• 대한한의학회지
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• 제28권2호통권70호
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• pp.126-136
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• 2007

Objectives : In the present study, the effect of Kuwonsimsin-hwan (KSS) was tested in methotrexate (MTX)-induced immunosuppressed SD rats. Methods : Methotrexate was fed to white rats once a day for 4 days. After the immune responses of the rats deteriorated, dried extracts of Kuwonsimsin-hwan mixed in water was fed to the rats once a day for 14 days. We then measured the number of lymphocytes in peripheral blood and the percentage of B-cells, T-cells, CD3+CD4+T-cells, CD3+CD8+ T-cells and IL-2 productivity sampled from spleen and peripheral region. Results : (1) The number of lymphocytes and the percentage of T-cells and CD3+CD4+ T-cellsin peripheral blood increased significantly in the KSS group as compared with the control group. (2) The percentage of B-cells, CD3+CD8+ T-cells, and CD4+/CD8+ T-cells in peripheral blood were not different statistically. (3) The percentage of T-cells in spleen and IL-2 productivity of spleen cells increased significantly in the KSS group as compared with the control group. (4) The percentage of CD3+CD4+ T-cells in spleen increased in KSS the group as compared with the control group but without statistical significance. (5) The percentage of B-cells, CD3+CD8+ T-cells, and CD4+/CD8+ T-cells in spleen were not different statistically. Conclusion : It is concluded that Kuwonsimsin-hwan has immunostimulating effect on MTX-induced immunosuppressed SD rats.

• 대한한방소아과학회지
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• 제22권1호
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• pp.123-147
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• 2008

Objectives This study is to investigate how dose Ikhwang-San can be effective on SD rats which deteriorated immunity caused by methotrexate. Methods The test sample were dosed once a day for 14 days by gastric gavage at the beginning of dosage 1000, 500 and 250㎎/㎏/10㎖ from 2 days after last MTX-dosing, and the changes of the body and spleen weight, total number of blood leukocytes, total number of lymphocytes, the percentage of B-cell, T-cell, CD3+CD4+ T-cell, CD3+CD8+ T-cell and CD4+/CD8+ T-cell ratios in the blood and spleen were observed. Results The changes of the body and spleen weight, the total number of blood leukocytes, the total number of lymphocyte in the blood and spleen were significantly increased in IHS Extracts groups comparing with the control group. The percentage of B-cell, T-cell, CD3+CD4+ T-cell in the blood and spleen were significantly increase in IHS groups and comparing with the control group. The ratio of CD4+/CD8+ T-cell in blood and spleen was significantly increased in IHS Extracts groups comparing with the control group. Conclusions According to those results, Ikhwang-San has good immunostimulating effect on SD rats which had deteriorated immunity caused by methotrexate.

• 한국응용과학기술학회지
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• 제30권2호
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• pp.251-257
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• 2013

Methotrexate의 영향은 혼탁매질에서 형광체, 산란체와 응흡수체에 의해 파장과 산란된 형광 세기로 규명되는데, laser induced fluorescence(LIF) 분광학에 의해 분자특성으로 나타난다. 산란매질에서 광학적 효과는 광학적 파라미터들((${\mu}_s$, ${\mu}_a$, ${\mu}_t$)에 의해 표현되고 응집은 고-액상 분리공정에서 중요하게 활용되고 있다. 따라서 입자가 서로 접근될 때 콜로이드 입자들의 상호작용을 LIF와 응집효과로 분석하였다. 산란계수는 산란매질, L-${\alpha}$-Phosphatidylcholine의 농도가 증가함에 따라 산란 광학적 파라미터가 증가하였으나 흡수 파라미터는 감소하였다. 광학적 파라미터들은 레이저 광원에서 검출기까지 깊이의 함수에 의해 깊이가 깊어짐에 따라 산란세기가 기하급수적으로 감소함을 알 수 있다. 이는 유지화학, 생의학 생성물, 레이저 의학, 의공학 분야적용에 LIF와 입자이동 현상은 아주 적합한 모델 연구에 큰 도움이 될 것이다.

• 대한한방소아과학회지
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• 제21권1호
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• pp.227-252
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• 2007

Objectives : In order to investigate the effect of Bobitang on SD rats with deteriorated immunity caused by methotrexate. Methods : The test sample were dosed once a day for 14 days by gastric gavage at a dosage 1,000, 500 and $250mg/kg/10m{\ell}$ from 2 days after last MTX-dosing, and the changes on body weight and gains, spleen weight and total blood leukocyte numbers, total lymphocyte numbers, the percentage of B-cell, T-cell, CD3+CD4+ T-cell, CD3+CD8+ T-cell and CD4+/CD8+ T-cell ratios in the blood and spleen were observed. Results : The changes on body weight gains, the spleen weight, the total blood leukocyte numbers, the total lymphocyte numbers in the blood and spleen, the ratio of T-cell in the blood and spleen, the ratio of CD3+CD4+ T-cell in the blood and spleen were increased significantly in BBT Extracts groups as compared with control group. The ratio of B-cell in the blood and spleen was not increased significantly in BBT Extracts groups as compared with control group. The percentage of CD3+CD8+ T-cell in the blood and spleen was decreased significantly in BBT Extracts groups as compared with control group. The ratio of CD4+/CD8+ T-cell in blood and spleen was increased significantly in BBT Extracts group as compared with control group. Conclusions : According to the above results, Bobi-Tang has an effect of increasing immune responses on SD rats with deteriorated immunity caused by methotrexate.

• 한국임상약학회지
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• 제8권1호
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• pp.1-12
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• 1998

Rheumatoid arthritis (RA) is a common systemic inflammatory disease which DMARDS have been widely used as a treatment modality both as monotherapy and combination therapy Bucillamine, one of newer DMARDS, has recently proven its efficacy as monotherapy in the treatment of RA. The objective of this study was to compare the efficacy and the safety of bucillamine monotherapy and bucillamine plus methotrexate combination therapy in the treatment of rheumatoid arthritis. Forty-nine mild RA patients were enrolled in this prospective, open-trial and were assigned to receive bucillamine 200 mg/day (n=18) or bucillamine 200 mg/day and methotrexate 7.5-15 mg/week (n=31) orally for 16 weeks. Concomitant use of NSAID and prednisolone <5 mg/day or equivalent dose of steroid were allowed. Both monotherapy group and combination therapy group have shown significant improvement in disease activities (Ritchie index, painful joints, swollen joints, morning stiffness, grip strength, ESR, RF, CRP, patient's self assessment of pain, physician's global assessment of disease activity) from the baseline. However, there was no statistically significant difference between two groups. The adverse effects were more frequently shown in combination therapy group than monotherapy group. In conclusion, in patients with mild RA monotherapy has shown to be equally efficacious as combination therapy with less side effects.

• Journal of Korean Neurosurgical Society
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• 제30권7호
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• pp.934-938
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• 2001

Oligodendrogiomas account for about 4 per cent of intracranial gliomas and surgery is known to be an essential first step to establish an accurate diagnosis and when oligodendrogliomas recur with or without anaplastic features after initial resection, radiation and chemotherapy consisting of the administration of procarbazine, lomustine, and vincristine are usually indicated. We report our experience of an excellent result with intraventricular methotrexate chemotherapy for a patient with disseminated anaplastic oligodendroglioma. A 29-year-old male patient presented with diplopia and headache for two months. MRI showed a irregular, faintly enhanced mass in the posterior fossa. The hisotological diagnosis was an anaplaplastic oligodendroglioma and he was treated with chemotherapy of PCV regimen and radiotherapy followed by surgery. CSF dissemination was revealed by a follow-up MRI during the period. Intraventricular methotrexate(0.175mg/kg) was given twice a week for 4 weeks through ommaya reservoir and the size of the multiple tumors was decreased significantly on follow-up MRI. This case report suggests that an aggressive treatment involving intravent-ricular chemotherapy may be helpful even when anaplastic oligodendrogliomas disseminates to leptomeninges.

• Archives of Pharmacal Research
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• 제15권2호
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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.

• 한국임상약학회지
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• 제1권1호
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• pp.1-7
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• 1991

Folates are involved in a variety of important biosynthesis by way of donating one carbon unit. Since folate metabolism was well understood a number of antifol have been developed. Among these antifols, aminopterin was first used in the treatment of childhood leukemia. However due to its toxicity and purity problems. it was immediately replaced by another antifols. methotrexate (MTX). MTX is shown to be active against various malignancies including leukemia breast cancer, osteogenic sarcoma, and head and neck cancer. Clinically, MTX therapy is divided into 3 categories. depeding on the dose administered; low-dose is defined as doses < $80\;mg/m^2$ intermediate-dose as doses $\geqq\;80\;mg/m^2$ and < $1000\;mg/m^2$ and high-dose as doses $\geqq\;1000\;mg/m^2$. Leucovorin should be administered to minimize MTX toxicities when MTX doses are greater than $80-100\;mg/m^2$. The clinical pharmacokinetics (ADME) of MTX is discussed in this text.

• Annals of Clinical Neurophysiology
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• 제22권1호
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• pp.41-45
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• 2020

Acute sarcoid myositis is rarely complicated by sarcoidosis, and steroid therapy is considered the standard treatment. We experienced a patient with acute sarcoid myositis who did not respond to aggressive high-dose corticosteroid therapy, but showed a dramatic improvement after the addition of weekly low-dose oral methotrexate (MTX). This intervention allowed the resumption of normal daily activities after 6 months. Our case strongly suggests that MTX should be considered in patients with acute sarcoid myositis that is resistant to corticosteroid therapy.

• Archives of Pharmacal Research
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• 제13권2호
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• pp.147-150
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• 1990

Methotrexate (MTX)-poly-L-lysine (PLL) conjugate was relatively stable in phosphate buffer of pH 7.4 and in plasma. However, liver homogenate accelerated the release of MTX from the conjugate. Pharmacokinetics and tissue distribution of MTX were compared after intramuscular injection of MTX (treatment I) and MTX-PLL conjugate (treatment II), 10 mg/kg as free MTX to rabbits. The peak concentration of MTX in treatment II were significantly lower than those in treatment I. The amount of MTX excreted in 24-hr urine was significantly reduced in treatment II and it suggested that MTX be more metabolized in treatment II than in treatment I. The amounts of MTX remaining in each organ after 24-hr of intramuscular injection were not significantly different in both treatments.