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International Journal of Pharmaceutics | 1994

Development of a novel drug delivery system, time-controlled explosion system (TES): V. Animal pharmacodynamic study and human bioavailability study

Takeshi Hata; Yasuo Shimazaki; Akira Kagayama; Shigeki Tamura; Satoshi Ueda

Abstract FK409, a new vasolidator, was applied to a time-controlled explosion system (TES). after oral administration of the TES with a lag time of 3 h to conscious dogs, both the blood FK409 level and blood pressure were monitored. FK409 appeared in the blood at 3 h and the maximum level was attained at 5 h according to the in vitro release profile. In response to the blood concentration profile of FK409, the blood pressure predominantly decreased after 3 h and minimized around 5 h. A human bioavailability study was also performed, using the TES with a lag time of 3 h. The in vivo lag time for the appearance of drug in the blood was consistent with the in vitro lag time for drug release. Compared with a rapid release formulation, the extent of FK409 absorbed did not decrease and the blood concentration profile was completely separated. Furthermore, the blood concentration profile was not influenced by food intake. These results suggest that the novel drug delivery system, the TES, has potential for use as a preparation of FK409 with prolonged activity.


Journal of Pharmaceutical Sciences | 2002

Tacrolimus is a class II low-solubility high-permeability drug: The effect of P-glycoprotein efflux on regional permeability of tacrolimus in rats

Shigeki Tamura; Atsuo Ohike; Rinta Ibuki; Gordon L. Amidon; Shinji Yamashita


Journal of Pharmacology and Experimental Therapeutics | 2003

The Site-Specific Transport and Metabolism of Tacrolimus in Rat Small Intestine

Shigeki Tamura; Yuji Tokunaga; Rinta Ibuki; Gordon L. Amidon; Hitoshi Sezaki; Shinji Yamashita


Archive | 1999

Sustained release preparation of a macrolide

Eiji Hashimoto; Takeo Chayamachi Hirose; Rinta Ibuki; Toshio Ideno; Yukihiro Nomura; Takashi Saitoh; Fumio Shimojo; Shigeki Tamura; Satoshi Ueda; Kazunari Yamashita


Archive | 2003

Sustained release formulations containing tacrolimus

Kazunari Yamashita; Eiji Hashimoto; Yukihiro Nomura; Fumio Shimojo; Shigeki Tamura; Takeo Hirose; Satoshi Ueda; Takashi Saitoh; Rinta Ibuki; Toshio Ideno


Drug Metabolism and Pharmacokinetics | 2004

Effect of Experimental Acute Renal and Hepatic Failure on Absorption of Tacrolimus in Rat Small Intestine

Shigeki Tamura; Atsuo Ohike; Yuji Tokunaga; Rinta Ibuki; Gordon L. Amidon; Hitoshi Sezaki; Shinji Yamashita


Archive | 1999

LIQUID AGENT FOR INTERNAL USE CONTAINING DIHYDROPYRIDINE- BASED COMPOUND

Takashi Higo; Rinta Ibuki; Shigeo Nakanishi; Shigeki Tamura; Toshihiko Toyoda; 茂雄 中西; リン太 伊吹; 繁樹 田村; 孝志 肥後; 俊彦 豊田


Archive | 2004

Regular Article EŠect of Experimental Acute Renal and Hepatic Failure on Absorption of Tacrolimus in Rat Small Intestine

Shigeki Tamura; L. Amidon; Shinji Yamashita


Archive | 1999

Retardpräparat mit Makroliden wie Tacrolimus Sustained-release macrolides such as tacrolimus

Kazunari Yamashita; Eiji Hashimoto; Yukihiro Nomura; Fumio Shimojo; Shigeki Tamura; Takeo Hirose; Satoshi Ueda; Takashi Saitoh; Rinta Ibuki; Toshio Ideno


Archive | 1999

Sustained release macrolide compositions

Kazunari Yamashita; Eiji Hashimoto; Yukihiro Nomura; Fumio Shimojo; Shigeki Tamura; Takeo Hirose; Satoshi Ueda; Takashi Saitoh; Rinta Ibuki; Toshio Ideno

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