• 약학회지
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• 제44권6호
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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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• 제32권4호
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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.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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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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• 제12권1호
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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.

• 대한본초학회지
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• 제25권2호
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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.

• 한국분말재료학회지
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• 제27권6호
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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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• 제9권4호
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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.

• 한국산학기술학회논문지
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• 제18권12호
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• pp.329-334
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• 2017

본 논문은 새로운 과립형태의 구강청결제 개발에 있어 동등한 항균력을 가지면서 고형상에서 주성분간의 공융혼합물 생성에 따른 과립의 흐름성 부족을 개선하기 위해 과립의 표면을 흡착시키는 Magnesium aluminometasilicate (Neusilin)이라는 물질을 활용하여 흐름성을 개선하고 부가적으로 구강에서의 붕해시간 및 잔물감이 적은 특성을 가지는 새로운 과립형태의 구강청결제를 제조하였다. 제조된 과립의 흐름성, 밀도, 건조감량 등의 과립특성에 대한 확인을 통해 Neusilin의 양이 전체 과립양 대비 10%이상이 투입되었을 경우 과립의 특성이 개선되는 결과를 확인하였다. 또한 인공타액에서의 붕해시험 및 사람의 구강에서 붕해시간과 잔여물시험 등의 관능시험을 진행하여 보다 개선된 붕해특성 및 관능시험 결과를 확인할 수 있었으며 항균시험을 통해서 이미 시장에서 판매중인 액제형 구강청결제와 동등한 항균력을 보여주는 것으로 확인하였다. 본 연구를 통해 제조된 과립형태의 구강청결제 조성물은 공융혼합물로서 유사한 특성을 가지는 서로 다른 약물을 동시에 함유하는 의약품의 개발에 활용될 수 있어 제약산업의 의약품 개발에서 유용할 것으로 사료된다.

• Toxicological Research
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• 제29권3호
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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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• 제11권4호
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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.