著者

青木 聡之

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.36, no.5, pp.409-410, 2000

参考文献数

3

著者

松村 靖

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.50, no.1, pp.39-43, 2014 (Released:2016-02-01)

参考文献数

21

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フッ素は他の元素には見られない独特の物理化学的性質を有するため,生体内での吸収や代謝に与える効果に加えて,薬理作用の発現や増強に及ぼす影響が注目されている.医薬や農薬の分野において開発される含フッ素化合物の増加には,目を見張るものがある.今やフッ素による構造修飾は,ドラッグデザインの重要な手段の1つと言えるかもしれない.しかし一方で,構造修飾の手法は芳香環部位へのフッ素原子やCF3基の導入がほとんどであり,化合物の主鎖となる骨格や脂肪族置換基にフッ素を導入した例は限られている.また,薬物が受容体に結合するときのフッ素と受容体アミノ酸残基との直接的な相互作用やフッ素の立体電子的効果については,いまだによく分かっていない.さて,読者の皆様は,研究対象の化合物の構造を眺めていて,ふと「ここにフッ素を入れたら,面白い活性や物性が出るかもしれないなあ…」などと思われたことはないだろうか.我々は1980年頃より,プロスタグランジン(PG)などの生理活性物質にフッ素を導入した誘導体を合成し,フッ素が生理活性や物性に及ぼす効果について研究を行ってきた.何かフッ素の特徴を生かしたユニークなドラッグデザインができないだろうかと考えるとき,どのようにして目指す位置に選択的にフッ素を導入するかが常に問題となり,新たな合成法の開発が鍵となることを痛感してきた.本稿では,主鎖にジフルオロメチレン(-CF2-)骨格を持つPG誘導体について,フッ素の効果に焦点を絞って,ドラッグデザインとフッ素導入法を中心に概説し,緑内障治療薬タフルプロスト(tafluprost)の誕生に至る経緯を交えて紹介したい.

著者

渡邉 文之 篠原 久仁子 土橋 朗 天貝 賢二 原 和夫 倉田 香織 飯嶋 秀郎 島川 清 島田 匡彦 阿部 櫻子 武井 敬司 亀井 美和子

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI

巻号頁・発行日

vol.136, no.9, pp.1243-1254, 2016

被引用文献数

3

---

&emsp;This study built a protocol for drug therapy management (hereinafter &ldquo;the protocol&rdquo;) that would enable continuous support from the decision making of smoking cessation therapy to the completion of therapy through the collaboration of physicians and community pharmacists, after which we evaluated whether the use of this protocol would be helpful to smoking cessation therapy. This study utilized the &ldquo;On the Promotion of Team-Based Medical Care&rdquo;, a Notification by the Health Policy Bureau as one of the resources for judgment, and referred to collaborative drug therapy management (CDTM) in the United States. After the implementation of this protocol, the success rate of smoking cessation at the participating medical institutions rose to approximately 70%, approximately 28-point improvement compared to the rate before the implementation. In addition to the benefits of the standard smoking cessation program, this result may have been affected by the intervention of pharmacists, who assisted in continuing cessation by advising to reduce drug dosage as necessary approximately one week after the smoking cessation, when side effects and the urge to smoke tend to occur. Additionally, the awareness survey for the intervention group revealed that all respondents, including patients who failed to quit smoking, answered that they were satisfied to the question on general satisfaction. The question about the reason for successful cessation revealed that the support by pharmacists was as important as, or more important than, that by physicians and nurses. This infers that the pharmacists' active engagement in drug therapy for individual patients was favorably acknowledged.<br>

著者

伊東 秀之 三宅 陽子 吉田 隆志

出版者

公益社団法人 日本薬学会

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.43, no.7, pp.1260-1262, 1995

被引用文献数

32

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Three new piscicidal triterpenens named irisgermanicals A, B and C along with seven known iridal-type triterpenes including iripallidal and iriflorental were isolated from the bark of Iris germanica rhizome, upon bioassay-guided fractionation using the Medaka (killie-fish; Oryzias latipes), and their bicyclic structures were elucidated based on the spectral analyses. Irisgermanicals B and C were characterized as geometrical iriflorental and iripallidal isomers, respectively, concerning the α, β-unsaturated aldehyde moiety. The piscicidal activity was observed for bicyclic iridals, among which iriflorental exhibited most potent activity.

著者

長井 紀章

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.136, no.10, pp.1385-1390, 2016 (Released:2016-10-01)

参考文献数

20

被引用文献数

5

---

The ophthalmic application of drugs is the primary route of administration for the therapy of glaucoma; however, in traditional formulations, only small amounts of the administered drug penetrate the cornea to reach the desired intraocular tissue due to corneal barriers. Recently, nanoparticulate drug delivery is expected as a technology to overcome the difficulties in delivering drugs across biological barriers (improvement of bioavailability). In this study, we attempted to establish a new method for preparing solid drug nanoparticles by using a bead mill and various additives, and succeeded in preparing a high quality dispersion containing drug nanoparticles. For a more concrete example, a mean particle size of disulfiram (DSF) treated with bead mill is 183 nm. The corneal penetration and corneal residence time of DSF from the ophthalmic dispersion containing DSF nanoparticles were significantly higher than those from a 2-hydroxypropyl-β-cyclodextrin solution containing DSF (DSF solution). It is known that the administration of DSF has intraocular pressure (IOP)-reducing effects. The IOP-reducing effects of the ophthalmic dispersion containing DSF nanoparticles were significantly greater than those of the DSF solution in rabbits (the IOP was enhanced by placing the rabbits in a dark room for 5 h). In addition, the ophthalmic dispersion containing DSF nanoparticles is better tolerated by corneal epithelial cells than DSF solution. It is possible that dispersions containing DSF nanoparticles provide new possibilities for effectively treating glaucoma, and that ocular drug delivery systems using drug nanoparticles may expand their usage for therapy in the ophthalmologic field.

著者

野本 裕也

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.50, no.10, pp.1024-1024, 2014 (Released:2016-09-30)

参考文献数

5

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クラウドソーシングは群衆(crowd)と人材資源利用(sourcing)を組み合わせた造語であり,アウトソーシング(専門性の高い業務委託)に比べて,よりオープンに不特定多数の人間の協力を募り,比較的安価にプロジェクトを遂行する手法とされ,現在,様々な分野で応用されている.なお,本稿は下記の文献に基づいて,その研究成果を紹介するものである.1) Lin D. et al., Angew. Chem. Int. Ed., 53, 804-809 (2014).2) Johnson R., Nature Chem., 6, 87 (2014).3) Stadler M., Keller N. P., Mycol. Res., 112, 127-130 (2008).4) Hawksworth D. L., Stud. Mycol., 50, 9-18 (2004).5) Lessl M. et al., Nat. Rev. Drug Discov., 10, 241-242 (2011).

著者

百瀬 和享

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.23, no.4, 1987

著者

島野 仁

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.9, pp.1003-1009, 2015 (Released:2015-09-01)

参考文献数

17

被引用文献数

4

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Recent studies suggest that chronic local inflammation and cellular stresses are the key steps in organ defects in obesity-related diseases such as atherosclerosis, diabetes, and fatty liver. We have shown that an excess energy state activates sterol regulatory element-binding protein (SREBP)-1c, a master transcription factor for fatty acid synthesis causing the accumulation of lipids leading to fatty liver, insulin resistance, insulin secretion defects, and dyslipidemia and we clarified their molecular mechanisms. Recently, we shifted focus to the quality aspect of accumulated lipids. It has long been known that saturated and poly-unsaturated fatty acids are atherogenic and anti-atherogenic, respectively. Besides desaturation, we found that the chain-length of fatty acids is another important factor. Elovl6 that we have cloned as an SREBP-1 target is a fatty acid elongase that catalises the last step of fatty acid synthesis. Elovl6 KO mice exhibit obesity and fatty liver on a high energy diet, but unexpectedly were immune to insulin resistance (Nat. Med., 13, 2007, Matsuzaka et al.), atherosclerosis (Arterioscler. Thromb. Vasc. Biol., 31, 2011, Saito et al.) and non-alcoholic steatohepatitis (NASH) pathology including liver damage, ROS, and fibrosis (Hepatology, 56, 2012, Matsuzaka et al.). Elovl6 is crucial for protection against lung fibrosis (Nat. Commun., 4, 2013, Sunaga et al.). These data implicate that fatty acid composition is a new therapeutic target for a variety of chronic metabolic diseases. In this symposium review, a novel strategy for the prevention of life-related diseases will be discussed in the standpoint of application of wet-dry fusion strategies for theoretical and medicinal chemistry.

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.52, no.4, pp.360-363, 2016 (Released:2016-04-01)

著者

落合 康

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.47, no.1, pp.42-45, 2011-01-01 (Released:2017-02-11)

著者

内藤 多喜夫 岩田 平太郎

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.9, no.2, pp.91-94, 1973

著者

川田 稔 高梨 茂 中島 靖夫

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.774-776, 1961-05-25 (Released:2010-02-19)

参考文献数

4

---

Ferrous [59Fe] D-glucuronate was prepared from glucuronic acid and ferrous [59Fe] carbonate which was obtained from 59FeCl3. In this reaction almost the whole process was carried out automatically in nitrogen atmosphere. Determination of glucuronic acid in ferrous glucuronate by naphthoresorcinol picrate was not disturbed by the presence of radioactive ferrous ion.

著者

綾田 渙

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.778-783, 1961-05-25 (Released:2010-02-19)

参考文献数

11

被引用文献数

1

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Resolution of dl-(2-hydroxy-3-cyanopropyl) trimethylammonium chloride (III) was carried out with d-tartaric acid or dibenzoyl-d-tartaric acid, and dextro- and levorotatory compounds of (III) were obtained. Hydrolysis of these optically active (III) with conc. hydrochloric acid by heating in a boiling water bath afforded the corresponding d- and l-(2-hydroxy-3-carboxypropyl) trimethylammonium chloride (VII). Of these, the levorotatory (VII) was found to correspond to the hydrochloride of natural carnitine (VIII). Infrared spectra of these compounds are given.

著者

市川 正孝 高木 康 一番ケ瀬 尚

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.768-771, 1961-05-25 (Released:2010-02-19)

参考文献数

4

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Nitration of ethyl 8-hydroxycoumarin-3-carboxylate (I) in glacial acetic acid solution affords ethyl 5-nitro-8-hydroxycoumari-3-carboxylate (III), m.p. 203.5-204°, and ethyl 7-nitro-8-hydroxycoumarin-3-carboxylate (IV), m.p. 201-202°. Methylation of (III) and (IV) with methyl iodide respectively gives 8-methoxy compounds, (VII) of m.p. 184-186°, and (VIII) of m.p. 152°, respectively. On the other hand, nitration of 3-methoxy-salicylaldehyde acetate (XVI) affords 4-nitro (IX), m.p. 92-93°, 5-nitro (X), m.p. 142°, and 6-nitro (XI), m.p. 104°, compounds. By condensation of (IX) and (XI) with ethyl malonate, in the presence of piperidine, the position of the nitro group in the foregoing (III) and (IV) was determined.Hydrolysis of (I), (III), and (IV) with hydrochloric acid respectively afforded 8-hydroxycoumarin-3-carboxylic acid, m.p. 292-293° (decomp.), 5-nitro-8-hydroxycoumarin-3-carboxylic acid, m.p. 292-293° (decomp.), 5-nitro-8-hydroxycoumarin-3-carboxylic acid (V), 257-258°, and 7-nitro-8-hydroxycoumarin-3-carboxylic acid (VI), m.p. 246-248°.

著者

桑野 晴光 田村 千尋

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.764-767, 1961-05-25 (Released:2010-02-19)

参考文献数

5

被引用文献数

2 2

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Polymorphism of chloramphenicol was examined by the X-ray diffraction method and quantitative relationship between the two crystal forms was examined. In general, proportionation of concentration to diffraction intensity can be quantitated in polymorphs but the method was inconvenient for use with organic compounds due to strict packing conditions. In the binary system (α- and β-forms) of chloramphenicol palmitate, specific intensity and specific concentration of the component were in proportion and quantitative straight line independent of packing codition was obtained. This was found to be effective in the range of over 3% of the β-form and precision is within 1%. As the quantitative linear equation: the following was obtained: xβ/xα=(0.347±0.005)⋅Iβ/Iα, where x is the concentration of the component and I is the intensity of reflection.

著者

田村 千尋 桑野 晴光

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.759-764, 1961-05-25 (Released:2010-02-19)

参考文献数

6

被引用文献数

1 1

---

From the consideration of X-ray diffraction, infrared absorption spectra, and various transition conditions of long-chain esters of chloramphenicol, and some assumptions were made on their crystal structure.1) According to X-ray diffraction, all-trans configuration for the long-chain portion of the β-form molecule results in good agreement between the molecular models and the long axis by X-ray measurement. In the case of α-form, the long axis of the crystal cannot be explained unless the molecule is assumed to have some cis linkages or the long chain part is a trans structure but deeply twined with each other.2) Infrared absorption spectra suggest that the α-form is closely resembled to a solution state and crystals with a cis configuration, having distorted molecule, may be assumed. The β-form is considered to have a higher order molecular arrangement as a crystal and it is convenient to assume an all-trans configuration by X-ray measurement.3) Stability of the β-form can be assumed form the measurement of melting point and specific gravity. On the other hand, similarity to the α-form and solution state (or amorphous state) as found from transition conditions and these agree well with the above two measurements.

著者

田村 千尋 桑野 晴光

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.755-759, 1961-05-25 (Released:2010-02-19)

参考文献数

6

被引用文献数

13 19

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It was found that chloramphenicol palmitate, myristate, and caprylate come in two kinds of crystalline form and one amorphous form. These compounds were prepared and their transition conditions were examined.1) When the crystals is dissolved in a solvent and crystallized out, optional form of crystals can be obtained by controlling crystallization rate and this form is not affected by polarity or pH of the solvent. Crystals of α-form is obtained by rapid crystallization while the β-form is obtained by gradual crystallization. When a small amount is fused and cooled rapidly in a refrigerator, a vitrious substance is obtained.2) Transition between the solids occur only in the direction of amorphous to α-form to β-form, and there is no reverse progress. The transition rate is faster, the nearer the melting point. The mechanism of such a transition is thought to be the transition to a stable form by the heat motion of the molecule itself. The transition rate becomes suddenly rapid after formation of β-form crystal and this is considered to be due to added effect of catalytic transition.

著者

関口 慶二

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.81, no.5, pp.664-669, 1961-05-25 (Released:2010-02-19)

参考文献数

9

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Solubilizing action of the sodium salt of benzoic acid, o-, m-, and p-hydroxy-, methoxy-, amino-, nitro-, and chloro-benzoic acid, and nicotinic acid on caffeine was determined and the effect of the kind and position on the solubilization was examined. The solubilizing action was found to be in the descending order, in molar equivalent of the salt, of salicylate≅m-chloro-, p-chloro-, m-hydroxy-≅p-hydroxy-≅m-methoxy-≅p-methoxy-, m-nitro-, p-nitro-, o-amino-, and p-amino-benzoate, benzoate, m-aminobenzoate, nicotinate, and o-chloro-, o-methoxy-, and o-nitro-benzoate. The solubilizing action of these benzoates is assumed to be not due to formation of a complex of established composition but due to the formation of a hydrogen bond between caffeine and benzoate, with the water molecule of the solvent acting as the hydrogen-bond donor.

著者

掛見 喜一郎 有田 隆一 大橋 貞

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.748-750, 1961-05-25 (Released:2010-02-19)

参考文献数

2

被引用文献数

1 1

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Potency determination of kanamycin solution was carried out as follows: To 5cc. of kanamycin solution in water, 0.5cc. of 20% sodium carbonate solution is added, followed by 0.5cc. of 1% solution of sodium 1, 2-naphthoquinone-4-sulfonate with cooling in ice water, and the mixture is allowed to stand at 0° to 2° for 20 minutes, protected from light. To this solution, 1.0cc. of acetone and 0.5cc. of 50% acetic acid are added and optical density of this solution, is measured at 420 mμ. As a control, the same procedure is carried out with distilled water in place of the sample solution. The potency of the sample solution is read from the calibration curve prepared with kanamycin of known potency.The same determination was carried on samples boiled with acid or alkali, and samples left at various temperatures. Comparison of the values so obtained with the values determined by the cup method, stipulated in the antibiotics standard, showed good agreement.

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

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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.