• Title/Summary/Keyword: Physicochemical stability

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Physicochemical Properties, Stabilities and Pharmacokinetics of Cephalosporin 3'-Quinolone Dithiocarbamate (세팔로스포린 3'-퀴놀론의 물리화학적 성질, 안정성 및 체내약물동태)

  • 나성범;공재양;김완주;지웅길
    • YAKHAK HOEJI
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    • v.37 no.6
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    • pp.638-646
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    • 1993
  • A cepfialosporin with an aminothiazoiylmethoxyimino-type side chain at the 7 position and bicyclic quinolone dithicarbamate at the 3' position was synthesized. It has broad and potent antivacterial activity in vitro. The antibacterial spectrum reflects contributions of both the cephalosporin moiety and the quinolone moiety. Thus, this compound was named DACD implying a dualaction cephalosporin derivative. In this paper, the physicochemical proper-ties (lipid-water partition, pKa), stability and pharmacokinetics of DACD were determined and compared with cefotaxime 3'-norfloxacin dithiocarbamate (CENO). Stability tests were studied in pH 1.20, 6.80 and 8.00 buffers and in the presence of AB type human plasma, rat liver homogenate and its .betha.-lactamase. The pharmacokinetic parameters of DACD were evaluated in mice after a single intravenous dose of 40 mg/kg. The results are as follows. The lipid-water partition coefficient of DACD was higher than that of CENO. The calculated pKa values of CENO and DACD, were 6.82$\pm$0.03, 7.53$\pm$0.21, respectively. In the hydrolysis test, half-lives (t$^{1/2}$) of CENO and DACD was 66.0 hr and 80.0 hr in pH 6.80 buffer, 190 hr and 91.4 hr in pH 8.00 buffer. CENO and DACD were rapidly hydrolyzed in human plasma and in rat liver hornogenate. Half-lives (t$_{1/2}$ of CENO and DACD were 1.29 hr and 1.15 hr in hyman plasma, 0.62 hr and 0.71 hr rat liver homogenate. In $\beta$-lactamase stability test, CENO and DACD were very stable to the .betha.-lactamases obtained from three different strains. Half-life (t$_{1/2}$) and areas under the curve (AUC) in mice were 2.33 hr and 15.97 (mg.h/1), respectively.

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Effects of Edible Insect Powders as Meat Partial Substitute on Physicochemical Properties and Storage Stability of Pork Patties

  • Nayoung Choi;Sanghun Park;Yunhwan Park;Gyutae Park;Sehyuk Oh;Yun-a Kim;Youngho Lim;Soyoung Jang;Youngjin Kim;Ki-Su Ahn;Xi Feng;Jungseok Choi
    • Food Science of Animal Resources
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    • v.44 no.4
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    • pp.817-831
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    • 2024
  • In this study, physicochemical and antioxidant properties, and storage stability (1, 3, and 7 days) of pork patties added with edible insect powders (EIP) of four species (Larvae of Tenenbrio molitor, Protaetia brevitarsis seulensis, Allomyrina dichotoma, and Gryllus bimaculatus) as meat partial substitutes were investigated. Twenty percent of each EIP was added to pork patties, and four treatments were prepared. On the other hand, two control groups were set, one with 0.1 g of ascorbic acid and the other without anything. Adding EIP decreased water content but increased protein, fat, carbohydrate, and ash contents. In addition, the use of EIP increased the water holding capacity and texture properties as well as decreased the cooking loss. However, the sensory evaluation and storage stability were negatively affected by the addition of EIP. The 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity had a positive effect on storage stability. It is believed that the addition of EIP resulted in high antioxidants due to the presence of polyphenol compounds in EIP. These results indicate that EIP has great potential to be used as meat partial substitute to improve the quality improvement and antioxidant in pork patties. However, in order to improve storage stability and consumer preference, further research is needed to apply it to patties by reducing the amount of EIP or adding auxiliary ingredients.

Chitosan-Iron casein succinylate nanoparticles as oral delivery systems: increasing the stability and enhancing the absorption of iron nanoparticles.

  • Cho, Jung-Hye;Oungbho Kwunchit;Park, Jeong-Sook;Kim, Chong-Kook
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.249.1-249.1
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    • 2003
  • The objective of the study was to develop an oral delivery system to increase the stability and efficacy of iron casein succinylate. Aqueous nanoparticles were prepared using complex coacervation of the oppositely charged chitosan and iron casein succinylate with polyethyleneglycol (PEG). The physicochemical properties of nanoparticles were investigated using dynamic light scattering, zeta potential and scanning electron microscopy. Chitosan-iron casein succinylate interactions were investigated in solid state by differential scanning calorimetry (DSC) and FT-IR spectrometry. (omitted)

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Stability of [D-Ala$^2$]-Methionine Enkephalinamide in Aqueous Solution (수용액중 [D-알라$^2$-메치오닌엔케팔린아미드의 안정성)

  • 전인구;양윤정;이치호
    • Biomolecules & Therapeutics
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    • v.1 no.1
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    • pp.31-36
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    • 1993
  • To evaluate the feasibility of transmucosal delivery of methionine enkephalin analog, [$D-Ala^2$]-me-thionine enkephalinamide (YAGFM), the influence of pH, temperature, ionic strength and initial peptide concentration on the physicochemical stability of YAGFM in aqueous buffered solutions were investigated using a stability-indicating HPLC method. The degradation of YAGFM followed the pseudo-first-order kinetics. From the pH-rate profile, the maximum stability of YAGFM was shown to be at the pH of about 5.0. The halflife for the degradation of YAGFM was found to be 181.3 days at pH 5.0 and $37^{\circ}C.$ Arrhenius plots of the data obtained at 25~$45^{\circ}C$ were reasonably linear with a correlation coefficient greater than 0.99, and the activation energy was calculated to be 8.9 kcal/mole. A higher ionic strength and/or a higher peptide concentration in buffered solutions retarded the degradation of YAGFM.

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Preparation of Hyaluronic Acid Microspheres with Enhanced Physical Stability by Double Cross-link or Alginate (이중 가교제 또는 알긴산에 의해 물리적인 안정성이 향상된 히알루론산 마이크로입자의 제조)

  • Kim, Dong-Hwan;Song, Chung-Kil;Balakrishnan, Prabagar;Park, Chun-Geon;Choi, Ae-Jin;Chung, Suk-Jae;Shim, Chang-Koo;Kim, Dae-Duk
    • YAKHAK HOEJI
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    • v.55 no.1
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    • pp.69-74
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    • 2011
  • Hyaluronic acid (HA) is a natural polymer consisting of disaccharide units of D-glucuronic acid and N-acetyl-D-glucosamine. It has a great potential and success in cosmetic and biomedical applications. However, native HA is highly soluble and easily metabolized by enzymes such as hyaluronidase. Thus, various studies have been reported on modifying the physicochemical properties of HA, while maintaining its biocompatibility. For controlled drug delivery, many trials for fabricating HA microspheres were achieved under chemical reaction. The HA microspheres fabricated to improve the physical stability of HA using adipic acid dihydrazide (ADH) by cross-linking reaction has been reported earlier, however it lacks the desired physical stability and rapidly decomposes by swelling or enzymes. Therefore, we prepared double cross-linked HA microspheres (DC-HA microspheres) and alginate containing HA microspheres (AC-HA microspheres) to enhance its physicochemical properties. DC-HA microspheres were prepared using trisodium trimetaphosphate (STMP) under crosslinking reaction after ADH cross-linking reaction. AC-HA microspheres were prepared by adding alginate as a networking polymer. These microspheres were characterized by morphology, particle size, zeta potential, stability against hyaluronidase. Results showed that the DC-HA and AC-HA microspheres are more stable than that of HA microspheres.

Development of Hydrophobically Modified Casein Derivative-Based Delivery System for Docosahexaenoic Acids by an Acid-Induced Gelation

  • Ho-Kyung Ha;Dan-Bi Woo;Mee-Ryung Lee;Won-Jae Lee
    • Food Science of Animal Resources
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    • v.43 no.2
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    • pp.220-231
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    • 2023
  • Although omega-3 fatty acids including docosahexaenoic acid (DHA) contain various health-promoting effects, their poor aqueous solubility and stability make them difficult to be induced in dairy foods. The aims of this research were to manufacture casein derivative-based delivery system using acid-induced gelation method with glucono-σ-lactone and to investigate the effects of production variables, such as pH and charged amount of linoleic acid, on the physicochemical properties of delivery systems and oxidative stability of DHA during storage in model milk. Covalent modification with linoleic acid resulted in the production of casein derivatives with varying degrees of modification. As pH was reduced from 5.0 to 4.8 and the charged amount of linoleic acid was increased from 0% to 30%, an increase in particle size of casein derivative-based delivery systems was observed. The encapsulation efficiency of DHA was increased with decreased pH and increased charged amount of linoleic acid. The use of delivery system for DHA resulted in a decrease in the development of primary and secondary oxidation products. An increase in the degree of modification of casein derivatives with linoleic acid resulted in a decrease in the formation of primary and secondary oxidation products than of free DHA indicating that delivery systems could enhance the oxidative stability of DHA during storage in model milk. In conclusions, casein derivatives can be an effective delivery system for DHA and charged amount of linoleic acid played a key role determining the physicochemical characteristics of delivery system and oxidative stability of DHA.

Study of the Percutaneous Absorption, Stability and Physicochemical Properties of $OMP-{\beta}-CD$ Inclusion Complex ($OMP-{\beta}-CD$ 포접화합물의 물리화학적 성질, 안정성 및 피부 투과 실험)

  • Lee, Sang-Young;Lee, Gye-Won;Choi, Hyun-Soon;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.27 no.4
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    • pp.271-277
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    • 1997
  • Because omeprazole(OMP) is very unstable in aqueous condition, $OMP-{\beta}-CD$, the inclusion complex of OMP and ${\beta}-cyclodextrin({\beta}-CD)$ was made and physicochemical properties of it were compared with those of OMP. Skin permeability of OMP and $OMP-{\beta}-CD$ in propylene glycol vehicle and the reciprocal action of ${\beta}-CD$ with various enhancers were examined through hairless mouse. Adhesive patches were prepared with polyisobutylene and the skin permeability and stability of OMP were investigated. The inclusion complex showed higher solubility and lower partition coefficient than OMP itself. DMSO, 1-methyl 2-pyrrolidone and sodium cholate had an enhancing effect. However ethanol and polysorbate 80 hardly showed the enhancing effect of OMP. When sodium lauryl sulfate and sodium cholate as enhancer were added in patch, the former case showed higher permeability of OMP.

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Preparation and Evaluation of Cubic Liquid Crystalline Phase Gel and Cubosome containing Polyethoxylated Retinamide (폴리에톡시레이티드레틴아마이드를 함유한 입방상 액정 젤 및 큐보좀의 제조 및 평가)

  • Kyong, Kee-Yeol;Jee, Ung-Kil;Cho, Wan-Goo
    • Journal of Pharmaceutical Investigation
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    • v.37 no.2
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    • pp.85-94
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    • 2007
  • The objective of this study is to prepare a stable delivery systems containing polyethoxylated retinamide(PERA) - derivatives of retinoic acid, effective anti-wrinkle and anti-acne agent. Cubic liquid crystalline phase gel (CLCPG) and cubosomes containing various concentrations of PERA were prepared to investigate the physicochemical properties. Furthermore, stability and transdermal absorption efficacy of the CLCPG containing PERA were investigated in comparison with oil-in-water (O/W) emulsions which are predominantly used as a topical formulation. CLCPG increase the stability of PERA in comparison with O/W emulsion. For tropical application, CLCPG containing PERA shows higher moisturizing effect than that of O/W emulsion. In skin permeation test, CLCPG shows higher PERA deposit on epidermis. With its specific physicochemical property caused by the glyceryl oleate, CLCPG itself could be used for stabilizer of various actives and applied as an effective delivery system for topical application. Cubosome, nano-sized dispersed CLCPG, is also expected to be applied in a various field of industry like food, cosmetics and pharmaceuticals.

Physicochemical Properties of Mung Bean Starch Paste, a Main Ingredient of Omija-eui

  • Jang, Keum-Il;Han, Hyun-Jeong;Lee, Kwang-Yeon;Bae, In-Young;Lee, Ji-Yeon;Kim, Mi-Kyung;Lee, Hyeon-Gyu
    • Food Science and Biotechnology
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    • v.18 no.4
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    • pp.991-995
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    • 2009
  • As a principle ingredient in omija-eui, the physicochemical properties of mung bean starch (MBS) paste were investigated and compared to those of rice and corn starch. The amylose and the protein content of MBS were higher than those of rice or corn starch while the total sugar content and the swelling power of MBS were lower. In addition, the clarity of MBS paste was higher than either rice or corn starch paste. Regarding pasting properties, the peak viscosity and cool paste viscosity of MBS were higher than those of either rice or corn starch. During the freeze-thaw cycle, MBS exhibited higher degree of syneresis than corn and rice starch, which decreased with high starch concentration and heating temperature. The paste properties and freeze-thaw stability of MBS showed a potential for improving the quality of omija-eui.