• YAKHAK HOEJI
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• v.44 no.6
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• pp.528-533
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• 2000

This study was to develop an effective itraconazole liquid preparation which exhibits an enhanced bioavailability. The solubility of itraconazole was increased (72-fold) in itraconazole liquid preparation as compared with itraconazole powder. The dissolution rate of itraconazole was higher for itraconazole liquid preparation filled into a hard gelatin capsule with 90% release within 20 min as compared to 55% for $Sporanox^{\circledR}$capsules. The oral absorption of itraconazole liquid preparation and $Sporanox^{\circledR}$tablets were studied in the rat. The area under the concentration-time curve $(AUC_{0-24hr})$ of itraconazole liquid preparation ($90.25\;{\pm}\;8.36\;{\mu}g{\cdot}hr/ml$) increased by 6.2 times compared to that of Sporanox tablets ($14.58\;{\pm}\;1.26\;{\mu}g{\cdot}hr/ml$) after oral administration of itraconazole 15 mg/rat each. $C_{max}$ also increased to $6.87\;{\pm}\;1.15\;{\mu}g/ml$ after administration of liquid preparation $1.58\;{\pm}\;0.16\;{\mu}g/ml$ of $Sporanox^{\circledR}$tablets. These results indicate that in vivo bioavailability of itraconazole liquid preparation was significantly enhanced as compared with $Sporanox^{\circledR}$tablets.

• Journal of Pharmaceutical Investigation
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• v.32 no.4
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• pp.299-303
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• 2002

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.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.226.1-226.1
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• 2003

The available period of oral pharmaceutical liquid preparations was decided according to the study of the stability of unopened preparations. But if one reuses the drug after opening the sealed cap, the major components of the drug could change in quality. In addition, there isn｀t any accurate information about the available period of opened oral pharmaceutical liquid preparations. In this study, a long term test, an accelerated test and a microbial limit test are run with C (pseudoephedrine and triprolidine), D (ibuprofen) that are marketed and used frequently. (omitted)

• Mass Spectrometry Letters
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• v.12 no.1
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• pp.16-20
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• 2021

We aimed to compare the content of ginsenosides and the pharmacokinetics after the oral administration of four different ginseng products at a dose of 1 g/kg in rats. The four different ginseng products were fresh ginseng extract, red ginseng extract, white ginseng extract, and saponin enriched white ginseng extract prepared from the radix of Panax ginseng C.A. Meyer. The ginsenoside concentrations in the ginseng product and the rat plasma samples were determined using a liquid chromatography-tandem mass spectrometry (LC-MS/MS). Eight or nine ginsenosides of the 15 tested ginsenosides were detected; however, the content and total ginsenosides varied depending on the preparation method. Moreover, the content of triglycosylated ginsenosides was higher than that of diglycosylated ginsenosides, and deglycosylated ginsenosides were not present in any preparation. After the single oral administrations of four different ginseng products in rats, only four ginsenosides, such as 20(S)-ginsenosides Rb1 (GRb1), GRb2, GRc, and GRd, were detected in the rat plasma samples among the 15 ginsenosides tested. The plasma concentrations of GRb1, GRb2, GRc, and GRd were different depends on the preparation method but pharmacokinetic features of the four ginseng products were similar. In conclusion, a good correlation between the area under the concentration curve and the content of GRb1, GRb2, and GRc, but not GRd, in the ginseng products was identified and it might be the result of their higher content and intestinal biotransformation of the ginseng product.

• The Korea Journal of Herbology
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• v.25 no.2
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• pp.81-88
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• 2010

Objectives : Sophorae Radix (SR), the dried root of Sophorae Flavescens Aiton, has been used to treat atherosclerosis, arrhythma and skin diseases including scabies and eczema. The present study was examined to evaluate antimicrobial activities of SR extracts against oral microorganism. Methods : Antimicrobial properties of SR extracts were determined by agar diffusion method and minimum inhibitory concentration (MIC) against Streptococcus mutans, Streptococcus sobrinus and Actinomyces viscosus. Analysis of kurarinone from SR extracts was conducted using UPLC (Ultra Performance Liquid Chromatography). Results : The ethanolic extracts of SR showed stronger antimicrobial effect than methanolic extracts, while the aqueous extracts of SR had no activity. In addition, the higher content of kurarinone was found in ethanolic extracts than methanolic extracts. The purified kurarinone from ethanolic extracts showed potent antimicrobial activity with the MIC value of $3.9{\sim}7.8{\mu}g/m{\ell}$. Conclusion : An ethanolic extract of SR showed antimicrobial properties against several oral microorganisms, and kuranrinone contributed to antimicrobial action of SR. Thus, ethanolic extracts of SR or purified kurarinone should be beneficial for the preparation of the useful agent for treating oral disease including anticaries.

• Journal of Powder Materials
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• v.27 no.6
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• pp.468-476
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• 2020

The bone cement used for vertebroplasty must be sufficiently injectable. The introduction of granules reduces the amount of liquid required for liquefaction, implying that higher fluidity is achieved with the same amount of liquid. By employing β-tricalcium phosphate granules with an average diameter of 50 ㎛, changes in injectability are observed based on the paste preparation route and granular fraction. To obtain acceptable injectability, phase separation must be suppressed during injection, and sufficient capillary pressure to combine powder and liquid must work evenly throughout the paste. To achieve this, the granules should be evenly distributed. Reduced injection rates are observed for dry mixing and excessive granular content, owing to phase separation. All these correspond to conditions under which the clustered granules weakened the capillary pressure. The injected ratio of the paste formed by wet mixing displayed an inverted U-type shift with the granular fraction. The mixture of granules and powder resulted in an increase in the solid volume fraction, and a decrease in the liquid limit. This resulted in the enhancement of the liquidity, owing to the added liquid. It is inferred that the addition of granules improves the injectability, provided that the capillary pressure in the paste is maintained.

• Mass Spectrometry Letters
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• v.9 no.4
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• pp.110-114
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• 2018

Since accumulation of chemicals in deciduous teeth can occur from the second trimester of fetal development to shedding, a deciduous tooth has been considered as an attractive biomatrix for estimating individual chemical exposures recently. Therefore, detection of organic chemicals from teeth has received an increasing attention in exposomics research. Most previous studies on organic chemical analysis of teeth not only focused on a few targeted chemicals but also ignored potential contaminants from an enamel surface or a dental pulp. Recently, our group started developing a multi-class organic analysis method for deciduous teeth and tried to find a proper incubation condition of tooth materials. Our results showed that incubation with methanolic HCl provided the best performance among tested.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.18 no.12
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• pp.329-334
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• 2017

In this study, a new granular type mouthwash with equivalent antibacterial activity to marketed liquid type mouthwash was developed using a material called magnesium aluminometasilicate (Neusilin). This material adsorbs the surface of granules to improve the flowability of granules due to the formation of a eutectic mixture of the main constituents, which have improved flow properties and rapid disintegration time and little residue in the oral cavity. The characteristics of the granules were improved when the amount of Neusilin was 10% or more according to measurements of the granule properties, such as flowability. In addition, a disintegration test in artificial saliva and a sensory test in the human oral cavity were carried out to confirm the improved disintegration characteristics and sensory test results. The antimicrobial test confirmed similar antibacterial activity to that of the liquid oral cleanser already sold in the market. The granular oral cleanser composition prepared in this study can be used for the development of pharmaceuticals containing different drugs with similar characteristics as eutectic mixtures at the same time, which is considered to be useful in the development of medicines in the pharmaceutical industry.

• Toxicological Research
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• v.29 no.3
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• pp.203-209
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• 2013

A simple and rapid liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the quantification of ${\varepsilon}$-acetamidocaproic acid (AACA), the primary metabolite of zinc acexamate (ZAC), in rat plasma by using normetanephrine as an internal standard. Sample preparation involved protein precipitation using methanol. Separation was achieved on a Gemini-NX $C_{18}$ column ($150mm{\times}2.0mm$, i.d., 3 ${\mu}m$ particle size) using a mixture of 0.1% formic acid-water : acetonitrile (80 : 20, v/v) as the mobile phase at a flow rate of 200 ${\mu}l/min$. Quantification was performed on a triple quadrupole mass spectrometer employing electrospray ionization and operating in multiple reaction monitoring (MRM) and positive ion mode. The total chromatographic run time was 4.0 min, and the calibration curves of AACA were linear over the concentration range of 20~5000 ng/ml in rat plasma. The coefficient of variation and relative error at four QC levels were ranged from 1.0% to 5.8% and from -8.4% to 6.6%, respectively. The present method was successfully applied for estimating the pharmacokinetic parameters of AACA following intravenous or oral administration of ZAC to rats.

• Mass Spectrometry Letters
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• v.11 no.4
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• pp.71-76
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• 2020

While montelukast (ML), a cysteinyl-leukotriene type 1 receptor (CysLT1) antagonist is widely used to treat symptoms of rhinitis or asthma, its formulations are mainly limited to solid preparation due to its instability. Recently, there have been attempts to develop various ML dosage forms, and this situation increases the demand of sensitive and creditable methods to determine ML in various samples such as plasma. Thus, here, a simple and efficient method to determine ML in rat plasma using liquid-liquid extraction (LLE) and multiple reaction monitoring was presented. The mixture of DCM:EtOAc (25:75, v/v), the optimized extract solvent for LLE was found to be effective to extract ML without hydrophilic salts and proteins from the sample with limited volume. Also, the use of zafirlukast, instead of expensive ML-d6, as the internal standard makes the present method economical. The developed method was successfully validated in terms of selectivity, matrix effects (-14.8--6.9%), linearity (r230.998 within 0.5-500 ng/mL), sensitivity (the limit of detection and the lower limit of quantitation, ≤0.5 ng/mL), accuracy (88.4-100.6%), precision (3.0-13.3%), and recovery (80.8-86.3%) by following the FDA guidelines. Finally, the applicability of the validated method to pharmacokinetics (PK) studies was confirmed by the successful determination of PK parameters through it following oral administration of Singulair® granule in rats. Therefore, the present method can contribute to the development of new ML formulations through its performance to determine ML in rat plasma efficiently and sensitively.