• Title/Summary/Keyword: water solubility

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DEVELOPMENT AND PHYSICOCHEMICAL CHARACTERIZATION OF PHASEINVERTED W/O MICROEMULSION CONTANING CYCLOSPORIN A.

  • Ryuu, Sang-A;Kim, Chong-Kook
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1996.04a
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    • pp.285-285
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    • 1996
  • Cyclosporin A (CyA) is widely used in the inhibition of graft rejection in organ transplantation. However, the bioavailability of CyA after oral administration is very low due to its poor solubility and dispersability hi water. To improve the solubility of CyA, microemulsion systems were developed and its physicochemical characteristics were evaluated by phase studies, solubility and dispersability tests. Phase studies on the systems composed of ethyl oleate (EO), PPG-20 methyl glucose ether (GP-20), poloxamer 123 (PL) and water U) were carried out to make stable w/o emulsions. Besides, based on CyA solubility test in various compositions of surfactant systems, a reasonable surfactant composition (GP-20/PL=4/1) was selected to enhance its solubility.

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Solubility and Physicochemical Stability of Ondansetron Hydrochloride in Various Vehicles (용제 중 염산온단세트론의 용해성 및 안정성)

  • Gwak, Hye-Sun;Oh, Ik-Sang;Chun, In-Koo
    • Journal of Pharmaceutical Investigation
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    • v.33 no.1
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    • pp.45-49
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    • 2003
  • The solubility and stability of ondansetron hydrochloride (OS) in various vehicles were determined. The effect of cyclodextrins (CD) on the solubility of OS in water was determined by equilibrium solubility method. The solubility of OS at $32^{\circ}C$ increased in the rank order of isopropyl myristate (IPM) < propylene glycol laurate (PGL) ${\ll}$ propylene glycol monolaurate < propylene glycol monocaprylate (PGMC) < poly(ethylene glycol) 400 < diethylene glycol mono ethyl ether (DGME) < ethanol < poly(ethylene glycol) 300 < water (36.1 mg/ml) ${\ll}$ propylene glycol (PG) (283 mg/ml). The addition of PG or DGME to non-aqueous vehicles such as IPM, PGL and PGMC markedly increased the solubility of OS. The addition of CDs in water increased the solubility. Apparent stability constant for the CD complexation with OS was calculated to be $25.5\;M^{-1}$ for $2-hydroxypropyl-{\beta}-CD\;(2HP{\beta}CD)$. Twenty mM ${\beta}-CD$, 69.4 mM sulfobutyl ether ${\beta}-CD$ and 115.4 mM $2HP{\beta}CD$ increased the aqueous solubilty of OS 1.27, 2.18 and 1.85 times, respectively. OS was stable in buffered aqueous solution (pH 5.0). However, OS was relatively unstable in non-aqueous vehicles in the order of PG

Influence of Extrusion on the Solubility of Defatted Soybean Flour in Enzymatic Hydrolysis

  • Cha, Jea-Yoon;Shin, Han-Seung;Cho, Yong-Jin;Kim, Chong-Tai;Kim, Chul-Jin
    • Food Science and Biotechnology
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    • v.16 no.4
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    • pp.543-548
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    • 2007
  • Low-energy processing technology, which enhances the utility of defatted soybean flour (DSF), was developed using extrusion processing. DSF was extruded at different conditions using a twin screw extruder and then, dried at $40^{\circ}C$ for 20 hr. The nitrogen solubility index (NSI), viscosity, water solubility index (WSI), and water absorption index (WAI) of DSF increased after extrusion processing. The density of DSF extrudates decreased with the decrease in water content from 53 to 33% and the increase in extrusion temperature from 110 to $160^{\circ}C$. The addition of NaOH from 1.2 to 1.8% and citric acid from 1 to 5% increased the total solubility (TS) of DSF due to the decrease of protein coiling and hydrophobic bonds formation during extrusion processing. When viscozyme was reacted first, TS, NSI, and soluble carbohydrate content of DSF hydrolysates increased about 12, 6, and 7%, respectively, compared to them reacted with protease first. The TS and NSI of DSF hydrolysates were increased about 15 and 10%, respectively, by extrusion processing at alkaline and acidic pH. Extrusion processing at alkaline and acidic pH contributed the increase of efficiency to hydrolyze DSF samples using enzyme.

Effects of Sulfobutyl Ether $\beta$-Cyclodextrin on Physicochemical Properties of Dexamethasone Dipropionate

  • Moon, Jee-Hyun;Oh, Ik-Sang;Chun, In-Koo
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1997.04a
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    • pp.116-116
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    • 1997
  • Complex formation of practically insoluble dexamethasone dipropionate (DDP) with ${\beta}$-cyclodextrin (${\beta}$-CD), dimethyl-${\beta}$-cyclodextrin (DMCD), trimethyl-${\beta}$-cyclodextrin (TMCD), 2-hydroxypropyl-${\beta}$-cyclodextrin (HPCD) and sulfobutyl ether ${\beta}$-cyclodextrin (SBCD) in water was investigated by solubility method at various temperatures. Water solubility of DDP was found to be 1.78 $\mu\textrm{g}$/$m\ell$ at 37$^{\circ}C$. Propylene glycol (PG)-water cosolvent increased the solubility of DDP, but the solubilization was not sufficient (8.93 $\mu\textrm{g}$/$m\ell$ in 20% PG). The addition of CD markedly increased the solubility of DDP in water, and A$\sub$L/ type phase solubility diagrams were obtained with ${\beta}$-CD, TMCD, HPCD and SBCD, where the apparent stability constants of the soluble complexes at 25$^{\circ}C$ were determined to be 1388, 216, 1054, and 1992 M$\^$-1/, respectively. However, DMCD remarkably increased the solubility of DDP, and showed an A$\sub$P/ type diagram, suggesting that DMCD forms a soluble complex of high order with DDP. The stability constant for the DDP-DMCD complex at 25$^{\circ}C$ was determined to be 19132 M$\^$-1/. The thermodynamic parameters were calculated for the inclusion complex formation in aqueous solution. CD (1${\times}$10$\^$-2/M) remarkably decreased the partition coefficients of DDP between isopropyl myristate/water in the order of TMCD < ${\beta}$-CD < HPCD < SBCD < DMCD, and in squalane/water system in the order of HPCD < TMCD < ${\beta}$-CD < DMCD < DMCD $\leq$ SBCD. This finding represents that, in a o/w type cream, cyclodextrin complexation with DDP may result in high concentration of DDP in aqueous phase. The permeation of DDP through a cellophane membrane was highly suppressed by the addition of CD, and the degree of suppression was different among CDs, indicating that CD may control the skin permeation of DDP. The dissolution rates of solid dispersions with CDs were much faster than those of drugs alone and corresponding physical mixtures. All DDP-CD solid dispersions exceeded the equilibrium solubility. Consequently these results suggest that complex formation of DDP with CDs may provide useful means to markedly enhance the solubility, and CDs are useful in the semi-solid preparations such as creams and gels for topical application.

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자화수에서 염류의 용해속도 변화와 자화수에 의한 NaCl, KCl 및 석고의 결정화 양상에 대한 연구

  • Jeon, Sang Il;Kim, Dong Ryul;Lee, Suk Keun
    • Journal of the Korean Chemical Society
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    • v.45 no.2
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    • pp.116-120
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    • 2001
  • In order to know the physicochemical properties of magnetized water, the experimental methods of column assay, crystalization of saltsand gypsom have been explored to elucidate the effects of magnetized water on the solubility speed of salts, crystal pattern from salt squeous solutions, and gypsom crystal pattern, respectively. In the column assay for salt solubility the magnetized water showed the decreased initial solubility speed of NaCl and slightly increased initial solubility spped of KCI, however, the maximum solugilities of NaCl and KCI in the magnetized aster were almost same in the double distilled water, respectively. The column assay also indicated that the magnetized water showed the decreased initial solubility speed of urea (CH$_4$N$_2$O), sodium citrate (HOC(CO$_2$Na)-(CH$_2$CO$_2$Na)$_2$-2H$_2$O) and (NH$_4$)$_2$compared to the double distilled water, while slightly increased solubility speed of glycine (NH$_2$CH$_2$COOH), boric acid (H$_3$BO$_3$), MgSO$_4$. Crystalization of 1% or 5% salt aqueous solutions by rapid evaporation disclosed that the magnetized water produced more condensed and bigger crystal structure than the control water. The pattern of gypsom crystal formation also indicated that the magntized water enhanced the crystal formation in the hydration reaction of gypsom plaster compared to the double distilled water. Taken together, it was presumed that the magnetized water showed the different physicochemical properties in the interaction with various salts, especially showed the contrast results between NaCl and KCI.

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Influences of Several Chemicals on the Solubility of Cocoon Sericin in Water (제사용수(製絲用水)에 대(對)한 몇가지 화학약제(化學藥劑)의 처리(處理)가 견층(繭層) Sericin의 용해성(溶解性)에 미치는 영향(影響))

  • Rhee, In Jeon;Lee, Dong Soo
    • Current Research on Agriculture and Life Sciences
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    • v.1
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    • pp.55-65
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    • 1983
  • The purpose of this study is to find out influences of several chemicals on the solubility of cocoon sericin in water, and there are several results of use to control the solubility of cocoon sericin in water. The results obtained are summarized as follows : The chemical which shows the strongest accelerating power of the solubility of cocoon sericin in water is Sodium Hydroxide (NaOH), the second is Potassium Hydroxide (KOH), the third is Sodium Silicate ($Na_2SiO_3$), and the weakest is Sodium Bicarbonate ($NaHCO_3$) in order among noticed silk-reeling accelerators. The chemical which shows the strongest inhibiting power of the solubility of cocoon sericin in water is Form Aldehyde (HCHO), the second is Ammonium Alum ($Al_2(SO_4)_2{\cdot}(NH_4)_2SO_4{\cdot}24H_2O$), the third is Acetic Acid ($CH_3COOH$), the weakest is Hydrochloric Acid(HCl) in order among noticed silk-reeling inhibitors. Particulary Hydrochloric Acid (HCl), which is expected to show strong inhibiting power of the solubility of cocoon sericin in water, shows accelerating power of the solubility of cocoon sericin at high temperature over 80 degrees of Celsius thermometer in water.

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Improvement of Dissolution Rate of Poorly Water Soluble Drug Using Self-microemulsifying Drug Delivery System (SMEDDS를 이용한 난용성 약물의 용출율 향상)

  • Kim, Kye-Hyun;Rhee, Yun-Seok;Bae, Joon-Ho;Chi, Sang-Cheol;Park, Eun-Seok
    • Journal of Pharmaceutical Investigation
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    • v.29 no.1
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    • pp.37-45
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    • 1999
  • ABSTRACT-A self-microemulsifying drug delivery system (SMEDDS) was developed to enhance the solubility and dissolution rate of poorly water soluble drug, biphenyl dimethyl dicarboxylate, DDB. The system was optimized by evaluating the solubility of DDB and the microemulsion existence range after the preparation of microemulsions with varying compositions of triacetin and surfactant-cosurfactant mixtures (Labrasol as surfactant (S) and the combination of Transcutol, Cremophor RH 40 and Plurol oleique as cosurfactant (CoS)). SMEDDS in this study markedly improved the solubility of DDB in water up to 10 mg/ml and the size of the o/w microemulsion droplets measured by dynamic light scattering showed a narrow monodisperse size distribution with an average diameter less than 50 nm. The microemulsion existing range is increased proportional to the ratio of S/CoS, however, it decreased remarkably as the oil content was more than 20%. In vitro dissolution study of SMEDDS showed a significantly increased dissolution rate of DDB in water (> 12 fold over DDB powder), and SMEDDS also had significantly greater permeability of DDB in Caco-2 cell compared to powders.

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Effects of Phosphate and Two-Stage Sous-Vide Cooking on Textural Properties of the Beef Semitendinosus

  • Nurul Nazirah Ruslan;John Yew Huat Tang;Nurul Huda;Mohammad Rashedi Ismail-Fitry;Ismail Ishamri
    • Food Science of Animal Resources
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    • v.43 no.3
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    • pp.491-501
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    • 2023
  • Comparing the effects of sodium tripolyphosphate (STPP) concentrations of 0.2% and 0.4% on beef semitendinosus is the objective of the current investigation. The samples were cooked at varied temperatures (45+60℃ and 45+70℃) and times (1.5+1.5 h and 3+3 h) using staged cooking. The colour properties, cooking loss, water retention, shear force, water-holding capacity, sarcoplasmic, and myofibrillar solubility, and total collagen were investigated. The cooking time and temperature affected the water-holding capacity, cooking loss, CIE L*, CIE a*, CIE b*, myofibrillar, and sarcoplasmic solubility, with lower temperature and short time having the lower detrimental effect. However, the significant effect can be intensified after the addition of STPP with higher water-holding capacity and tender meat obtained with 0.4% phosphate concentration at any cooking conditions. The STPP lowered the collagen content and increased the protein solubility of myofibrillar and sarcoplasmic, which this degradation is used as a good indicator of tenderness.

Fabrication and Evaluation of Powders Containing Calcium Silicate for Solid Self-emulsifying System of Oil (오일 성분의 고형 자가 유화 시스템을 위한 규산칼슘 함유 분말의 제조 및 평가)

  • Sung Giu, Jin
    • Journal of Powder Materials
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    • v.29 no.6
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    • pp.499-504
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    • 2022
  • The objective of this study is to assess the impact of spray drying conditions on medium-chain triglyceride (MCT) loading, solubility, and release of an MCT-loaded solid self-emulsifying system in a water-insoluble oily substance. MCT-loaded solid self-emulsifying systems are prepared by spray drying with SDS and calcium silicate. The effects of inlet temperature (60, 80, or 100℃) and feed solution composition (0, 10, 50, 90, or 100% ethanol) on physicochemical properties of MCT-loaded solid self-emulsifying systems are studied. The inlet temperature significantly affects the water solubility of MCT. Moreover, the feed solution composition significantly affects water solubility, release rate, and MCT loading. The MCT-loaded solid self-emulsifying system obtained at 60℃ using 90% ethanol feed solution shows the best physicochemical properties among the synthesized products and exhibits better water solubility (4.43 ± 0.44 vs. 0 ㎍/mL) and release (94.4 ± 1.6 vs. 32.8 ± 7.4%, 60 min) than a commercial product. Furthermore, the MCT-loaded solid self-emulsifying system shows an excellent emulsion droplet size (approximately 230 nm).

Strategy on the Development of Acetal$^{\circledR}$ Capsule Containing Poorly Water-soluble Aceclofenac

  • Lee, Beom-Jin
    • Proceedings of the PSK Conference
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    • 2003.10a
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    • pp.50-53
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    • 2003
  • Aceclofenac (AFC) as a model has poor solubility in water, resulting in lower dissolution rate and bioavailability. A solid dispersion (SD) is one of effective methods to enhance the solubility or dissolution rate of various poorly water-soluble drugs. Polyvinylpyrrolidone (PVP) that is a nontoxic, water-soluble and generally applicable pharmaceutical excipient has been widely used as a carrier in the preparation of solid dispersions. (omitted)

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