著者

大谷 道輝 川端 志津 假家 悟 内野 克喜 伊藤 敬 小瀧 一 籾山 邦男 森川 亜紀 瀬尾 巖 西田 紀子

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.122, no.5, pp.323-329, 2002-05-01 (Released:2003-02-18)

参考文献数

19

被引用文献数

11 12

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The effect of the intake of 200g of grapefruit pulp (corresponding to one grapefruit) on the pharmacokinetics of the calcium antagonists nifedipine (NF) and nisoldipine (NS) were investigated in 8 healthy Japanese male volunteers. A crossover design was used for the study: group I did not ingest any grapefruit (control group); group II ingested grapefruit 1 h after drug administration; and group III ingested grapefruit 1 h before drug administration. The intake of grapefruit pulp increased the plasma concentrations of both NF and NS, an effect that has previously been reported with grapefruit juice. The increase was most marked when grapefruit was eaten before drug administration. For both NF and NS, subjects who ingested grapefruit 1 h before drug administration exhibited a greater Cmax and AUC0—24 than did subjects in the control group. For NF, the Cmax was 1.4 times higher and the AUC0—24 1.3 times larger in group III than in group I. For NS, the Cmax was 1.5 times higher and the AUC0—24 1.3 times larger in group III than in group I. The increase in the AUC0-24 was significant for both drugs (p<0.05). The finding that the ratios of Cmax and AUC0—24 for unchanged drug and metabolites did not vary greatly among the three groups for either drug suggests that the increase in serum concentration produced by grapefruit intake may be due to other factors than an inhibitory effect on drug metabolism. Also, the increases in Cmax and AUC0—24 of NS produced by grapefruit intake were smaller than those produced by grapefruit juice intake, indicating that grapefruit pulp and juice have different effects on the pharmacokinetics.

著者

大谷 道輝 山田 伸夫 高山 和郎 小瀧 一 江藤 隆史 假家 悟 内野 克喜 伊賀 立二

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.122, no.1, pp.107-112, 2002-01-01 (Released:2003-02-13)

参考文献数

14

被引用文献数

8 8

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A commonly used admixture of commercially available ointments and/or creams was selected from the prescribed sheets in our hospital, and questionnaire to dermatologists. To assess the relationship between permeability of corticosteroid through murine skin and clinical effects in human, we attempted to investigate the vasoconstrictor activity of these admixtures of topical corticosteroid by double-blind controlled study. Test samples were occluded at random on the back of 20 healthy volunteers for 4 hours. The vasoconstrictor activity of corticosteroid creams (Lidomex®) alone was significantly large as compared with that of ointments alone. The vasoconstrictor activity of corticosteroid in the admixture of Lidomex® ointment and urea ointments or heparinoid ointment was 1.5—2 fold significantly larger than that from ointments alone. The extent of the stability of the emulsion after mixing was related to the vasoconstrictor activity. These experiments demonstrated a close relationship between the vasoconstrictor activity of human skin and permeability of hairless mice skin. These results suggested that the vasoconstrictor activity of topical corticosteroids mixed with commercially available ointments and/or creams depends upon their physicochemical characteristics.

著者

松元 美香 大谷 道輝 馬島 裕子 並木 路広 假家 悟 内野 克喜

出版者

一般社団法人日本医療薬学会

雑誌

医療薬学 (ISSN:1346342X)

巻号頁・発行日

vol.28, no.5, pp.450-455, 2002-10-10 (Released:2011-03-04)

参考文献数

5

被引用文献数

2 1

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It is important that laboratory data to be constantly checked according to described package inserts during usage of medicines. However, many hepatic and renal disorders were reported to have strong adverse reactions for prescription drugs. We investigated the necessity of hepatic and renal function checks in package inserts for 3300 prescription drugs. As a result, the number of drugs which recommended checks on hepatic and renal functions were 240 (7.3%) and 209 (6.3%) respectively. The described expression or place regarding checks of hepatic and renal functions on package inserts were various types of unclear information to doctors and pharmacists. We thus found that the present style of package inserts unapprehensive to the necessity of hepatic and neral function checks. So, in our hospital, we decided to provide a list of drugs that required hepatic and renal function checks during administration of drugs.These findings suggest that the need of hepatic and renal functions monitoring during the administration of drugs by the establishment of a new Clinical Checks item in the package inserts is therefore necessary.

著者

大谷 道輝 川端 志津 假家 悟 内野 克喜 伊藤 敬 小瀧 一 籾山 邦男 森川 亜紀 瀬尾 巖 西田 紀子

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.122, no.5, pp.323-329, 2002-05-01

被引用文献数

1 12

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The effect of the intake of 200g of grapefruit pulp (corresponding to one grapefruit) on the pharmacokinetics of the calcium antagonists nifedipine (NF) and nisoldipine (NS) were investigated in 8 healthy Japanese male volunteers. A crossover design was used for the study: group I did not ingest any grapefruit (control group); group II ingested grapefruit 1 h after drug administration; and group III ingested grapefruit 1 h before drug administration. The intake of grapefruit pulp increased the plasma concentrations of both NF and NS, an effect that has previously been reported with grapefruit juice. The increase was most marked when grapefruit was eaten before drug administration. For both NF and NS, subjects who ingested grapefruit 1 h before drug administration exhibited a greater C_<max> and AUC_<0-24> than did subjects in the control group. For NF, the C_<max> was 1.4 times higher and the AUC_<0-24> 1.3 times larger in group III than in group I. For NS, the C_<max> was 1.5 times higher and the AUC_<0-24> 1.3 times larger in group III than in group I. The increase in the AUC_<0-24> was significant for both drugs (p<0.05). The finding that the ratios of C_<max> and AUC_<0-24> for unchanged drug and metabolites did not vary greatly among the three groups for either drug suggests that the increase in serum concentration produced by grapefruit intake may be due to other factors than an inhibitory effect on drug metabolism. Also, the increases in C_<max> and AUC_<0-24> of NS produced by grapefruit intake were smaller than those produced by grapefruit juice intake, indicating that grapefruit pulp and juice have different effects on the pharmacokinetics.

著者

大谷 道輝 中井 達郎 大沢 幸嗣 金 素安 松元 美香 江藤 隆史 假家 悟 加野 象次郎 内野 克喜

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.122, no.12, pp.1153-1158, 2002-12-01 (Released:2003-02-18)

参考文献数

24

被引用文献数

10 12

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Twenty percent of dermatologists have experienced a separation of water or deterioration of topical corticosteroids mixed with commercially available ointments and/or creams. However, few investigations of this deterioration of admixtures have been reported. To assess the effects of preservatives in preventing microbial contamination of these admixtures, we attempted to investigate the concentration of preservative agents in admixtures and the microbial contamination of these admixtures with a topical corticosteroid ointment (Antebate®). The concentration of parabens was reduced by half using an admixture of corticosteroid ointment with four types of moisturizing creams, Urepearl, Pastaronsoft, Hirudoid, and Hirudoidsoft. After a further 3 months, no decrease in parabens was seen. No microbial contamination was found in any admixture stored at room temperature for 1 week and touched two times daily with a finger. The concentration and ratio of the parabens in the aqueous phase and oil phase were entirely different in the admixtures before being centrifuged. The aqueous phase of the admixtures of the oil/water (O/W)-type emulsions of Urepearl and Hirudoid was not found to have microbial contamination immediately after being centrifuged. All aqueous phases stored at room temperature or in a refrigerator for 1 week and touched with a finger twice daily exhibited microbial contamination. These experiments demonstrated that O/W-type emulsions, in which the water easily separates from the bases, should be thoroughly mixed to prevent microbial contamination.