• Title/Summary/Keyword: Release conditions

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Development of Drug-Loaded PLGA Microparticles with Different Release Patterns for Prolonged Drug Delivery

  • Choi, Yeon-Soon;Joo, Jae-Ryang;Hong, Areum;Park, Jong-Sang
    • Bulletin of the Korean Chemical Society
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    • v.32 no.3
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    • pp.867-872
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    • 2011
  • For the prolonged delivery and sustained release rates of low molecular weight drugs, poly(lactic-co-glycolic acid) (PLGA) microparticles containing the drug SKL-2020 have been investigated. On increasing polyvinyl alcohol (PVA) concentration (from 0.2% to 5%), the size of microparticles decreased (from $48.02{\mu}m$ to $10.63{\mu}m$) and more uniform size distribution was noticeable due to the powerful emulsifying ability of PVA. A higher drug loading (from 5% to 20%) caused a larger concentration gradient between 2 phases at the polymer precipitation step; this resulted in decreased encapsulation efficiency (from 34.19% to 25.67%) and a greater initial burst (from 61.71% to 70.05%). SKL-2020-loaded PLGA microparticles prepared with different fabrication conditions exhibited unique release patterns of SKL-2020. High PVA concentration and high drug loading led to an initial burst effect by rapid drug diffusion through the polymer matrix. Since PLGA microparticles enabled the slow release of SKL-2020 over 1 week in vitro and in vivo, more convenient and comfortable treatment could be facilitated with less frequent administration. It is feasible to design a release profile by mixing microparticles that were prepared with different fabrication conditions. By this method, the initial burst could be repressed properly and drug release rate could decrease.

Agarwood Inhibits Histamine Release from Rat Mast Cells and Reduces Scratching Behavior in Mice -Effect of Agarwood on Histamine Release and Scratching Behavior-

  • Inoue, Eiji;Shimizu, Yasuharu;Masui, Ryo;Tsubonoya, Tomoe;Hayakawa, Tomomi;Sudoh, Keiichi
    • Journal of Pharmacopuncture
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    • v.19 no.3
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    • pp.239-245
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    • 2016
  • Objectives: This study was conducted to clarify the effects of agarwood on histamine release from mast cells in rats and on the scratching behaviors in mice. Methods: Histamine release from rat mast cells induced by compound 48/80 or concanavalin A (Con A) and compound 48/80-induced scratching behavior in mice were examined to investigate the effects of agarwood. The hyaluronidase activity and the 3',5'-cyclic adenosine monophosphate (cAMP) levels in mast cells were examined to investigate the mechanisms for the inhibition of histamine release. The correlation between the inhibitory effects of agarwood on histamine release and the content of its typical ingredients, a 2-(2-phenylethyl)chromone derivatives, was analyzed using thin-layer chromatography. Results: Agarwood showed an inhibitory effect on mast-cell histamine release induced by compound 48/80 or Con A without any effect on hyaluronidase activity; this effect involves an increase in the cAMP levels in mast cells. Oral administration of agarwood showed an inhibitory effect on compound 48/80-induced scratching behavior in mice. The inhibitory effects of agarwood on histamine release were quite different, depending on the area where the agarwood was produced, its quality, and its market price. No correlation was found between the inhibitory effects of agarwood on histamine release and the typical ingredients of agarwood, which are 2-(2-phenylethyl)chromone derivatives. Conclusion: These results show that agarwood inhibits histamine release from mast cells partially through an increase in the cAMP levels in cells. We suggest that some active ingredients of agarwood must be effective on oral intake and that agarwood can be used to treat patients with a number of conditions, including urticaria, atopic dermatitis, and bronchial asthma, in which an increase in histamine release occurs. Differences in the pharmacological effects of this crude drug among markets may provide important information for the quality control of this herbal medicine.

The Word Recognition Score According to Release Time on Automatic Gain Control (자동이득 조절에서 해제시간에 따른 어음인지점수 변화)

  • Hwang, S.M.;Jeon, Y.Y.;Park, H.J.;Song, Y.R.;Lee, S.M.
    • Journal of Biomedical Engineering Research
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    • v.31 no.5
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    • pp.385-394
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    • 2010
  • Automatic gain control(AGC) is used in hearing aids to compensate for the hearing level as to reduced dynamic range. AGC is consisted of the main 4 factors which are compression threshold, compression ratio, attack time, and release time. This study especially focus on each individual need for optimum release time parameters that can be changed within 7 certain range such as 12, 64, 128, 512, 2094, and 4096ms. To estimate the effect of various release time in AGC, twelve normal hearing and twelve hearing impaired listeners are participated. The stimuli are used by one syllable and sentence which have the same acoustic energy respectively. Then, each of score of the word recognition score is checked in quiet and noise conditions. As a result, it is verified that most people have the different best recognition score on specific release time. Also, if hearing aids is set by the optimum release time in each person, it is helpful in speech recognition and discrimination.

Advanced One-zone Heat Release Analysis for IDI Diesel Engine (IDI 디젤기관의 개선된 단일영역 열발생량 계산)

  • Kim Gyu-Bo;Jeon Choung-Hwan;Chang Young-Jun;Lee Suk-Young
    • Journal of Advanced Marine Engineering and Technology
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    • v.28 no.7
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    • pp.1101-1110
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    • 2004
  • An one-zone heat release analysis was applied to a 4 cylinder indirect injection diesel engine. The objective of the study is to calculate heat release accurately considering the effect of specific heat ratio. heat transfer and crevice model and to find out combustion characteristics of an indirect diesel engine considering the effect of the pressures in main and swirl chambers. Especially specific heat ratio indicating combustion characteristics is adapted. instead of that indicating matter properties, which has been used in former studies Moreover by adaption of blowby model, cylinder gas mass became accurately calculated. Therefore, with ideal gas equation, calculating cylinder gas temperature, it was found to affect heat transfer loss and heat release. Determining heat transfer constants $C_1$. $C_2$ as 0.6 respectively. the integrated gross heat release values were predicted well for the measured value at various engine speed, full load operating conditions. The curve of heat release rate was similar to SI engine rather than DI engine. That is originated from that swirl chamber reduce an instant combustion which occurs in DI engine due to ignition delay on early stage of combustion.

Controlled Release of Gentamicin Sulfate from Poly(3-hydroxybu-tyrate-co-3-hydroxyvalerate) Wafers for the Treatment of Osteomyelitis

  • Gilson Khang;Park, Hak-Soo;John M. Rhee;Yoon, Sung-Chul;Cho, Jin-Cheol;Lee, Hai-Bang
    • Macromolecular Research
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    • v.8 no.6
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    • pp.253-260
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    • 2000
  • Biodegradable wafers were prepared with poly (hydroxybutyrate-co-hydroxyvalerate) (PHBV;5, 10, and 15 mole% for 3-hydroxyvalerate) by simple heat pressing method for the sustained release of antibiotic agent, gentamicin sulfate (GS) to investigate the possibility of the treatment for osteomyelitis. The effects of hydroxyvalerate (HV) content, thickness of wafers, various types of additives such as sodium dodecyl sulfate (SDS), microcrystalline cellulose, polyvinylpyrrolidone, and hydroxypropylcellulose (HPC), and different initial drug loading ratio on the release profile have been investigated. In vitro release studies showed that different release patterns and rates could be achieved by simply modifying factors in the preparation conditions. PHBV wafers with 3 mm thickness, 10% of GS initial loading, 15% of HV content and addition of 5% of SDS and HPC were free from initial burst and a near-zero-order sustained release was observed for over 30 days. It might be suggested that the mechanisms of G5 release may be more predominant simple dissolution and diffusion of GS than erosion of PHBV in our system.

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Preparation of Lacosamide Sustained-release Tablets and Their Pharmacokinetics in Beagles and Mini-pigs

  • Ahn, Jae Soon;Kim, Kang Min;Nam, Dae Sik;Kang, Kyoung Un;Choi, Peter S.;Jeong, Seo Young
    • Bulletin of the Korean Chemical Society
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    • v.35 no.2
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    • pp.557-561
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    • 2014
  • The aim of the present study was to improve dosing of lacosamide, a functionalized amino acid used as an antiepileptic agent, from twice daily to once daily for the convenience of patients. A sustained-release lacosamide tablet was developed and dissolution testing was employed to determine in vitro release behavior using water or buffer solutions at pH 1.2, 4.0, or 6.8. Lacosamide was released for 12 h from the sustainedrelease (SR) tablet, as compared to complete release within 1 h from an immediate-release $Vimpat^{(R)}$ tablet. Each formulation (100 mg) was orally administered to six beagle dogs and six mini-pigs under fasted conditions, and pharmacokinetic parameters such as the area under the concentration time curve ($AUC_t$), the maximum plasma concentration ($C_{max}$), and the time at which this occurred ($T_{max}$) were calculated. These results showed similar values for $AUC_t$, $C_{max}$, and $T_{max}$ following oral administration of immediate-release ($Vimpat^{(R)}$) and SR lacosamide tablets.

Analysis and Simulation of SF6 Tracer Experiments for Tracking the Pollutant Transport (오염물질 이동 추적을 위한 SF6 추적자 실험 분석과 모사 연구)

  • 김영성;조성호
    • Journal of Korean Society for Atmospheric Environment
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    • v.14 no.5
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    • pp.397-410
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    • 1998
  • Tracer experiments were performed 4 times in December 1992 on the relatively flat terrain and nearby building area adjacent to the Taedok Science Town in Korea. Each experiment was continued for relatively short period of 1 or 2 hours with intermittent release of SF6 up to 2.07g/s at 10m height. Movement of tracer plume was tracked by a continuous tracer analyzer installed on an air monitoring van. Simulation with INPUFF was carried out to analyze and predict experiments. Measured profiles of tracer plume were narrow and sharp while predicted profiles by INPUFF were broad and slowly varied. Tracer plumes were detected at a short distance of 0.5 to 2.2 km mainly due to intermittent release and high value of lower detectable limit. Various experimental conditions were tested by INPUFF simulation in order to find desirable conditions. Higher wind speed and less variable wind direction could yield longer distance of plume tracking only when the lower detectable limit was sufficiently low. Distance of plume tracking was long and did not much depend on the lower detectable limit in stable atmospheric conditions.

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Simulating Daily Inflow and Release Rates for Irrigation Reservoirs (1) -Modeling Inflow Rates by A Linear Reservoir Model- (관개용 저수지의 일별유입량과 방류량의 모의발생(I)-선형 저수지 모형에 의한 유입량의 추정-)

  • 김현영;박승우
    • Magazine of the Korean Society of Agricultural Engineers
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    • v.30 no.1
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    • pp.50-62
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    • 1988
  • This study refers to the development of a hydrologic model simulating daily inflow and release rates for irrigation reservoirs. A daily - based model is needed for adequate operation of an irrigation reservoir sufficing the water demand for paddy fields which is closely related to meteorological conditions. Inflow rates to a reservoir need to be accurately described, which may be simulated using a hydrologic model from daily rainfall data. And the objective of this paper is to develop, test, and apply a hydrologic model for daily runoff simmulation. A well - known tank model was selected and modified to simulate daily inflow rates. The model parameters were calibrated using observed runoff data from twelve watersheds, Relationships between the parameters and the watershed characteristics were derived by a multiple regression analysis. The simulation results were in agreement with the data. The inflow model was found to simulate low flow conditions more accurately than high flow conditions, which may be adequate for water resources utilization.

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Verification of Enhanced Phosphate Removal Capability in Pure Cultures of Acinetobacter calcoaceticus under Anaerobic/Aerobic Conditions in an SBR

  • Kim, Hyung-Jin;Krishna R. Pagilla
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.7 no.6
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    • pp.335-339
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    • 2002
  • Laboratory experiments were conducted using pure cultures of Acinetobacter under an-aerobic/aerobic cyclic conditions to explain the release and uptake of soluble phosphate in an activated sludge process showing enhanced biological phosphate removal (EBPR). Under anaerobic/aerobic cyclic conditions in a Sequencing Batch Reactor (SBR), COD uptake concurrent with soluble phosphate release by Acinetobacter was not significant during the anaerobic periods, indicating that EBPR would not be established in pure cultures. However Acinetobacter cells accumulated higher phosphate content (5.2%) in SBR than that obtained (4.3%) from batch experiments. These results suggest that Acinetobacter sp. may not follow the proposed pattern of behavior of poly-P bacteria in EBPR activated sludge Plants.

Comparative Study of the Dissolution Profiles of a Commercial Theophylline Product after Storage

  • Negro, S.;Herrero-Vanrell, R.;Barcia, E.;Villegas, S.
    • Archives of Pharmacal Research
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    • v.24 no.6
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    • pp.568-571
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    • 2001
  • The purpose of this work was to study the effect of storage time and temperature on the in vitro release kinetics of a commercial sustained-release dosage form of theophylline, at different pHs of the dissolution medium. The formulation was stored at $35^{\circ}C$ for 16 months and at $45^{\circ}C$ for 8 months, with a relative humidity of 60%. The in vitro release tests were performed at pHs 2, 4, 6 and 7.4. The mean values of the transport coefficient n, were close to 0.5 in all the conditions tested, which indicates that the transport system is not modified after storage of the formulation at $35^{\circ}C$ and $45^{\circ}C$. The mean values of the dissolution rate constant ranged from 0.036 to 0.043 $min^{-n}$, under all the conditions tested. Significant differences (${\alpha}=0.05$) were found between pHs 2, 4 and 6, 7.4 for all the model-independent parameters studied. When the formulation was kept at $35^{\circ}C$ for 16 months, the mean percentage of drug dissolved at 8 hours was 25.61% (pHs 2, 4) and, 36.12% (pHs 6, 7.4), representing a 26% and 24% reduction, respectively. Simitar results were obtained after storing the formulation at $45^{\circ}C$ for 8 months, corresponding to 33.3% (pHs 2, 4) and, 22.5% (pHs 6, 7.4) diminution, respectively. The values of the similarity factory $f_2$, obtained were lower than 50, which indicates the lack of similarity among the dissolution profiles, after storing the formulation under the experimental Conditions tested.

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