• 제목/요약/키워드: derivative method

검색결과 1,090건 처리시간 0.036초

타이레놀이알서방정(아세트아미노핀 650 mg)에 대한 타이리콜이알정의 생물학적동등성 (Bioequivalence of Tylicol ER Tablet to Tylenol® ER Tablet (Acetaminophen 650 mg))

  • 강현아;김동호;박선애;윤화;김경란;박은자;조혜영;이용복
    • Journal of Pharmaceutical Investigation
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    • 제36권3호
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    • pp.201-207
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    • 2006
  • Acetaminophen (paracetamol), a para-aminophenol derivative, has analgesic and antipyretic properties and weak anti-inflammatory activity. The purpose of the present study was to evaluate the bioequivalence of two acetaminophen tablets, $Tylenol^{\circledR}$ ER (Janssen Korea Ltd.) and Tylicol ER (Hana Pharmaceutical Co., Ltd.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The release of acetaminophen from the two acetaminophen formulations in vitro was tested using KP VIll Apparatus II method with pH 1.2 buffer solution. Twenty six healthy male subjects, $22.8{\pm}1.99$ years in age and $65.6{\pm}8.03$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After a single tablet containing 650 mg as acetaminophen was orally administered, blood samples were taken at predetermined time intervals and the concentrations of acetaminophen in serum were determined using HPLC with UV detector. The dissolution profiles of two formulations were similar in pH 1.2 buffer solution. The pharmacokinetic parameters such as $AUC_t$, $C_{max}$ and $T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t$, $C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, $Tylenol^{\circledR}$ ER, were 2.84, 1.89 and -1.36% for $AUC_t$, $C_{max}$ and $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log 0.8 to log 1.25 (e.g., log $0.987{\sim}log$ 1.08 and log $0.944{\sim}log$ 1.17 for $AUC_t$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Tylicol ER tablet was bioequivalent to $Tylenol^{\circledR}$ ER tablet.

HPLC/UV-vis을 이용한 과일류 중의 지베렐린 산 분석 (Analysis of gibberellic acid from fruits using HPLC/UV-vis)

  • 마경나;조현우;명승운
    • 분석과학
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    • 제26권1호
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    • pp.19-26
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    • 2013
  • 자외선 흡광도가 거의 없는 농작물의 생장 조절용 농약으로 사용되고 있는 지베렐린(GAs) 중 하나인 지베렐린 산($GA_3$)은 발색단이 미약해서 자외선 검출기를 이용하여 분석하기가 어려운 물질이다. 액체-액체 추출법을 이용하여 과일류로부터 지베렐린 산을 효과적으로 추출하기 위하여 시료의 pH와 추출용매에 대한 최적의 추출조건을 확립하고자 하였다. 페나실 브로마이드를 유도체화 시약으로 사용함으로써 자외선 검출기에 선택적이며 감도가 좋은 $GA_3$-유도체 화합물을 만들었으며, 최적의 유도체화 조건을 확립하기 위해서 반응온도 및 시간, 유도체화 시약의 양, 염기의 양 등을 변화시켜주는 실험이 수행되었다. 유도체화 된 $GA_3$는 C18 컬럼을 사용하여 방해물질이 없이 HPLC/UV-vis로 효과적으로 분석되었으며, HPLC/ESI-MS를 사용하여 유도체화된 화합물의 구조를 확인하였다. 사과의 경우, 검출한계(LOD)와 정량한계(LOQ)는 각각 0.008 mg/kg, 0.027 mg/kg로, 배의 경우, 검출한계(LOD)와 정량한계(LOQ)는 각각 0.003 mg/kg, 0.012 mg/kg로 낮은 검출한계와 정량한계를 보였다. 확립된 유도체화 방법은 과일류 중에 존재하는 $GA_3$의 효과적이고 편리한 분석에 응용될 수 있을 것이다.

Nanopharmaceutical Approach for Enhanced Anti-cancer Activity of Betulinic Acid in Lung-cancer Treatment via Activation of PARP: Interaction with DNA as a Target -Anti-cancer Potential of Nano-betulinic Acid in Lung Cancer-

  • Das, Jayeeta;Samadder, Asmita;Das, Sreemanti;Paul, Avijit;Khuda-Bukhsh, Anisur Rahman
    • 대한약침학회지
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    • 제19권1호
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    • pp.37-44
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    • 2016
  • Objectives: This study examined the relative efficacies of a derivative of betulinic acid (dBA) and its poly (lactide-co-glycolide) (PLGA) nano-encapsulated form in A549 lung cancer cells in vivo and in co-mutagen [sodium arsenite (SA) + benzo[a]pyrene (BaP)]-induced lung cancer in mice in vivo. Methods: dBA was loaded with PLGA nanoparticles by using the standard solvent displacement method. The sizes and morphologies of nano-dBA (NdBA) were determined by using transmission electron microscopy (TEM), and their intracellular localization was verified by using confocal microscopy. The binding and interaction of NdBA with calf thymus deoxyribonucleic acid (CT-DNA) as a target were analyzed by using conventional circular dichroism (CD) and melting temperature (Tm) profile data. Apoptotic signalling cascades in vitro and in vivo were studied by using an enzyme-linked immunosorbent assay (ELISA); the ability of NdBA to cross the blood-brain barrier (BBB) was also examined. The stage of cell cycle arrest was confirmed by using a fluorescence-activated cell-sorting (FACS) data analysis. Results: The average size of the nanoparticles was ~ 110 nm. Confocal microscopy images confirmed the presence of NdBA in the cellular cytoplasm. The bio-physical properties of dBA and NdBA ascertained from the CD and the Tm profiles revealed that NdBA had greater interaction with the target DNA than dBA did. Both dBA and NdBA arrested cell proliferation at G0/G1, NdBA showing the greater effect. NdBA also induced a greater degree of cytotoxicity in A549 cells, but it had an insignificant cytotoxic effect in normal L6 cells. The results of flow cytometric, cytogenetial and histopathological studies in mice revealed that NdBA caused less nuclear condensation and DNA damage than dBA did. TEM images showed the presence of NdBA in brain samples of NdBA fed mice, indicating its ability to cross the BBB. Conclusion: Thus, compared to dBA, NdBA appears to have greater chemoprotective potential against lung cancer.

지역특산주류 소비자 구매 결정 요인분석 (An Analysis of Consumer Purchasing Decision Determinants on Local Liquors)

  • 유재은;최종우
    • 산경연구논집
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    • 제10권6호
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    • pp.39-50
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    • 2019
  • Purpose - Since the local liquor industry uses the agricultural products produced in the region as the main raw material, cultivation of the industry can be a way to expand the demand for domestic agricultural products and can contribute to the income increase of the farmers. In addition, the local liquor industry can be developed into a region-specific industry differentiated from other regions by linking with the region's tourism resources. Therefore, in order to achieve various derivative effects through promotion of the local liquor industry, it is necessary to precisely understand the factors related to the purchase and consumption of local liquor which then will lead to an increase in consumption. This study analyzes the current status and problems of local liquor industries and examines the determinants of consumers' purchasing decisions of regional specialties through questionnaires. We will then propose a strategy to promote consumption of locally produced alcoholic beverages. Research design, data, and methodology - An online Domestic Consumer Survey was conducted to identify the actual purchases and uses of local liquors for 500 consumers nationwide. Based on the questionnaire results, the analysis uses an ordered probit model. Results - As a result of analyzing the effect of consumer characteristics on the purchase of local liquors, it was found that the average cost of drinking, income, local specialty, brewery experience, and health concerns have a significant effect on gender, drinking frequency. All the variables except the participation in the training of the special provincial manufacturing method were found to be statistically significant. The statistical significance was at a 1% significance level for the remaining factors excluding the bottle design. This shows that the higher taste, quality, price, and harmony with food, the higher the probability of purchasing local liquors. Conclusions - In the analysis of factors influencing the purchase intention of local liquors, it was found that factors such as taste, quality, price, and harmony with food had a significant effect. Given the diversity of purchasing factors, the importance of diversification strategies is emphasized again. In particular, it will be important to secure wide publicity for local liquors through various PR strategies.

가바펜틴 800밀리그람 정제의 생물학적동등성시험 (Bioequivalence Test of Gabapentin 800 mg Tablets)

  • 김세미;신새벽;강현아;조혜영;이용복
    • 약학회지
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    • 제52권4호
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    • pp.299-305
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    • 2008
  • Gabapentin, 1-(aminomethyl) cyclohexaneacetic acid, is a amino acid derivative, and is clinically effective in the treatment of neuropathic pain and partial seizures of epilepsy as a complementary therapy. The purpose of the present study was to evaluate the bioequivalence of two gabapentin tablets, $Neurontin^{R}$ tablet 800 mg (Pfizer Pharmaceuticals Co., Ltd.) and Gabapenin tablet 800 mg (Hanmi Pharm. Co., Ltd.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The release of gabapentin from the two gabapentin formulations in vitro was tested using KP VIII Apparatus II method with 0.06 M HCI dissolution media. Twenty six healthy male subjects, $23.85{\pm}2.24$ years in age and $69.40{\pm}11.11$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ crossover study was employed. After a single tablet containing 800 mg as gabapentin was orally administered, blood samples were taken at predetermined time intervals and the concentrations of gabapentin in serum were determined using HPLC with fluorescence detector. The dissolution profiles of two formulations were similar in the tested dissolution media. The pharmacokinetic parameters such as $AUC_{t}$, $C_{max}$ and $T_{max}$ were calculated, and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_{t}$, $C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, $Neurontin^{R}$, were 1.28%, 0.63% and 0.62% for $AUC_{t}$, $C_{max}$ and $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log 0.8 to log 1.25 (e.g., $log0.9097{\sim}log1.1598$ and $log0.8919{\sim}log1.1262$ for $AUC_{t}$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Gabapenin tablet 800 mg was bioequivalent to $Neurontin^{R}$ tablet 800 mg.

선체운동 예측을 이용한 Dynamic Positioning System의 피드포워드 제어 알고리즘에 관한 연구 (A Study on the Feedforward Control Algorithm for Dynamic Positioning System Using Ship Motion Prediction)

  • 송순석;김상현;김희수;전마로
    • 해양환경안전학회지
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    • 제22권1호
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    • pp.129-137
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    • 2016
  • 본 연구의 목적은 가까운 미래의 선박운동정보를 이용하는 피드포워드 제어알고리즘과 FPSO 운동 수치 시뮬레이션 모델을 개발하고 시뮬레이션을 통하여 제어알고리즘의 성능을 검증하는 것이다. 본 논문에서는 조류, 바람, 파력 등의 환경하중에 의하여 발생한 선체운동의 미래 예측치를 활용한 피드포워드 제어력을 추가적으로 가지는 Dynamic Positioning System에 대하여 연구한다. 먼저, 조류력, 풍력 및 파력에 대한 수학모델을 선정하여 환경하중에서의 선체운동을 계산하고, 현재의 선체운동 값과 Brown 지수평활 예측모형을 활용하여 미래 선체운동 값을 예측하였다. 또한 위치 유지와 Heading angle 제어를 위한 제어력을 PID(Proportional-Integral-Derivative)이론을 이용하여 결정한 피드백 제어기와 미래 선체운동 값을 이용하여 결정한 피드포워드 제어기로 구성하였다. 그리고 각 Thruster에 요구되는 추력은 라그랑지승수법을 활용하여 분배하였다. 마지막으로 FPSO(Floating Production Storage and Offloading)의 운동과 Dynamic Positioning System에 대한 시뮬레이션 모델을 구축하여 선박의 위치 및 Heading angle 제어에 관한 시뮬레이션을 수행하여 제안하는 피드백 제어기와 피드포워드 제어기를 동시에 가지는 제어시스템의 성능을 평가하였다. 본 연구의 결과, 피드백 및 피드 포워드 제어기가 적용된 DPS 제어시스템이 기존의 피드백 제어기보다 위치유지 및 헤딩각 유지 능력에서 개선되었고 각 Thruster에 요구되는 평균 제어력 및 최대 제어력의 크기도 감소함을 보였다. 이에 따라 DPS에 요구되는 동력 감축과 Azimuth Thruster 용량의 감소로 인하여 비용 절감의 효과를 기대할 수 있다.

임의의 잡음 신호 추가를 활용한 적대적으로 생성된 이미지 데이터셋 탐지 방안에 대한 연구 (Random Noise Addition for Detecting Adversarially Generated Image Dataset)

  • 황정환;윤지원
    • 한국정보전자통신기술학회논문지
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    • 제12권6호
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    • pp.629-635
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    • 2019
  • 여러 분야에서 사용되는 이미지 분류를 위한 딥러닝(Deep Learning) 모델은 오류 역전파 방법을 통해 미분을 구현하고 미분 값을 통해 예측 상의 오류를 학습한다. 엄청난 계산량을 향상된 계산 능력으로 해결하여, 복잡하게 설계된 모델에서도 파라미터의 전역 (혹은 국소) 최적점을 찾을 수 있다는 것이 장점이다. 하지만 정교하게 계산된 데이터를 만들어내면 이 딥러닝 모델을 '속여' 모델의 예측 정확도와 같은 성능을 저하시킬 수 있다. 이렇게 생성된 적대적 사례는 딥러닝을 저해할 수 있을 뿐 아니라, 사람의 눈으로는 쉽게 발견할 수 없도록 정교하게 계산되어 있다. 본 연구에서는 임의의 잡음 신호를 추가하는 방법을 통해 적대적으로 생성된 이미지 데이터셋을 탐지하는 방안을 제안한다. 임의의 잡음 신호를 추가하였을 때 일반적인 데이터셋은 예측 정확도가 거의 변하지 않는 반면, 적대적 데이터셋의 예측 정확도는 크게 변한다는 특성을 이용한다. 실험은 공격 기법(FGSM, Saliency Map)과 잡음 신호의 세기 수준(픽셀 최댓값 255 기준 0-19) 두 가지 변수를 독립 변수로 설정하고 임의의 잡음 신호를 추가하였을 때의 예측 정확도 차이를 종속 변수로 설정하여 시뮬레이션을 진행하였다. 각 변수별로 일반적 데이터셋과 적대적 데이터셋을 구분하는 탐지 역치를 도출하였으며, 이 탐지 역치를 통해 적대적 데이터셋을 탐지할 수 있었다.

전자유압 비례밸브와 경사센서를 이용한 농용 프론트 로더 버켓 능동수평유지 시스템 개발 (Development of a self-leveling system for the bucket of an agricultural front-end loader using an electro hydraulic proportional valve and a tilt sensor)

  • 이창주;하종우;최덕수;김학진
    • 드라이브 ㆍ 컨트롤
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    • 제12권4호
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    • pp.60-70
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    • 2015
  • A front-end loader (FEL) mounted on an agricultural tractor is one of the most commonly used implements for farm work. However, when the tractor carries material using the bucket attached to the FEL on a sloping ground, the materials can spill or roll back over the operator due to the tilted body, thereby requiring the bucket surface to remain level at a constant value regardless of varying slopes. In this study, an active system for controlling the angle of the FEL bucket on a tractor based on the real-time measurement of ground slopes was developed to enable the bucket to constantly remain level. A FEL simulator operated based on an electro hydraulic proportional valve (EHPV) was constructed in the laboratory to develop a proportional-integral-derivative (PID) controller forming a virtual electronic control unit (ECU) on the computer, which could automatically adjust the bucket angles depending on varying input angles while sending SAE-J1939 associated messages via CAN BUS to the EHPV. The different parameter values for the PID controller due to the gravity effect of the bucket were determined using a manual PID tuning method while assuming that the tractor travels on either an ascending slope or a descending slope. The developed PID control-based self-leveling system showed a mean of steady-state errors of within $1^{\circ}$ and a mean of delayed times of ~ 0.8s when the step input of $+20^{\circ}$ was given, implying that the developed system and control algorithm would be effective in maintaining the bucket angle at a certain value. Future studies include the improvement of the control algorithm to reduce such a time delay as well as the application of the developed algorithm to the FEL mounted on a tractor tested at a testing ground.

UWB 시스템의 성능개선을 위한 TDMG 펄스 발생기의 성능과 구조에 관한 연구 (A Study on TDMG Pulse Performance and Structure for Performance Improvement of UWB system)

  • 고영은;방성일
    • 정보처리학회논문지C
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    • 제11C권3호
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    • pp.395-400
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    • 2004
  • 본 논문에서는 급증되는 무선통신 서비스의 요구에 맞추어 제안된 UWB 시스템 중 반송파를 사용하지 않은 단일 밴드 UWB 시스템용 임펄스를 제안하였다. 기존의 UWB 시스템의 펄스로 제안된 펄스들의 특성과 문제점을 분석하였고, 이를 토대로 펄스폭의 감쇄기술 없이 초광대역의 신호를 발생시키는 TDMG(Time Delay Multiple Gaussian) 펄스를 제안하였다. 제안한 펄스를 수학적으로 전개하였고, 이를 바탕으로 단일밴드 UWB 시스템용 TDMG 펄스 발생기의 하드웨어 구조를 모델링 하였다. 제안한 TDMG 펄스는 컴퓨터 모와 실험을 통해 기존에 제안되었던 펄스의 성능과 비교하였다. 그 결과 기존의 펄스보다 TDMG 펄스가 중심주파수는 약 1GHz이상 높은 대역으로 이동하였고, l0dB fractional bandwidth는 약 1GHz 이상 넓어졌다. 또 n차로 미분한 경우에도 TDMG 펄스의 중심주파수가 각각 1GHz정도 높은 대역으로 이동하였고, 10dB fractional bandwidth도 각각 1GHz 이상 넓어졌다. 즉 기존에 제안된 펄스보다 TDMG 펄스가 주파수 특성도 우수하고, FCC가 권고한 주파수 대역과 스펙트럼 특성을 만족함으로서 다른 이동 무선 통신시스템과의 간섭이 감소한 것을 확인할 수 있었다.

수술후 통증관리를 위한 Buprenorphine의 지속적 경막외 투여효과 (Effects of Continuous Epidural Infusion of Buprenorphine for Postoperative Pain Management)

  • 윤희동;박영철;임혜자
    • The Korean Journal of Pain
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    • 제9권1호
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    • pp.151-158
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    • 1996
  • Background: Buprenorphine, a new synthetic thebaine derivative, is a partial agonist of the opioid $\mu$-receptor with high receptor affinity, great lipid solubility, and slow rate of opiate receptor association and dissociation. Continuous epidural infusion of opioid can possibly produced undesirable effects, such as respiratory depression, pruritus, etc, in spite of effective postoperative analgesia. Methods: The present study was undertaken to compare the analgesic properties and side effects of continuous epidural infusion of buprenorphine combined with bupivacaine, and morphine combined with bupivacaine in 90 patients following elective gynecologic lower abdominal surgery. At the end of surgery, the initial bolus doses were 3 mg morphine (M group), 0.15 mg buprenorphine (0.15B group), 0.3 mg buprenorphine (0.3B group) combined with 0.25% bupivacaine 10ml, and subsequent continuous infusion doses were 6 mg morphine plus 0.125% bupivacine 100 ml (M group) and 0.6mg buprenorphine plus 0.125% bupivacaine 100 ml (0.15B, 0.3B, group) during 48 hours. The assessment of analgesic efficacy and side effects were made at arrival of recovery room, 1 hr, 4 hr, 8 hr, 24 hr, 36 hr, and 48 hr after the epidural injection. Results: The pain score during 48 hours was significantly higher in the 0.15B group than in the M group and 0.3B group (P<0.05), and the number of patients requiring additional analgesics was significantly higher in the 0.15B group than in the M group and 0.3B group (P<0.05). Signs of respiratory depression were not noted, and the incidence of pruritus, nausea, and vomiting was slightly lower in the 0.15B group and 0.3B group than in the M group, and the incidence of sedation and urinary retention was similar in three group. The subjective rating of satisfaction was better in the 0.3B group than in the M group and 0.15B group (P<0.05). Conclusion: The above results suggest that continuous epidural infusion of buprenorphine combined with low-dose bupivacaine is an advisable method of postoperative analgesia.

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