著者

加瀬 佳年 由井薗 倫一

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.81, no.5, pp.740-747, 1961-05-25 (Released:2010-02-19)

参考文献数

30

被引用文献数

3

---

The pharmacology of d-N, N, 1-trimethyl-3-(ethylsulfonyl)-3, 3-diphenylpropylamine hydrochloride (A-5) was described in detail. A-5 showed a long-acting antitussive activity, duration of the effect being 18.9 times that of codeine (intravenous) and 13.5 times that of codeine (oral), though 50% antitussive dose is only 1.4 and 1.7 times that of codeine in dogs and cats, respectively. The site of action seemed to be the cough center per se. Toxicity in mice (subcutaneous) is 1.5 times that of codeine and 30% that of Methadone. No tendency to establish tolerance, cumulative action, or addiction liability was found by long-term administration. Analgesic action and other actions were discussed.

著者

角 保男

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.81, no.5, pp.652-655, 1961-05-25 (Released:2010-02-19)

参考文献数

5

---

Leucoriboflavin 5′-phosphate derivatives were prepared by reductive acylation of riboflavin 5′-phosphate. These compounds were rather unstable and were easily hydrolyzed to riboflavin 5′-phosphate derivatives, regaining the yellow color. On heating with 17% hydrochloric acid, leucoriboflavin 5′-phosphate tetraacetate and monoethylformate yielded riboflavin 2′, 5′-anhydride, m.p. 300-302°. This substance was sensitive to light and formed lumichrome as the photo-decomposition product on exposure to light.

著者

角 保男

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.81, no.5, pp.647-651, 1961-05-25 (Released:2010-02-19)

参考文献数

3

---

Leucoriboflavin, reduced form of riboflavin, is easily oxidized to riboflavin when shaken with air. To retain the leuco state, riboflavin was reduced with sodium dithionite or with zinc in acid solution to the leuco compound and its acylation with acetic anhydride or benzoyl chloride gave leucoriboflavin acylate. These compounds were stable in solid state but were easily decomposed to riboflavin acylate on exposure to sunlight or by heating, regaining the yellow color. Several decomposition products of leucoriboflavin acylate are described.

著者

立浪 良介 高橋 恭兵 大場 達也 丹保 好子

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.129, no.1, pp.147-153, 2009 (Released:2009-01-01)

参考文献数

32

被引用文献数

2 6

---

Methylglyoxal (MG), a highly reactive dicarbonyl compound, is a metabolic by-product of glycolysis. MG is often detected at high levels in the blood of diabetic patients. We examined whether MG was capable of inducing reactive oxygen species (ROS) production in bovine aortic endothelial cells (BAECs). The viability of BAECs decreased with time on treatment with 5 mM MG, and was almost completely lost at 24 h. In contrast, MG at 1 mM had little influence on BAEC viability up to 24 h, but induced the elevation of intracellular glutathione content at 24 h. Exposure of BAECs to MG caused a dose-dependent increase in oxidized-hydroethidine fluorescence intensity, indicating ROS production. In addition, aconitase inactivation, which is an indicator of intracellular superoxide, was observed in MG-treated cells. Finally, we found that MG at 5 mM increased the fluorescence intensity of BES-So, a specific probe for superoxide. Together, the results suggest that MG induces superoxide production in endothelial cells, and that the accumulation of ROS may be linked to cytotoxic effects.

著者

吉富 英助 甲斐 晋

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.1926, no.530, pp.307-308, 1926-04-26 (Released:2009-10-22)

著者

岸本 桂子 羽坂 亜希子 山浦 克典 福島 紀子

出版者

日本薬学会

雑誌

薬学雑誌 (ISSN:00316903)

巻号頁・発行日

vol.136, no.10, pp.1401-1413, 2016

著者

岸本 桂子 羽坂 亜希子 山浦 克典 福島 紀子

出版者

公益社団法人 日本薬学会

雑誌

薬学雑誌. 乙号 (ISSN:00316903)

巻号頁・発行日

vol.136, no.10, pp.1401-1413, 2016

被引用文献数

3

---

&emsp;Pharmacy is required to shift toward human service such as hearing the complaints of health. But the study about help-seeking behavior to pharmacist is not really investigated. We hypothesized that a decrease in expression visibility, due to pharmacists' typical masks, may negatively impact help-seeker' trust in pharmacist. The sample included 100 drugstore customers aged ≥18 years. Participants were stratified by gender and randomly assigned to two groups: evaluation of clear-masked and normal-masked pharmacists. After viewing a video with either male or female pharmacists wearing either clear or normal masks, participants completed a questionnaire. The primary outcome was trust in pharmacist measured by the Trust Scale and the secondary outcome was impression of the pharmacist measured by nineteen pairs of adjectives. There were no differences by gender on trust scores. Results revealed that both male and female pharmacists who wore clear masks were rated as more trustworthy than normal-masked pharmacists (<i>p</i><0.001, d=0.903, and <i>p</i>=0.001, d=0.716, respectively). Sixteen of nineteen adjectives reported for pharmacists wearing normal masks indicated greater negative intention than those with clear masks (d=0.431-1.469). In most cases, among pharmacists wearing clear masks, results showed positive correlations between trust and each impression adjective (r=0.279-0.710). Our findings indicate that pharmacists wearing normal masks, which partially hide facial expressions, may decrease customer's trust in pharmacist. Further, normal masks were associated with negative impression. To avoid the inhibition of help-seek behavior, we recommend that pharmacists wear a clear mask and increase non-verbal communication.<br>

著者

樽井 敦

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.135, no.11, pp.1245-1253, 2015 (Released:2015-11-01)

参考文献数

51

被引用文献数

2

---

Multi-substituted β-lactam compounds have not only attracted considerable interest as core structures of pharmaceutical compounds such as antibiotics but also have been used as building blocks for the construction of β-amino acids. Electrophilic β-lactams can be used to enhance essential biological activities. Furthermore, the ring-opening reactions of electrophilic β-lactams can be used to provide facile access to β-amino acids. The introduction of an electronegative fluorine atom to a β-lactam ring to give the corresponding fluoro-β-lactam can be used as an effective strategy for the preparation of electrophilic β-lactams. In this review, we provide a summary of our recent research towards the direct functionalization of fluoro-β-lactams. This review has been divided into four topics, including: 1) the alkylation and hydroxyalkylation of α-bromo-α-fluoro-β-lactams (1); 2) the nickel-catalyzed cross coupling reaction of 1; 3) the asymmetric synthesis of fluoro-β-lactams using chiral ligands; and 4) the utilization of fluoro-β-lactams as highly electrophilic building blocks.

著者

南 基泰 四方 恒生 長谷川 千晃 大江 千里 芦田 馨 杉野 守

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.115, no.10, pp.832-842, 1995-10-25

被引用文献数

6

---

We studied that the morphological and histological characteristics, and the content (%DW) of saikosaponins on the root of Bupleurum falcatum cultivated in an Ebb & Flood system (E&F), a kind of soilless culture system, by both the direct sowing and the transplanting methods, and that effects of pinching on the root growth and the content (%DW) of saikosaponins in each part of root. Yield of root and content (%DW) of saikosaponins in each part of root, 8-months-old, cultivated in E&F by both methods were at the same level as that cultivated for the same period in soil conditoin by generally standard procedures. Morphological characteristics of the root cultivated by the direct sowing method were the same appearance as that by soil condition, but by the transplanting method main root branched off in all direction and the lateral root were more developed than by the direct sowing method. By pinching lignification in xylem on the main root were inhibited, but the dried weight of total root part and content (%DW) of saikosaponins in each part of the root were not shown to be significantly changed.

著者

山浦 克典 吉原 正義

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.123, no.10, pp.887-891, 2003-10-01

被引用文献数

3 11

---

インフルエンザは毎年日本国内において12月から3月の間に大流行し,小児ではインフルエンザ脳炎・脳症を,高齢者では肺炎などの重篤な合併症を引き起こす危険性のある呼吸器系感染症である.近年,インフルエンザウイルスの特効薬となるノイラミニダーゼ阻害剤が開発され,インフルエンザ治療においても特異的な薬物治療が行われるようになり,治療効果も格段に向上した.現在日本国内で臨床使用されているノイラミニダーゼ阻害剤は内服薬のオセルタミビルと吸入薬のザナミビルの2剤である.2002年度のインフルエンザ流行シーズンにおいては,オセルタミビル製造供給メーカーによる供給計画の狂いと,前年より1ヵ月早いインフルエンザの流行により,オセルタミビルの供給滞り問題が発生したことから出荷調整が行われ,全国的にノイラミニダーゼ阻害剤の在庫不足に陥った.いずれの薬剤も保険適応は5日間処方であるが,全国各地の医療機関において,2日又は3日間処方により在庫不足に対応せざるを得ない状況が多くみられた.そこで,本研究においては,オセルタミビル供給滞りに伴い,短縮処方された患者の医療費及び治療効果について,適応の5日間処方患者と比較検討した.

著者

水田 博彰 鮫元 博文 小川 建志

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.111, no.8, pp.445-450, 1991-08-25 (Released:2008-05-30)

参考文献数

13

被引用文献数

1 1

---

The effects of triglycerides on the gastrointestinal absorption of 2-[3-(3, 5-di-tert-butyl-4-hydroxyphenyl)-1H-pyrazolo [3, 4-b] pyridin-1-yl] ethyl acetate (1) were investigated in dogs. The enhancing abilities of the triglycerides on the absorption of 1 were demonstrated as in the order of trilinolein>triolein>tristearin>tripalmitin. Among the series of fatty acids and monoglycerides, namely, digestive products of triglycerides by pancreatic lipase, linoleic acid and monolinolein showed the most potent solubilizing activities of 1 in a solution of bile salt. The incorporation of 1 into mixed micelle formed by lipids and bile salts was presumed to play an important role in the accelerated absorption of 1 after ingestion of triglycerides. On the basis of these findings, an emulsion containing 1 was prepared with soybean oil. The emulsion exhibited a remarkable improvement of the absorption of 1 compared to a suspension of the drug in methylcellulose solution.

著者

近藤

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

no.253, pp.250-251, 1903-03-26

著者

小菅 卓夫 神谷 弘子 足立 太平

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.82, no.1, pp.190-190, 1962-01-25 (Released:2010-02-19)

参考文献数

3

被引用文献数

10

著者

戸口 始 小川 泰亮 岡田 弘晃 山本 眞樹

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.111, no.8, pp.397-409, 1991-08-25 (Released:2008-05-30)

参考文献数

61

被引用文献数

10 14

---

Leuprorelin (leuprolide, D-Leu6-(des-Gly10-NH2)-LH-RH ethylamide) acetate is a superactive agonist of luteinizing hormone-releasing hormone (LH-RH). We developed once-a-month injectable microcapsules of this agonist by our novel in-water drying method. This depot formulation can release the drug at an apparent zero-order rate over one month with bioerosion of copoly (lactic/glycolic acid) utilized as a wall material of the polycore microcapsules. A dramatic prolonged depression of pituitary-gonadal axis, chemical castration, was achieved by the once-a-month injection in experimental animals ; it expects a reliable effcacy for treating hormone-dependent prostatic, breast cancers and endometriosis. Studies on the dosage design of this new delivery system of leuprorelin are summarized.

著者

山口 智子 向井 志乃 魚谷 茂雄 大谷 壽一 澤田 康文

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.331-338, 2002 (Released:2003-02-18)

参考文献数

10

被引用文献数

1

---

Phenytoin (PHT) exhibits nonlinear pharmacokinetics in the therapeutic range. Therefore a slight increase in dose may lead to considerable elevation of the serum PHT level. Although its bioavailability is dependent on the formulation, bioequivalence is considered to be preserved between the three major formulations, of tablet, 97% fine granules, and 10% powder. However, we experienced many cases of increases serum PHT concentration after changes in formulation from 97% fine granules to 97/4% hospital-made fine granules, and from the latter to 10% powder. Retrospective analysis revealed that these alterations were accompanied by 55% and 16% increases in the serum concentration-to-dose ratio of PHT, respectively. We investigated the factors of this increase by analyzing the weight of remaining powder in a package and the PHT content of each formulation. Each package of PHT formulation prepared with 97% fine granules and 10% powder was unsealed, and the contents were weighed to calculate the rate of recovery. The rate of ingestion was estimated by correcting the rate of recovery by PHT strength (i. e., 1.0 for 10% powder and 0.97 for fine granules). The rates of recovery and ingestion for 10% powder were 13% and 16% higher than those for 97% fine granules, respectively (p<0.01). In conclusion, Changing the PHT formulation from 97% fine granules to 10% powder may lead to a considerable increase in the serum PHT concentration and possibly induce PHT toxicity.

著者

野田 幸裕 鍋島 俊隆

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.120, no.8, pp.677-682, 2000-08-01 (Released:2008-05-30)

参考文献数

24

被引用文献数

1 9

---

To develop an animal model for negative symptoms, in particular avolition, of schizophrenia, the effect of phencyclidine (PCP) on immobility (regarded as avolition) in the forced swimming test was investigated in mice, since PCP produces negative symptoms in humans. Unlike single, repeated treatment with PCP prolonged the immobility time in the forced swimming test 24 h after the final injection compared with saline treatment. The enhancing effect of PCP on the immobility persisted for 21 d after the withdrawal of the drug. Atypical antipsychotics attenuated the enhancing effect of PCP on the immobility. Since these attenuating effects were antagonized by a serotonin-S2 receptor agonist, (±)-2, 5-dimethoxy-4-iodamphetamine (DOI), the effects may be mediated via serotonin-S2 receptors. In contrast with atypical antipsychotics, typical antipsychotics, antidepressants and anxiolytics had no effect. No functional changes in post-synaptic serotonin-S2 reseptors were observed in PCP-treated mice following the forced swimming test. Serotonin utilization in the prefrontal cortex was increased, but dopamine utilization was decreased in PCP-treated mice showing the enhancement of immobility. The enhancing effect of PCP was significantly attenuated by D-cycloserine, an agonist for glycine binding site of N-methyl-D-aspartate (NMDA) receptor ionophore complex. Decreases of NMDA receptor function or of the cortical glutamate and glycine levels were observed in PCP-treated mice showing the enhancement of immobility. These results suggest that the enhancing effect of PCP on immobility is mediated by the imbalance of the cortical serotonergic, dopaminergic and glutamatergic systems and could be used as an animal model for negative symptoms of schizophrenia.

著者

川島 嘉明

出版者

公益社団法人日本薬学会

雑誌

薬学雑誌 (ISSN:00316903)

巻号頁・発行日

vol.89, no.10, pp.1386-1391, 1969-10

---

Berberine was extracted from slices of Berberis thunbergii, cut into various sizes (#1-#4), with water and methanol at 37°. Results of analysis of extraction rate, indicated that the mechanism of extraction consists of washing, diffusion, and capillary extraction, and mass transfer coefficients for each mechanism were determined. Comparing with the extraction of berberine from the cortex of phellodendron, ^<3)> mass transfer coefficients were distinctly larger.

著者

杉本 八郎

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.130, no.4, pp.521-526, 2010 (Released:2010-04-01)

参考文献数

8

被引用文献数

6 6

---

Currently, there are five anti-Alzheimer's disease drugs approved. These are tacrine, donepezil, rivastigmine, galantamine, and memantine. The mechanism of the first four drugs is acetylcholinesterase inhibition, while memantine is an NMDA-receptor antagonist. However, these drugs do not cure Alzheimer's, but are only symptomatic treatments. Therefore, a cure for Alzheimer's disease is truly needed. Alzheimer's disease is a progressive neurodegenerative disease characterized by cognitive deficits. The cause of the disease is not well understood, but research indicates that the aggregation of β-amyloid is the fundamental cause. This theory suggests that β-amyloid aggregation causes neurotoxicity. Therefore, development of the next anti-Alzheimer's disease drug is based on the β-amyloid theory. We are now studying natural products, such as mulberry leaf extracts and curcumin derivatives, as potential cure for Alzheimer's disease. In this report, we describe some data about these natural products and derivatives.

著者

岡﨑 敬之介 渡邊 徹 齋藤 勲 村山 純一郎

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.132, no.2, pp.231-236, 2012 (Released:2012-02-01)

参考文献数

10

被引用文献数

2 2

---

Our aim was to clarify the side effects of irinotecan which occurred in patients admitted to Showa University Hospital to investigate whether the UGT1A1 genetic polymorphism status was reflected in the discontinuation or dose reduction of irinotecan. We retrospectively investigated UGT1A1 genetic polymorphisms, irinotecan dosage, dose discontinuance or reduction, and laboratory results from May 1 2009 to April 30 2010. The analysis of UGT1A1 genetic polymorphisms in 23 patients showed that frequencies of the UGT1A1*6 and UGT1A1*28 polymorphisms were 35% (eight patients) and 22% (five patients), respectively, and 17% (three patients) were UGT1A1*6/UGT1A1*28 compound heterozygotes. Of all patients who received irinotecan, dose reduction occurred in six patients (38%) and discontinuance in two patients (13%) due to neutropenia and other factors. Of these eight patients, seven (88%) had the UGT1A1*6 and/or *28 polymorphism. The most common irinotecan dose reduction was about 25% of the initial dose. Grade 4 neutropenia was observed in two patients who had the UGT1A1*6 and/or *28 mutation (13%), and one patient was a compound heterozygote. Our investigation confirmed that the UGT1A1 genetic polymorphism status of the patients was reflected in the discontinuance or dose reduction of irinotecan. Our results suggest that Grade 4 neutropenia may occur in patients who are compound heterozygotes and that these patients may need careful selection of treatment regimens possibly involving discontinuance or reduction in irinotecan dosage.

著者

富松 利明 松井 又夫 宇治 昭 加納 蓉子

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.82, no.11, pp.1560-1563, 1962-11-25 (Released:2010-02-19)

参考文献数

5

被引用文献数

6

---

Experimental evidences suggest that the bases contained in Thalictrum thunbergii DC. (Japanese name “Akikaramatsu”) differs slightly by its habitat. In order to elucidate this point, the root of this plant collected in Nagano Prefecture was processed and a comparatively large amount of magnoflorine (I) was obtained, while its leaves and stems yielded takatonine (II). The leaves and stems of the same plant collected in Kochi Prefecture yielded magnoflorine (I) and berberine (III). These results are summarized in Table I.