• Title/Summary/Keyword: solubility curve

Search Result 27, Processing Time 0.026 seconds

Enhancement of Solubility and Disolution Rate of Poorly Water-soluble Naproxen by Coplexation with $2-Hyldroxypropylo-{\beta}-cyclodextrin$

  • Lee, Beom-Jin;Lee, Jeong-Ran
    • Archives of Pharmacal Research
    • /
    • v.18 no.1
    • /
    • pp.22-26
    • /
    • 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.

  • PDF

Preparing Method and Physico-chemical Characteristics of $Terfenadine-{\beta}-Cyclodextrin$ Inclusion Compound (테르페나딘-${\beta}$-시클로덱스트린 포접화합물의 제조방법 및 물리화학적 특성)

  • Choi, Han-Gon;Ryu, Jei-Man;Yoon, Sung-June
    • Journal of Pharmaceutical Investigation
    • /
    • v.27 no.3
    • /
    • pp.219-223
    • /
    • 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.

  • PDF

Enzymatic hydrolysis of insoluble silk sericin by Alcalase

  • Jung, Hye-Young;Bae, Do-Gyu
    • Journal of Sericultural and Entomological Science
    • /
    • v.42 no.1
    • /
    • pp.48-57
    • /
    • 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.

  • PDF

Inclusion Complex of Analgesic and Antiinflammatory agents with Cyclodextrins (I): Enhancement of Dissolution of Ibuprofen by $2-Hydroxypropyl-{\beta}-cyclodextrin$ (시클로덱스트린과 소염진통제 간의 포접복합체에 관한 연구(I): 2-히드록시프로필-${\beta}$-시클로덱스트린에 의한 이부프로펜의 용출 증가)

  • Oh, In-Joon;Park, Jeong-Gyu;Lee, Yong-Bok;Shin, Sang-Chul
    • Journal of Pharmaceutical Investigation
    • /
    • v.23 no.1
    • /
    • pp.11-18
    • /
    • 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.

  • PDF

계면활성제/1-Hoxanol/물 혼합물의 상태도와 전기 전도도에 관한 연구

  • 오성근;김종득
    • Journal of the Society of Cosmetic Scientists of Korea
    • /
    • v.12 no.1
    • /
    • pp.34-61
    • /
    • 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.

  • PDF

States of Am in Aqueous Solution (수용액중의 Am의 상태)

  • Won Mok Jae
    • Nuclear Engineering and Technology
    • /
    • v.14 no.4
    • /
    • pp.172-177
    • /
    • 1982
  • The state of Am in the concentration of 10$^{-5}$M has been studied in the pH range of 5 to 10 by filtration and centrifugation method. By the experiments, we could estimate possible Am hydrolysis products and solubility constants. If the solubility of Am (OH)$_3$ estimated by Baes and Mesmer is increased about a factor of 10, i.e. changing logk=-l8.7 to logk=-17 5 it was found that the calculated curve of Am concentration versus pH agreed completely with experimental values.

  • PDF

The Effects of Solvent and Nonsolvent on Asymmetric Membrane Structure of 6FDA-p-TeMPD Polyimide (6FDA-p-TeMPD 폴리이미드 비대칭막 제조에서 용매와 비용매가 막구조에 미치는 영향)

  • 박노춘;김건중;남세종
    • Membrane Journal
    • /
    • v.8 no.3
    • /
    • pp.157-169
    • /
    • 1998
  • The effects of solvents (DMAc, NMP, 1,4-dioxane) and nonsolvents ($H_2O$, Methanol, n-hexane) on the morphology of 6FDA-p-TeMPD polyimide membrane, prepared by the wet phase inversion method, were studied. In the polymer/solvent/nonsolvent ternary system, the binodal curve, the coagulation value and the relative light transmission were measured, and the solubility parameter difference was calculated. The onset state and rate of liquid-liquid alemixing were predicted and the morphology of membrane was analyzed. It is found that the finger-like pores are formed within discontinuous polymer nodules when the binoclal curve is close to the polymer-solvent (P-S) axis, the coagulation value is small, the reduction of light transmission is easy to occur and the order of solubility parameter difference ($\Delta \delta_{i-j}$) is $\Delta \delta_{S-NS} > \Delta \delta_{P-NS} > \Delta \delta_{P-S}$. The dense skin with small nodules and the sponge type sublayer with macrovoid are formed in the case that the binodal curve is distant from the P-S axis, the onset time of liquid-liquid demixing is long and the order of $\Delta \delta_{i-j}$ is $\Delta \delta_{P-NS} >(\Delta \delta_{S-NS} < > \Delta \delta_{P-S})$. The thick layer of fine nodule coagulation and loosely grown sublayer of nodules appear when the binodal curve is distant from the P-S axis, the onset time of liquid-liquid demixing is very long and the order of $\Delta \delta_{i-j}$$\Delta \delta_{S-NS} > (\Delta \delta_{P-NS}$\lessgtr$ > (\Delta \delta_{P-NS} < >)\Delta \delta_{P-S}$ ).

  • PDF

Hydrothermal Synthesis of 6mol% Yttria Stabilized Cubic ZrO2 Nano Powders (이트리아 안정화 지르코니아 나노 분말 합성)

  • Lee, Jae-Hoon;Bae, Sung-Hwan
    • Korean Journal of Materials Research
    • /
    • v.27 no.8
    • /
    • pp.445-450
    • /
    • 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.

A Biopharmaceutical Study on Rifampicin-Polyvinylpyrrolidone Coprecipitate (Rifampicin-Polyvinylpyrrolidone 공침물에 관한 생물약제학적 연구)

  • 김영일
    • YAKHAK HOEJI
    • /
    • v.23 no.2
    • /
    • pp.81-94
    • /
    • 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.

  • PDF

Application of Edible Films to Food System Packaging (식품 포장재에 대한 가식성 필름의 응용성에 관한 연구)

  • Chun, Dong-Ho;Park, Jang-Woo
    • KOREAN JOURNAL OF PACKAGING SCIENCE & TECHNOLOGY
    • /
    • v.5 no.1
    • /
    • pp.6-12
    • /
    • 1999
  • This study was conducted to investigate the application of edible films to Raymyun soup packaging. The sorption isotherm curve and BET monolayer moisture content of Raymyun soup were estimated as a basic experiment. Also, the mechanical properties, water vapor permeability, and solubility of the films were investigated. Methylcellulose, sodium caseinate, and K-carrageenan films were used as edible films and glycerol and polyethylene glycol(MW 400) were used as plasticizers. In case tensile strength, methylcellulose films was 68.56 MPa and sodium caseinate film was 7.11 MPa. The elongations of sodium caseinate, methylcellulose, and K-carrageenan film were 115.41%, 23.79% and 0.60%, respectively. The water vapor permeabilties values of methylcellulose, sodium caseinate, and K-carrageenan film between 50% and 70% RH were $0.25-0.38ng{\cdot}m/m^2{\cdot}sec{\cdot}Pa,\;0.62-0.84ng{\cdot}m/m^2{\cdot}sec{\cdot}Pa\;and\;0.31-0.55ng{\cdot}m/m^2{\cdot}sec{\cdot}Pa$, respectively. For the solubility of films, sodium caseinate film showed the highest solubility and methylcellulose film showed the lowest solubility.

  • PDF