• Title/Summary/Keyword: P solubility

Search Result 939, Processing Time 0.029 seconds

Pharmaceutical Study on Clonixin Argininate (Clonixin Argininate의 약제학적 연구)

  • Jee, Ung-Kil;La, Sung-Bum
    • Journal of Pharmaceutical Investigation
    • /
    • v.16 no.2
    • /
    • pp.43-54
    • /
    • 1986
  • To increase the bioavailability of clonixin, clonixin argininate was prepared and compared with clonixin by determining solubility, pKa, lipid-water partition coefficient, dissolution rate and in vivo tests. The results are summerized as followings; 1) The solubility of clonixin argininate was increased by 20 times in water, about 1.2 times in pH 1.2 and pH 8.0 buffer solution, and about 1.8 times in pH 6.8 buffer solution compared with that of clonixin. 2) pKa values of clonixin, clonixin lysinate and clonixin argininate were 6.32, 7.20 and 7.45, respectively. 3) The lipid-water partition coefficient of clonixin argininate was increased more than that of the clonixin in n-hexane, carbon tetrachloride, chloroform, methylene chloride, and n-butanol, but the partition coefficient of clonixin was increased more than that of clonixin argininate in benzene/pH 1.2 buffer solution, ether/pH 8.0 buffer solution, and 3-methylbutyl acetate/pH 1.2, pH 8.0 buffer solution. 4) The time required to dissolve 60% $(T_{60%},\;min.)$ of clonixin argininate was about 1.5 min. in water and pH 1.2 buffer solution, and about 5 min. in pH 6.8 buffer solution. $T_{60%}$ of clonixin lysinate was about 1.5 min. in water, about 1.8 min. in pH 6.8 buffer solution, and about 8 min. in pH 1.2 buffer solution. But $T_{60%}$ of clonixin was about 96 min. in pH 6.8 buffer solution, over 2 hours in water and pH 1.2 buffer solution. 5) Anti-inflammatory effect of clonixin argininate was increased more than that of clonixin over 6 hours, and that of clonixin lysinate was followed by lapse of time. 6) Analgesic effect of clonixin argininate was increased by 1.5 times more than that of clonixin and the effect of clonixin argininate was nearly identical with that of clonixin lysinate. 7) The absorption rates (Ka) of clonixin, clonixin lysinate and clonixin argininate were $0.169\;hr^{-1},\;0.652\;hr^{-1}$ and $0.723\;hr^{-1}$ in situ, respectively.

  • PDF

Development of Pharmaceutical Dosage Form with New Sibutramine Salt (시부트라민 신규염을 이용한 새로운 시부트라민 제제의 개발)

  • Moon, Jin-Wook;Shin, Teak-Hwan;Lee, Dong-Wook;Cho, Jun-Young;Chang, Sung-Ju;Hwang, Sung-Joo
    • Journal of Pharmaceutical Investigation
    • /
    • v.40 no.1
    • /
    • pp.15-21
    • /
    • 2010
  • Sibutramine is an orally administered centrally-acting antiobesity agent and inhibits both noradrenaline(norephinephirine) and serotonin(5-HT) reuptake. These effects are contributed by its active metabolites, M1 and M2. However, as the free base form of sibutramine is an oil form in room temperature, it had the problem of handling and stability. Thus, this drug should be used in the form of acid salt form in the pharmaceutical application. Unfortunately, anhydrous sibutramine hydrochloride is highly hygroscopic and unstable. In order to solve the hygroscopicity of the anhydrous salt form, another sibutramine acid salt form must be developed as a hydrate form. In this study. to overcome these problems, various of sibutramine acid salt forms were prepared with the pharmaceutically available salts such as maleate, esylate, mandelate, camsylate, besylate, salicylate, tartrate, isethionate and malate forms, and their physicochemical properties were investigated. Sibutramine malate was selected for excellent solubility and stability among the listed salt forms above. Its pharmacokinetic parameters were evaluated in rats comparing with sibutramine HCl, resulting in similar parameters. In vitro dissolution study of sibutramine malate-loaded capsule was performed comparison with commercial product ($Reductil^{(R)}$) in pH 1.2, pH 4.0, pH 6.8 and water medium. Our results indicated that there were no significant differences in their dissolution profiles were similar in all tested medium. Thus, sibutramine malate-loaded capsule should be a potential candiate due to its excellent solubility, good stability and biosimilar absorption.

Marination and Physicochemical Characteristics of Vacuum-aged Duck Breast Meat

  • Khan, Muhammad Issa;Lee, Hyun Jung;Kim, Hyun-Joo;Young, Hae In;Lee, Haelim;Jo, Cheorun
    • Asian-Australasian Journal of Animal Sciences
    • /
    • v.29 no.11
    • /
    • pp.1639-1645
    • /
    • 2016
  • We investigated marinade absorption and physicochemical characteristics of vacuum-aged duck breasts that were halved and individually vacuum-packed for chiller aging at $4^{\circ}C$ for 14 d. One half was marinated for 0, 7, or 14 d, while the second half was used as a control. Marinade absorption, cooking loss, cooking yield, texture profile, pH, color, protein solubility, and thiobarbituric acid reactive substances (TBARS) values were evaluated, and protein sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) was performed. Marinade absorption and pH did not vary significantly after 14 d of aging. Marination increased the pH, color ($a^*$ and $b^*$) values, and cooking yield and reduced cooking loss. TBARS values significantly increased with aging time, but were significantly reduced by marination. Myofibril and total protein solubility increased with aging and marination, while SDS-PAGE showed protein degradation. Hence, aging and marination can be used simultaneously to improve physicochemical quality and cooking yield of vacuum-aged duck breast.

Properties of Calcium Lactate Prepared from Calcined Littleneck Clam Ruditapes philippinarum Shell Powder (바지락(Ruditapes philippinarum) 패각 소성분말로 제조한 젖산칼슘의 특성)

  • Lee, Gyoon-Woo;Yoon, In Seong;Lee, Hyun Ji;Lee, Jung Suck;Kim, Jin-Soo;Heu, Min Soo
    • Korean Journal of Fisheries and Aquatic Sciences
    • /
    • v.49 no.4
    • /
    • pp.436-444
    • /
    • 2016
  • Clamshells, which comprise more than 50% of a clam’s weight, are a major byproduct of the clam industry and are mainly composed of insoluble calcium carbonate. This study investigates the use of clamshells as a natural calcium resource. Highly soluble powdered calcium lactate (LCCL) was prepared from the calcined powdered shells of littleneck clams (LCCP) using response surface methodology (RSM) to predict optimum conditions. These conditions, as derived from pH, solubility, and yield of 11 LCCLs manufactured according to the RSM model, were 1.80 M lactic acid and 1.13 M LCCP. The actual values of pH (6.98), solubility (93.99%), and yield (351.23%) under the optimized conditions were as predicted. The derived LCCL exhibited a strong buffering capacity in the range of pH 2.78-3.90 when combined with less than 2 mL of 1 N HCl. The ranges of calcium content and solubility of LCCL were 7.7-17.5 g/100 g and 96.6-98.9%, respectively. Fourier transform infrared spectroscopy (FT-IR) of the LCCL identified it as calcium lactate pentahydrate, and field emission scanning electron microscopy (FESEM) revealed an irregular and rod-like microstructure. These results confirm the potential use of clamshells, converted to highly soluble organic acid calcium, as an additive to enhance calcium content in food ingredients.

Effects of Emulsion Mapping in Different Parts of Pork and Beef (우육 및 돈육 부위에 따라 고기 유화물의 유화맵에 미치는 영향)

  • Choi, Yun-Sang;Jeong, Tae-Jun;Hwang, Ko-Eun;Kim, Hyun-Wook;Kim, Cheon-Jei;Sung, Jung-Min;Oh, Nam-Su;Kim, Young-Boong
    • Korean journal of food and cookery science
    • /
    • v.31 no.3
    • /
    • pp.241-247
    • /
    • 2015
  • This study was conducted in order to evaluate emulsion mapping between emulsion stability and moisture content, cooking yield, hardness, protein solubility, apparent viscosity, and overall acceptability of pork or beef emulsion batters. The pork and beef emulsion batters were added to different parts of the meat. The formulations indicating low emulsion stability and high cooking yield were T1 (pork shoulder), T2 (pork ham), and T5 (beef tenderloin) treatments. Low stability, low hardness and protein solubility were also T1 (pork shoulder), T2 (pork ham), and T5 (beef tenderloin) treatments. The Pearson's correlation coefficients show that emulsion stability is negatively correlated with cooking yield (p<0.05), with a value of -0.90, and positively correlated with hardness (p<0.05), and protein solubility (p<0.01) with values of 0.65 and 0.59, respectively. This approach has been found to be particularly useful for highlighting differences among the emulsified properties in emulsion meat products. Therefore, the results obtained with emulsion mapping are useful in the making of new emulsified meat products of the desired quality.

Preparation and Stability Evaluation of Docetaxel-Loaded Oral Liposome

  • Chon, Chong-Run;Kim, Hyun-Mi;Lee, Pung-Sok;Oh, Eui-Chaul;Lee, Ma-Se
    • Journal of Pharmaceutical Investigation
    • /
    • v.40 no.2
    • /
    • pp.85-90
    • /
    • 2010
  • Docetaxel-loaded liposomes were prepared by emulsion-solvent evaporation method, then coated with chitosan at room temperature and lyophilized. This system was designed in order to improve solubility and stability of docetaxel in the GI tract for oral drug delivery. The solubilizing effect of some frequently used solubilizers and/or liposome was determined. Among the results docetaxel-loaded liposomes prepared with 0.5% TPGS as a solubilizer showed 100-fold higher solubility than docetaxel. In a stability test, mean particle size of different liposome formulations was measured by a particle size analyzer in simulated gastric fluid (SGF) and in simulated intestinal fluid (SIF). The particle size of uncoated liposomes was significantly increased compared with that of chitosan-coated liposomes in SGF, however, there was no significant difference between coated and uncoated liposome in SIF. It is evident that chitosan-coated liposomes were more stable in GI conditions. The release characteristics of docetaxel-loaded liposomes were also investigated in three buffer solutions (pH 1.2, 4.0, 6.8). Docetaxel release did not occur in pH 1.2 for 4 hrs. However, in pH 4.0 and 6.8 conditions, docetaxel was gradually released over 24 hrs as a sustained release. It seems that aggregation and precipitation of particles by electrostatic interaction might protect docetaxel from being released. In Conclusion, the results from this study show that the chitosan-coated liposomes may be useful in enhancing solubility and GI stability of docetaxel.

Studies on the Functional Properties of Modified Soy Protein Isolate (변형대두 단백질의 기능 특성에 관한 연구)

  • Kim, Young-Sug;Hwang, Jae-Kwan;Cho, Eun-Kyung;Lee, Shin-Young;Pyun, Yu-Ryang
    • Korean Journal of Food Science and Technology
    • /
    • v.17 no.5
    • /
    • pp.383-388
    • /
    • 1985
  • Soy protein isolate was acylated with succinic anhydride and acetic anhydride. The functional properties are markedly improved by acylation of the $\varepsilon$-amino groups. Acylation of the available amino groups shifted the isoelectric point from 4.5 to 4.0 and enhanced the solubility between pH 4.0-6.0. In the 0.03M-$CaCl_2$ solution the solubility of the modified soy protein is much larger than that of the unmodified protein above the isoelectric point. The emulsion properties and foaming properties also improved by the modification and the effects of pH on the properties paralleled its effect on protein solubility. The changes of reduced viscosity with concentration followed Huggin's equation and by modification the intrinsic viscosity of the soy protein increased and the interaction coefficient decreased.

  • PDF

Hyperaccumulation mechanism in plants and the effects of roots on rhizosphere soil chemistry - A critical review (고축적식물의 중금속 흡수기작과 뿌리에 의한 근권 토양의 화학변화 - 총설)

  • Kim, Kwon-Rae;Owens, Gary;Naidu, Ravi;Kim, Kye-Hoon
    • Korean Journal of Soil Science and Fertilizer
    • /
    • v.40 no.4
    • /
    • pp.280-291
    • /
    • 2007
  • Much research has been conducted in the field of phytoremediation since the discovery of the range of plants known as hyperaccumulators. Research has focused simultaneously on elucidating the mechanism of metal(loid) accumulation and development of practical techniques to enhance accumulation efficiency. To date, it is generally understood that there are five specific mechanisms employed by hyperaccumulating plant species that are either not or under utilized by non-hyperaccumulators. These include 1) enhanced metal(loid)s uptake through the root cell, 2) enhanced translocation in plant tissue, 3) detoxification and sequestration, 4) enhanced metal availability in soil:root interface, and 5) active root foraging toward metal(loid) enriched soils. Among these mechanisms, understanding of the plant-root effect on metal(loid) dynamics and subsequent plant uptake is vital to overcome the inherit limitation of phytoremediation caused by low metal(loid) solubility in soils. Plant roots can influence the soil chemistry in the rhizosphere through changes in pH and exudation of organic compounds such as low-molecular-weight organic acids (LMWOAs) which consequently change metal(loid) solubility. The decrease in soil pH by plant release of $H^+$ results in increased metal solubility. Elevated levels of organic compounds in response to high metal soil concentrations by plant exudation may also increases metal concentration in soil solution through formation of organometallic complexes.

Study on the Stability of Biotin-containing Nano-liposome (바이오틴 함유 나노리포좀의 안정성에 관한 연구)

  • Yang, Seong Jun;Kim, Tae Yang;Lee, Chun Mong;Lee, Kwang Sik;Yoon, Kyung-Sup
    • Journal of the Society of Cosmetic Scientists of Korea
    • /
    • v.46 no.2
    • /
    • pp.133-145
    • /
    • 2020
  • This study utilized nano-liposomes for the purpose of stabilizing and increasing the solubility of biotin, a water-soluble active material with low solubility. The particle size, zeta potential, and polydispersity index were confirmed with a nano zetasizer. It was possible to manufacture nano liposomes at 100 to 250 nm of particle size and -80 to -30 mV of zeta potential. Dialysis membrane method (DMM) was used to measure the capsulation efficiency of biotin in biotin nano-liposomes, and results showed that pH increased biotin nano-liposomes had higher capsulation efficiency than normal biotin nano-liposome. Through this experiment, it was confirmed that the pH has a great influence on the stability of biotin nano-liposomes. In vitro franz diffusion cell method was used to measure in vitro skin absorption rate of biotin nano-liposomes. The shape of the formulation and biotin solubility in nano-liposome was observed by cryogenic transmission electron microscopy (cryo-TEM). Through this study, we confirmed that biotin, which is introduced as closely related to hair health, can be incorporated into a nano-liposome drug delivery system, to make biotin nano-liposome with improved solubility and precipitation problems.

Hydrolysis characteristics and applications of silk sericin I. Control of molecular weight of sericin (실크 세리신의 가수분해 특성과 응용 I. 세리신의 분자량 제어)

  • 김정호;배도규
    • Journal of Sericultural and Entomological Science
    • /
    • v.45 no.1
    • /
    • pp.46-57
    • /
    • 2003
  • This study was carried out to investigate the characteristics of the soluble sericins after degumming and after hydrolysis of insoluble sericin with various enzymes. Especially, the hydrolysis characteristics were examined in terms of molecular weight of the soluble sericin. Amino acid composition and molecular weight characteristics of the soluble sericins were also studied. When the insoluble sericin was hydrolyzed with kojizyme and flavourzyme, the solubility was highest at pH 7 and 50$^{\circ}C$. On the other hand, in the cases of protamex and alcalase, the highest solubility was obtained at 60$^{\circ}C$. In these cases, solubility increased with pH. In enzymatic hydrolysis, the solubility was increased with concentration of enzymes until 4 hours. After then, a slight difference was found along with treatment times. In enzymatic hydrolysis, the absorbance of the soluble sericin was increased with concentration of enzymes and treatment times. Average degree of polymerization was decreased with treatment time and concentration. The amino acid compositions were similar in low(low molecular weight by degumming) and high (high molecular weight by degumming). Those of PK (soluble sericin hydrolyzed with kojizyme), PP (soluble sericin hydrolyzed with protamex), and PA(soluble sericin hydrolyzed with alcalase) were similar to each other. Serine and tyrosine compositions were higher in low and high than those of PK, PP, and PA. However proline was absent in low and high. Molecular weights of the various sericins became higher as KP>high>PP>low>PA and those of KP and PA were 9,800 and 905 respectively.