• Biomolecules & Therapeutics
• /
• v.8 no.4
• /
• pp.332-337
• /
• 2000

Physicochemical properties of aspalatone (acetylsalicylic acid maltol ester, AM), which has been recently found to have an antithrombotic effect, were studied in terms of solubility, dissolution, partition coefficient (Pc) and stability. The solubility of AM at 37$^{\circ}C$ was about 1.2 mg/ml and the P$_{c}$ value for n-octanol/water and chloroform/water was 11.4 and 382.6, respectively. Dissolution rates of AM at pH 1.2 and 6.8 were more than 80% within 30 min. The degradation of AM followed apparent first-order kinetics, and was dependent on temperature, pH and ionic strength. From the pH-rate profile, the optimal pH was found to be at around 4.0. Half-lives at pH 1.2 and 6.8 were 33.5 and 44.4 hr, respectively. The degradation rate of AM at pH 1.2 was somewhat faster than that of aspirin, but at pH 7.0, the degradation rate of AM was slower than that of aspirin.n.

• Carbon letters
• /
• v.10 no.3
• /
• pp.208-212
• /
• 2009

Alginate-chitosan blend containing coconut-based activated carbon was prepared as a drug delivery carrier in order to improve the loading and releasing capacity of the drug. The activated carbon was incorporated as effective adsorbent for drug due to the extremely high surface area and pore volume, high adsorption capacity, micro porous structure and specific surface activity. Alginate-chitosan blend containing coconut-based activated carbon showed the sustained release for a longer period. Alginate-chitosan blend showed higher release of drug as the pH increased and higher release of drug as the content of chitosan decreased due to the pH-dependent solubility of blend components.

• YAKHAK HOEJI
• /
• v.46 no.3
• /
• pp.168-173
• /
• 2002

The physicochemical properties of aloesin, which has been recently found to reduce renal toxicity induced by cis-platin, were studied including solubility, partition coefficient ( $P_{c}$ ), osmolality, and stability. The solubility of aloesin was about 500 mg/mι, and the $P_{c}$ value for n-octanol/water was 1.01 $\pm$ 0.03. The degradation of aloesin followed the pseudo-first-order kinetics and was dependent on temperature, pH and ionic strength. From the pH-rate profile, the optimal pH was found to be 2.0~3.0. Some metal ions increased the degradation rate in the rank order of M $n^{2+}$ ＞ F $e^{3+}$ ＞ C $u^{2+}$ ＞ F $e^{2+}$. On the other hand, other metal ions such as B $i^{3+}$, $Ba^{2+}$, Z $n^{2+}$, N $i^{2+}$, $Co^{2+}$ and $Mg^{2+}$ did not show the unfavorable effects. After autoclaving, aloesin contents remaining were 81.8~98.8% of initial concentrations depending on pH. The most stable pH was 3.98 in the autoclaving. Osmolality increased linearly as concentration increased.sed.creased.sed.

• Bulletin of the Korean Chemical Society
• /
• v.17 no.10
• /
• pp.925-929
• /
• 1996

Uranyl hydrolysis precipitates were obtained by increasing pH value of aqueous uranyl solution in the range of neutral to alkaline pH value and their phase transformation during the solubility experiment under various conditions has been examined. The precipitates formed in the hydrolysis reaction of uranyl ion had a layered structure such as a meta-schoepite phase, a schoepite structure, or a mixed phase of meta-schoepite and schoepite. Phase transformation between them was strongly dependent on the pH value at which the precipitate was formed. The distance between the layers in meta-schoepite or schoepite phase was ∼7.35 Å, and it was increased with the pH value at which the precipitate was synthesized as well as the pH values of the aqueous solution. The phase transformation from a meta-schoepite to schoepite was fast for the precipitates formed at low pH values, however, it was not the case for the precipitates formed at high pH values. A small difference of pH value in aqueous solution gave a great change on its solubilities near pH 9.7, because a layered structure of the precipitates became amorphous above that pH value. Greater solubility for the precipitate formed at higher pH value can be explained from the fact that the precipitates formed at low pH value had a better crystallinity and also that the precipitates formed at higher pH value has a slower rate of crystallization.

• YAKHAK HOEJI
• /
• v.28 no.3
• /
• pp.161-167
• /
• 1984

To improve the solubility properties of indomethacin, a poorly water-soluble drug, some attempts were made with surfactants, such as sodium deoxycholate, sodium laurylsulfate and polysorbate-80. The enhancement effect in solubility was found to be due to the micellar solubilization and dependent on the concentration of surfactants, pH and temperature. The mechanism of interaction was suggested to be attributed to the formation of mixed micelles between the drug and solubilizers.

• Biotechnology and Bioprocess Engineering:BBE
• /
• v.11 no.4
• /
• pp.299-305
• /
• 2006

Aromatic L-amino acid transaminase is an enzyme that is able to transfer the amino group from L-glutamate to unnatural aromatic ${\alpha}-keto$ acids to generate ${\alpha}-ketoglutarate$ and unnatural aromatic L-amino acids, respectively. Enrichment culture was used to isolate thermophilic Bacillus sp. T30 expressing this enzyme for use in the synthesis of unnatural L-amino acids. The asymmetric syntheses of L-homophenylalanine and L-phenylglycine resulted in conversion yields of >95% and >93% from 150 mM 2-oxo-4-phenylbutyrate and phenylglyoxylate, respectively, using L-glutamate as an amino donor at $60^{\circ}C$. Synthesized L-homophenylalanine and L-phenylglycine were optically pure (>99% enantiomeric excess) and continuously pre-cipitated in the reaction solution due to their low solubility at the given reaction pH. While the solubility of the ${\alpha}-keto$ acid substrates is dependent on temperature, the solubility of the unnatural L-amino acid products is dependent on the reaction pH. As the solubility difference between substrate and product at the given reaction pH is therefore larger at higher temperature, the thermophilic transaminase was successfully used to shift the reaction equilibrium toward rapid product formation.

• KSBB Journal
• /
• v.31 no.4
• /
• pp.219-227
• /
• 2016

Valsartan, a drug for the treatment of cardiovascular disease, exhibited low bioavailability which was caused by, at least in part, limited solubility at low pH. Present investigation deals with the preparation and characterization of gastro-retentive drug delivery system (GRDDS) using valsartan solid dispersion. We prepared solid dispersion using surfactants (Poloxamer 407) and alkalizer ($Na_2CO_3$) which may to be useful for improving solubility of valsartan at low pH and evaluated by saturated solubility of valsartan in distilled water. Valsartan gastro-retentive (GR) tablets containing solid dispersion prepared and evaluated by weight variation, floating time and dissolution rate. Compression at lower pressures resulted in the tablets floating over simulated gastric fluid (pH 1.2) for more than 17 h. In vitro release of valsartan from GR tablet was dependent on the amount of poloxamer 407 and hydroxypropyl methylcellulose. On the basis of evaluation parameter, formulation E-3 was selected as a final formulation. Therefore, it can be concluded that the GR tablets containing solid dispersion may be exploited successfully for the delivery of poorly drug such as valsartan.

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.35 no.10
• /
• pp.1394-1398
• /
• 2006

Functionalities of drum-dried fish muscle protein from pH shifting process have been investigated by determining solubility, emulsion activity, rehydration, fat-adsorption capacity, viscosity, and color. Solubility was higher in recovered protein at pH 7.0 than that at pH 5.5, and not dependent on ionic strength. Solubility of the dried protein recovered at pH 7.0 depended on pH of solvent, and lowest in the range of pH 3 to pH 6. The dried protein showed relatively low emulsion capacity in all the samples. Emulsion stability, foam capacity and foam stability were not observed in the samples. Viscosity was in the range of $50,200\sim39,000cP$. Rehydration and fat-binding capacities were $2.63\sim2.89g$-water/g and $2.13\sim2.17g$-oil/g, respectively, and not dependent on particle size and pH. Drum-dried fish muscle protein has a potential application as an ingredient of meat patty products.

• Journal of Pharmaceutical Investigation
• /
• v.35 no.6
• /
• pp.453-460
• /
• 2005

4-Aminopyridine (AP) is a potassium channel blocker used in the treatment of neurological disorders such as multiple sclerosis and Alzheimer disease. AP‘s window of therapeutic effect appears to correlate with its plasma halflife (3.5 hours). It demonstrates pH-dependent solubility because of a weakly basic drug. In addition, the resulting release from conventional matrix tablets decreases with increasing pH-milieu of the gastrointestinal tract. The aim of this study is to design sustained release matrix tablet containing AP, overcoming this problem. $Eudragit^{\circledR}$ L 100 (EuL) and sodium alginate were used in an effort to achieve pH independent drug release. The effect of sodium alginate and EuL on drug release from matrix tablet was investigated. The drug release behavior from the different tablets was analyzed by $t_{20%},\;t_{40%},\;t_{60%}$, The exponential diffusion coefficient n, kinetic constant K were calculated according to the Korsmeyer-Peppas equation. The drug release from matrix tablets prepared with sodium alginate was decreased with increasing the content of sodium alginate in pH 7.4 while there is no significant difference in pH 1.2. The exponent n values were determined to be approximately 0.5 and 0.8 respectively, in both pH 1.2 and 7.4. These values indicate diffusion-based anomalous mechanism and erosion-based anomalous mechanism, respectively. The drug release from sodium alginate matrix tablets prepared with solid dispersion of EuL containing drug showed a slow drug release in an acidic medium and a more fast drug release in phosphate medium, compared with sodium alginate matrix tablets prepared with physical mixture. These results may be attributed to the gel forming ability of sodium alginate and pH dependent solubility of EuL. Therefore, sustained-release AP matrix tablets using sodium alginate and EuL were successfully prepared.

• Nuclear Engineering and Technology
• /
• v.29 no.2
• /
• pp.127-137
• /
• 1997

Equilibrium concentrations of major elements in an underground repository with a capacity of 100,000 drums have been simulated using the geochemical computer code (EQMOD). The simulation has been carried out at the conditions of pH 12 to 13.5, and Eh 520 and -520 mV. Solubilities of magnesium and calcium decrease with the increase of pH. The solubility of iron increases with pH at Eh -520 mV of reducing environment while it almost entirely exists as the precipitate of Fe(OH)$_3$(s) at Eh 520 mV of oxidizing environment. All of cobalt and nickel are predicted to be dissolved in the liquid phase regardless of pH since the solubility limit is greater than the total concentration. In the case of cesium and strontium, all forms of both ions are present in the liquid phase because they have negligible sorption capacity on cement and large solubility under disposal atmosphere. And thus the total concentration determines the equilibrium concentration. Adsorbed amount of iodide and carbonate are dependent on adsorption capacity and adsorption equilibrium constant. Especially, the calcite turns out to be a solubility-limiting phase on the carbonate system. In order to validate the model, the equilibrium concentrations measured for a number of systems which consist of iron, cement, synthetic groundwater and radionuclides are compared with those predicted by the model. The concentrations between the model and the experiment of nonadsorptive elements cesium, strontium, cobalt nickel and iron, are well agreed. It indicates that the assumptions and the thermodynamic data in this work are valid. Using the adsorption equilibrium constant as a free parameter, the experimental data of iodide and carbonate have been fitted to the model. The model is in a good agreement with the experimental data of the iodide system.