• Title/Summary/Keyword: Acidic drug

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Effects of Ultra-high Pressure Homogenization on the Emulsifying Properties of Whey Protein Isolates under Various pH

  • Lee, Sang-Ho;Subirade, Muriel;Paquin, Paul
    • Food Science and Biotechnology
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    • v.17 no.2
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    • pp.324-329
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    • 2008
  • The effect of ultra-high pressure homogenization on the emulsifying properties of whey protein was investigated in a model emulsion made with whey protein isolate and soya oil under various pH. The emulsifying properties, the average diameter of the oil droplets ($d_{vs}$), and the protein load, were measured for each emulsion produced at different homogenization pressures (50 to 200 MPa) and pH values (4.6 to 8.0). According to the results of variance analysis and response surface, the pH had more influence on oil droplet size and protein load than homogenization pressure. The model equations, which were obtained by response surface analysis, show that pH and homogenization pressure had the major effect on oil droplet size and protein load. Higher homogenization pressure decreased the average droplet size and the protein load. Homogenization at high pressure, as opposed to low pressure, causes no overprocessing, but the effect was pH-dependent. The average diameter of the oil droplets increased slightly by decreasing the pH from 8.0 to 6.5 and then increased dramatically toward the isoelectric point of whey protein (i.e., at pH 4.6). Moreover associated droplets were found at acidic pH and their size was increased at high temperature.

Drug Interaction between Pranoprofen and Aspirin in Rats (프라노프로펜과 아스피린과의 상호작용)

  • Choi, Jun-Shik;Choi, Byung-Chul
    • Korean Journal of Clinical Pharmacy
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    • v.15 no.1
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    • pp.50-54
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    • 2005
  • The purpose of this study is to investigate the effect of aspirin on the pharmacokinetics of pranoprofen by oral coadministration of pranoprofen (5 mg/kg) with aspirin (5, 10 and 20 mg/kg) in Sprague-Dawley rats. After oral coadministration of pranoprofen with aspirin, the area under the plasma concentration-time curves (AUC) of pranoprofen was increased significantly by 10 mg/kg (p<0.05) and 20 mg/kg (p<0.01) of aspirin coadministration, and peak concentrations ($C_{max}$) of pranoprofen was increased significantly by coadministration of 20 mg/kg aspirin (p<0.05) compared to pranoprofen alone. Relative bioavailabilities (RB${\%}$) of pranoprofen in coadmistration were higher (from 1.42 to 1.67 fold) than control. The half-lives ($t_{1/2}$) of pranoprofen in coadministration were increased significantly (p<0.05) by 20-mg/kg aspirin. Based on these results, we might be considered that the pharmacokinetics of pranoprofen would be affected by coadministration of aspirin, by inhibit its metabolism in the liver and the tubular secretion of the kidney with the same acidic property. It should take into consideration in dosage regimen of pranoprofen when coadministration of pranoprofen with aspirin in treatment of rheumatoid arthritis.

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Development and Stability Evaluation of Enteric Coated Diclofenac Sodium Tablets Using AquaPolish E.

  • Zaid, A.N.;Fadda, A.M.;Nator, S.;Qaddumi, A.
    • Journal of Pharmaceutical Investigation
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    • v.41 no.4
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    • pp.211-215
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    • 2011
  • The aim of this study was to develop a stable enteric coated diclofenac sodium (DFS) tablets using Aqua-Polish E without using a subcoat. DFS uncoated tablets were manufactured through the non direct compression process. AquaPolish E white aqueous coating dispersion was used as enteric coating material. This film forming polymer is a mixture of selected polymethacrylic/ethylacrylate copolymers. The stability of the obtained enteric coated tablets was evaluated according to ICH guidelines. No signs of disintegration or cracking was observed when they placed in 0.1N HCl solution (pH1.2), but they were completely disintegrated within 10 minutes when they placed in buffered solution at pH6.8. Dissolution test was also conducted by placing tablets in 0.1 N HCl for 2 hours and then 1 hour in phosphate buffer at pH 6.8. Less than 0.9 % of drug was released in the acidic phase and up to 97% in the basic medium. These findings suggest that aqueous enteric coating with AquaPolish E system is an easy and economical approach for preparing stable DFS enteric coat without the use of a subcoating layer.

Effect of Sam Hwa San on Na-K-ATPase Activity in Microsomal Fraction of Rabbit Cerebral Cortex (삼화산(三和散)이 대뇌피질(大腦皮質) microsome분획(分劃)에서 Na-K-ATPase활성(活性)에 미치는 영향(影響))

  • Kim, Gil-Seop;Jeong, Ji-Cheon
    • The Journal of Korean Medicine
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    • v.16 no.1 s.29
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    • pp.281-294
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    • 1995
  • The effect of Sam Hwa San on the Na-K-ATPase activity was evaluated in microsomal fraction prepared from rabbit cerebral cortex to determine whether Sam Hwa San affects Na-K-ATPase activity of nervous system. Sam Hwa San markedly inhibited the Na-K-ATPase activity in a dose-dependent manner with an estimated $I_{50}$ of 0.12%. Optimal pH for the Na-K-ATPase activity was at 7.5 in the presence or absence of Sam Hwa San. The degree of inhibition by the drug more increased at acidic and alkalic pHs than neutral pH. Kinetic studies of substrate and cationic activation of the enzyme indicate classic noncompetitive inhibition fashion for ATP, Na and K, showing significant reduction in Vmax without a change in Km. Dithiothreitol, a sulfhydryl reducing reagent, partially protects the inhibition of Na-K-ATPase activity by Sam Hwa San. Combination of Sam Hwa San and ouabain showed higher inhibition than cumulative inhibition. These results suggest that Sam Hwa San inhibits Na-K-ATPase activity in central nervous system by reacting with, at least a part, sulfhydryl group and ouabain binding site of the enzyme protein, but with different binding site from those of ATP, Na and K.

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Controlled Release and Stabilization of Cefaclor from Alginate-based Matrices for Oral Delivery Design

  • Bak, So-Im;Lee, Jue-Yeon;Song, Hye-Won;Hwang, Jeong-Hyo;Lee, Seung-Jin
    • Journal of Pharmaceutical Investigation
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    • v.32 no.4
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    • pp.327-330
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    • 2002
  • Alginate based polymeric matrices were designed for controlled release and stabilization of cefaclor in gastrointestinal fluid. Cefaclor is known to be acid stable and subjected to be degraded at neutral and alkaline pHs. In order to achieve an effective release profile of cefaclor in gastrointestinal tract, a particular strategy in dosage form design should be required from the view point of maintaining its activity. The amphiphilic nature of cefaclor allowed its controlled release using ionic polymers based on ionic interaction between the drug and polymers. The thrust of this study was to develop a technique that delivers cefaclor keeping effective release rate in the intestinal tract. Considering the fast degradation of cefaclor in the intestinal fluid, the matrices were designed to release surplus amount of cefaclor. The alginate based matrices demonstrated increase in release rate in the simulated intestinal fluid, which was favorable to compensate the degraded portion of cefaclor. In addition, stabilization of cefaclor in the intestinal fluid was obtained by employing citric acid that provides an local acidic environment. The matrices might be valuably used for the development of an oral cefaclor dosage form.

Properties and Application as the Indicator of N-4-Salicyloamido-2-Amino-6-Piperidinopyrimidine 3-Oxide Fe(III) Complex (N-4-살리실로아미도-2-아미노-6-피페리디노피리미딘 3-옥사이드${\cdot}$철(III) 착체의 물성 및 지시약적 응용성)

  • Lee, Jong-Pill;Shin, Joon-Su;Kim, Kyoung-Soon;Hong, Seon-Pyo;Kim, Kyeong-Ho;Kim, Bak-Kwang
    • YAKHAK HOEJI
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    • v.40 no.6
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    • pp.670-678
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    • 1996
  • The combinations of N-4-salicyloamido-2-amino-6-piperidinopyrimidine 3-oxide (Salmi) and two transitional metals were colored. Among metals, Fe(III) made a distinct colored comp lex with Salmi. The mole ratio of Salmi and Fe(III) in the complex was 1:1. This Salmi-Fe(III) complex was recrystallized in Hexane/Acetone(=10/1, v/v) and investigated its physicochemical properties. The color of this complex was changed by pH.; deep violet pink in acids, orange in neutral, and yellow in bases. The range of color change was approximately 0.7 pH unit. Acid-base titration of various acidic or basic drugs using Salmi-Fe(III) complex as an indicator showed good accuracy and reproducibility.

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Swelling of Commercial Matrix Tablets Based on Carboxymethyl Cellulose Sodium and Alginic Acid (시판중인 메트릭스 정제의 팽윤력 비교 연구)

  • Kim, Ki Taek;Kim, Ji Su;Park, Ju-Hwan;Lee, Jae-Young;Jo, Yeong Woo;Yang, Jae-Gwon;Jang, Jun Hee;Choi, Eun-Sun;Kim, Dae-Duk
    • YAKHAK HOEJI
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    • v.60 no.2
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    • pp.73-77
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    • 2016
  • Alginic acid and carboxymethyl cellulose sodium are dietary fibers from plants. They have a swelling property and delay the gastric emptying time, thereby resulting in feeling satiated after oral administration, which may eventually contribute to loss of body weight. The goal of this study was to compare swelling property of three commercial matrix tablets based on alginic acid and carboxymethyl cellulose sodium. When the swelling was determined by the Korean Ministry of Food and Drug Safety (MFDS) guideline, the tablet prepared by direct compression method with highly viscous swelling agent showed the highest swelling in acidic conditions. Water uptake of these tablets was rapid and completed within 30 min. Moreover, when the pH was changed from 2.5 to 6.8 buffer, the water uptake was not significantly changed in all tablets.

Analysis of DA-6034, a New Flavonoid Derivative in Biological Fluids by HPLC (HPLC를 이용한 생체 시료중의 새로운 플라보노이드 유도체인 DA-6034의 분석)

  • Lee, Jong-Jin;Son, Mi-Won;Yoo, Moo-Hi;Jang, Min-Sun;Kim, Won-Bae;Lee, Kang-Chun
    • YAKHAK HOEJI
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    • v.42 no.2
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    • pp.149-152
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    • 1998
  • A high performance liquid chromatographic method was developed for the determination of DA-6034 in biological fluids using internal standard. Plasma containing DA-6034 and inter nal standard was extracted by liquid-liquid extraction at an acidic pH. After evaporation of the organic layer, the drug and internal standard were reconstituted with mobile phase and injected into the column. They were separated by high performance liquid chromatography on inertsil ODS II column at 334 nm. The detection limit of DA-6034 in plasma was 0.02 ${\mu}$g/ml. In this method, the range of recovery and coefficients of variation were 96-110% and 0.40-3.78%, respectively. There was no interference from endogenous substances. Urine and bile were analysed using the deproteinization method and the detection limit of DA-6034 was 1${\mu}$g/l.

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Preparation and Evaluation of Aceclofenac Microemulsion for Transdermal Delivery System

  • Yang, Jae-Heon;Kim, Young-Il;Kim, Kyung-Mi
    • Archives of Pharmacal Research
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    • v.25 no.4
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    • pp.534-540
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    • 2002
  • To develop novel transdermal formulation for aceclofenac, microemulsion was prepared for increasing its skin permeability. Based on solubiity and phase studies, oil and surfactant was selected and composition was determined. Microemulsion was spontaneously prepared by mixing ingredients and the physicochemical properties such was investigated. The mean diameters of microemulsion were approximately 90 nm and the system was physically stable at room temperature at least for 3 months. In addition, the in vitro and in vivo performance of microemulsion formulation was evaluated. Aceclofenac was released from microemulsion in acidic aqueous medium, and dissolved amounts of aceclofenac was approximately 30% after 240 min. Skin permeation of aceclofenac from microemulsion formulation was higher than that of cream. Following transdermal application of aceclofenac preparation to delayed onset muscle soreness, serum creatine phosphokinase and lactate dehydrogenase activity was significantly reduced by aceclofenac. Aceclofenac in microemulsion was more potent than cream in the alleviation of muscle pain. Therefore, the microemulsion formulation of aceclofenac appear to be a reasonable transdermal delivery system of the drug with enhanced skin permeability and efficacy for the treatment of muscle damage.

A Convenient Manufacturing Method for Mass Production of EGCG Rich Green Tea Extract (Epigallocatechin Gallate 고함유 녹차추출물의 제조공정 개선)

  • Seo, Eun Hye;Kim, Eun Jeong;Cheon, Seong Bong;Yoon, Min Ji;Choi, Sang Un;Ryu, Geon-Seek;Ryu, Shi Yong
    • Korean Journal of Pharmacognosy
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    • v.50 no.3
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    • pp.198-204
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    • 2019
  • A facile and convenient method was developed for the mass production of epigallocatechin gallate (EGCG) rich green tea extract (Er-GTE). The Er-GTE was successfully obtained from the crude water extract of green tea by the combination of two step purification, i.e., a simple adsorption process on the cation exchange resins (Trilite SCR-B) followed by the chromatography with Diaion HP-20 resins. The green tea extract produced by water extraction under $45^{\circ}C$ was subjected to adsorb on the strongly acidic cation exchange resin, Trilite SCR-B. The eluate passed through the resin was reabsorbed on Diaion HP-20 resin, which was subjected to elute with a mixture of water and alcohol by conventional chromatographical manner. The EGCG content in Er-GTE was estimated above 97% by HP-LC analysis and the newly developed method was regarded as the most suitable and appropriate process for the mass production of epigallocatechin gallate rich green tea extract (Er-GTE).