• Archives of Pharmacal Research
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• 제24권6호
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• pp.568-571
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• 2001

The purpose of this work was to study the effect of storage time and temperature on the in vitro release kinetics of a commercial sustained-release dosage form of theophylline, at different pHs of the dissolution medium. The formulation was stored at $35^{\circ}C$ for 16 months and at $45^{\circ}C$ for 8 months, with a relative humidity of 60%. The in vitro release tests were performed at pHs 2, 4, 6 and 7.4. The mean values of the transport coefficient n, were close to 0.5 in all the conditions tested, which indicates that the transport system is not modified after storage of the formulation at $35^{\circ}C$ and $45^{\circ}C$. The mean values of the dissolution rate constant ranged from 0.036 to 0.043 $min^{-n}$, under all the conditions tested. Significant differences (${\alpha}=0.05$) were found between pHs 2, 4 and 6, 7.4 for all the model-independent parameters studied. When the formulation was kept at $35^{\circ}C$ for 16 months, the mean percentage of drug dissolved at 8 hours was 25.61% (pHs 2, 4) and, 36.12% (pHs 6, 7.4), representing a 26% and 24% reduction, respectively. Simitar results were obtained after storing the formulation at $45^{\circ}C$ for 8 months, corresponding to 33.3% (pHs 2, 4) and, 22.5% (pHs 6, 7.4) diminution, respectively. The values of the similarity factory $f_2$, obtained were lower than 50, which indicates the lack of similarity among the dissolution profiles, after storing the formulation under the experimental Conditions tested.

• 대한의용생체공학회:의공학회지
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• 제23권3호
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• pp.189-196
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• 2002

피부를 통한 약물 전달 방법은 국소 병변 부에 직접적으로 약물을 전달할 수 있는 장점을 가졌으나 피부의 가장 바깥 층인 각질층의 장벽기능으로 인해 약물 전달 능력에 제한이 있다. 본 연구에서는 산소 압력 방법과 초음파 방법을 결합하는 방법을 시도하여 약물 전달 능력의 향상 정도를 검증해 본다. 흡수 물질로는 수분을 사용하였고 수분의 흡수도를 측정하기 위해 피부 임피던스 방법을 선택하였다. 실험은 총 42명을 대상으로 각각 대조군(13명) 초음파군(13명), 산소 압력군(6명). 초음파와 산소압력 결합군(10명)으로 나누어서 시행하였다. 각 군마다 다른 약물 전달방법을 손등 부위에 적용하여 20분간 피부 임피던스 변화를 측정 한 값을 PC에 저장하였다. 수분을 적용한 대조군의 경우 피부 임피던스의 변화가 거의 일어나지 않고. 초음파를 적용한 군과 산소를 적용한 군은 수분을 적용한 군보다 25-30배정도 높은 수분 홉수를 보였으며. 초음파와 산소 압력을 결합한 방법은 수분을 적용한 군보다 70배정도 높은 수분 흡수를 보였다. 이러한 평균의 타이를 반복 측정된 분산방법(Repeated Measures Analysis of Variance)의 다변량 검증과 다중비교를 통해 변화량간의 차이를 검증하여 유의성을 확인하였다

• Journal of Pharmaceutical Investigation
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• 제2권1호
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• pp.18-30
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• 1972

Renal pathways for excretion of sulfadiazine has been studied by standard clearance technique in the rabbit. 1. Large part of sulfadiazine filtered in the glomeruli is reabsorbed in the tubules, as visualized from the fact that Csd (clearance of sulfadiazine) amounts only a fraction of simultaneously measured Ccr (GFR). 2. Csd changed linearly with the rate of urine flow, whether it is increased by the duir etics or decreased by clamping u reter. 3. Csd remained unchanged until the plasma level of the Csdremained unchanged drug reached 10.0 mg%, and the amount transported in the tubules increased linearly with the increase in the load, exhibiting No maximum capacity for transport. 4. Csd was increased by 2,4-dinitrophenol which is an uncoupling agent of oxidative phosphorylation and decreased by probenecid which is on uricosuric agent. 5. During sodium bicarbonate infusion net secretion of sulfadiazine by tubules observed. All the evidences obtained in the rabbit indicated that sulfadiazine was reabsorbed by active, energy-requiring, or passive, simple diffusion, process, and secreted simultaneously by a probenecid-sensitive, active procss.

• Journal of Advanced Marine Engineering and Technology
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• 제21권2호
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• pp.126-135
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• 1997

Drag reduction in polymer solutions is the phenomenon where by extremely dilute solutions of high molecular weight polymers exhibit frictional resistance to flow much lower than the pure solvent. This effect, largely unexplained as yet, has attracted the attention of polymer scientists and fluid flow specialists. Although applications are beginning to appear, the principle interest to data has been in attempting to relate the effect to the fluid mechanics of turbulent flow. Drag reduction in two phase flow can be applied to the transport of crude oil, phase change system such as chemical reactor, and pool and boiling flow. But the research on drag reduction in two phase flow is not intensively investigated. Therefore, experimental investigations have been carried out to analyze the drag reduction produced by polymer addition in the single phase and two phase flow system. The objectives of the proposed investigation are primarily in identifying and developing high performance polymer additives for fluid transportations with the benefits of turbulent drag. Also we want to is to evaluate the drag reduction in horizontal flow by measuring pressure drop and mean velocity. Experimental results show higher drag reduction using co - polymer(A611P) then using polyacrylamide (PAAM) and faster degradation using PAAM than using A611P under the same superficial velocity.

• BMB Reports
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• 제51권2호
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• pp.59-64
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• 2018

The airway epithelium is the first place, where a defense mechanism is initiated against environmental stimuli. Mucociliary transport (MCT), which is the defense mechanism of the airway and the role of airway epithelium as mechanical barriers are essential in innate immunity. To maintain normal physiologic function, normal oxygenation is critical for the production of energy for optimal cellular functions. Several pathologic conditions are associated with a decrease in oxygen tension in airway epithelium and chronic sinusitis is one of the airway diseases, which is associated with the hypoxic condition, a potent inflammatory stimulant. We have observed the overexpression of the hypoxia-inducible factor 1 (HIF-1), an essential factor for oxygen homeostasis, in the epithelium of sinus mucosa in sinusitis patients. In a series of previous reports, we have found hypoxia-induced mucus hyperproduction, especially by MUC5AC hyperproduction, disruption of epithelial barrier function by the production of VEGF, and down-regulation of junctional proteins such as ZO-1 and E-cadherin. Furthermore, hypoxia-induced inflammation by HMGB1 translocation into the cytoplasm results in the release of IL-8 through a ROS-dependent mechanism in upper airway epithelium. In this mini-review, we briefly introduce and summarize current progress in the pathogenesis of sinusitis related to hypoxia. The investigation of hypoxia-related pathophysiology in airway epithelium will suggest new insights on airway inflammatory diseases, such as rhinosinusitis for clinical application and drug development.

• 동의생리병리학회지
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• 제24권6호
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• pp.903-906
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• 2010

The spleen is the source of gi, blood, body fluid and plays a vital role in maintaining life. The function of the spleen is to transform food nutrients and water, and to transport them to the heart and the lung. The movement of splenic gi is marked by elevation. The spleen governs the activity of elevating the lucid. The function of transportation and transformation is usually disturbed in the state of Gi deficiency of the spleen. The main clinical manifestations of gi deficiency of the spleen can be divided into as followers: anorexia, loose stool if the digesting and absorbing functions are disturbed; phlegm and edema if dampness and water are retained due to unhealthy water metabolism. Sagunja-tang can be applied for gi deficiency syndrome of the spleen. Ingredient bakchul(Rhizoma Atractylodis Macrocephalae) and bokryeung(Poria) can be used as monarch drug to eliminate dampness and strengthen the spleen.

• Journal of Pharmaceutical Investigation
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• 제37권5호
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• pp.311-314
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• 2007

Paclitaxel (PTX) is an antineoplastic agent approved for the treatment of ovarian and breast carcinomas. However, the use of paclitaxel as an anticancer drug is limited by its extremely poor water solubility (below $0.3\;{\mu}g/mL$). Furthermore, it has very low bioavailability when administered orally because paclitaxel is a substrate of P-glycoprotein (P-gp) efflux pump. In this study, buccal delivery of PTX was investigated as one of the alternatives for PTX delivery. Ethanol and glyceryl monooleate (GMO) were selected as permeation enhancing agents to increase solubility and permeation across buccal mucosa of PTX. At the different concentrations of ethanol solution ($30{\sim}70\;w/w\;%$), PTX permeation was studied, followed effects of GMO in the concentration range of $2.5{\sim}25%$ with ethanol vesicle. The transbuccal ability of PTX was evaluated in vitro using Franz diffusion cells mounted with rabbit buccal mucosa. As a result, incorporation of PTX into ethanol vesicle with GMO significantly enhanced the PTX permeation in rabbit buccal mucosa. Particularly, the mixtures of ethanol:water:GMO at the ratio of 50:47.5:2.5 showed the most excellent enhancing ability. The results showed a promising possibility for buccal delivery of PTX.

• 한국수정란이식학회지
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• 제25권4호
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• pp.273-279
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• 2010

Follicular cystic follicles (FCFs) show delayed regression with persistent follicle growth. However, the mechanism by which follicles are persistently grown remains unclear. Glutathione S-transferases (GSTs) are drug-metabolizing and detoxification enzymes that are involved in the intracellular transport and metabolism of steroid hormones. In this study, a proteomic analysis was performed to identify whether GST expression is changed in bovine FCFs and to predict the interactions between GST and other proteins. Normal follicles and FCFs were classified based on their sizes (5 to 10 mm and 25 mm). In bovine follicles, GST mu 1 (GSTM1) was detected as a differentially expressed protein (DEP) and significantly up-regulated in FCFs compared to normal follicles (p<0.05). Consistent with the proteomic results, semi-quantitative PCR data and western blot analysis revealed an up-regulation of GSTM1 in FCFs. Expression levels of aromatase and dehydrogenase proteins were changed in FCFs. These results show that the up-regulation of GSTM1 that is observed in bovine FCFs is likely to be responsible for the persistent follicle growth in FCFs as the activity of aromatase and the dehydrogenases.

• Archives of Pharmacal Research
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• 제28권8호
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• pp.988-994
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• 2005

The purpose of the present study was to prepare multivesicular liposomes with a high drug loading capacity and to investigate its potential applicability in the oral delivery of a peptide, human epidermal growth factor (rhEGF). The multivesicular liposomes containing rhEGF was prepared by a two-step water-in-oil-in-water double emulsification process. The loading efficiency was increased as rhEGF concentration increased from 1 to 5mg/mL, reaching approximately $60\%$ at 5 mg/mL. Approximately $47\%$ and $35\%$ of rhEGF was released from the multivesicular liposomes within 6 h in simulated intra-gastric fluid (pH 1.2) and intra-intestinal fluid (pH 7.4), respectively. rhEGF-loaded multivesicular liposomes markedly suppressed the enzymatic degradation of the peptide in an incubation with the Caco-2 cell homogenate. However, the transport of rhEGF from the multivesicular liposomes to the basolateral side of Caco­2 cells was two times lower than that of the rhEGF in aqueous solution. The gastric ulcer healing effect of rhEGF-loaded multivesicular liposomes was significantly enhanced compared with that of rhEGF in aqueous solution; the healing effect of the liposomes was comparable to that of the cimetidine in rats. Collectively, these results indicate that rhEGF-loaded multivesicular liposomes may be used as a new strategy for the development of an oral delivery system in the treatment of peptic ulcer diseases.

• Mass Spectrometry Letters
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• 제8권2호
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• pp.34-38
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• 2017

The purpose of this study was to develop a cocktail approach for the measurement of the permeability of marker compounds, caffeine and propranolol (high permeability), ofloxacin (intermediate), atenolol (low), and quinidine (P-glycoprotein substrate), simultaneously. Then we compared the permeability in Caco-2 cells with that in rat intestinal segments. The difference between individual measurement and cocktail approach was less than 20 %, and the permeabilities of these compounds were similar to those previously reported, suggesting that the cocktail transport study and simultaneous drug analysis were successfully developed and validated in this study. Additionally, in the application of this cocktail method, the permeability of five drugs in rat jejunum was similar to that in ileum but different from that in colon, which was measured using the Ussing chamber system. Moreover, permeability in jejunum and ileum was similar to that in Caco-2 cells. In conclusion, the permeability in Caco-2 cells was equivalent to the permeability in rat jejunum and ileum determined with the Ussing system. Therefore, this newly developed cocktail assay and its application to the Ussing system can be a useful tool for robust and rapid screening for site-specific permeability in rat intestine, thus accelerating the prediction of absorption of new chemical entities.