glycol on the Electrical Properties of Skin
Oh, Seaung-Youl ; Guy, Richard H. ;
Journal of Pharmaceutical Investigation, volume 24, issue 4, 1994, Pages 281~287
The effects of oleic acid, propylene glycol and 5% (w/w) oleic acid in propylene glycol on the electrical properties of hairless mouse skin were studied and the results were compared. The complex electrical impedance was measured as a function of frequency, and resistance and capacitance were determined from the Nyquist plot. Immediately after the treatment with oleic acid, resistance was 145% of the pretreatment value. However it decreased with time and, after 20 hours, it was about 25% of its pretreatment value. Capacitance increased; immediately after the treatment, it was about 125% of pretreatment value and it seemed to increase slowly with time. When the skin was treated with propylene glycol, resistance decreased about 5O% and capacitance increased about 65%. Similar results were observed when the skin was treated with 5% (w/w) oleic acid in propylene glycol, except that the magnitude of resistance drop was much larger. Oleic acid acted synergistically with propylene glycol. Together with the flux data in the literature, the results obtained in this work indicate that electrical resistance is closely related to the permeability of drug molecules through the skin. The results are discussed in terms of the mechanism of action of these penetration enhancers. Overall, this work provided further mechanistic insight into the role of SC lipids in skin resistance and capacitance.
Drug Interaction between Phenytoin and Verapamil in Rabbits
Choi, Jun-Shik ; Lee, Il-Kyun ;
Journal of Pharmaceutical Investigation, volume 24, issue 4, 1994, Pages 289~295
Pharmacokinetic drug interaction between phenytoin and verapamil was investigated following i.v. administration of two drugs concomitantly to rabbits. Verapamil was coadministered with phenytoin (5 mg/kg) to rabbits at the doses of 0.5,1 and 2 mg/kg, respectively. Plasma concentration and AUC of phenytoin were increased significantly, but volume of distribution and total body clearance were decreased significantly (p<0.05) at doses of 1mg and 2mg/kg of verapamil, respectively. From the results of this experiment, it is desirable that dosage regimen of phenytoin should be adjusted and that therapeutic drug monitoring should be performed for reduction of side or toxic effect when phenytoin should be administered with verapamil in clinical practice.
Studies on Diet Regimens for the Developement of Hyperlipidemic Animal Model
Ro, Hwan-Seong ; Kim, Oon-Ja ; Park, Kun-Ku ; Cho, Young-Hwan ; Park, Hyung-Sup ;
Journal of Pharmaceutical Investigation, volume 24, issue 4, 1994, Pages 297~300
Development of hyperlipidemic animal model is prerequisite for the screening of drugs lowering the blood lipoprotein level. In this study, two kinds of diet regimens were tried for the hyperlipidemic effect. The model will be used for the screening of current prescriptions to a variety of diseases related to hyperlipidemia by practioner of traditional herbal medicine. Fifteen male Wister rats of 200g were divided into three groups, and given normal, or either one of the two high cholesterol diets for up to 2 weeks. Regimen HC-1 and regimen HC-2 contained I% and 2% cholesterol in diet, respectively. Total cholesterol (TC), triglyceride (TG), high density lipoprotein cholesterol (HDL) and lower density lipoprotein cholesterol (LDL) levels in the serum were measured before the start of the diet, at 1 week after the start, and at 2 week point. Both regimens resulted in hyperlipidemia with the typical characteristics of increase in TC and LDL, and reduction in HDL, and showed no observable side effects such as diarrhea. In conclusion, both of HC-1 and HC-2 regimens appeared appropriate as diet regimens for the hyperlipidemic rat model.