• Bulletin of the Korean Chemical Society
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• 제31권10호
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• pp.3035-3037
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• 2010

• Bulletin of the Korean Chemical Society
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• 제33권6호
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• pp.2091-2094
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• 2012

• 한국약용작물학회지
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• 제19권6호
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• pp.464-471
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• 2011

Conventional Thiamine Dilauryl Sulfate (TDS) powder has a low stability. In order to solve this problem, this study was performed to improve the solubility of TDS. The process for enhance solubility of TDS was nano grinding mill and ultrasonic dispersion process. TDS paticle was manufactured to nano size through nano grinding mill process. The size of TDS nanoparticle was measured as average 220 nm by DLS. And The TDS nanoparticle in water solution manufactured through ultrasonic dispersion process. The TDS nanoparticle in water solution was showed the highest solubility with 40% ethanol. These results was increased the concentration of TDS from 200 ppm to 240 ppm in water solution. The TDS nanoparticle in water solution showed diameter of Colletotrichum gloeosporioides growth with smaller than about 1.56 cm compared to the TDS paticle in water solution at same concentration. Also, TDS nanoparticle in water solution showed growth inhibition activity as 59.2% with higher than about 10% compared to the TDS paticle water solution in same concentration. Finally, TDS nanoparticle in water solution was increased solubility through nano grinding mill and ultrasonic dispersion process. Also, the increase of concentration in TDS nanopaticle in water solution according to solubility enhancement lead to an result enhancement of antifungal activity. Consequently, we suggested that the TDS nanoparticle in water solution was more effective than TDS particle in water solution owing to the sub-cellular particle size, ability to persistence and targeting to cell membrane of Colletotrichum gloeosporioides. Furthermore we expected the applicating possibility with bio pesticide.

• 한국잠사곤충학회지
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• 제41권3호
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• pp.211-215
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• 1999

The pure-separation of calcium chloride-treated fibroin hydrolysates could be carried out using gel filtration chromatography. Also, the effect of its enzymatic hydrolysis was investigated in order to find out the enhancement of their functionality. The average molecular weight(Mw), solubility and free amino acid compositions of three hydrolysates samples (calcium chloride, calcium chloride-flavourzyme and calcium chloride-thermoase)were measured to compare their characteristics. The molecular weight of calcium chloride hydrolysate was about Mw 46,800 and it can be reduced to Mw 12,500 and 1,070 upon the enzymatic hydrolysis by flavourzyme and thermoase, repectively. A solubility of calcium chloride-treated samples shows about 60% while calcium chloride/enzyme-treated samples are perfectly soluble (100% solubility). The total amino acid composition of calcium chloride enzymatic hydrolysates are much higher than that of calcium chloride hydrolysate.

• Bulletin of the Korean Chemical Society
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• 제31권11호
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• pp.3460-3462
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• 2010

• 약학회지
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• 제37권3호
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• pp.216-227
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• 1993

Complex formations of practically insoluble antelmintic drugs such as mebendazole (MBZ), albendazole (ABZ) and flubendazole (FBZ) with dimethyl-$\beta$-cyclodextrin (DM-$\beta$-CyD) and 2-hydroxypropyl-$\beta$-cyclodextrin (HP-$\beta$-CyD) together with $\alpha$-, $\beta$- and $\gamma$-cyclodextrins(CyDs) in duffered solutions were investigated by solubility method. $A_{L}$ type phase solubility diagrams were obtained in all cases except for the complexation (B$_{s}$, type) of FBZ with $\gamma$-CyD. The highest stability constants were obtained with DM-$\beta$-CyD, followed by $\alpha$-CyD > $\beta$-CyD > HP-$\beta$-CyD > $\gamma$-CyD for ABZ, and HP-$\beta$-CyD > $\gamma$-CyD > $\beta$-CyD > $\alpha$-CyD for FBZ at pH 1.2. On the other hand, solid dispersion systems of ABZ and FBZ with $\beta$- and DM-$\beta$-CyDs were prepared by solvent evaporation method and evaluated by dissolution, differential thermal analysis and powder x-ray diffractometry. The dissolution rates of ABZ- and FBZ-DM-$\beta$-CyD solid dispersions were much faster than those of drugs alone, corresponding physical mixtures and tablets on market both at pH 1.2 and 6.8. Although dissolution rates of all samples at pH 6.8 were by far lower than those obtained at pH 1.2, as explained by pH-solubility profiles for ABZ and FBZ, the dissolution rates at pH 6.8 of ABZ from $\beta$- and DM-$\beta$-CyD solid dispersions exceeded the respective equilibrium solubility (23.9 $\mu\textrm{g}$/ml). Fast dissolution of ABZ from solid dispersions with CyDs was attributed to the reduction of drug crystallinity and particle size which was supported by DTA and powder x-ray diffractometry. Consequently these results suggest that solid dispersion systems with CyDs may provide useful means to markedly enhance the solubility and dissolution of benzimidazole antelmintic drugs.

• 한국약용작물학회지
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• 제26권4호
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• pp.317-327
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• 2018

Background: The root of Angelica gigas Nakai is used as a traditional herbal medicine in Korea for the treatment of many diseases. However, the poor water solubility of the active components in A. gigas Nakai is a major obstacle to its bioavailability. Methods and Results: This work aimed at enhancing the solubility of the active compounds of A. gigas Nakai by a chemical (using a surfactant) and physical (hot melt extrusion, HME) crosslinking method. Fourier transform infrared spectroscopy revealed multiple peaks in the case of the extrudate solids, attributable to new functional groups including carboxylic acid, alkynes, and benzene derivatives. Differential scanning calorimetry analysis showed that the extrudate soilid had a lower glass transition temperature ($T_g$) and enthalpy (${\Delta}H$) ($T_g:43^{\circ}C$, ${\Delta}H$ : < 6 J/g) as compared to the non-extrudate ($T_g:68.5^{\circ}C$, ${\Delta}H:123.2$) formulations. X-ray powder diffraction analysis revealed the amorphization of crystalline materials in the extrudate solid. In addition, enhanced solubility (53%), nanonization (403 nm), and a higher amount of extracted phenolic compounds were achieved in the extrudate solid than in the non-extrudate (solubility : 36%, nanonization : 1,499 nm) formulation. Among the different extrudates, acetic acid and span 80 mediated formulations showed superior extractions efficiency. Conclusions: HME successfully enhanced the production of amorphous nano dispersions of phenolic compound including decursin from extrudate solid formulations.

• Journal of Pharmaceutical Investigation
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• 제26권3호
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• pp.169-174
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• 1996

Inclusion complexes of diclofenac sodium with ${\beta}-cyclodextrin$ were prepared in aqueous solution, alkaline solution and solid phase. The interaction of diclofenac sodium with ${\beta}-cyclodextrin$ in pH 9.0 alkaline solution was evaluated by the solubility method and the instrumental analysis such as thermal analysis, infrared spectroscopy, X-ray diffractometry. The solubility of diclofenac sodium was increased linearly with the increase in the concentration of ${\beta}-cyclodextrin$up to 0.15 mol and showed that the aqueous solubility rate of diclofenac sodium was significantly increased by complex with ${\beta}-cyclodextrin$. The optimum composition of this complex was one molecule of ${\beta}-cyclodextrin$ included 1.59 molecular weight of diclofenac sodium as a guest molecule. The pharmacokinetic parameters of the diclofenac sodium and the complex with ${\beta}-cyclodextrin$ were studied in rats by oral route. $T_{max}$ between drug alone and inclusion complex showed significant difference to be 120 minute and 20 minute respectively. Both of $C_{max}$ and AUC of inclusion complex was about 40% higher than drug alone. It is estimated from the data in this study that complexation of diclofenac sodium with ${\beta}-cyclodextrin$ increased the absorption rate and improved the bioavalability of the diclofenac sodium by the formation of a water-soluble complexes.

• Journal of Pharmaceutical Investigation
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• 제23권1호
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• pp.11-18
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• 1993

Inclusion complex of ibuprofen with $2-Hydroxypropyl-{\beta}-cyclodextrin\;(HP-{\beta}-CD)$ in aqueous solution and in the solid state was evaluated by the solubility method and the instrumental analysis such as infrared spectroscopy, thermal analysis and x-ray diffractometry. The aqueous solubility of ibuprofen was increased linearly with the increase in the concentration of $HP-{\beta}-CD$, showing an $A_L$ type phase solubility diagram. The results showed that the dissolution rate of ibuprofen was significantly increased by complexation with $HP-{\beta}-CD$. $Ibuprofen-HP-{\beta}-CD$ complex enhanced the mean plasma concentration levels and the area under plasma concentration-time curve after oral administration compared to those of the drug alone. It is concluded that the complex of ibuprofen with $HP-{\beta}-CD$ increases the dissolution rate and improves the bioavailability of the ibuprofen by the formation of a water-soluble complex.

• Bulletin of the Korean Chemical Society
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• 제22권1호
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• pp.46-52
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• 2001

To evaluate the non-ionic polymer, poly(ethylene glycol) (PEG), as a component in cationic copolymers for non-viral gene delivery systems, PEG was coupled to polyethylenimine (PEI). We present the effects of different degrees and shapes of pegylation of PEI on cytotoxicity, water solubility and transfection efficiency. This work reports the synthesis and characterization of a series of cationic copolymers on the basis of the conjugates of PEI with PEG. The modified molecules were significantly less toxic than the original polymer. Moreover, the chemical modification led to enhancement of their solubility. The comparison of pegylated PEIs with different degrees of derivation showed that all the polymers tested reached comparable levels of transgene expression to that of native PEI. As assessed by agarose gel electrophoresis, even highly substituted PEI derivatives were still able to form polyionic complexes with DNA. However, aside from an increase in solubility and retention of the ability to condense DNA, methoxy-PEG-modified PEIs resulted in a significant decrease in the transfection activity of the DNA complexes. In fact, the efficiency of the copolymer was compromised even at a low degree of modification suggesting that the PEG action resulting from its shape is important for efficient gene transfer. The mode of PEG grafting and the degree of modification influenced the transfection efficiency of PEI.