• Journal of Pharmaceutical Investigation
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• 제30권1호
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• pp.33-37
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• 2000

One of the methods to increase the solubility of a drug is to use complexation with a cyclodextrin. Due to the hydrophobic nature of the interior cavity of the cyclodextrin, it has been known that undissociated lipophilic drugs can be included within the cyclodextrin by hydrophobic interaction. Recently, inclusion of hydrophilic or dissociated form of a drug has been investigated. In this study, the synergism of pH and complexation with $hydroxypropy-{\beta}-cyclodextrin\;(HP\;{\beta}\;CD)$ to increase the solubility of two oxicam derivatives was investigated. In addition, the effect of partition coefficient of dissociated and undissociated form of the drug on the extent of complexation with HP ${\beta}$ CD was studied. The solubility was measured by equilibrium solubility method. The solubility of tenoxicam and piroxicam increased exponentially with an increase in solution pH above the pKa of the drug in the presence and absence of HP ${\beta}$ CD. The solubility of the drugs increased linearly as a function of HP ${\beta}CD$ concentration at fixed pH. Although the stability constant of ionized species is less than that of the unionized species, the concentration of the ionized drug complex is greater than that of the unionized drug complex due to higher concentration of ionized species at pH 7.3.

• Mass Spectrometry Letters
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• 제7권3호
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• pp.79-83
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• 2016

We prepared solid dispersion formulations of quercetin to enhance its solubility and dissolution rate. Various quercetin-loaded solid dispersion were tested with quercetin, poloxamer 407, and carrier such as hydroxypropyl methyl cellulose (HPMC), polyethylene glycol 8000 (PEG 8000), and polyvinylpyrrolidone K40 (PVP K40) using solvent evaporation and freeze drying methods in terms of both the aqueous solubility and the dissolution rates of quercetin. The solubility of quercetin as its solid dispersion formulations was markedly improved compared with that of quercetin powder. Especially, highest solubility of quercetin was observed when HPMC was used as a carrier. The cumulative dissolution of quercetin within 360 min from solid dispersion composed of quercetin, poloxamer 407, and HPMC was 8.8-fold higher than the dissolution of pure quercetin. The results of powder X-ray diffraction (XRD) and scanning electron microscope (SEM) indicated that quercetin transformed from a crystalline to an amorphous form through the solid dispersion formulation process. These results suggest that the solid dispersion formulation of quercetin with poloxamer 407 and HPMC could be a promising option for enhancing the solubility and dissolution rate of quercetin.

• 약학회지
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• 제45권4호
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• pp.357-365
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• 2001

The purpose of this study is to investigate the influence of cyclodextrins (CDs) and different acids on the solubility of fluconazole, and o formulate its more concentrated parenteral aqueous solution. Solubility studies of fluconazole with 7-CD, 2-hydroxypropyl-$\beta$-CD (HPCD), sulfobutyl ether $\beta$-CD (SBCD) and dimethyl-$\beta$-CD(DMCD) were performed. The aqueous solubility of fluconazole was measured in different concentrations of different acids with or without addition of CDs. Solubility of fluconazole increased in the rank order of $\beta$-CD$^1$H-NMR studies confirmed the formation of an inclusion complex of fluconazole with HPCD. It was also shown by the NMR studies that the complex formed was a 1:1 complex. Among the different acids used, maleic acid and phosphoric acid increased solubility of fluconazole. The lower the pH of solution is, the more fluconazole dissolved, regardless of acids. Addition of HPCD (50 mM) to acid solutions increased the solubility about two times. New fluconazole injections at a dose of 10 mg/ml could be prepared in aqueous solutions containing 10% HPCD or 15% SBCD. These parenteral solutions did not form any precipitates at 4$^{\circ}C$ and was very stable at elevated temperatures. These results demonstrate that it is possible to develop a parenteral aqueous solution of fluconazole with a smaller injection volume using HPCD or SBCD.

• Bulletin of the Korean Chemical Society
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• 제29권3호
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• pp.590-594
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• 2008

The inclusion complexes of cyclodextrins (CDs) with flavones in aqueous solution were investigated by phase solubility measurements. The effect of b -cyclodextrin (b -CD), heptakis (2,6-di-O-methyl) b -cyclodextrin (DM-b -CD) and 2-hydroxypropyl-b -cyclodextrin (HP-b -CD) on the aqueous solubility of three flavones, namely, chrysin, apigenin and luteolin was investigated, respectively. Solubility enhancements of all flavones obtained with three CDs followed the rank order: HP-b -CD > DM-b -CD > b -CD, and besides, CDs show higher stability constant on luteolin than that on others flavones. 1H-nuclear magnetic resonance (NMR) spectroscopy and molecular modeling was used to help establish the model of interaction of the CDs with luteolin. NMR spectroscopic analysis suggested that A-C ring, and part of the B ring of luteolin display favorable interaction with the CDs, which was also confirmed by docking studies based on the molecular simulation. The observed augmentation of solubility of luteolin by three CDs was explained by the difference of electrostatic interaction of each complex, especially hydrogen bonding.

• Restorative Dentistry and Endodontics
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• 제15권1호
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• pp.88-96
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• 1990

The purpose of this study was to investigate the fluoride release and solubility of glass ionomer cement associated with three pH media. For this study, GC Fuji II discs (20.0mm in diameter ${\times}$ 1.5mm thick) were immersed in pH 4.0 lactic acid, pH 7.0 distilled water and pH 10.0 KOH solutions for 1, 7, 14 and 28 days. The amount of fluoride release from the cement into three pH media were measured by fluoride specific ion electrode and the solubility was measured by weight loss of discs. The results were as follows: 1. The lower was the pH of media, the more was the amount of release of fluoride. 2. The amount of fluoride release was increased with time lapse. 3. After I day, the solubility was the highest, and after 7 days that was the least. 4. The lower was the pH of media, the more was the solubility, but there was no statistical difference in solubility according to the pH change.

• 한국수소및신에너지학회논문집
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• 제10권2호
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• pp.101-106
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• 1999

Hydrogen solubility in internally oxidized Pd-Mo(Al) alloys has been studied at 323 K from the measurements of pressure-composition(p-c) isotherms. Internal oxidation of $Pd_{0.985}Al_{0.015}$ and $Pd_{0.97}Mo_{0.03}$ alloys results in the precipitation of Al and Mo particles in a matrix of pure Pd. It has been observed that the presence of the aluminum and molybdenum oxide precipitates results in an enhanced hydrogen solubility in the dilute phase region of Pd-H in a Pd/aluminum(molybdenum)oxide composites. Hydrogen solubility enhancements due to the presence of residual stresses around ceramic particles have been observed from p-c isotherms determined at 323 K after oxidation at 1073 K. The solubility enhancements in completely internally oxidized alloys are greater than that in partially oxidized alloys. The stress fields near the ceramic precipitates are the major source of the solubility enhancements. Transmission electron microscopy indicates that alumina precipitates are nanometer-sized and coherent with the Pd matrix after oxidation.

• Journal of Pharmaceutical Investigation
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• 제27권3호
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• pp.199-205
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• 1997

In order to formulate biphenyl dimethyl dicarboxylate(DDB) aqueous solutions, the effects of various solubilizing agents such as cosolvents(PG, PEG 400, glycerin, ethanol), surfactants,$(poloxamer\;407,\;Cremophor^{\circledR}\; RH40,\;Solutol^{\circledR},\;Tween\;80,\;sodium\;lauryl\;sulfate)$, complexation agent$(CELDEX^{\circledR}\;CH-20)$ and others(urea, niacinamide, propylene carbonate, HPMC) on the solubility of DDB in water were evaluated. The solubility of DDB in water was about $0.21\;{\mu}g/ml\;at\;20^{\circ}C$, while its solubility in PEG 400 was 5,000 times higher than that in water. 60% PEG 400 aqueous solution was selected as an optimum solvent system, and surfactants or other solubilizing agents were added to prevent DDB from recrystalization. The addition of surfactants in water increased the solubility of DDB from 15- to 34-fold, however, $CELDEX^{\circledR}\;CH-20$ and other agents studied showed negligible effects on the solubility of DDB in water. The 60% PEG 400 aqueous solution containing 5% $Cremophor^{\circledR}$　RH40 was appeared as the formula of choice. It showed acceptable physical stability after stored for 7 days at $4^{\circ}C$.

• 대한치과의사협회지
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• 제57권5호
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• pp.264-268
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• 2019

Objectives: This study aimed to measure the water sorption / solubility of Biodentine, composite resin and glass ionomer cement. Materials and Methods: The materials used in this study were Biodentine(BD), Filtek Z250(FZ) and Ketac Molar(KM). Twenty disc-shaped specimens of each material were prepared of 6mm diameter and 1mm thickness. All specimens were desiccated for 24 hours and weighed(m1). After then, They were immersed in distilled water and stored at $37^{\circ}C$. 1 week later, They were washed with running water, wiped with absorbent paper and weighed(m2). Finally, They were dried for 24 hours and weighed(m3). Water sorption and solubility, net water uptake were calculated. Results: KM and BD showed high water sorption than FZ(P<0.05). KM and BD exhibited similar water sorption(P<0.05). BD exhibited high solubility than KM(P=0.012). BD exhibited high net water uptake than FZ(P=0.008). Conclusion: Biodentine showed higher water sorption, solubility and net water uptake than Filtek Z250 and Ketac Molar. Within limitation of this study, it is not recommended to use Biodentine for permanent restoration.

• 방사성폐기물학회지
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• 제19권1호
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• pp.113-121
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• 2021

A safety assessment of radioactive waste repositories is a mandatory requirement process because there are possible radiological hazards owing to radionuclide migration from radioactive waste to the biosphere. For a reliable safety assessment, it is important to establish a parameter database that reflects the site-specific characteristics of the disposal facility and repository site. From this perspective, solubility, a major geochemical parameter, has been chosen as an important parameter for modeling the migration behavior of radionuclides. The solubilities were derived for Am, Ni, Tc, and U, which were major radionuclides in this study, and on-site groundwater data reflecting the operational conditions of the Gyeongju low and intermediate level radioactive waste (LILW) repository were applied to reflect the site-specific characteristics. The radiation dose was derived by applying the solubility and radionuclide inventory data to the RESRAD-OFFSITE code, and sensitivity analysis of the dose according to the solubility variation was performed. As a result, owing to the low amount of radionuclide inventory, the dose variation was insignificant. The derived solubility can be used as the main input data for the safety assessment of the Gyeongju LILW repository in the future.

• Korean Chemical Engineering Research
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• 제62권1호
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• pp.53-69
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• 2024

The solubility of Cloxacillin sodium in ethanol, 1-propanol, isopropanol, and acetone solutions was measured at different temperatures. The melting property was also tested by using a differential scanning calorimeter (DSC). Then, the solubility data were fitted using Apelblat equation and λh equation, respectively. The Wilson model and NRTL model were not utilized to correlate the test data, since Cloxacillin sodium will decompose directly after melting. For comparison purposes, the four empirical models, i.e., Apelblat equation, λh equation, Wilson model and NRTL Model, were evaluated by using 1155 solubility curves of 103 solutes tested under different monosolvents and temperatures. The comparison results indicate that the Apelblat equation is superior to the others. Furthermore, a new method (named the calculation method) for determining the Apelblat equation using only three data points was proposed to solve the problem that there may not be enough solute in the determination of solubility. The log-logistic distribution function was used to further capture the trend of the correlation and to make better quantitative comparison between predicted data and the experimental ones for the Apelblat equation determined by different methods (fitting method or calculation method). It is found that the proposed calculation method not only greatly reduces the number of test data points, but also has satisfactory prediction accuracy.