• Journal of Pharmaceutical Investigation
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• 제22권3호
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• pp.205-210
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• 1992

In order to develop a controlled-release oral drug delivery system (DDS) of theophylline (TP), microporous membrane-coated tablets were prepared and evaluated in vitro and in vivo. Rapidly water-soluble core tablets of TP (300 mg) were prepared by wet granulation and compression technique, Then the core tablets were spray-coated with polyvinylchloride (PVC) in which micronized sucrose particles were dispersed. Effect of formula compositions of coating suspensions on the pharmaceutical characteristics such as membrane strength and dissolution was investigated in vitro. The membranes remained unbroken in pH 1.2 buffer at $37^{\circ}C$ at least for 2 hours after the disintergration test. TP was released from the coated-released tablets at a zero-order rate over 8 hours. The release at pH 1.2 and 4.0 was similar in rate but a little more rapid than that at pH 6.8. The coated tablets were administered to three healthy male volunteers and their saliva profiles of TP were compared with those from the commercial sustained release TP tablets such as Slobid and Asconthin. Saliva TP concentrations from the coated tablets were successfully sustained over 48 hours after the dosing and were comparable to those of the commercial sustained-release tablets. The membrane-coating technique is very simple and does not need any sophisticated equipments. In this respect, the membrane-coated tablets may be superior to the commercial sustained-release tablets and this technique is worth adopting by the pharmaceutical industries.

• KSBB Journal
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• 제11권6호
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• pp.676-680
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• 1996

키토산을 10%-아세트산에 팽윤시킨 용액과 SD 를 인산염 완충용액에 녹인 용액을 흔합하여 키토산 매트릭스를 제조하였다. 키토산 매트릭스로부터 pH 7 7.4와 pH 1.2에서 약물방출 거통을 규명하고 지속적이고 조절된 약물방출형 제제로서의 사용 가능성 을 고찰하였다. 키토산 매트릭스내의 약물 함유량이 증가함에 따 라 약물 방출 시간이 늦어졌으며, pH 1.2에서보다 p pH 7.4에서 약물 방출 시간이 더 지연되었다. 그 이 유는 약물전달체가 엽기성 용액에서보다 산성 용액 에서 팽윤를 더 잘하기 때문이라고 생각된다. 약물 방출 속도에 있어서는 pH 7.4에서보다 pH 1.2에서 더 빨랐으며, 겉보기 방출속도상수(K)값도 역시 증가하였다. 결과적으로 본 실험에셔 약물전달체로 사 용된 키토산은 방출조절형 제제로서 그 가능성을 타진할 수 있었다.

• 한국화재소방학회논문지
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• 제31권5호
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• pp.19-27
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• 2017

밀폐된 구획실 화재에서 화원의 면적 및 위치, 화재성장률, 구획 체적의 변화가 열발생률을 포함한 주요 화재특성에 미치는 영향이 검토되었다. 이를 위해 닫힌 개구부가 적용된 ISO 9705 화재실을 대상으로 Fire Dynamics Simulator (FDS)를 활용한 화재시뮬레이션이 수행되었다. 주요 결론으로서, 화원의 면적 및 위치의 변화는 최대 열발생률, 총 열량, 상층부의 최대 온도 및 화학종 농도를 포함한 구획 내의 열적 특성과 화학적 특성에 큰 영향을 주지 않음을 확인하였다. 그러나 화재성장률과 구획 체적의 증가는 최대 열발생률 및 총 열량의 증가를 가져오며, 한계산소농도의 감소 및 최대 CO 농도의 증가를 발생시킨다. 마지막으로 화재성장률과 구획 체적의 함수로 표현된 최대 열발생률의 상관식을 도출하여, 밀폐된 구획실 화재에 대한 화재성장곡선의 적용을 위한 방법론이 제안되었다.

• 약학회지
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• 제58권4호
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• pp.245-249
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• 2014

Murrayafoline-A (1-methoxy-3-methylcarbazole) is a monomeric carbazole alkaloid found in Murraya euchrestifolia HAYATA and Glycosmis stenocarpa. We have recently shown that murrayafoline-A has positive inotropic effect in isolated rat ventricular myocytes. To know possible mechanisms for the positive inotropic effect of murrayafoline-A we examined the effects of murrayafoline-A on in situ behavior of cardiac $Ca^{2+}$ release units ('$Ca^{2+}$ sparks') and sarcoplasmic reticulum (SR) $Ca^{2+}$ loading using confocal $Ca^{2+}$ imaging method in single rat ventricular myocytes. Murrayafoline-A significantly increased the frequency (events/($10^3{\mu}m^2{\cdot}s$)) of $Ca^{2+}$ sparks in a concentration-dependent manner, with an $EC_{50}$ of $28{\pm}6.4{\mu}M$ and a maximal ~twofold change. The $Ca^{2+}$ content in the SR, measured as caffeine (10 mM)-induced $Ca^{2+}$ transient, was significantly increased by murrayafoline-A (${\approx}$116% and ${\approx}$123% of control at 25 and 100 ${\mu}M$, respectively). In addition, murrayafoline-A significantly increased the fractional $Ca^{2+}$ release, suggesting increase in the efficacy of $Ca^{2+}$ release at given SR $Ca^{2+}$ loading. These results suggest that murrayafoline-A may enhance contractility via increase in $Ca^{2+}$ release from the SR through the ryanodine receptors in ventricular myocytes.

• 대한의생명과학회지
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• 제12권2호
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• pp.57-63
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• 2006

Deazaadenosine analogs such as 3-deazaadenosine (DZA), 3-deazaaristeromycin (DZAri) and ara-3-deazaadenine (DZAra-A) were developed as inhibitors of S-adenosylhomocysteine (Ado-Hcy) hydrolase (EC 3.3.1.1). These analogs were reported to induce apoptosis in human and murine leukemic cells. But, the mechanism involved in this apoptosis was not clarified yet. In the present study, we analyze the apoptosis induced by deazaadenosine analogs in human cervival cancer cell line, HeLa and the effect of Bcl-2 on this apoptosis. Whereas neither DZAri nor DZAra-A showed inhibitory effect on HeLa cell growth, DZA induced apoptosis in HeLa cells accompanied by cytochrome c release and activation of various caspases such as caspase-2,-8,-9 and -3. In HeLa-bcl-2 cell line, a stable transfectant of HeLa cell to overexpress Bcl-2, cytochrome c release, activation of all these caspases and the resulted apoptosis by DZA were completely prevented. By in vitro assay of cytochrome c release, in addition, DZA induced cytochrome c release from purified mitochondria of HeLa-pcDNA3 cells, but not HeLa-bcl-2 cells, even in the absence of cytosolic fraction. Therefore, it can be suggested that DZA might damage directly mitochondria leading to activate intrinsic pathway of caspase and thus induce apoptosis. DZA-induced apoptosis in HeLa cells may be in a bcl-2-inhibitable manner and irrelative of Ado-Hcy hydrolase.

• The Korean Journal of Pain
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• 제13권1호
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• pp.60-66
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• 2000

Background: For terminal cancer pain management, controlled-release oral morphine (morphine sulfate tablet, MST) is a simple and convenient regimen. Recently, fentanyl transdermal therapeutic system (F-TTS, transdermal fentanyl) has been developed and became one of the alternative ways of providing adequate pain relief. This open prospective study was designed to compare the analgesic efficacy and safety of MST and transdermal fentanyl in the management of terminal cancer pain. Methods: In this open comparative and randomized study, 64 terminal cancer patients received one treatment for 15 days, controlled-release oral morphine (MST group) or fentanyl transdermal therapeutic system (F-TTS group). Daily diaries about the vital sign, visual analogue scale (VAS) for pain, opioids requirement, co-anagesics, adjuvant drugs and adverse effects were completed with 24 patients in MST group, 18 patients in F-TTS group. Results: The majority of patients in both treatment groups were late-stage cancer and their distribution was not different in both groups. Daily opioids requirement was 126.4 mg in MST uced in F-TTS group (P<0.05). The incidence of nausea, vomiting and constipation was lower in F-TTS group (P<0.05). Patients satisfaction was similar, but F-TTS patient group favored continous use of same treatment compared with MST group after the study was finished. Conclusions: Transdermal fentanyl seems to be safe and similar analgesic effect to controlled-release oral morphine for the control of the terminal cancer patients. However, transdermal fentanyl provides a simpler and more convenient especially in respect to constipation, nausea & vomiting. To determine the exact analgesic effect, cost-effectiveness and complications, controlled trials should be followed.

• Nuclear Engineering and Technology
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• 제26권1호
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• pp.90-99
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• 1994

손상 핵연료에서 발생하는 주요한 현상중의 하나는 수중기의 분해로 갭에 존재하는 산소에 의해 $UO_2$ 가 $UO_{2+}$x/로 산화되고, 이로 인해 결정립내에서의 핵분열기체 확산계수가 증가하여 결과적으로 핵분열 기체의 방출이 증대하는 현상이다. 본 논문은 일반적인 원자로 운전 조건하에서 원자로 및 손상 핵연료의 운전조건을 고려하여 소결체의 산화거동을 모사하고 이를 바탕으로 소결체 산화가 핵분열기체의 방출 중대에 미치는 영향을 분석하였다. 소결체 산화거동은 갭에는 150기압의 포화된 순수한 수증기만이 존재한다는 가정하에 분석하였고, 산화에 의한 핵분열기체의 방출 증대 효과를 정량적으로 분석하기 위해 방출중대 인자를 도입하였다. 실험 치와 비교한 결과 방출증대 인자는 소결체 산화에 의한 핵분열기체의 방출증대 효과를 잘 예측하였다.

• Journal of Pharmaceutical Investigation
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• 제41권6호
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• pp.363-369
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• 2011

In this study, we demonstrated the release behavior of carvedilol with the content of polyvinylpyrrolidone K-30 (PVP K-30) and the effect of citric acid and fumaric acid as acidifiers on the release behavior of drug. In addition, it tries to inquire into the release behavior difference of the carvedilol according to the manufacturing method. The release behavior of the tablets was compared with Dilatrand$^{(R)}$ in the simulated gastric fluid (pH1.2). Differential scanning calorimeter (DSC), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FT-IR) were characterized for the physicochemical properties of the tablets. In case of mixing the carvedilol and PVP K-30, in case the ratio of the carvedilol and PVP K-30 was 1:5, the release behavior was the highest among. As well as the dissolution rate of tablets manufactured by lyophilization and rotary evaporator was higher than physical mixture. The dissolution rate of containing acidifiers was more improved. But, rather the excessive amount of the acidifier addition reduced the dissolution rate.

• 공업화학
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• 제29권2호
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• pp.147-154
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• 2018

현재 항암제의 낮은 치료 효율과 부작용을 해결하기 위해 고분자 기반의 약물전달체의 연구가 활발하게 진행되고 있다. 기존의 고분자기반의 약물 전달체는 우수한 결과를 보이는 등 상당한 진전이 있었음에도 불구하고, 대부분 혈중에서 안정성이 감소하여 표적 부위에 도달하기 전에 약물이 방출될 뿐만 아니라 오랜 시간 동안에 약물을 방출함으로써 부작용 및 낮은 치료 효율을 초래한다는 문제점을 가지고 있다. 본 총론에서는 이러한 비효율적인 약물 방출의 문제점을 개선하기 위한 방법으로 독성이 없고 생체 적합한 천연 고분자 키토산에 자극 응답성 물질을 도입하여 혈중에서 안정성을 높이고 표적 부위에서 약물을 과다 방출하여 치료 효율을 극대화할 수 있는 방법을 제시하고자 한다.

• 접착 및 계면
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• 제12권4호
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• pp.144-150
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• 2011

폴리스티렌을 저수축제로 사용하고 Zn-stearate를 이형제로 사용하여 함량변화에 따라 벌크 몰드컴파운드의 표면형태 및 기계적 물성에 미치는 영향을 고찰하였다. XPS, 접촉각 측정기 등을 이용하여 표면과 깊이 방향에 대한 원소함량과 접촉각을 측정하였고, 표면형태는 FESEM을 이용하여 관찰하였으며, 표면조도 측정은 AFM을 이용하였다. 저수축제를 첨가하지 않은 경우에 비교하여 저수축제를 9.0 wt% 첨가하였을 경우에는 체적수축률은 0.35%에서 0.05%로 감소하였으며, 표면조도는 $0.27{\mu}m$에서 $0.12{\mu}m$로 감소하였다. 이형제의 함량을 1.8 wt%에서 3.6 wt%로 증가시켰을 경우에는 이형제가 주로 표면에 존재하고 표면조도를 증가시키는 것을 확인하였다. 저수축제의 함량을 5.0 wt%에서 9.0 wt%로 증가시킴에 따라 굴곡탄성율과 충격강도가 약 30% 감소하였다.