• Title/Summary/Keyword: Release Times

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Preparation and In vitro Release Characteristics of Hydrophilic Albumin Microspheres Containing Methotrexate and Methotrexate-Human Serum Albumin Conjugates

  • Hwang, Sung-Joo;Lee, Myung-Gulll;Kim, Chong-Kook
    • Archives of Pharmacal Research
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    • v.15 no.2
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    • pp.162-168
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    • 1992
  • Release characteristics of five different types of hydrophilic albumin microspheres (HAM) containing different ratios of methotrexate-albumin (MTX-HSA) conjugates to free MTX: 1 : 0 (HAMC), 3 :1 (HAMC 3F), 1 :1 (HAMCF), 1:3 (HAMCF3) and 0 : 1 (HAMF) were investigated in the absence or presence of protease using dissolution tester. In all the HAMs studied except HAMC, the MTX was released bi-exponentially in the absence of protease; an initial fast release period up to approximately 6h, and thereafter the release rate was very much slower. The fast release of MTX from the HAMs (such as HAMC3F, HAMCF, HAMCF3 and HAMF) at the initial phase in probably due to the release of "physically associated" MTX from the core of the HAMs. The initial rate constants were 7.2, 8.7, 8.5 and 5.9 times greater than the second rate constants for HAMF, HAMCF3, HAMCF and HAMC3F, respectively. MTX release from HAMC was very slow and mono-phasic. It was at most 2.2% of the total entrapped amount by 24 h. The protease accelerated the release of MTX from the HAMs. The percentages of MTX released from HAMs up to 24 h were 100, 89.0, 75.0, 66.0 and 61.0% for HAMF, HAMCF3, HAMCF, HAMC3F and HAMC, respectively in the presence of protease and the corresponding values in the absence of protease were 30.2 19.0, 10.0, 6.5 and 2.2%, respectively. In vitro release of MTX in the presence of protease varied according to the ratios of MTX-HSA conjugates to MTX; the data set from HAMF, HAMCF3 and HAMCF fits better to monophasic first-order profile more adequately than to zero-order profile, that of HAMC3 monophasic first-order, and that of HAMC to bi-phasic zero-order. Above results suggested that zero-order release rate can be achieved by adjusting the ratio of MTX-HSA conjugates to MTX in the preparation of HAMs such as HAMC3F.as HAMC3F.

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The Study on Mucin Release by Airway Goblet Cells in Primary Culture

  • Yang, Ji-Sun;Kim, Ok-Hee;Roh, Yong-Nam;Yi, Sook-Young;Park, Ki-Hwan;Rheu, Hang-Mook
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1995.04a
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    • pp.89-89
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    • 1995
  • Surface epithelial cells isolated from hamster tracheas and grown on a thick collagen gel become a highly enriched population of mucus-secreting cells. Epithelial cells from tracheas of hamsters were collected using enzymatic procedures and cultured under various conditions. The medium used consisted of a 1:1 mixture of medium 199 and Dulbecco's modified Eagle's (DME) medium which was conditioned before use. Insulin, transferrin, hydrocortisone, epidermal growth factor, and extract from bovine hypothalamus were used as supplement. Due to relatively low basal rates of min secretion from in vitro cultures, cultures are generally radiolabeled using $^3$H-glucosamine as a metabolic precursor. The radiolabeled mucinsreleased are quantitated by precipitation with TCA/PTA. Using this cell culture system, we investigated mucin release of goblet cells by altering the media bathing the apical surface of hamster tracheal surface epithelial(HTSE) cells. Acidic media added sulfuric acid caused sigcificant increases in mucin relesse (155${\pm}$20% at pH 4 and 146${\pm}$16% at, pH 5). Ammonium hydroxide also increased mucin release at pH 9.0(156${\pm}$17%) and pH 10(295${\pm}$9%) respectively. This additional mucin release seems to be associated with cell membrane damage as indicated by release of cellular LDH. SP stimulates secretion of mucin in cultured HTSE cells(154${\pm}$16% at 1${\times}$10$\^$-6/M and 165${\pm}$25% at 1${\times}$10$\^$-5/M. PAF at 5${\times}$10$\^$-6/M and 5${\times}$10$\^$-5/M enhanced by HTSE cells in vitro 168${\pm}$34% and 259${\pm}$30% of mucin secretion, respectively. The increase in mucin release by PAF and SP was not secondary to cell damage or necrosis. SP and PAF may be in mediating mucous secretion induced by inflammation irritantion and infection.

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The Froude Scaling Study on the Ventilation of Non-isothermal Concentrated Fume from the Semi-closed Space (반밀폐형 공간에서 비등온 고농도 연무의 배연산출량 산정을 위한 Froude 상사연구)

  • Chang, Hyuk-Sang;Choi, Byung-Il;Park, Jae-Cheul;Kim, Myung-Bae
    • Journal of Korean Society of Environmental Engineers
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    • v.27 no.8
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    • pp.877-885
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    • 2005
  • The Froude scaling between the prototype and the model was tried to estimate the necessary ventilation rate for non-isothermal concentrated fume from the semi-closed inner space. Based on the non-dimensional similitude equations derived from the Zukoski plume rise analysis, the scaling experiments were done to verify the relationship of the non-dimensional energy release rate and the non-dimensional mass flow rate by using two different scaled volume models, model A ($1\;m{\times}1\;m{\times}1\;m$) and model B ($0.5\;m{\times}0.5\;m{\times}0.5\;m$). The experimental results showed that the theoretical similitude between the models is acceptable for the prediction of ventilation rate of the concentrated fume. The maximum energy release rate used for the experiments was $20\;kW/m^3$. In the experimental range, the similitude between the energy release rate and the ventilation mass flow rate was well defined and the necessary ventilation rates were 20-30% higher than the stoichiometric ventilation mass flow rate. Based on results of current study, the design of the local air ventilation system can be improved by correcting the effects of buoyancy and diffusion of the non-isothermal concentrated fume.

Effect of Myofascial Release Therapy on Newborns and Infants with Congenital Torticollis (근막이완술이 영유아 근성사경의 치료효과에 미치는 영향)

  • Park, Tae-Kyu;Kim, Jong-Ryul;Cho, Mi-Suk;Park, Rae-Joon
    • The Journal of Korean Physical Therapy
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    • v.18 no.5
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    • pp.1-11
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    • 2006
  • Purpose: This study was to evaluate effects of myofascial release therapy for newborns and infants with congenital torticollis. Methods: In a two month period, thirty-six newborns and infants diagnosed with congenital muscular torticollis received treatment thirty times; then divided into a myofascial release group and stretching group. Crying frequency was used to measure the amount of crying time during treatment. Ultrasonography was used to measure the size of fibromatosis. Physical examinations were used to measure the degree of head tilting and rotation. Results: The results were as follows: 1. Crying frequency was significantly decreased in myofascial degree group. 2. The size of fibromatosis was not significantly decreased in ultrasonography. 3. Head tilt was significantly decreased in myofascial release group. 4. Rotation was not significantly increased in myofascial release and control group. Conclusion: The above results suggest that myofascial release therapy is helpful decreasing head tilt, crying frequency, and increasing head rotation.

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A Economic Effects of Fish Seed Release (수산종묘방류사업의 경제성 평가)

  • Hwang Jin-Wook;Lee Kwon-Hyuk;Jeong Dal-Sang;Kim Kwang-Soo
    • The Journal of Fisheries Business Administration
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    • v.36 no.1 s.67
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    • pp.121-138
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    • 2005
  • This study was conducted to investigate the economic effect of the release of seed flounder to the central area of the West Sea, which was analyzed into both direct and indirect effects. The results showed that based on the data collected from partial area, the economic effect of flounder seed release reached 6.97 times, average catch proportion was 32.27$\%$, and recapture rate was 11.26$\%$, suggesting that economic effect was very high. In addition, it was observed that the recapture rate was greatly higher than 2.05$\%$, that of Break-Even-Point. It was noted that the increased catch by the release of seed flounder resulted in the increase in commission of sales and the increase in sports fishing. Another economic effect observed were diverse including the increase in income of fishing village, elevated spirit to proper management of fisheries resources, maintaining of willingness to live in fishing village through activation of local fishing village, prevention of illegal fishing including capture of juvenile fish, and the increase in the supply of sea food of high quality. It is emphasized that although the investigation was conducted in the same area, the results will vary by size at release, time at release and other factors. Finally, there is a need to expand species and area of study for more active economic analysis incorporating natural sciences.

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A Heuristic for Parallel Machine Scheduling with Due Dates and Ready Times (납기와 조립가능 시점을 고려한 병렬기계의 스케쥴링을 위한 발견적 해법)

  • 이동현;이경근;김재균;박창권;장길상
    • Journal of the Korean Operations Research and Management Science Society
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    • v.25 no.2
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    • pp.47-57
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    • 2000
  • In this paper we consider an n-job non-preemptive and identical parallel machine scheduling problem of minimizing the sum of earliness and tardiness with different release times and due dates. In the real world this problem is more realistic than the problems that release times equal to zero or due dates are common. The problem is proved to be NP-complete. Thus a heuristic is developed to solve this problem To illustrate its suitability a proposed heuristic is compared with a genetic algorithm for a large number of randomly generated test problems. Computational results show the effectiveness and efficiency of proposed heuristic. In summary the proposed heuristic provides good solutions than genetic algorithm when the problem size is large.

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The Formulation and Bioavailability of Oral Sustained Release Sulindac Delivery System (설린닥의 경구용 지속성 제제설계 및 생체이용율)

  • Rhee, Gye-Ju;Park, Sun-Hee;Whang, Sung-Joo
    • YAKHAK HOEJI
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    • v.41 no.1
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    • pp.60-73
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    • 1997
  • In order to design a 24 hr sustained release preparation of sulindac for oral administration, fast release pellet (FR), slow release pellet (SR) and two combined formulation (1 : 1 and 1 : 2) were prepared. The pharmacokinetic effect of such preparations has been evaluated using rabbits as a suitable in vivo model, and tested in man. Dose determination was carried out using curve fitting according to RSTPJP II program. In bioavailability test using rabbit, AUCs of sulindac in a few designed formulations were similar to each other. $C_{max}$- of RF and SR were 1.8 times and 1.2 times higher, respectively, compared to that of combined formulation (FR:SR=1:1). While plasma concentration of FR and SR decreased rapidly, that of combined formulation (FR:SR 1:1) lasted at the level close to $C_{max}$ for 24 hrs. Plasma concentration of sulfide form from the combined pellet(FR:SR=1:1) lasted for 24 hrs, and its AUC value was 1.4-fold, 2.7-fold. and 1.2-fold greater than FR pellet, SR pellet and combined pellet (FR:SR 1 : 2). Thus, the combined pellet of 1:1 ratio was found to be the most effective for oral sustained release formulation. Bioavailability test in human showed that AUC of sulfide from TSRP (1 : 1) was approximately 1.5 times greater than total AUC of Immbaron$^{\circledR}$ administered twice in a day. While $T_{max}$ of sulfide from lmmbaron$^{\circledR}$ was 4.33 +/- 1.37 hr (lst administration) and 3.33 ${pm}$ 0.82 hr (2nd administration), respectively, that of sulfide from TSRP increased to 7.17 ${pm}$ 2.86 hr. Plasma concentration of sulfide from TSRP was sustained at more, than 1.0 ${\mu}g{\cdot}$hr/ml until 24 hrs after one dose administration. In addition, TSRP may decrease local adverse reaction in the stomach, since plasma concentration of sulfide from the combined pellet was low within 2hrs in the stomach. In conclusion, it is suggested that TSRP formulation may be effective for oral 24 hr sustained release formulation of sulindac dosing 300 ~ 350mg once a day.

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Controlled Release Dosage Form of Narcotic Antagonist(I): Synthesis of Biodegradable Polyphosphazenes and Preparation and Release Characteristics of Naloxone Implant (마약길항제의 방출 제어형 제제 (제1보) : 생체분해성 polyphosphazenes의 합성과 나록손 이식제제의 제조 및 용출특성)

  • Park, Joo-Ae;Lee, Seung-Jin;Kim, Hyung-Kuk;Kim, Kil-Soo
    • Journal of Pharmaceutical Investigation
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    • v.25 no.2
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    • pp.109-116
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    • 1995
  • For the administration of narcotic antagonist with short half-life and low patient compliance, the sustained release system using biodegradable matrix is effective. Polyphosphazenes are of considerable interest as biodegradable matrix systems for controlled release of drugs. In this study, biodegradable polyphosphazenes available for the sustained release implantable device were synthesized, and their application was examined. Poly[dichlorophosphazene] was synthesized by solution polymerization method and confirmed with IR spectrum. Poly[bis(ethyl glycinate) phosphazene] and poly[ (diethyl glutamate)-co-(ethyl glycinate)phosphazene] were then produced by substitution of amino acid alkyl esters for chloride side groups. Using these polymers, the implantable devices of 1 mm thickness and $10{\times}10\;mm$ size containing naloxone hydrochloride were prepared and their release and degradation profiles were measured. In the case of poly[bis(ethyl glycinate)phosphazene] with swelling characteristics, degradation rate was slower than the release rate, showing that the release rate is partly dependent on the swelling rate. In contrast, the degradation rate of polyl[(diethyl glutamate)-co-(ethyl glycinate)phosphazene] matrix was identical with release rate of naloxone hydrochloride. On the basis of these results, it is expected that these polymers can be applied to sustained release implantable systems delivering narcotic antagonist.

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Release of 5-Fluorouracil from Ethylene-Vinyl Acetate Matrices Containing Hydrophilic Additives (수용성 첨가제를 함유하는 에틸렌초산비닐 매트릭스로부터 5-플루오로우라실의 방출)

  • Oh, Seaung-Youl;Yoo, Young-Mee;Kim, Sung-Soo;Shin, Byung-Chul;Yuk, Soon-Hong;Lee, Hai-Bang
    • Journal of Pharmaceutical Investigation
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    • v.26 no.4
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    • pp.281-289
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    • 1996
  • In our previous work, we have studied the effect of lactose and sodium alginate (SA) on the rate of release of 5-fluorouracil (5-FU) from ethylene-vinyl acetate (EVA) matrix. These hydrophilic additives promoted the rate of 5-FU release and the increase in rate was larger when SA was used. Both additives showed better ability to increase the rate than 5-FU itself. In this paper, we extended our study to another hydrophilic additive, Carbopol 940 (CP). Compared to SA or lactose, CP increased the rate of 5-FU release markedly. Release rate increased as the loading amount and the pH of the release medium increased. After release experiment, matrix volume increased up to 15 times of that before release experiment, depending on the amount of CP dispersed in the matrix and the pH of the release medium. On the other hand, the volume of the matrix containing lactose or SA decreased. The weight changes of the dry matrix before and after release experiment imply that CP is not released out of the matrix, to the contrary of lactose and SA. Scanning electron microscope study clearly showed that large cavities and pores are generated on the surface and the inside of the matrix. These results indicate that the mechanism by which CP increases the release rate is quite different from that of monomeric additives such as lactose or SA.

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A Study on the Surface Finish of Concrete Corresponding to Aluminum Form (알루미늄 거푸집을 이용한 모의구조체의 표면 마감성에 관한 연구)

  • Kim, Tae-Cheong;Lee, Dong-Gyu;Baek, Dae Hyun;Han, Min-Cheol;Han, Cheon-Goo
    • Proceedings of the Korean Institute of Building Construction Conference
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    • 2008.05a
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    • pp.47-50
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    • 2008
  • This study analyzed the effect of increasing the number of times using aluminum form to the surface quality of concrete through small sized test, and the result was summarized as following. At the early stage, there was no remarkable change between aluminum and coated plywood form, and the surface quality of concrete both forms slightly declined corresponding with increasing the number of times using.As void on the surface corresponding to the number of times, the voids ranged 0.1~1mm were increased corresponding to increasing the number of times using forms, and the other range voids were also increased according to increasing the number of times using forms. It was confirmed that the surface of concrete was damaged gradually. For comparison with aluminum and coated plywood form though this experimental results, there might be no difference, if release agent was used properly.

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