• Title/Summary/Keyword: zero order release

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Buccal Delivery of [D-Ala2, D-Leu5]Enkephalin Incorporated in Mucoadhesive Poly(acrylic acid) Hydrogels

  • Lee, Jae-Hwi;Lee, Yoon-Jin;Kang, Kyoung-Hoon;Nam, Dae-Young;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
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    • v.35 no.5
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    • pp.369-373
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    • 2005
  • The objectives of the current work is to understand the factors impacting the formulation and performance of a Carbopol mucoadhesive buccal delvery system for a model peptide drug, $[D-Ala{^2},\;D-Leu{^5}]$enkephalin (DADLE, Mw=569.7) with comparable chemical and enzymatic stability. Specifically, in vitro buccal DADLE delivery from the cross-linked poly(acrylic acid) (PAA) hydrogel system was characterized. In addition, the influences of several penetration enhancers on the ex vivo buccal absorption of DADLE were also studied. In this study, the PAA hydrogels generally swell to 100% of their original weight in the phosphate pH 7.4 buffer. The water penetration into the PAA hydrogel occurred based on a zero-order kinetics for the first 60 min and steadily decreased afterwards. From the release study, it can be seen that the initial DADLE release was so rapid and the rate of release of DADLE decreased as the time elapsed. The porcine buccal tissue was found to be permeable to DADLE with a flux value of $0.07%/cm{^2}/hr({\pm}0.01\;SD)$. From the ex vivo diffusion study, it was found that sodium taurodihydrofusidate showed a greater degree of enhancement compared to the phospholipids with an Enhancement Ratio (ER) of 8.7 compared to 2.7 and 1.9 for didecanoylphosphatidylcholine and lysophosphatidylcholine, respectively. The work encompassed within this paper has demonstrated the feasibility of using the PAA hydrogel delivery system with its good mucoadhesive properties for the buccal delivery of peptides.

Preparation and Characteristics of Ipriflavone-Loaded PLGA Microspheres (이프리플라본을 함유한 생분해성 미립구의 제조와 특성분석)

  • 이진수;강길선;이종문;신준현;정제교;이해방
    • Polymer(Korea)
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    • v.27 no.1
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    • pp.9-16
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    • 2003
  • Ipriflavone (IP) stimulates proliferation and differentiation of osteoblast and also enhances calcitonin secretion in the presence of estrogen. Poly(lactide-co-glycolide) (PLCA) due to its controllable biodegradability and relatively good biocompatibility is one of the most significant candidates for the study of drug controlled release system. In this study, IP-loaded PLGA microspheres (MSs) was prepared by using conventional O/W solvent evaporation method. The size of MSs was in the range of 5~200 $mu extrm{m}$. The morphology of MSs was characterized by SEM. And, in vitro release amounts of IP were analyzed by HPLC. The highest encapsulation efficiency were obtained by using gelatin and polyvinyl alcohol (PVA) as emulsifiers. The morphology, size distribution, and in vitro release pattern of MSs were changed by several preparation parameters such as molecular weights (8, 20, 33 and 90 kg/mol), polymer concentrations (2.5, 5, 10 and 20%), emulsifier types (PVA, gelatin and Tween 80), initial drug loading amount (5, 10, 20 and 30%) and stirring speed (250, 500 and 1000 rpm). The release of IP in vitro was more prolonged over 30 days, with close to zero-order pattern by controlling the preparation parameters. The physicochemical properties of IP-loaded PLGA MSs were investigated by XRD and DSC.

A New Bootstrap Simulation Method for Intermittent Demand Forecasting (간헐적 수요예측을 위한 부트스트랩 시뮬레이션 방법론 개발)

  • Park, Jinsoo;Kim, Yun Bae;Lee, Ha Neul;Jung, Gisun
    • Journal of the Korea Society for Simulation
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    • v.23 no.3
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    • pp.19-25
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    • 2014
  • Demand forecasting is the basis of management activities including marketing strategy. Especially, the demand of a part is remarkably important in supply chain management (SCM). In the fields of various industries, the part demand usually has the intermittent characteristic. The intermittent characteristic implies a phenomenon that there frequently occurs zero demands. In the intermittent demands, non-zero demands have large variance and their appearances also have stochastic nature. Accordingly, in the intermittent demand forecasting, it is inappropriate to apply the traditional time series models and/or cause-effect methods such as linear regression; they cannot describe the behaviors of intermittent demand. Markov bootstrap method was developed to forecast the intermittent demand. It assumes that first-order autocorrelation and independence of lead time demands. To release the assumption of independent lead time demands, this paper proposes a modified bootstrap method. The method produces the pseudo data having the characteristics of historical data approximately. A numerical example for real data will be provided as a case study.

Poloxamer 407 Hydrogels for Intravesical Instillation to Mouse Bladder: Gel-Forming Capacity and Retention Performance

  • Kim, Sang Hyun;Kim, Sung Rae;Yoon, Ho Yub;Chang, In Ho;Whang, Young Mi;Cho, Min Ji;Kim, Myeong Joo;Kim, Soo Yeon;Lee, Sang Jin;Choi, Young Wook
    • The Korean Journal of Urological Oncology
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    • 제15권3호
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    • pp.178-186
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    • 2017
  • Purpose: Poloxamer 407 (P407) thermo-sensitive hydrogel formulations were developed to enhance the retention time in the urinary bladder after intravesical instillation. Materials and Methods: P407 hydrogels (P407Gels) containing 0.2 w/w% fluorescein isothiocyanate dextran (FD, MW 4 kDa) as a fluorescent probe were prepared by the cold method with different concentrations of the polymer (20, 25, and 30 w/w%). The gel-forming capacities were characterized in terms of gelation temperature (G-Temp), gelation time (G-Time), and gel duration (G-Dur). Homogenous dispersion of the probe throughout the hydrogel was observed by using fluorescence microscopy. The in vitro bladder simulation model was established to evaluate the retention and drug release properties. P407Gels in the solution state were administered to nude mice via urinary instillation, and the in vivo retention behavior of P407Gels was visualized by using an in vivo imaging system (IVIS). Results: P407Gels showed a thermo-reversible phase transition at $4^{\circ}C$ (refrigerated; sol) and $37^{\circ}C$ (body temperature; gel). The G-Temp, G-Time, and G-Dur of FD-free P407Gels were approximately $10^{\circ}C-20^{\circ}C$, 12-30 seconds, and 12-35 hours, respectively, and were not altered by the addition of FD. Fluorescence imaging showed that FD was spread homogenously in the gelled P407 solution. In a bladder simulation model, even after repeated periodic filling-emptying cycles, the hydrogel formulation displayed excellent retention with continuous release of the probe over 8 hours. The FD release from P407Gels and the erosion of the gel, both of which followed zero-order kinetics, had a linear relationship ($r^2=0.988$). IVIS demonstrated that the intravesical retention time of P407Gels was over 4 hours, which was longer than that of the FD solution (<1 hour), even though periodic urination occurred in the mice. Conclusions: FD release from P407Gels was erosion-controlled. P407Gels represent a promising system to enhance intravesical retention with extended drug delivery.

Trend in Research and Development of Lithium Complex Hydrides for Hydrogen Storage (리튬계 수소저장재료의 연구개발 동향)

  • Shim, Jae-Dong;Shim, Jae-Hyeok;Ha, Heon-Phil
    • Korean Journal of Materials Research
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    • v.22 no.3
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    • pp.159-167
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    • 2012
  • Hydrogen is in the spotlight as an alternative next generation energy source for the replacement of fossil fuels because it has high specific energy density and emits almost no pollution, with zero $CO_2$ emission. In order to use hydrogen safely, reliable storage and transportation methods are required. Recently, solid hydrogen storage systems using metal hydrides have been under extensive development for application to fuel cell vehicles and fuel cells of MCFC and SOFC. For the practical use of hydrogen on a commercial basis, hydrogen storage materials should satisfy several requirements such as 1) hydrogen storage capacity of more than 6.5wt.% $H_2$, moderate hydrogen release temperature below $100^{\circ}C$, 3) cyclic reversibility of hydrogen absorption/desorption, 4) non toxicity and low price. Among the candidate materials, Li based metal hydrides are known to be promising materials with high practical potential in view of the above requirements. This paper reviews the characteristics and recent R&D trends of Li based complex hydrides, Li-alanates, Li-borohydrides, and Li-amides/imides.

Experimental Study on the Characteristics of Pressure Fluctuation in the Combustion Chamber with Branch Tube (분기관을 가진 연소 챔버 내 압력변동 특성에 관한 실험적 연구)

  • Park, Jang-Hee;Lee, Dae-Keun;Shin, Hyun-Dong
    • Transactions of the Korean Society of Mechanical Engineers B
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    • v.33 no.7
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    • pp.552-558
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    • 2009
  • An experimental study using the combustor with branch tube was conducted in order to model the industry combustor with FGR (flue gas recirculation) system and to study a thermo-acoustic instability generated by a branch tube. The branch tube is a structure used to modify a system geometry and then to change its pressure field, and the thermo-acoustic instability, usually occurs in a confined geometry, can result in serious problems on industrial combustors. Thus understanding of the instability created by modifying geometry of combustor is necessary to design and operate combustor with FGR system. Pressure fluctuation in the combustion chamber was observed according to diameter and length of branch and it was compared with the solution of 1-D wave equation. It was found that branch tube affects the pressure field in the combustion chamber, and the pressure fluctuation in the combustion chamber was reduced to almost zero when phase difference between an incipient wave in the combustion chamber and a reflected wave in the branch tube is $\pi$ at the branch point. Also, the reduction of pressure fluctuation is irrespective of the installed height of branch tube if it is below $h^*=0.9$ in the close-open tube and open-open tube.

Dispersion in the Unsteady Separated Flow Past Complex Geometries (복합지형상에서 비정상 박리흐름에 의한 확산)

  • Ryu, Chan-Su
    • Journal of the Korean earth science society
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    • v.22 no.6
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    • pp.512-527
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    • 2001
  • Separated flows passed complex geometries are modeled by discrete vortex techniques. The flows are assumed to be rotational and inviscid, and a new techlnique is described to determine the stream functions for linear shear profiles. The geometries considered are the snow cornice and the backward-facing step, whose edges allow for the separation of the flow and reattachment downstream of the recirculation regions. A point vortex has been added to the flows in order to constrain the separation points to be located at the edges, while the conformal mappings have been modified in order to smooth the sharp edges and to let the separation points free to oscillate around the points of maximum curvature. Unsteadiness is imposed to the flow by perturbing the vortex location, either by displacing the vortex from the equilibrium, or by imposing a random perturbation with zero mean to the vortex in equilibrium. The trajectories of passive scalars continuously released upwind of the separation point and trapped by the recirculating bubble are numerically integrated, and concentration time series are calculated at fixed locations downwind of the reattachment points. This model proves to be capable of reproducing the trapping and intermittent release of scalars, in agreement with the simulation of the flow passed a snow cornice performed by a discrete multi-vortex model, as well as with direct numerical simulations of the flow passed a backward-facing step. The results of simulation indicate that for flows undergoing separation and reattachment the unsteadiness of the recirculating bubble is the main mechanism responsible for the intense large-scale concentration fluctuations downstream.

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Effects of Soil Temperature on Biodegradation Rate of Diesel Compounds from a Field Pilot Test Using Hot Air Injection Process (고온공기주입 공법 적용시 지중온도가 생분해속도에 미치는 영향)

  • Park Gi-Ho;Shin Hang-Sik;Park Min-Ho;Hong Seung-Mo;Ko Seok-Oh
    • Journal of Soil and Groundwater Environment
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    • v.10 no.4
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    • pp.45-53
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    • 2005
  • The objective of this study is to evaluate the effects of changes in soil temperature on biodegradation rate of diesel compounds from a field pilot test using hot air injection process. Total remediation time was estimated from in-situ biodegradation rate and temperature for optimum biodegradation. All tests were conducted by measuring in-situ respiration rates every about 10 days on highly contaminated area where an accidental diesel release occurred. The applied remediation methods were hot air injection/extraction process to volatilize and extract diesel compounds followed by a bioremediation process to degrade residual diesels in soils. Oxygen consumption rate varied from 2.2 to 46.3%/day in the range of 26 to $60^{\circ}C$, and maximum $O_2$ consumption rate was observed at $32.0^{\circ}C$. Zero-order biodegradation rate estimated on the basis of oxygen consumption rates varied from 6.5 to 21.3 mg/kg-day, and the maximum biodegradation rate was observed at $32^{\circ}C$ as well. In other temperature range, the values were in the decreasing trend. The first-order kinetic constants (k) estimated from in-situ respiration rates measured periodically were 0.0027, 0.0013, and $0.0006d^{-1}$ at 32.8, 41.1, and $52.7^{\circ}C$, respectively. The estimated remediation time was from 2 to 9 years, provided that final TPH concentration in soils was set to 870 mg/kg.