• Title/Summary/Keyword: dissolution properties

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A New Formulation of Controlled Release Amitriptyline Pellets and Its In Vivo/In Vitro Assessments

  • Park, Eun-Seok;Lee, Dong-Soo;Kwon, Seok-Young;Chi, Sang-Cheol
    • Archives of Pharmacal Research
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    • v.26 no.7
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    • pp.569-574
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    • 2003
  • Controlled-release amitriptyline pellets (ATP) were formulated and its oral bioavailability was assessed in human volunteers after oral administration under fasting conditions. Core pellets were prepared using a CF granulator by two different methods (powder layering and solvent spraying) and coated with Eudragit RS or RL 100. Physical characteristics and dissolution rates of core pellets and coated pellets were evaluated to optimize the formulation. Powder layering method resulted in a better surface morphology than solvent spraying method. However, physical properties of the products were poorer when prepared by powder layering method with respect to hardness, friability and density. The dissolution profile of amitriptyline coated with Eudragit RS 100 was comparable to that of commercially available amitriptyline enteric-coated pellets ($Saroten^{\circledR}$ retard). After the oral administration of both products at the dose of 50 mg, the mean maximum concentrations ($C_{max}$) were 36.4 and 29.7 ng/mL, and the mean areas under the concentration-time curve ($AUC_{0-96}$) were 1180.2 and 1010.7 ng.h/mL for ATP and Saroten retard, respectively. The time to reach the maximum concentrations ($T_{max}$) was 6 h for both formulations. Statistical evaluation suggested that ATP was bioequivalent to Saroten retard.

Self-Nanoemulsifying Drug Delivery System of Lutein: Physicochemical Properties and Effect on Bioavailability of Warfarin

  • Yoo, Juno;Baskaran, Rengarajan;Yoo, Bong-Kyu
    • Biomolecules & Therapeutics
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    • v.21 no.2
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    • pp.173-179
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    • 2013
  • Objective of present study was to prepare and characterize self-nanoemulsifying drug delivery system (SNEDDS) of lutein and to evaluate its effect on bioavailability of warfarin. The SNEDDS was prepared using an oil, a surfactant, and co-surfactants with optimal composition based on pseudo-ternary phase diagram. Effect of the SNEDDS on the bioavailability of warfarin was performed using Sprague Dawley rats. Lutein was successfully formulated as SNEDDS for immediate self-emulsification and dissolution by using combination of Peceol as oil, Labrasol as surfactant, and Transcutol-HP or Lutrol-E400 as co-surfactant. Almost complete dissolution was achieved after 15 min while lutein was not detectable from the lutein powder or intra-capsule content of a commercial formulation. SNEDDS formulation of lutein affected bioavailability of warfarin, showing about 10% increase in $C_{max}$ and AUC of the drug in rats while lutein as non-SNEDDS did not alter these parameters. Although exact mechanism is not yet elucidated, it appears that surfactant and co-surfactant used for SNEDDS formulation caused disturbance in the anatomy of small intestinal microvilli, leading to permeability change of the mucosal membrane. Based on this finding, it is suggested that drugs with narrow therapeutic range such as warfarin be administered with caution to avoid undesirable drug interaction due to large amount of surfactants contained in SNEDDS.

Real-time Simulation Technique for Visual-Haptic Interaction between SPH-based Fluid Media and Soluble Solids (SPH 기반의 유체 및 용해성 강체에 대한 시각-촉각 융합 상호작용 시뮬레이션)

  • Kim, Seokyeol;Park, Jinah
    • Journal of the Korean Society of Visualization
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    • v.15 no.1
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    • pp.32-40
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    • 2017
  • Interaction between fluid and a rigid object is frequently observed in everyday life. However, it is difficult to simulate their interaction as the medium and the object have different representations. One of the challenging issues arises especially in handling deformation of the object visually as well as rendering haptic feedback. In this paper, we propose a real-time simulation technique for multimodal interaction between particle-based fluids and soluble solids. We have developed the dissolution behavior model of solids, which is discretized based on the idea of smoothed particle hydrodynamics, and the changes in physical properties accompanying dissolution is immediately reflected to the object. The user is allowed to intervene in the simulation environment anytime by manipulating the solid object, where both visual and haptic feedback are delivered to the user on the fly. For immersive visualization, we also adopt the screen space fluid rendering technique which can balance realism and performance.

Effect of Cd Addition on the SCC Properties of Al-Cu-Mn Cast Alloys (Al-Cu-Mn주조합금의 SCC특성에 미치는 Cd첨가의 영향)

  • Lee, Chan-Hui;Kim, Gyeong-Hyeon;Kim, In-Bae
    • Korean Journal of Materials Research
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    • v.11 no.4
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    • pp.266-271
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    • 2001
  • Effect of Cd addition on the stress corrosion cracking(SCC) resistance of Al-Cu-Mn cast alloy was investigated by C-ring test and electrical conductivity measurement. With increasing Cd contents, the electrical conductivity and the SCC resistance were increased. The PFZ and coarse precipitates along the grain boundary were observed from TEM micrographs. The fracture made of the alloys was confirmed as intergranular type and showed brittle fracture surface. As a result, it was concluded that the SCC mechanism of these alloys is the anodic dissolution model. The maximum hardness was increased from 127Hv in the Cd-free alloy to 138∼145Hv in the Cd addition alloys.

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Zero-order Delivery of Alfuzosin Hydrochloride with Hydrophilic Polymers

  • Park, Jun-Bom;Hwang, Chang-Hwan;Noh, Hyung-Gon;Chae, Yu-Byeong;Song, Jun-Woo;Kang, Chin-Yang
    • Journal of Pharmaceutical Investigation
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    • v.40 no.5
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    • pp.285-289
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    • 2010
  • Manufacturing a multi-layered tablet such as Xatral XL$^{(R)}$ is more complex and expensive than monolayered tablets, but mono-layered tablets may have less favorable release properties depending on the pharmacodynamics and pharmacokinetics of the active ingredient. We therefore sought to develop a monolayer tablet with a similar dissolution profile to the commercial alfuzosin sustained-release triple layered tablet (Xatral XL$^{(R)}$). We prepared four different mono-layered alfuzosin tablets with different concentrations of hydroxypropyl methycellulose and PVP K-90. Fomulation III with alfuzosion/mg-stearate/ HPMC/ PVP K-90 (10/5/110/95 mg/tab) has a similar dissolution rate to Xatral XL$^{(R)}$, with a similarity factor score of 81.4. However, the swelling and erosion rates of the two formulations were different, and NIR analysis showed differences in the mechanisms of drug release. Thus, although formulation III and Xatral XL$^{(R)}$ show similar dissolution rates, the mechanisms of drug release are different.

Effect of VC Addition on the Microstructure & Mechanical Properties of Ti(CN)-based Cermet (VC 첨가가 Ti(CN)계 써메트의 미세구조 및 기계적 성질에 미치는 영향)

  • 안성용;강신후
    • Journal of the Korean Ceramic Society
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    • v.35 no.12
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    • pp.1316-1322
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    • 1998
  • The amount of VC and C/N ratio in Ti(CN) was varied to investigate the effect of VC addition on the mi-crostructural change in Ti(CN)-Ni system. As the amount of VC addition increases in Ti(C0.7N0.3)-20Ni sys-tem a complete solid solution was observed in Ti(C0.7N0.3)-20Ni-25VC system. It implies that the ratio of the dissolution rates of Ti(C0.7N0.3)to that of VC is nearly 2:1 at the sintering conditions used in this study. It was found from the experiments that the system composed of the Ti(C0.7N0.3) phase exhibits a rimless structure and relatively small amount of solid solution. That is among Ti(C0.7N0.3) phase exhibits a rimless structure and relatively small amount of solid solution. This is among Ti(C1-xNx) phases the dissolution rate of Ti(C0.3N0.7) is the lowest. Also fracture toughness(KIC) of the cermet was measured by indentation method. Attentions were paid to crack propagation path to look for a dominant fracture mode and to cor-relate it with fracture toughness values. The fracture toughness was relatively high with the addition of VC content. But the addition of a large VC content reduced the overall toughness of the cermet. This result is explained with the difference in fracture mode.

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Radiolarian Biostratigraphy and Paleoceanographic Study from the Northeast Equatorial Pacific (북동태평양지역의 방산충 생층서 및 고해양환경 연구)

  • Kim, Ki-Hyune;Park, Jeoung-Hee
    • Ocean and Polar Research
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    • v.21 no.2
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    • pp.127-136
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    • 1999
  • Radiolarian assemblages from KODOS area were analyzed in order to understand the biostratigraphy and paleoceanography of deep-sea sediment from the Northeast Equatorial Pacific. The sediment core was divided into two or three units on the basis of the chemical and physical properties. In the upper sediment, mixtures of Quaternary and Tertiary radiolarians are found indicating active reworking processes. Dissolution of radiolarians seem to increase with depth. Radiolarians are seldom in Unit III presumably due to dissolution and corrosion. The middle part of unit I appears to correspond to Collosphaera invaginata Zone (0.21 Ma). Unit II belongs to Collosphaera tuberosa Zone. Based on the absence of Stylatractus universus, we estimate its age to be younger than 0.42 Ma. Based on our analyses of radiolarians in Unit I and II, we estimated the age of unit III as Tertiary, particularly from Oligocene to Miocene. There may to be hiatuses of more than 3 My from late Miocene to Pliocene, which probably resulted from erosion and dissolution by the Antarctic Bottom Water Sedimentation rates during Quaternary range from 0.15 to 0.50 mm/ky with significant variabilities among stations. Radiolarians in the study area were mostly warm-water species.

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Structural, Optical, and Chemical Properties of Cadmium Phosphate Glasses

  • Chung, Jae-Yeop;Kim, Jong-Hwan;Choi, Su-Yeon;Park, Hyun-Joon;Hwang, Moon-Kyung;Jeong, Yoon-Ki;Ryu, Bong-Ki
    • Journal of the Korean Ceramic Society
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    • v.52 no.2
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    • pp.128-132
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    • 2015
  • In this study, we prepared cadmium phosphate glasses with various compositions, given by $xCdO-(100-x)P_2O_5$ (x = 10-55 mol%), and analyzed their Fourier transform infrared spectra, dissolution rate, thermal expansion coefficient, glass transition temperature, glass softening temperature, and optical band gap. We found that the thermal expansion coefficient and dissolution rate increased while the glass transition temperature and glass softening temperature decreased with increasing CdO content. These results suggest that CdO acts as a network modifier in binary phosphate glass and weakens its structure.

Inorganic Compound and Cycloserine Composite Particles for Improved Stability (안정성 개선을 위한 무기화합물과 사이클로세린 복합 입자)

  • Dongwon Kim;Heeseo Kim;Hongjun Yoon;Hyuk Jun Cho;Sung Giu Jin
    • Journal of Powder Materials
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    • v.31 no.2
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    • pp.126-131
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    • 2024
  • The aim of this study was to improve the chemical stability of cycloserine containing organic and inorganic compounds. Composite particles were manufactured with a 1:1 weight ratio of organic/inorganic compounds and cycloserine. The influence of organic/inorganic compounds on the stability of cycloserine was investigated under accelerated stress conditions at 60℃/75% RH for 24 hours. In addition, the properties of the composite particles were evaluated using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and the dissolution of the drug was assessed by preparing it as a hard capsule. Among the organic and inorganic compounds investigated, calcium hydroxide most improved the stability of cycloserine under accelerated stress conditions (53.3 ± 2.2% vs 1.7 ± 0.2%). DSC results confirmed the compatibility between calcium hydroxide and the cycloserine, and SEM results confirmed that it was evenly distributed around the cycloserine. Calcium hydroxide also showed more than 90% cycloserine dissolution within 15 minutes. Therefore, the calcium hydroxide and cycloserine composite particles may be candidates for cycloserine oral pharmaceuticals with enhanced drug stability.

Effects of Pulping Conditions in the Reconstituted Tobacco Sheet Making Process on the Properties of the Pulp Slurry (판상엽 펄퍼 운전 조건에 따른 펄핑특성 변화)

  • Sung, Yong-Joo;Han, Young-Lim;Kim, Kun-Soo;Rhee, Moon-Soo;Ha, In-Ho;Lee, Ki-Yeul;Lee, Young-Eh;Kim, You-Choul
    • Journal of the Korean Society of Tobacco Science
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    • v.28 no.2
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    • pp.117-123
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    • 2006
  • The pulping process in a papermaking process for a reconstituted tobacco sheet (RECON) was evaluated. For the practical information, the experiments were conducted in a real mill. Two pulping conditions were chosen and changed depending on the feasibility, such as the pulping temperature and the properties of pulping water. The higher pulping temperature resulted in the easier dissolution of solubles from the raw materials. However, the efficiency of screw press process was decreased by the higher pulping temperature, which resulted in the reduction of the HWS and the concentration in the #1 screw press filtrate. The addition of SEL(Strong extracted liquor) to pulper affected the efficiency of dissolution and the final concentration of #1 screw press filtrate. Although the higher SEL resulted in the less dissolution of the solubles from the raw materials, the concentration of the #1 screw press filtrate was greatly increased by the higher addition of SEL, which could provide much better efficiency to the following evaporation process of the filtrate and could increase the whole productivity.