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项与 Hoechst Japan Ltd. 相关的药物

MRK-17

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P-gp

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P-gp抑制剂

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Hoechst Japan Ltd.

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肿瘤

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100 项与 Hoechst Japan Ltd. 相关的临床结果

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0 项与 Hoechst Japan Ltd. 相关的专利（医药）

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327

项与 Hoechst Japan Ltd. 相关的文献（医药）

2011-04-12·Journal of Pharmacy and Pharmacology3区 · 医学

Sustained release of buserelin acetate, a luteinizing hormone-releasing hormone agonist, from an injectable oily preparation utilizing ethylated β-cyclodextrin

3区 · 医学

Article

作者: Matsubara, Kazutaka ; Arima, Hidetoshi ; Irie, Tetsumi ; Uekama, Kaneto ; Kuriki, Takeo

AbstractThe possible use of heptakis (2,6-di-O-ethyl)-β-cyclodextrin (DE-β-CyD) as a parenteral sustained-release carrier for buserelin acetate, a luteinizing hormone-releasing hormone superagonist, has been examined. The in-vitro release of buserelin from the oily suspension was significantly retarded by the complexation with DE-β-CyD, mainly due to the poor water solubility of the complex. A single subcutaneous injection of the suspension containing the buserelin-DE-β-CyD complex to rats provided an effective continuous plasma level of buserelin lasting for at least one month, indicating a potential therapeutic efficacy for the treatment of the endocrine-dependent diseases. These results suggest that DE-β-CyD serves as an injectable sustained-release drug carrier suitable for chronic treatment with buserelin acetate.

2011-04-12·Journal of Pharmacy and Pharmacology3区 · 医学

In-vivo Blood-brain Barrier Transport of a Novel Adrenocorticotropic Hormone Analogue, Ebiratide, Demonstrated by Brain Microdialysis and Capillary Depletion Methods

3区 · 医学

Article

作者: Deguchi, Yoshiharu ; Tsuji, Akira ; Terasaki, Tetsuya ; Shimura, Takesada ; Tabata, Shigeru

AbstractThe transport of ebiratide, a novel adrenocorticotropic hormone (ACTH) analogue, [H-Met-(O2)-Glu-His-Phe-d-Lys-Phe-NH(CH2)8-NH2], through the blood-brain barrier was directly demonstrated in-vivo. [125I]Ebiratide (16·9 MBq mL−1) or [14C]sucrose (29·2 MBq mL−1) known to be restrictively transported through the blood-brain barrier was infused into the rat internal carotid artery at a flow rate of 50 μL min−1 for 10 min, and after 15 min infusion the distribution volume of each compound in the brain parenchyma was determined by the capillary depletion method. The distribution volume of [125I]ebiratide was 167·8 ± 62·2 μL (g brain)−1, which was about seven times higher than that of [14C]sucrose (24·9 ± 4·0 μL g brain)−1, indicating the uptake of ebiratide into brain parenchymal cells. During the infusion into the internal carotid artery, brain microdialysis was simultaneously performed to directly collect the brain interstitial fluid as the dialysate. Radioactivity was detected in the dialysate during the [125I]ebiratide infusion and HPLC analysis of the dialysate revealed that the intact ebiratide accounted for ≥ 80% total radioactivity. The concentrations of [125I]ebiratide and [14C]sucrose in the brain interstitial fluid were estimated based on the relative recovery obtained in the in-vitro recovery study. The brain interstitial fluid/internal carotid arterial blood concentration ratio for [125I]ebiratide was determined to be 1·47 × 10−2 ± 0·17 × 10−2 and was about eight times higher than that for [14C]sucrose (1·92 × 10−3 ± 0·36 × 10−3), indicating significant transport of ebiratide to the brain interstitial fluid. Accordingly, it was demonstrated that ebiratide is taken up into the brain in the intact form possibly via an absorptive-mediated transport through the blood-brain barrier.

1999-02-01·The Journal of pharmacology and experimental therapeutics

Oral administration of leflunomide (HWA486) results in prominent suppression of immunoglobulin E formation in a rat type 1 allergy model.

Article

作者: Ogata, K ; Mizushima, Y ; Kitagawa, H ; Amano, Y

Leflunomide, a drug being developed for use in the treatment of rheumatoid arthritis, was evaluated in an ovalbumin (OVA)-induced rat type 1 allergy model. In a dose of 1 mg/kg/day, it strongly suppressed the formation of OVA-specific IgE, thus preventing the elevation of the plasma histamine level and induction of anaphylactic shock observed after i.v. challenge with OVA. Studies on leflunomide's effects on the secondary antibody response showed that administration during the primary immune response remarkably diminished the secondary antibody responses, except IgM, even without further drug administration. Furthermore, when administered during the secondary response after rechallenge, both the total IgE and OVA-specific IgE serum levels declined rapidly to nearly baseline levels. Although OVA-specific IgG1, IgG2a, and IgM did not decrease from their primary response levels, these classes' secondary responses were strongly suppressed. In an in vitro study, the proliferation and antibody production of OVA-stimulated spleen cells, derived from Brown Norway rats, were strongly inhibited by A77 1726, leflunomide's active metabolite. When uridine was added to the cell culture, this molecule's effect on cell proliferation was completely restored, whereas the antibody production was partially restored. These findings are consistent with data indicating that leflunomide is a dihydroorotate dehydrogenase inhibitor. Taken together, the above findings suggest the therapeutic potential of leflunomide against type 1 allergic diseases.

100 项与 Hoechst Japan Ltd. 相关的药物交易

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100 项与 Hoechst Japan Ltd. 相关的转化医学

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