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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 23, Issue 4 - Dec 1993
Volume 23, Issue 3 - Sep 1993
Volume 23, Issue 3 - Sep 1993
Volume 23, Issue 2 - Jun 1993
Volume 23, Issue 1 - Mar 1993
Selecting the target year
Synthesis and Biopharmaceutical Studies of Cefazolin Phthalidyl Ester Prodrug
Lee, Jin-Hwan ; Kim, Ga-Na ;
Journal of Pharmaceutical Investigation, volume 23, issue 2, 1993, Pages 61~69
Prodrug of cefazolin (CFZ) was prepared with the objective of improving its oral bioavailability. Cefazolin phthalidyl ester (CFZ-PT) was synthesized and evaluated as potential prodrug form. The successful synthesis of CFZ-PT was identified by spectroscopic analysis. Partition coefficient studies showed that CFZ-PT is more lipophilic than CFZ and the ester was hydrolyzed enzymatically into the parent drug in blood, liver and intestinal homogenates. The pharmacokinetic characteristics of CFZ-PT and CFZ were compared following oral administrations to rabbits. Serum CFZ concentration was determined by HPLC method and the ester compound (prodrug) was not detected in serum following oral administration of CFZ-PT. CFZ-PT did not have antimicrobial activity in vitro against Bacillus subtilis ATCC 6633, whereas CFZ-PT in serum after oral administration to rabbits had antimicrobial activity. From above observations, it was noted that CFZ-PT is rapidly hydrolyzed to CFZ in the body and the bioavailability of CFZ-PT was increased by 3.5-fold than that of CFZ. From these results of this study, it was concluded that CFZ-PT may be a novel prodrug of CFZ which can improve the oral absorption of CFZ.
Effect of Mixed Micelles on Jejunal and Nasal Absorption Enhancement of Piperacillin
Park, Gee-Bae ; Lee, Yong-Suk ; Rho, Hyun-Goo ; Lee, Kwang-Pyo ;
Journal of Pharmaceutical Investigation, volume 23, issue 2, 1993, Pages 71~80
The purpose of this study was to compare the intrinsic absorptivity of piperacillin in the jejunum and the nasal cavity, to investigate the effect of bile salts, fatty acids and their mixed micelles on the intestinal and nasal absorption of piperacilIin, to examine the reversibiIity of bile salt-fatty acid mixed micelles absorption promoting action and to design an effective intranasal drug delivery system for antibiotics. And absorption promoters used were bile salts [sodium cholate (NaC), sodium glycocholate (NaGC)], unsaturated fatty acids [oleic acid (OA), linoleic acid (LA)] and their mixed micelles (NaC-LA). The present study employed the in situ nasal and intestinal perfusion technique in rats. The apparent permeabilities
of piperacillin were
in the jejunum and
in the nasal cavity, which indicated that intrinsic absorptivity of piperacillin was greater in the nasal cavity than in the jejunum. When absorption promoters were used in the rat nasal cavity, the decreasing order of apparent piperacillin permeability
, corrected for surface area of absorption, was NaC-LA
. The increase in permeability of piperacillin was 3.5-fold in the rat nasal cavity and 1.5-fold in the rat jejunum for formulations containing NaC-LA mixed micelles as compared to those without absorption enhancer. The effect of NaC-LA mixed micellar solutions was synergistic and was greater than that with single adjuvant. The reversibility of nasal mucosal permeability was observed within approximately 2 hr after removal of NaCLA mixed micelles from the nasal cavity. These results suggest that NaC-LA mixed micelles can be used as nasal mucosal absorption promoters of poorly absorbed drugs.
Study on Polymorphism of Cimetidine
Sohn, Young-Taek ; Kim, Ki-Soo ;
Journal of Pharmaceutical Investigation, volume 23, issue 2, 1993, Pages 81~87
Five crystalline forms of cimetidine, four anhydrous and a monohydrate, have been prepared, and their thermal behavriours have been studied by differential thermal analysis and thermo-gravimetry. The dissolution rates of the five forms were determined in distilled water at
. The results showed a significant difference in the dissolution rate. Polymorphic transformation occurred spontaneously during storage at room condition and was accelerated by applied energy during formulation process-milling.
Permeability Characteristics of Cholesterol-Containing Polymerized Vesicles
Cho, I-Whan ; Bae, Duck-Hwan ; Shin, Jae-Sup ;
Journal of Pharmaceutical Investigation, volume 23, issue 2, 1993, Pages 89~95
Polymerized vesicles were prepared from the monomeric cholesterol-containing surfactant. Spacer groups were introduced into [(cholesteryloxy)carbonylmethyl] [2-(methacryloyloxy)ethyl]dimethylammonium chloride (CHODAMA). In case of introducing the spacer groups to the cholesterol moiety, both permeability of vesicles and that of polymerized vesicles were decreased. In case of introducing the spacer groups to monomeric moiety, permeability of vesicles was increased, while that of polymerized vesicles was decreased.
Utilization of Computer System for Outpatient's Dispensing Affairs in Hospital Pharmacy
Ro, Hwan-Seong ;
Journal of Pharmaceutical Investigation, volume 23, issue 2, 1993, Pages 97~102
Hospital pharmacy services are divided into dispensing affairs for inpatients and outpatients, pharmaceutical service, stock control, intravenous admixture service, drug information service, pharmacokinetic consultation service, education and research work, etc. But among those affairs, dispensing affair for outpatient is perceived as the most important work in Korea, because it is linked directly with hospital service for patients. Therefore, total computer system for dispensing area was adopted from opening point of hospital in 1989 in Asan Medical Center. Utilization of computer system for outpatient dispensing area is as follows; 1) Order communication system of prescription by Total Hospital Information System, 2) Automatic print-out system of direction for use by sticker connected with on-line net work, 3) Use of automatic tablet counting and packaging machines connected with on-line net work. Those computer system resulted in curtailment of pharmacy manpower and shortening of waiting-time for outpatient.
Biopharmaceutical Evaluation of Sustained-Release
Microcapsules Containing Cephalexin
Han, Kun ; Kim, Kwang-Dug ; Chung, Youn-Bok ; Jee, Ung-Kil ; Kim, Shin-Keun ;
Journal of Pharmaceutical Investigation, volume 23, issue 2, 1993, Pages 103~110
Microcapsules(Mc) of cephalexin (CEPH), using Eudragit RS, RL, L, S and polyethylene glycol 1540, were evaluated biopharmaceutically. The area under the curve of CEPH-Eudragit RS/RL Mc administered orally once was larger than that of cephalexin powder twice every 6 hrs. Controlledrelease effectiveness and the absorption rate effectiveness, two important parameters of Vallner's method, of CEPH-Eudragit RS/RL Mc indicate that these Mc can be good sustained-release preparations. And a simple pharmacokinetic model is introduced which allows the gastric emptying and intestinal-transit rates of a drug itself and a solid-state drug contained in Mc. Decreasing
, without change in
, showed that the rate-limiting step of absorption moved from absorption step to releasestep.
The Hemolytic Characteristics of Amphotericin B-Containing Egg PC Liposomes
Kim, J.C. ; Lee, E.O. ; Kim, J.D. ;
Journal of Pharmaceutical Investigation, volume 23, issue 2, 1993, Pages 111~118
The hemolytic characteristics of amphotericin B-containing liposomes have been investigated in vitro. From the hemolysis of human erythrocytes against free and liposomal amphotericin B, the marked reduction in the toxicity of amphotericin B was observed by incorporating the drug in egg PC liposomes. For 45 min, free amphotericin B at
could completely lyse 2 wt% human erythrocytes. However, liposomal amphotericin B had essentially no lytic effect even in the range over
. In the 66 hr-hemolysis experiment, liposomal amphotericin B showed the slowly hemolysing chracteristics during the experimental period regardless of the concentration of amphotericin B but rapid hemolysis only for 12 hr was observed in the case of free amphotericin B and the degree of hemolysis for 12 hr was maintained after that time. Also the hemolysing ability of liposomal amphotericin B at
was lower than that of free amphotericin B at the same concentration for 66 hr. On the other hand, the dependence of hemolysis on amphotericin B contents in egg PC liposomes was significant between 1.64 mole% amphotericin B-containing liposomes and 15.79 or 27.27 mole% amphotericin B-containing liposomes. But no marked difference in hemolysis was observed between 15.79 and 27.27 mole% amphotericin B-containing liposomes. Especially, cholesterol as an excipient in amphotericin B-containing liposomes significantly reduced the hemolysis of human erythrocyte. The degree of hemolysis in 5 mole% amphotericin B-containing liposomes was reduced to approximately 50% of value in the cholesterol-free liposomes by adding 50% cholesterol.