• Journal of Pharmaceutical Investigation
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• 제13권1호
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• pp.10-22
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• 1983

The interactions of ${\alpha}-cyclodextrin({\alpha}-CyD)$ and ${\beta}-cyclodextrin({\beta}-CyD)$ with several non-steroidal antiinflammatory drugs were studied on the effects of ${\alpha}-$ and ${\beta}-CyD$ on the solubility of the drugs in aqueous medium. Indoprofen, niflumic acid, alclofenac, and naproxen were chosen as representatives of antiinflammatory drugs. The solubility of all drugs studied increased with the addition of ${\beta}-CyD$, while not with glucose or ${\alpha}-CyD$. The increase of the solubility with ${\beta}-CyD$ was considered due mainly to the formation of inclusion complexes between ${\beta}-CyD$ and drugs. From the solubility data, the apparent stability constants K of the complex could be calculated. Ultraviolet absorption and circular dichroism confirmed the inclusion of indoprofen, niflumic acid and naproxen with ${\beta}-CyD$ in the molar ratio of 1 : 1. Inclusion complexes in solid powder form were obtained by the freeze-drying method and the inclusion formation was confirmed again by infrared, diffential thermal analysis, and X-ray diffraction measurements.

• Archives of Pharmacal Research
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• 제28권4호
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• pp.438-442
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• 2005

A series of 3-[1-(4-(2-methylpropyl) phenyl) ethyl]-1,2,4-triazole-5-thione (I) and its bicyclic condensed derivatives 6-benzylidenethiazolo[3,2-b]-1, 2,4-triazole-5(6H)-ones (IIa-IIf) were investigated for the prevention of ethanol-induced oxidative stress in liver and brain of mice. Administration of ethanol (0.1 mL/mice, p.o.) resulted in a drop of total thiol groups (T-SH) and non-protein thiol groups (NP-SH), and an increase in thiobarbituric acid reactive substances (TBARS) in both liver and brain tissue of mice (p<0.001). Among the compounds investigated (at a dose of 200 mg/kg, p.o.), I and IId ameliorated the peroxidative injury in these tissues effectively. Compounds IIa, IIc and IIe improved the peroxidative tissue injury only in brain. These findings suggest that certain condensed thiazolo-triazole compounds may contribute to the control of ethanol-induced oxidative stress in an organ selective manner.

• Journal of Microbiology and Biotechnology
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• 제34권4호
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• pp.828-837
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• 2024

Vancomycin (VAN) and metronidazole (MTR) remain the current drugs of choice for the treatment of non-severe Clostridioides difficile infection (CDI); however, while their co-administration has appeared in clinical treatment, the efficacy varies greatly and the mechanism is unknown. In this study, a CDI mouse model was constructed to evaluate the therapeutic effects of VAN and MTR alone or in combination. For a perspective on the intestinal ecology, 16S rRNA amplicon sequencing and non-targeted metabolomics techniques were used to investigate changes in the fecal microbiota and metabolome of mice under the co-administration treatment. As a result, the survival rate of mice under co-administration was not dramatically different compared to that of single antibiotics, and the former caused intestinal tissue hyperplasia and edema. Co-administration also significantly enhanced the activity of amino acid metabolic pathways represented by phenylalanine, arginine, proline, and histidine, decreased the level of deoxycholic acid (DCA), and downregulated the abundance of beneficial microbes, such as Bifidobacterium and Akkermansia. VAN plays a dominant role in microbiota regulation in co-administration. In addition, co-administration reduced or increased the relative abundance of antibiotic-sensitive bacteria, including beneficial and harmful microbes, without a difference. Taken together, there are some risks associated with the co-administration of VAN and MTR, and this combination mode should be used with caution in CDI treatment.

• Archives of Pharmacal Research
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• 제23권6호
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• pp.564-567
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• 2000

The use of amino acid derivatives as building blocks in peptide synthesis is increasingly being recognized as a potential route for the development of pharmaceutical agents. Side chain protection of polyfunctional amino acids such as Ser, Thr, Tyr is viewed as being particularly important. Although these derivatives are commercially listed, they are expensive and not widely available. We describe here a practical large-scale synthesis of t-butyl introduced D-serine, one of the building blocks of zoladex, a peptide drug.

• 대한한의학회지
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• 제32권6호
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• pp.117-121
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• 2011

Objectives: We report one patient with pleural effusion and effusion-related symptoms in small cell lung cancer (SCLC) successfully treated with Gunreyngtang-gagambang. Methods: Gunreyngtang-gagambang was administered at 30 minutes after mealtime, three times a day, for two months. Except for herbal medicine, the patient did not take any treatment including pharmaceutical or non pharmaceutical for effusion. Result: Two months later, the symptoms and the pleural effusion had disappeared from chest X-ray. Conclusion: Gunreyngtang-gagambang was effective for treatment of malignant pleural effusion due to small cell lung cancer.

• Journal of Pharmaceutical Investigation
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• 제25권4호
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• pp.283-289
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• 1995

The aim of this study is to increase the solubility and dissolution rate of clonixin by inclusion complex formation. Inclusion complexes of clonixin, a non-steroidal antiinflammatory drug, with ${\beta]-cyclodextrin$ were $2-hydrolrypropyl-{\beta]-cyclodextrin$ were prepared by freeze drying method. Inclusion complex formation of clonixin with cyclodextrins was determined by UV, IR and DSC. The apparent stability constants were calculated from the phase solubility diagrams. Dissolution rate and solubility of clonixin in water markedly increased by the complex formation.

• Journal of Pharmaceutical Investigation
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• 제10권1호
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• pp.1-3
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• 1980

The model of an isolated organ system has been developed to simulate the kinetic behavior of drug levels in an acting organ or site. The model is developed from basic considerations of drug distribution with hemodynamical and pharmacokinetical meanings. Model: It is considered a situation in which non-metabolic drug substance is injected into the arterial inflow of an isolated organ at constant rate. The volume of distribution and the concentration of drug in the venous outflow can be mathematically expressed as a function of time.

• 약학회지
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• 제36권4호
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• pp.397-401
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• 1992

Four new derivatives of 2-(3-phenoxyphenyl)propionic acid, widely used as non-sterioidal antiinflammatory and analgesic drug were synthesized.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-1
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• pp.54-55
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• 2003

Radiation therapy has been used for the cancer treatment externally or internally. The external radiation therapy has been widely used, but for the lack of its selectivity it requires strong radiation dose causing the dermal irritation and radiation effect of the normal tissues or organs. So we investigate non-clinical and clinical studies of “Milican inj.”, in which chitosan is chelated with 166-Holmium, as an anticancer agent for internal radiation therapy. (omitted)

• 대한수학회지
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• 제49권5호
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• pp.907-925
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• 2012

In this paper the boundedness for a large class of multi-sublinear operators is established on product generalized Morrey spaces with non-doubling measures. As special cases, the corresponding results for multilinear Calder$\acute{o}$n-Zygmund operators, multilinear fractional integrals and multi-sublinear maximal operators will be obtained.