• Archives of Pharmacal Research
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• 제18권1호
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• pp.22-26
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• 1995

The solubility and dissolution rate of naproxen (NPX) complexed with 2-hydroxypropyl-.betha.-cyc-lodextrin (2-HP.betha.CD) using coprecipitation, evaporation, freeze-drying and kneading method were investigated. Solubility of NPX linearly increased (correlation cefficient, 0.995) as $2-HP\betaCD$ concentraction increased, resutling in $A_l$ type phase solubility curve. Inclusion complexes prepared by four different methods were compared by different methods were compared by dfferential scanning calorimetry(DSC). The NPX showed sharp endothemic peak around $156^{\circ}C$ but inclusion complexes by evaporation, freeze-drying and kneading method showed very broad peak without distinct phase transtion temperature. In contrast, inclusion complex prepared by coprecipitation method resulted in detectable peak around $156^{\circ}C$ which is similar to NPX, suggesting incoplete formation of indusion co plex. Dissolution rate of inclusion complexes prepared by evaporation, frezz-drying and kneding except coprecipitation method was largely enhanced in the simultaed gastric and intestinal fluid when compared to NPX powder and commercial $NA-XEN^\registered$tablet. However, about 65% of NPX in gstric fluid. in case of inclusion complex prepared by coprecipitation method, formation of inclusion complex appeared to be incoplete, resulting in no marked enhancement of dissolution rate. From these findings, inclusion complexes of poorly water-soluble NPX with $2-HP\betaCD$ were useful to increase soubility and dissolution rate, resting in enhancement of bioavailability and minimization of gastrointestinal toxicity of drug upon oral administration of inclusion complex.

• Journal of Pharmaceutical Investigation
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• 제27권3호
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• pp.219-223
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• 1997

Terfenadine, antihistaminic drug, is poorly soluble in water. The purpose of this study is to investigate the possibility of using $terfenadine-{\beta}-cyclodextrin$ inclusion compound, instead of terfenadine, as the active substance of solid dosage form by improving the solubility, dissolution and anti-histaminic activity of terfenadine. The solubility and binding characteristics of $terfenadine-{\beta}-cyclodextrin$ complex in pH $1.2{\sim}6.8$ were investigated. Furthermore, the preparing method of $terfenadine-{\beta}-\;cyclodextrin$ inclusion compound was setting up and its physico-chemical characteristics such as DSC curve, solubility, dissolution and anti-histaminic activity were investigated. In conclusion, the solubility of terfenadine was increasing ${\beta}-cyclodextrin$ and with the decreasing pH. $Terfenadine-{\beta}-cyclodextrin$ inclusion compound, whose yield is almost 100%, was prepared by neutralization method. This inclusion compound was 200-times as soluble as terfenadine in pH 1.2-6.8. In addition, it had the faster dissolution and anti-histaminic activity than terfenadine. Therefore, it is used to the active substance of solid dosage form such as tablet and capsule in stead of terfenadine.

• 한국잠사곤충학회지
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• 제42권1호
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• pp.48-57
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• 2000

This study was undertaken to figure out the effects of hydrolysis conditions on the solubility of insoluble sericin, molecular weight distribution and thermal characteristics of hydrolysates in enzymatic hydrolysis by Alcalase 2.5L. It was indicated that the optimum treatment temperature and pH for the insoluble sericin were 50$\^{C}$ and 11, respectively. When the insoluble sericin was hydrolyzed with a various treatment conditions, the solubility of all hydrolysates were represented above 85% at given conditions. As the enzyme concentration increased, the solubility increased roughly, but the solubility increasement ratio was less above 2% enzyme concentration. As the treatment time increased, the solubility was also increased. It was showed in the molecular weight distribution of hydrolysates treated various enzyme concentrations and treatment times that when enzyme concentrations were 0.5, 2, 3%, the peaks of the distribution curve were shifted to left side which meant low molecular weight and was distributed much quantity with shifted to be left side, but treatment time was 6 hr. the peak was shifted to right side. When enzyme concentration was 5% and treatment time was below 2 hr., the peaks were shifted to right side, but treatment time was above 4hr. the peak was shifted to left side. The number-average molecular weights were distributed from 300 to 800 and those were decreased when treatment time was up to 4 hr., but increased a little when treatment time was 6hr. It was showed in the DSC curves of hydrolysates treated with treatment time of 0.5, 1, 2, 4, 6 hr. fixed 1% o.w.s enzyme concentration and control that the endothermic peak was observed near at 200$\^{C}$. The denaturation peak of the hydrolysates depending on treatment times had a tendency to shift to higher temperature. But, when the treatment time was 6 hr., the peak was shifted to lower temperature comparing another hydrolysates.

• 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.

• 대한화장품학회지
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• 제12권1호
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• pp.34-61
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• 1986

The microstructural transitions of aqueous micellar solutions of cetyltrime-thylammonium bromide and sodiumdodecyl sulfate by adding 1-hexanol were investigated, measuring the concentrations of equilibrated phases and the electrical conductivities at the low concentrations of surfactants, where the solobilities of 1-hexanol varied significantly, at 3$0^{\circ}C$ and 45$^{\circ}C$. Ternary phase diagrams of multiphase regions, constructed by liquid chromatography analysis and by counting the number of phase of samples, consisted of one three-phase region and three two-phase regions. One of the two-phase regions was found to equilibrate an aqueous micellar solution and a liquid crystal, and had a critical point between them. Near this region, the solubility curve varied abruptly, and the isotropic solution turned birefrigent. The conductivities of the single phase regions above the critical point increased up to a certain point as 1-hexanol added, and then decreased, representing the microstructural transition at the supercritical region. Further, the solubility of 1-hexanol in aqueous micellar solution was found to increase as temperature and the number of hydrophilelipophile balance of surfactants increase.

• Nuclear Engineering and Technology
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• 제14권4호
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• pp.172-177
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• 1982

pH변화 5~10 범위에서 $10^{-5}$M Am 수용액의 상태를 여과법 및 인심분리법에 의하여 조사하였다. 이 실험에서 Am의 가능한 가수분해 생성물 및 용해도 상수를 추정할 수 있었다. 이때 Baes 및 Mesmer에 의하여 이론적으로 계산한 Am(OH)$_3$의 용해도를 약 10배 증가하면 즉 log k=-18.7를 log k=-17.5로 변화시키면 계산에 의한 PH변화에 따른 Am농도곡선은 실험치와 완전히 일치하였다.

• 멤브레인
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• 제8권3호
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• pp.157-169
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• 1998

폴리이미드(6FDA-p-TeMPD) 비대칭막을 습식 상분리법으로 제조하는데 있어서 그 구조에 미치는 용매 (DMAc, NMP, 1,4-dioxane)와 비용매($H_2O$, Methanol, n-hexane)의 영향을 고찰하였다. 고분자/용매/비용매 분리 속도를 예측함으로써 생성된 비대칭막의 구조를 해석하였다. 용해도 곡선이 용매-고분자 축에 가깝고, 응결값이 작으며, 광투과도가 즉시 감소하고, 용해도 계수차가 $\Delta \delta_{S-NS} > \Delta \delta_{P-NS} > \Delta \delta_{P-S}$ 순이면 생성막은 고분자 결절의 불연속 결집속에 finger-like pore가 형성되었다. 용해도 곡선이 용매-고분자 축에서 멀고, 응결값이 크며, 상분리 시간이 길고, 용해도 계수차 $\Delta \delta_{i-j}$ 가 $\Delta \delta_{P-NS} >(\Delta \delta_{S-NS} < > \Delta \delta_{P-S})$ 일때, 생성되는 막은 미소 고분자 결절구가 치밀하게 응집된 표피가 있으며, 고분자 연속상 스폰지층에 macropore가 발달되었다. 용해도 곡선이 용매-고분자 축으로부터 멀리 떨어지고, 응결값이 대단히 크며, 상분리 시간이 길고, 용해도 계수차 $\Delta \delta_{i-j}$가 $\Delta \delta_{S-NS} > (\Delta \delta_{P-NS}$\lessgtr$)\Delta \delta_{P-S}$인 경우는 고분자 미소 결절의 두터운 응집층과 다음에 성근 결절응집층이 나타났다.

• 한국재료학회지
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• 제27권8호
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• pp.445-450
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• 2017

YSZ (Yttria-stabilized zirconia) is a ceramic material that is used for electronic and structural materials due to its excellent mechanical properties and specific electrical characteristics according to the Yttrium addition. Hydrothermal synthesis has several advantages such as fine particle size, uniform crystalline phase, fast reaction time, low process temperature and good dispersion condition. In order to synthesize YSZ nanoparticles with high crystallinity, hydrothermal synthesis was performed at various concentrations of NaOH. The hydrothermal process was held at a low temperature ($100^{\circ}C$), with a short process time (2,4,8 hours); the acidity or alkalinity of solution was controlled in a range of pH 2~12 by addition of NaOH. The optimum condition was found to be pH 12, at which high solubility levels of Y(OH) and Zr(OH) were reported. The synthesized nano powder showed high crystallinity and homogenous composition, and uniform particle size of about 10 nm.

• 약학회지
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• 제23권2호
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• pp.81-94
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• 1979

Rifampicin-polyvinylpyrrolidone coprecipitates were prepared by the solvent method to increase the solubility and dissolution rate, thereby improving absorption of rifampicin. It was found that the solubility and dissolution rate were greater with the 1 : 5 (w/w) coprecipitate than with the pure drug, physical mixtures or coprecipitates of any other ratio of the two components. The blood concentration data in non-fasted rats showed that the extent of absorption of rifampicin were significantly enhanced following the oral administration of the 1 : 5 coprecipitate; The area under the serum concentration curve (0-8hr) was 1.3 times greater with the 1 : 5 coprecipitate than with the pure drug. The blood concentration reached its peak (4. 38$\pm$1.36mcg/ml) within two hours in the case of oral administration of the 1 : 5 coprecipitate and, on the other hand, it reached the maximum (3.77$\pm$0.90mcg/ml) after four hours of oral administration of the pure drug. It was observed that there was no significant difference between the 1 : 5 coprecipitate and the pure drug in the extent and rate of absorption of rifampicin when fasted rats were used. When the 1 : 5 coprecipitate was orally administered to human subjects 20 minutes after meal, it was found that the blood concentration reached the maximum after one hour; in the case of the pure drug, it reached its peak after four hours.

• 한국포장학회지
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• 제5권1호
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• pp.6-12
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• 1999

본 실험은 라면 스프 포장재에 대한 가식성 필름의 응용성을 조사하였다. 기본 실험으로서는 라면 스프의 등온흡습곡선 및 BET 단분자막 수분함량을 조사하였으며, 응용성 실험으로서는 가식성 필름의 인장강도, 신장률, 수분 투과도 및 용해도를 대하여 조사하였다. 가식성 필름으로서는 methylcellulose, sodium caseinate 및 K-carrageenan을 사용하였으며, 가소제로서는 glycerol과 polyethylene glycol (MW 400)을 사용하였다. 인장강도의 경우, methylcellulose 필름의 수치가 68.56 MPa로 가장 크게 나타났으며, sodium caseinate 필름이 가장 낮은 수치인 7.11 MPa로 나타났다. 신장률에 대한 실험 결과, sodium caseinate 필름이 가장 높은 수치인 115.41 %를 나타냈으며, methylcellulose 및 K-carrageenan 필름은 각각 23.79% 및 0.60%로 나타났다. 상대습도 50% - 70%사이에서 methylcellulose와 sodium caseinate 및 K-carrageenan 필름의 측정된 수분 투과도 값의 범위는 각각 $0.25-0.38ng\;m/m^2{\cdot}sec{\cdot}Pa$와 $0.62-0.84ng{\cdot}m/m^2{\cdot}sec{\cdot}Pa$ 및 $0.31-0.55ng{\cdot}m/m^2{\cdot}sec{\cdot}Pa$로 나타났다. 가식성 필름의 용해도에 대해서는 sodium caseinate film의 경우 뜨거운 물에 대한 높은 용해성을 나타내어 5초 이내에 이 필름은 물에 용해되었으며, K-carrageenan film은 높은 팽윤율을 나타내어 150초 이후에 필름의 붕괴 현상이 일어났다. Methylcellulose film의 경우는 물에 대한 용해도가 떨어지는 것으로 나타났다.