• Title/Summary/Keyword: Phase solubility

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Budesonide Microemulsions for Enhancing Solubility and Dissolution Rate

  • Piao, Hong-Mei;Cho, Hyun-Jong;Oh, Eui-Chaul;Chung, Suk-Jae;Shim, Chang-Koo;Kim, Dae-Duk
    • Journal of Pharmaceutical Investigation
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    • v.39 no.6
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    • pp.417-422
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    • 2009
  • Budesonide belongs to Class II in the Biopharmaceutics Classification System (BCS) for its high permeability and poor aqueous solubility. The purpose of this study was to improve the solubility and dissolution rate of budesonide using an o/w microemulsion system in order to develop a nasal formulation. Based on the results of the solubility study and pseudo ternary phase diagrams, microemulsions of about 80 nm in mean diameter were formulated using isopropyl myristate and Labrasol$^{(R)}$ as an oil phase and a surfactant, respectively. Solubility of budesonide in the microemulsions increased up to 6.50 mg/mL, which is high enough for a nasal formulation. In vitro release profiles of budesonide significantly increased from the microemulsions compared to that of the budesonide powder. These results suggest that the microemulsions of budesonide could further be developed into a clinically useful nasal formulation.

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
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    • v.18 no.1
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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.

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

  • 오성근;김종득
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.12 no.1
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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.

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Partitioning of Recombinant Human Interleukin-2 in a Poly(ethylene glycol)-Dextran Aqueous Two-Phase System

  • Lee, In-Young;Lee, Sun-Bok
    • Journal of Microbiology and Biotechnology
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    • v.2 no.2
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    • pp.135-140
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    • 1992
  • The partitioning of recombinant human interleukin-2(rhII-2) in PEG 8000-dextran 38800 aqueous two-phase system has been investigated using three different sources of rhIL-2. In the case of pure rhIL-2, the solubility in a PEG-dextran two-phase system was low and most of rhIL-2 was partitioned into the bottom phase. For the recovery of rhIL-2 from insoluble protein aggregates, the inclusion bodies of recombinant E. coli were solubilized by the treatment with sodium dodecyl sulfate (SDS). The addition of SDS significantly enhanced not only the solubility of rhIL-2 but also the partitioning of rhIL-2 to the top phase. When the ratio of SDS to rhIL-2 was 2.0, the partition coefficient(K) and the recovery yield(Y) at the top phase were 4.5 and 88%, respectively, at pH 6.8. In order to reduce the recovery steps further, SDS was directly added to the intact recombinant E. coli cells and then partitioned into the PEG/dextran aqueous two-phase system. The observed partition coefficient ($K{\cong{3.0$) and recovery yield ($Y{\geq}80%$ )of this method were comparable to the rhIL-2 recovery from insoluble protein aggregates. The results obtained in this work indicate that PEG-dextran two-phase partitioning might provide a simple way for the recovery and partial purification of recombinant proteins which are produced as inclusion bodies.

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Effect of Cyclodextrins on the Solubility and Stability of Aspalatone in Aqueous Solutions (수용액중 시클로덱스트린류가 아스팔라톤의 용해성과 안정성에 미치는 영향)

  • Gwak, Hye-Sun;Chun, In-Koo
    • Journal of Pharmaceutical Investigation
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    • v.30 no.4
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    • pp.267-271
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    • 2000
  • The effect of cyclodextrins on the solubility and stability of aspalatone (acetylsalicylic acid maltol ester, AM, CAS 147249-33-0), which has been recently found to have an antithrombotic effect, was investigated. The addition of ${\beta}-cyclodextrin\;({\beta}-CD),\;dimethyl-{\beta}-cyclodextrin\;(DMCD)\;or\;2-hydroxypropyl-{\beta}-cyclodextrin\;(HPCD)$ to the aqueous solution increased the solubility of AM concentration-dependently. From the phase solubility diagram, stability constants for $AM-{\beta}-CD$, -DMCD or -HPCD complexes were calculated to be 43.1, 78.3 and $53.0\;M^{-1}$. The addition of ${\beta}-CD$, DMCD or HPCD to AM solution retarded the degradation rate of AM in the acidic region. However, ${\beta}-CD$ and HPCD rather acted as an accelerator of degradation in the neutral and alkaline regions. DMCD had a stabilizing effect at all pHs studied.

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A study on phase transition of Hydrogel: (II)Solubility of N-Isopropylacrylamide Gel (수화겔의 상전이에 관한 연구 : (II)폴리(N-이소프로필아크릴아미드)겔의 용해도)

  • Park, Sang-Bo;Hwa, Won-Jo
    • Journal of the Korean Graphic Arts Communication Society
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    • v.21 no.1
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    • pp.81-90
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    • 2003
  • To understand the thermoresponsive volume phase transition of an N-isopropyl acrylamide(NIPA) gel on water, the solubility parameter of neutral NIPA gel was determined by swelling the gel with various solvents. Water was found not to be a good solvent for NIPA gel. Equilibrium swelling curves of NIPA gel were respectively obtained by immersing in pure water, ethanol, n-propanol and some mixed solvents. On adding a small amount of alcohols to water, volume phase transition of NIPA gel in water was changed. Phase transition temperature of this gel was decreased with the increase of the carbon number of alcohol.

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Superconducting Properties of Ge Substitution for the Bi Site in the 2212 Phase of Bi-Sr-Ca-Cu-O Superconductors (Bi계 산화물 초전도체 2212상에 있어서 Bi 자리에 Ge 치환에 따른 초전도 특성)

  • 신재수;이민수;최봉수;송승용;송기영
    • Journal of the Korean Ceramic Society
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    • v.37 no.8
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    • pp.787-791
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    • 2000
  • Samples with the nominal composition, Bi2-xGexSr2CaCu2O8+$\delta$ (x=0, 0.1, 0.2, 0.3, 0.4, 0.5) were prepared by the solid-state reaction method. We have studied the effect of substitution Ge for Bi and investigated the superconducting properties by changing oxygen content with Ge substitution. It was found that temperature difference, ΔK, between TCon and TCzero was considerably smaller in the samples prepared by the intermediate pressing method than that in the samples by the solid-state reaction method. We found the solubility limit of Ge to the 80 K single phase was around x=0.3. Within the solubility limit, lattice constant c decreased with the increase of x. In the region of the 80K single phase, the onset critical temperature TCon increased and excess oxygen content decreased with increase of x.

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Solvent Induced Crystallization of Polycarbonate in Mixed Solvent (혼합용매에 의한 Polycarbonate의 결정화)

  • 황덕근;이창엽;설용건
    • Polymer(Korea)
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    • v.25 no.6
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    • pp.811-817
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    • 2001
  • Crystallization behaviour of bisphenol A polycarbonate(PC) from amorphous phase was studied by varing solvent/nonsolvent ratios in liquid phase. Chloroform and isopropanol were used as a solvent and a nonsolvent, respectively. Samples were characterized by optical microphotography, scanning electron microscope (SEM), X-ray diffaction (XRD), and differential scanning calorimeter (DSC). DSC and XRD measurement were used to determine the crystallinity of PC. The solubility constant seems to critical to control the PC crystallinity in solvent/nonsolvent mixture. The difference in PC crystallinity is explained by the difference in solubility constant of the mixture depending on the solvent/nonsolvent ratio. PC solution of 75/25 wt% (solvent/nonsolvent) ratio produced PC powder showing maximum crystallinity. At this condition solubility constant (9.85) of the mixed solvent was close to PC (9.9).

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Solubility of Mixed Lanthanide Hydroxide and Oxide Solid Solutions

  • Moniruzzaman, Mohammad;Kobayashi, Taishi;Sasaki, Takayuki
    • Journal of Nuclear Fuel Cycle and Waste Technology(JNFCWT)
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    • v.19 no.3
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    • pp.353-366
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    • 2021
  • The solubilities of different multicomponent lanthanide oxide (Ln2O3) solid solutions including binary (Ln1 and Ln2 = La, Nd, Eu, or Tm), ternary (Ln1, Ln2, and Ln3 = La, Nd, Eu, or Tm), and higher systems (Ln = La, Ce, Pr, Nd, Sm, Eu, Gd, Tb, Dy, Ho, Er, Tm, Yb, and Lu) were studied after aging for four weeks at 60℃. Our recent study revealed that the phase transformations in binary ((La, Nd) and (La, Eu)) and ternary (La, Nd, Eu) systems are responsible for the formation of (La, Nd)(OH)3, (La, Eu)(OH)3, and (La, Nd, Eu)(OH)3 solid solutions, respectively. The variations in the mole fractions of La3+, Nd3+, and Eu3+ in the sample solutions of these hydroxide solid solutions indicated that a thermodynamic equilibrium might account for the apparent La, Nd, and Eu solubilities. Conversely, the binary and ternary systems containing Tm2O3 as the heavy lanthanide oxide retained the oxide-based solid solutions, and their solubility behaviors were dominated by their congruent dissolutions. In the higher multicomponent system, the X-ray diffraction patterns of the solid phases, before and after contact with the aqueous phase indicated the formation of a stable oxide solid solution and their solubility behavior was explained by its congruent dissolution.

Evaluation of Americium Solubility in Synthesized Groundwater: Geochemical Modeling and Experimental Study at Over-Saturation Conditions

  • Hee-Kyung Kim;Hye-Ryun Cho
    • Journal of Nuclear Fuel Cycle and Waste Technology(JNFCWT)
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    • v.20 no.4
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    • pp.399-410
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    • 2022
  • The solubility and species distribution of radionuclides in groundwater are essential data for the safety assessment of deep underground spent nuclear fuel (SNF) disposal systems. Americium is a major radionuclide responsible for the long-term radiotoxicity of SNF. In this study, the solubility of americium compounds was evaluated in synthetic groundwater (SynDB3), simulating groundwater from the DB3 site of the KAERI Underground Research Tunnel. Geochemical modeling was performed using the ThermoChimie_11a thermochemical database. Concentration of dissolved Am(III) in Syn-DB3 in the pH range of 6.4-10.5 was experimentally measured under over-saturation conditions by liquid scintillation counting over 70 d. The absorption spectra recorded for the same period suggest that Am(III) colloidal particles formed initially followed by rapid precipitation within 2 d. In the pH range of 7.5-10.5, the concentration of dissolved Am(III) converged to approximately 2×10-7 M over 70 d, which is comparable to that of the amorphous AmCO3OH(am) according to the modeling results. As the samples were aged for 70 d, a slow equilibrium process occurred between the solid and solution phases. There was no indication of transformation of the amorphous phase into the crystalline phase during the observation period.