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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 32, Issue 4 - Dec 2002
Volume 32, Issue 3 - Sep 2002
Volume 32, Issue 2 - Jun 2002
Volume 32, Issue 1 - Mar 2002
Selecting the target year
Evolution of the Patent for Osmotic Drug Delivery
Lee, Hai-Bang ; Lee, Dong-Hun ; Kang, Bok-Ki ; Jeung, Sang-Young ; Khang, Gil-Son ;
Journal of Pharmaceutical Investigation, volume 32, issue 4, 2002, Pages 241~258
DOI : 10.4333/KPS.2002.32.4.241
Such osmotic drug delivery systems are based on osmosis, the diffusion of water transversely from a medium with a low osmotic pressure to a medium with a high osmotic pressure for the controlled delivery of active agents. In this review, U.S. Patents on osmotic drug delivery analyze 261 patents until December 2001. These devices form now a major market of drug delivery products. Because of their advantage and innovate idea, it appears that the future of oral drug delivery mark,εt in Korea is promising.
Phonophoretic Delivery of Piroxicam
Chung, Kyu-Ho ; Kim, Young-Il ; Yang, Jae-Heon ;
Journal of Pharmaceutical Investigation, volume 32, issue 4, 2002, Pages 259~265
DOI : 10.4333/KPS.2002.32.4.259
Piroxicam is one of the NSAID, which is used in the systemic and topical treatment of a variety of inflammatory conditions. Conventionally, for topical use, the drug is formulated in gel. We designed an phonophoretic drug delivery system to investigate the piroxicam permeability and the influence of ultrasound application (continuous mode, pulsed mode), frequency (1.0 MHz, 3.0 MHz) and intensity
with 0.5% piroxicam gel. Per cutaneous absorption studies were performed in vitro models to determine the rate of drug absorption via the skin. Permeation study using hairless mouse skin was performed at
using buffered saline (pH 7.4, 10% propylene glycol solution) as the receptor solution. Anti-inflammatory activity was determined using carrageenan-induced foot edema model in rat. A pronounced effect of ultrasound on the skin absorption of the piroxicam was observed at all ultrasound energy level studied. Ultrasound was carried out for 10 hr. The highest permeation was observed at intensity of
, frequency of 1.0 MHz and continuous output. The inclusion of phonophoresis was found to improve significantly the skin permeation in vitro and the anti-inflammatory activity in vivo.
Improvement of Bioavailability for Lovastatin using Self-microemulsifying Drug Delivery System
Yoon, Bok-Young ; Kang, Bok-Ki ; Jeung, Sang-Young ; Lee, Young-Won ; Lee, Si-Beum ; Hwang, Sung-Joo ; Yuk, Soon-Hong ; Khang, Gil-Son ; Lee, Hai-Bang ; Cho, Sun-Hang ;
Journal of Pharmaceutical Investigation, volume 32, issue 4, 2002, Pages 267~275
DOI : 10.4333/KPS.2002.32.4.267
A self-microemulsifying drug delivery system (SMEDDS) was developed to increase the dissolution rate, solubility, and ultimately bioavailability of a poorly water soluble drug, lovastatin. SMEDDS was thε mixtures of oils, surfactants, and cosurfactants, which emulsify under conditions of gentle agitation, similar to those which would be encountered in the gastro-intestinal (GI) tract. Various types of self-emulsifying formulations were prepared using four types of oil (Capryol 90, Lauroglycol 90, Labrafil M 1944 CS and Labrafil M 2125), two surfactants (Cremophor EL and Tween 80), and three cosurfactants (Carbitol, PEG 400 and propylene glycol). Thε efficiency of emulsification was studied using a laser diffraction size analyzer to determine particle size distributions of the resultant emulsions. Optimized formulations selected for bioavailability assessment were Carpryol 90 (40%), Cremophor EL (30%) and Carbitol (30%). SMEDDS containing lovastatin (20 mg and 5 mg) were compared to a conventional lovastatin tablet
by the oral administration as prefilled hard gelatin capsules to fasted beagle dogs for in vivo study. The arεa under the serum concentration-time curve from time zero to the last measured time in serum,
, was significantly greater in SMEDDS, suggesting that bioavailability increase 130% and 192% by the SMEDDS, respectively. The self-emulsifying formulations of lovastatin afforded the improvement in absolute oral bioavailability relative to previous data of lovastatin tablet formulation. These data indicate the utility of dispersed self-emulsifying formulations for the oral delivery of lovastatin and potentially other poorly absorbed drugs.
The Effect of Sodium Alginate Coating on the Storage Stability and Dissolution Rate of Enteric Coated Lansoprazole
Kim, Jung-Hoon ; Oh, Jung-Min ; Khang, Gil-Son ; Jeong, Je-Kyo ; Lee, Jung-Sik ; Jeung, Sang-Young ; Lee, Hai-Bang ;
Journal of Pharmaceutical Investigation, volume 32, issue 4, 2002, Pages 277~284
DOI : 10.4333/KPS.2002.32.4.277
Lansoprazole, pharmaceutics for acid-related diseases, is unstable in low pH environments and generally coated with enteric polymer to obtain gastroresistance in stomach. Because its storage stability is influenced by acidic substitutes of enteric polymer, alkaline chemicals wεre generally addεd to dosage form as a stabilizer. In this experience, we coated lansoprazole bead with sodium alginate and evaluated the effect of bead size and sodium alginate coating on the storage stability and dissolution profile of lansoprazole. Sodium alginate solution containing lansoprazole was sprayed as a droplet into 3% (w/v)
solution and the resultant bead was coated with starch, sodium alginate, and hydroxypropyl methylcellulose phthalate. The content of lansoprazole granule not coated with sodium alginate decreased to 57.96% of initial content when stored at a severe condition for 4 weeks, but that of lansoprazole granule coated with sodium alginate before enteric coating decreased little and as the thickness of sodium alginate film increased, the content of bead didn't decreased for 4 weeks. Sodium alginate film also improved the gastroresistance without much influencing the maximum dissolution rate.
In Vitro Determination of Intracellular Phosphorylated Metabolites of Antiviral Pyrimidine Analogs
Han, Kyu-Won ; Kim, Kil-Soo ;
Journal of Pharmaceutical Investigation, volume 32, issue 4, 2002, Pages 285~290
DOI : 10.4333/KPS.2002.32.4.285
In order to assay the efficacy of newly synthesized antiviral compounds, in vitro studies of their active intracellular phosphorylated metabolites were established as compared with Zidovudine (ZDV). Antiviral base analogs require intracellular phosphorylation prior to the inhibition of HIV replication. Therefore, antiviral drugs concentrations in plasma have not reflected any direct relationship with activity or toxicity. A method has been developed to measure the concentration of total phosphorylated metabolites inside peripheral blood mononuclear cells using modified commercial radioimmunoassay (RIA). ZDV 5'-monophosphate was synthesized and used as a procedural control for RIA modification. PBMCs were isolated from whole blood and incubated with ZDV for 20 h to allow metabolic phosphorylation. Viable cells were extracted overnight with 60% methanol. After evaporation, the extract was reconstituted in Tris buffer. Samples were split into two fractions, one of which was treated with alkaline phosphatase (AP) to liberate phosphate groups. Concentrations of phosphorylated metabolites were determined by subtracting thε concentration of non-AP-treated fraction from that of the treated fraction. Recovery of phosphorylated ZDV from cell extracts was approximately 90%, and reproducibility was acceptable (coefficients of variation <15% for concentrations
0.25 ng/mL). Intracellular concentrations
followed a nonlinear dose-response relationship over the range
extracellular ZDV, with concentration-dependant saturation.
Preparation and Evaluation of Titrated Extract of Centella Asiatica Niosome/W/O System Cream for Site Specific Targeting
Kim, Dong-Woo ; Cho, Mi-Hyun ; Park, Sun-Young ; Lee, Jong-Hwa ; Lee, Gye-Won ; Park, Mork-Soon ; Park, Jin-Kyu ; Jee, Ung-Kil ;
Journal of Pharmaceutical Investigation, volume 32, issue 4, 2002, Pages 291~297
DOI : 10.4333/KPS.2002.32.4.291
For preventing and curing the stretching mark, TECA Niosome/W/O system creams were formulated using Titrated Extract of Centella Asiatica (TECA) which is well known for its excellent wound healing effect. The lipid-water partition coefficients and the stabilities of TECA were evaluated and TECA Niosome/W/O system (TECA N/W/O) creams were prepared with different concentrations of cetyl alcohol and ceramide. TECA N/W/O cream was evaluated with respect to their rheological properties, permeation through excised skin of hairless mouse and in vitro and in vivo accumulation in the skin of hairless mouse. In addition, dermal thicknesses of hairless mouse skins were determined following the in vivo application of TECA N/W/O cream and control cream. TECA N/W/O creams showed pseudoplastic flow and hysteresis loop. The permeation of TECA from formulations through excised skin of hairless mouse did not observed. Amount of accumulated drug in the excised skin of hairless mouse was deσeased with an increase in the concentration of cetyl alcohol and showed no relationship with concentration of ceramide. Amount of accumulated drug in formulation A-3 was higher than in niosome suspension and other formulations. In in vivo experiment, amount of accumulated drug in formulation A-2 and A-3 was much higher than that of niosome suspension. Being treated with the N/W/O cream for 8 weeks, the dermal thickness of hairless mouse skin was increased 3.2 times than that of 16 weeks-control group.
Formulation of Liquid Oral Preparations Containing Itraconazole
Jung, Ki-Seop ; Hong, Ji-Woong ; Choi, Ki-Song ; Chi, Sang-Cheol ; Park, Eun-Seok ;
Journal of Pharmaceutical Investigation, volume 32, issue 4, 2002, Pages 299~303
DOI : 10.4333/KPS.2002.32.4.299
The oral bioavailability of itraconazole is variable and low in fasting state. This is mainly due to the low solubility of this drug. Bioavailability can be improved by changing the formulation and it is general that the liquid preparations show greater bioavailability than the solid dosage forms such as tablets and capsules do. Benzyl alcohol-water binary mixture showed the excellent solubilizing capacity for itraconazole but the release of the drug from the preparation needs to be enhanced. In this study, various nonionic surfactants and hydrophilic polymers, poloxamers, were screened to investigate their effects on the releasε of itraconazole from the liquid preparations. Poloxamer 407 showed the most enhancing effect on the drug release and the release rate was proportional to thε amount of poloxamer 407 added. A liquid preparation of itraconazole, consisting of benzyl alcohol/water/poloxamer 407 ternary solvent system, releasεd more than 80% of the total drug amount at 5 min and showεd the possibility of a new formulation development.
Effect of Poloxamer Content on Dissolution of Diltiazem Hydrochloride from Core Pellets
Lee, Seung-Woo ; Kam, Sung-Hoon ; Hong, Ji-Woong ; Choi, Ki-Song ; Park, Eun-Seok ; Chi, Sang-Cheol ;
Journal of Pharmaceutical Investigation, volume 32, issue 4, 2002, Pages 305~311
DOI : 10.4333/KPS.2002.32.4.305
In order to evaluate the effect of poloxamer 407 content on the dissolution profiles of pellets, diltiazem HCl (DTL) core pellets were prepared with poloxamer 407 (50-90% w/w, with lactose as filler) using an extruder and a spheronizer. Any possible interaction between the drug and excipients was evaluated using DSC, IR and TLC. Dissolution tests were performed using USP basket method. In addition, scanning electron micrograph was performed to examine the surface roughness and cross sections. The release of DTL from the core pellets was decreased with increasing poloxamer 407 content. Cracks appeared on the surface of the core pellets with increasing the poloxamer 407 content, which may play a role on the retardation of the release of DTL from core pellets. There was no any significant interaction between the drug and excipients employed to prepare the core pellets.
In vitro Rat Skin Permeation of Various NSAIDs
Kim, Min-Jung ; Doh, Hea-Jeong ; Cho, Won-Jea ; Yong, Chul-Soon ; Choi, Han-Gon ; Lee, Chi-Ho ; Kim, Dae-Duk ;
Journal of Pharmaceutical Investigation, volume 32, issue 4, 2002, Pages 313~319
DOI : 10.4333/KPS.2002.32.4.313
Rat skin permeation of various nonsteroidal antiinflammatory drugs (NSAIDs) was investigated in vitro using Franz diffusion cell at
. The effect of various skin permeation enhancers was also observed as a preliminary study of developing transdermal delivery systems of NSAIDs. Lipophilicity of NSAIDs was determined from thε partition coefficient (log P) in 1-octanol/water and 1-octanol/IPB mutual-saturated solutions. The solubility was determined in water, isotonic phosphate buffer (IPB), and propylene glycol (PG) at
. The rat skin permeation rate of acetaminophen, piroxicam, and aceclofenac was almost negligible, although they were saturated in PG. Addition of 1 % permeation enhancer increased the permeation rate of ketoprofen, ketorolac, and diclofenac. However, the skin permeation rate of ibuprofen did not increase with the addition of various enhancers. Among the permeation enhancers testεd, oleic acid was the most effective for various NSAIDs. Based on the daily dose, lipophilicity, and the skin permeation ratε achieved in this study, ketoprofen and ketorolac seem to be the most promising drug candidates for transdermal delivery systems, especially when formulated with unsaturated fatty acids, such as oleic acid.
In vitro/In vivo Correlation of Sustained Release Diltiazem
Choi, Myoeng-Sin ; Kang, Chan-Soon ; Choi, Bo-Kyung ; Hong, Chong-Hui ; Kim, Kil-Soo ;
Journal of Pharmaceutical Investigation, volume 32, issue 4, 2002, Pages 321~325
DOI : 10.4333/KPS.2002.32.4.321
IVIVC (In vitro/in vivo correlation) is useful for predicting in vivo results from in vitro data. The aim of this study was to develop IVIVC of sustained release diltiazem. For this purpose, three types of diltiazem tablets with different in vitro dissolution rates were prepared. An in vitro dissolution testing method comprising of paddle apparatus, 50 rpm, water as dissolution medium was developed. Under these condition, we demonstrated that AUCinf could be predicted by evaluating
(time dissolved 70%) in vitro since the in vivo AUCinf was correlated with the in vitro
Controlled Release and Stabilization of Cefaclor from Alginate-based Matrices for Oral Delivery Design
Bak, So-Im ; Lee, Jue-Yeon ; Song, Hye-Won ; Hwang, Jeong-Hyo ; Lee, Seung-Jin ;
Journal of Pharmaceutical Investigation, volume 32, issue 4, 2002, Pages 327~330
DOI : 10.4333/KPS.2002.32.4.327
Alginate based polymeric matrices were designed for controlled release and stabilization of cefaclor in gastrointestinal fluid. Cefaclor is known to be acid stable and subjected to be degraded at neutral and alkaline pHs. In order to achieve an effective release profile of cefaclor in gastrointestinal tract, a particular strategy in dosage form design should be required from the view point of maintaining its activity. The amphiphilic nature of cefaclor allowed its controlled release using ionic polymers based on ionic interaction between the drug and polymers. The thrust of this study was to develop a technique that delivers cefaclor keeping effective release rate in the intestinal tract. Considering the fast degradation of cefaclor in the intestinal fluid, the matrices were designed to release surplus amount of cefaclor. The alginate based matrices demonstrated increase in release rate in the simulated intestinal fluid, which was favorable to compensate the degraded portion of cefaclor. In addition, stabilization of cefaclor in the intestinal fluid was obtained by employing citric acid that provides an local acidic environment. The matrices might be valuably used for the development of an oral cefaclor dosage form.
The Guidelines for the Nomenclature of Drugs
Choi, Myoeng-Sin ; Choi, Bo-Kyung ; Han, Kyu-Won ; Kim, Kil-Soo ; Jang, Seung-Jae ; Kang, Chan-Soon ;
Journal of Pharmaceutical Investigation, volume 32, issue 4, 2002, Pages 331~337
DOI : 10.4333/KPS.2002.32.4.331
Nonproprietary name may be used without restriction by the public at large and can be called common name, generic name. Nomenclature agencies exist in US, Great Britain, Japan and so on. The agencies maintain liaison with onε another in an effort to secure the wide adoption of thε most appropriate and universally acceptable designation for each drug. To prevent the confusion which arises when several nonproprietary names are used for a single drug, either in the same country or in several different countries, the WHO has assumed the responsibility of coordination existing nomenclature at the international level. In this study, the nomenclature for new drugs and the terminology to harmonize specifications for revision of Korean Pharmacopoeia (KP) were established.