• Title/Summary/Keyword: penetration enhancement

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Transmucosal Delivery of Luteinizing Hormone Releasing Hormone(LHRH): Evaluation of Membrane Permeability Enhancement of $[D-Ala^6]$ LHRH in Rabbit Mucosa and Ovulation Inducing Effect in Vaginal Administration of Rat by the Addition of Several Absorption Enhancers (황체호르몬 유리호르몬의 경점막 수송: 수종의 흡수촉진제를 사용한 $[D-Ala^6]$ LHRH의 점막투과촉진 및 흰쥐에 있어서의 배란유도효과 향상)

  • Han, Kun;Jeong, Nam-Joo;Park, Jeong-Sook;Park, Hee-Beom;Chung, Youn-Bok;Moon, Dong-Cheul
    • YAKHAK HOEJI
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    • v.38 no.4
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    • pp.440-450
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    • 1994
  • Due to the limited bioavailability of $[D-Ala^6]$LHRH from nonparenteral transmucosal sites of administration, enhancement of mucosal permeability by coadministration of several protease inhibitors and/or penetration enhancers were studied in rabbit mucosa. As a reliable bioassay method for $[D-Ala^6]$LHRH, ovulation-inducing effect were measured after vaginal administration in the rat. The permeation of $[D-Ala^6]$LHRH through the mucosal membrane of rabbit mounted on George-Grass diffusion cells were examined in the presence of polyoxyethylene 9-lauryl ether (POE), ${\beta}$-cyclodextrin$({\beta}-CyD)$ or ethylene diamine tetra acetate disodium salt(EDTA). The vaginal membrane showed higher permeability of $[D-Ala^6]$LHRH than the rectal and nasal membrane. POE and ${\beta}-CyD$ showed a small promoting effect on the membrane permeation of $[D-Ala^6]$LHRH, but EDTA showed significant enhancement. Ovaluation was enhanced by the coadministration of sodium laurate(0.5%), a protease inhibitor but was not enhanced by EDTA, a penetration enhancer. On the other hands, coadministration of sodium tauro 24,25 dihydrofusidate(1%) and EDTA(2%) enhanced the ovulation inducing-effect 2.8 times. These results suggest that the vaginal administration of $[D-Ala^6]$LHRH with STDHF or sodium laurate as a protease inhibitor, and EDTA as a penetration enhancer, may become an elective method for transmucosal delivery of $[D-Ala^6]$ LHRH.

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Penetration behavior of biopolymer aqueous solutions considering rheological properties

  • Ryou, Jae-Eun;Jung, Jongwon
    • Geomechanics and Engineering
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    • v.29 no.3
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    • pp.259-267
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    • 2022
  • The rheological and penetration characteristics of sodium alginate and xanthan gum aqueous solutions were analyzed for the development of biopolymer-based injection materials. The results of viscosity measurements for the rheological characteristics analysis show that all aqueous biopolymer solutions exhibit a tendency for shear-thinning, i.e., the apparent viscosity decreases as the shear rate increases. In addition, a regression analysis using several models (Power-law, Casson, Sisko, and Cross) was applied to the shear-thinning fluid analysis results, the highest accuracy was determined by applying the power-law model. The micromodel experiment for the penetration characteristics analysis determined that all biopolymer aqueous solutions show higher pore saturation than water, and that pore saturation tends to increase as the flow rate and concentration increases. When comparing the rheological and penetration characteristics of the biopolymer aqueous solution used in this study, the xanthan gum aqueous solution showed a fully developed shear-thinning tendency, unlike the sodium alginate aqueous solution. This tendency is considered to have the advantage of enhancement injectability and pore saturation.

The Effect of Enhancers on the Penetration of Clenbuterol through Hairless Mouse Skin (클렌부테롤의 피부투과에 미치는 경피흡수촉진제의 영향)

  • Choi, Han-Gon;Rhee, Jong-Dal;Yu, Bong-Kyu;Yong, Chul-Soon
    • Journal of Pharmaceutical Investigation
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    • v.33 no.1
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    • pp.29-36
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    • 2003
  • Clenbuterol, a selective ${\beta}_2-adrenergic$ receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic obstructive bronchial disease, chronic bronchitis and pulmonary emphysema. The percutaneous permeation of clenbuterol was investigated in hairless mouse skin after application of 50/50 buffer(pH 10)/propylene glycol solvent mixture. The enhancing effects of various penetration enhancers such as terpenes, non-ionic surfactants, pyrrolidones, fatty acids and some other enhancers on the permeation of clenbuterol were evaluated using Franz diffusion cell. Among terpenes studied, 1,8-cineole was the most effective enhancer, which increased the permeability of clenbuterol approximately 39.33-fold compared with the control without penetration enhancer, followed by menthone with enhancement ratio of 23.57. Nonionic surfactants did not have significant enhancing effects. N-Lauryl-2-pyrrolidone increased the permeability of clenbuterol approximately 4.51-fold compared with the control. Lauric acid increased the permeability of clenbuterol approximately 35.57-fold with decreasing the lag time from 2.64 to 0.52 hr. Oleic acid, linoleic acid, linolenic acid and capric acid showed enhancement ratio of 22.62, 19.60, 17.45 and 16.51, respectively. $Labrafil^{\circledR}$ enhanced the permeability of clenbuterol 9.24-fold compared with that without enhancer.

Micro-Grids Reliability Enhancement Under Different Penetration Levels of Hybrid DG Units

  • Essam, M.;Atwa, Y.M.;El-Saadany, Ehab F.;Conti, Stefania;Rizzo, Santi Agatino
    • Journal of Electrical Engineering and Technology
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    • v.13 no.4
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    • pp.1407-1418
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    • 2018
  • Novel mechanism of customized adequacy formulation is proposed in order to enhance micro grids system reliability. The mechanism accounts for 2-levles of load curtailment, and is mainly based on probabilistic load profile and hybrid Distributed Generation (DG) units modeling. The two load curtailments are needed in order to ensure adequate technical constraints at steady state condition during islanding mode of operation. The effectiveness of the proposed formulation has been verified using system independent analytical expressions for the evaluation of both reliability and Expected Energy Not Served (EENS) indices. The evaluation has examined the impact of different penetration levels of Hybrid DG Units in case study islands. Results show the enhancement of the overall distribution system reliability and the recommended conditions for successful islanding mode of operation.

Semi-Empirical Analysis of the Mass Transfer Characteristics of the Slug Flow in Vertical Mesoscale Tubes (작은 수직관을 흐르는 슬러그 유동의 물질전달 특성에 대한 반경험적 해석)

  • Kim, Dong-Seon
    • Korean Journal of Air-Conditioning and Refrigeration Engineering
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    • v.26 no.8
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    • pp.366-374
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    • 2014
  • Experimental mass transfer data, which were obtained for the $CO_2$-water slug flows in vertical tubes with 2, 5, and 8mm diameters, were analyzed in comparison with the penetration theory. It was found that a penetration model with molecular diffusion coefficient cannot predict the experimental data accurately. An effective diffusion coefficient, which considers enhancement effect of interfacial waves, was suggested to improve prediction. Another empirical factor was also suggested to consider the effect of non-uniform interface velocity. A modified penetration model was found to be capable of predicting the experimental data reasonably well.

Groutability enhancement by oscillatory grout injection: Verification by field tests

  • Kim, Byung-Kyu;Lee, In-Mo;Kim, Tae-Hwan;Jung, Jee-Hee
    • Geomechanics and Engineering
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    • v.18 no.1
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    • pp.59-69
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    • 2019
  • Grout injection is mainly used for permeability reduction and/or improvement of the ground by injecting grout material into pores, cracks, and joints in the ground. The oscillatory grout injection method was developed to enhance the grout penetration. In order to verify the level of enhancement of the grout, field grout injection tests, both static and oscillatory tests, were performed at three job sites. The enhancement in the permeability reduction and ground improvement effect was verified by performing a core boring, borehole image processing analysis, phenolphthalein test, scanning electron microscopy analysis, variable heat test, Lugeon test, standard penetration test, and an elastic wave test. The oscillatory grout injection increased the joint filling rate by 80% more and decreased the permeability coefficient by 33-68%, more compared to the static grout injection method. The constrained modulus of the jointed rock mass was increased by 50% more with oscillatory grout injection compared to the static grout injection, indicating that the oscillatory injection was more effective in enhancing the stiffness of the rock mass.

Effect of Vehicles and Penetration Enhancers onthe Percutaneous Absorption of Ketorolac Tromethamine across Hairless Mouse Skin

  • Cho, Young-Ah;Gwak, Hye-Sun
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.234.1-234.1
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    • 2003
  • The effects of vehicles and penetration enhancers on the in vitro permeation of ketorolac tromethamine (KT) across excised hairless mouse skins were investigated. Among pure vehicles examined, propylene glycol monolaurate (PGML) showed the highest permeation flux, which was 94.3${\pm}$17.3 mg/cm$^2$/hr. Even though propylene glycol monocaprylate (PGMC) alone did not show high permeation rate, the skin permeability of DT was markedly increased by the addition of diethylene glycol monoethyl ether (DGME); the enhancement factors were 19.0 and 17.1 at 20 and 40% of DGME, respectively. (omitted)

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Development of Reactor Vessel Head Penetration Performance Demonstration System in Korea (국내 원자로 상부헤드관통관 기량검증 기술개발)

  • Kim, Yongsik;Yoon, Byungsik;Yang, Seunghan
    • Transactions of the Korean Society of Pressure Vessels and Piping
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    • v.10 no.1
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    • pp.44-50
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    • 2014
  • There were many flaw issues of reactor vessel head penetration in USA fleets. USNRC issued 10CFR50.55a to implement reactor vessel head penetration ultrasonic examination performance demonstration(PD) in US for enhancement of inspection reliability. After September 2009, all US utilities inspected their RVHP with PD qualified system. Korea Hydro and Nuclear Power Company(KHNP) have developed reactor vessel head penetration performance demonstration system for ultrasonic test to apply for pressurized light-water reactor power plants in accordance with 10CFR50.55a since September 2011. RVHP configuration surveying and analysis, code requirement analysis, and performance demonstration specimen design were performed up to this day. Fingerprinting of manufactured specimen, development of test data management program, development of operation procedure, input of flawed data, and development of final report will be performed for the next step. This paper describes the development status of the performance demonstration system for reactor vessel head penetration ultrasonic examination in Korea.

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.

Effect of Polyoxyethylene Alkyl Esters on Permeation Enhancement and Impedance of Skin

  • Kim, Hee-Sun;Oh, Seaung-Youl
    • Biomolecules & Therapeutics
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    • v.19 no.1
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    • pp.109-117
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    • 2011
  • In this work, we have investigated the effect of polyoxyethylene alkyl ester nonionic surfactants on percutaneous permeation enhancement of a model drug, ketoprofen. We also investigated the mechanism involved in the enhancement using impedance and solubility measurement. Three groups of nonionic surfactants with different ethylene oxide content were studied. The permeation results showed that all surfactants enhanced the percutaneous absorption, irrespective of the molecular weight. The permeation results from PEG-45 monostearate (PEGMS45) were rather unexpected. Impedance and solubility results indicate that the mechanism involved in the enhancement of permeation by PEG-10 monooleate (PEGMO10) and PEGMS45 is rather different. The results from PEGMS45 suggest that it could be a potential candidate as a skin penetration enhancer with high molecular weight, which may poses less skin irritation and systemic side effect than the smaller surfactant molecules. Overall, this work provided some useful information on percutaneous transport enhancement and the mechanistic insights involved in skin permeation for these nonionic surfactants.