Chemical and Pharmaceutical Bulletin
The Pharmaceutical Society of Japan, established in 1880, is one of Japan’s oldest and most distinguished academic societies. The Society currently has around 18,000 members. It publishes three monthly scientific journals. Chemical and Pharmaceutical Bulletin (Chem. Pharm. Bull.) began publication in 1953 as Pharmaceutical Bulletin. It covers chemistry fields in the pharmaceutical and health sciences. Biological and Pharmaceutical Bulletin (Biol. Pharm. Bull.) began publication in 1978 as the Journal of Pharmacobio-Dynamics. It covers various biological topics in the pharmaceutical and health sciences. A fourth Society journal, the Journal of Health Science, was merged with Biol. Pharm. Bull. in 2012. Yakugaku Zasshi (Japanese for “Pharmaceutical Science Journal”) has the longest history, with publication beginning in 1881. Yakugaku Zasshi is published mostly in Japanese, except for some articles related to clinical pharmacy and pharmaceutical education, which are published in English.
The main aim of the Society’s journals is to advance the pharmaceutical sciences with research reports, information exchange, and high-quality discussion. The average review time for articles submitted to the journals is around one month for first decision. The complete texts of all of the Society’s journals can be freely accessed through J-STAGE. The Society’s editorial committee hopes that the content of its journals will be useful to your research, and also invites you to submit your own work to the journals.

Chairman of Committee
Ken-ichi Hosoya
Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama



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27,025 registered articles
(updated on September 25, 2017)
Online ISSN : 1347-5223
Print ISSN : 0009-2363
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Volume 65 (2017) Issue 9 Pages 862-868
Ethereal C–O Bond Cleavage Mediated by Ni(0)-Ate Complex: A DFT Study

Density functional theory calculations were performed to explore the mechanism of Ni-catalyzed cross-coupling reactions involving organo-lithium and -zinc reagents through ethereal C–O bond cleavage. Based on this work, together with our previous mechanistic study on etheric Kumada–Tamao reaction, we identify and characterize a novel catalytic cycle for cross-coupling mediated by Ni(0)-ate complex.

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Density functional theory calculations were performed to explore the mechanism of Ni-catalyzed cross-coupling reactions involving organo-lithium and -zinc reagents though ethereal C–O bond cleavage. In comparison with our previous mechanistic study on etheric Kumada–Tamao reaction, it shows that the the Ni(0)-ate complex-mediated reaction pathway is a new and general mechanism for ethereal cross-coupling reactions, which can well explain the experimental findings for several ethereal C–O bond cleavage couplings.  The present work also suggests that the anionic character of organometallic nucleophiles can change oxidative addition mechanisms/pathways, which may provide new reactivity and selectivity.



Volume 65 (2017) Issue 9 Pages 848-853
Effect of the External Lubrication Method for a Rotary Tablet Press on the Adhesion of the Film Coating Layer

External lubrication is a useful method which reduces the adhesion of powder to punches and dies by spraying lubricants during the tableting process. However, no information is available on whether the tablets prepared using an external lubrication system can be applicable for a film coating process. In this study, we evaluated the adhesion force of the film coating layer to the surface of tablets prepared using an external lubrication method, compared with those prepared using internal lubrication method. We also evaluated wettability, roughness and lubricant distribution state on the tablet surface before film coating, and investigated the relationship between peeling of the film coating layer and these tablet surface properties. Increasing lubrication through the external lubrication method decreased wettability of the tablet surface. However, no change was observed in the adhesion force of the film coating layer. On the other hand, increasing lubrication through the internal lubrication method, decreased both wettability of the tablet surface and the adhesion force of the film coating layer. The magnesium stearate distribution state on the tablet surface was assessed using an X-ray fluorescent analyzer and lubricant agglomerates were observed in the case of the internal lubrication method. However, the lubricant was uniformly dispersed in the external lubrication samples. These results indicate that the distribution state of the lubricant affects the adhesion force of the film coating layer, and external lubrication maintained sufficient lubricity and adhesion force of the film coating layer with a small amount of lubricant.

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We evaluated the adhesion force of the film coating layer to the surface of tablets prepared using an external lubrication method. Increasing lubrication decreased wettability of the tablet surface. However, no change was observed in the adhesion force of the film coating layer. The magnesium stearate distribution state on the tablet surface was assessed and the lubricant was uniformly dispersed in the external lubrication samples. The distribution state of the lubricant affects the adhesion force of the film coating layer, and external lubrication maintained sufficient lubricity and adhesion force of the film coating layer with a small amount of lubricant.



Volume 65 (2017) Issue 9 Pages 840-847
Four New Lignans and IL-2 Inhibitors from Magnoliae Flos

Four new lignans, a furofuran lignan medioresinol B (10) and three tetrahydrofuran lignans kobusinol C (16), 7′-methoxy magnostellin A (21), and mangnostellin D (23), along with 19 known lignans, were isolated from the flower buds of Magnolia biondii PAMP. The structures of the isolates were elucidated using spectroscopic analysis, mainly one- and two-dimensional NMR, high resolution-MS, and circular dichroism techniques as well as Mosher’s esterification method. The anti-allergic effects of the isolated compounds were evaluated by analyzing the inhibition of interleukin-2 (IL-2) expression in Jurkat T-cells. Compounds 1114 reduced IL-2 expression in a dose-dependent manner.

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Four new lignans, a furofuran lignan medioresinol B (10) and three tetrahydrofuran lignans kobusinol C (16), 7'-methoxy magnostellin A (21), and mangnostellin D (23), along with 19 known lignans, were isolated from the flower buds of Magnolia biondii Pamp. The structures of the isolates were elucidated using spectroscopic analysis, mainly one- and two-dimensional NMR, high resolution mass spectrometry, and circular dichroism techniques as well as Mosher’s esterification method. The anti-allergic effects of the isolated compounds were evaluated by analyzing the inhibition of interleukin-2 (IL-2) expression in Jurkat T-cells. Compounds 1114 reduced IL-2 expression in a dose-dependent manner.



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    Current Topics: Cutting-edge Science of Cyclodextrin


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    Current Topics: Reversal or Control of the Innate Reactivity of Functional groups




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