著者

河島 進 井上 陽子 示野 哲也 藤原 洋

出版者

公益社団法人日本薬学会

雑誌

Chemical & pharmaceutical bulletin (ISSN:00092363)

巻号頁・発行日

vol.38, no.2, pp.498-505, 1990-02-25

被引用文献数

2

---

Rectal absorption of morphine from various kinds of suppository bases was investigated. The extent of bioavailability of morphine by rectal administration varied with the bases used (30.5-97.5%), but every value was higher than that in the case of oral administration (13.5%). Witepsol bases were preferable to macrogol base for the rectal absorption of morphine. In particular, Witepsol S-55 or W-35 gave a higher plasma peak level than H-15 or E-75,whereas the difference in the mean residence times obtained from these bases could not be regarded as significant. Sustained-release suppositories of morphine could be prepared simply by mixing alginic acid (Alg) with morphine in a suppository base. Further, prolonged rectal absorption could be obtained by using these sustained-release suppositories, and the absorption rate was controlled by the amount of Alg added. It seems likely that the sustained release was due to the binding of morphine to Alg from the results of partition coefficient and binding ratio measurements in aqueous solution. The rapid initial absorption and the subsequent prolonged absorption of morphine simultaneously obtained from the morphine-Alg suppository may be useful in the clinical context.

著者

Jeon Jeong-Ryae Kim Jong-Yeon

出版者

公益社団法人日本薬学会

雑誌

Biological & pharmaceutical bulletin (ISSN:09186158)

巻号頁・発行日

vol.29, no.10, pp.2111-2115, 2006-10-01

参考文献数

19

被引用文献数

1 28

---

The present study examined the anti-obesity effects of pine needle extract (PNE) in 3T3-L1 preadipocytes and <i>in vivo</i> studies. PNE treatment suppressed both glycerol-3-phosphate dehydrogenase activity and expression of peroxisome proliferator-activated receptor (PPAR) &gamma; in cultured 3T3-L1 adipocytes. To investigate the effect of PNE on obesity in rats fed high-fat diet, four types of diet, which included a normal diet (ND), high-fat diet (HFD), ND+PNE, and HFD+PNE diets, were fed to the rats <i>ad libitum</i> for 6 weeks. The PNE supplement significantly decreased body weight gain and visceral fat mass compared to the HFD group. The total cholesterol, TG, and leptin levels in the plasma were significantly reduced by PNE supplementation compared with those of the HFD group. Histological findings in liver tissue showed that PNE supplementation alleviated steatosis induced by HFD. In conclusion, PNE treatment suppressed differentiation of 3T-L1 adipocytes, in part by down-regulating expression of PPAP&gamma; mRNA, and reduced adipose tissue mass, hyperlipidemia, and hepatic steatosis in obese rats fed HFD. Therefore, pine needle water extract may be considered for use in therapy to control obesity.

著者

Harada Shigeyoshi Haneda Eiji Maekawa Toshiro MORIKAWA Yuko FUNAYAMA Shinji NAGATA Nobuyuki OHTSUKI Kenzo

出版者

公益社団法人日本薬学会

雑誌

Biological & pharmaceutical bulletin (ISSN:09186158)

巻号頁・発行日

vol.22, no.10, pp.1122-1126, 1999-10-15

参考文献数

18

被引用文献数

7 33

---

The physiological significance of the casein kinase II (CK-II)-mediated phosphorylation of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) on its three enzymatic activities [RNA-dependent DNA polymerase (RDDP), DNA-dependent DNA polymerase (DDDP) and ribonuclease H (RNase H)] was investigated in vitro. It was found that (i) the purified recombinant RT (rRT) functioned as an effective phosphate acceptor for CK-II; (ii) the RDDP, DDDP and RNase H activity of rRT was stimulated about 2.8-, 4.1- and 3.9-fold, respectively, after full phosphorylation by CK-II; and (iii) this stimulation was selectively inhibited by potent CK-II inhibitors, such as neocarzinostatin-chromophore (NCS-chrom) and three polyphenol-containing anti-oxidant compounds [quercetin, epigallocatechin gallate (EGCG) and 8-chloro-3', 4', 5,7-tetrahydroxyisoflavone (8C-3', 4', 5,7-THI)]. These results suggest that (i) CK-II may be responsible for activation of RT in HIV-1-infected cells; and (ii) the selective inhibition of CK-II-mediated activation of HIV-1 RT by potent CK-II inhibitors may be involved in the mechanism of their anti-HIV-1 effects at the cellular level.

著者

比良野 矯

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.1925, no.520, pp.567-577, 1925

著者

尾崎 幸紘

出版者

公益社団法人日本薬学会

雑誌

Biological & pharmaceutical bulletin (ISSN:09186158)

巻号頁・発行日

vol.18, no.4, pp.559-562, 1995-04-15

参考文献数

23

被引用文献数

5 40

---

This study was carried out to examine the antiinflammatory effect of aqueous extracts of Kakkon-to (K), Kakkon-oren-ogon-to (KO), Kikyo-to (KK), Haino-to (H), Haino-san (HS), Mao-to (M) and Senkinkeimei-san (SK), which have been used for the treatment of stomatitis, tonsillitis, cold and chronic inflammatory diseases, and to elucidate the mode of their effects. Oral administration of K, KO, KK, H, HS, M and SK inhibited dose-dependently the increase of dye leakage induced by acetic acid in mice. Further antiinflammatory study was carried out on KK, H and HS which showed potent inhibition. All three extracts significantly inhibited the carrageenin-induced edema and the cotton pellet-induced granuloma formation. From these results, it is suggested that KK, H and HS may inhibit both the early exudative stage and the late proliferative stage in inflammatory processes. These extracts are comprised of Platycodon root as do other crude drugs, and the root may be partly responsible for the antiinflammatory effects induced.

著者

野島 庄七

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.28, no.4, 1992-04-01

著者

増田 克忠 神谷 高明 今城 芳夫 金児 龍彦

出版者

公益社団法人日本薬学会

雑誌

CHEMICAL & PHARMACEUTICAL BULLETIN (ISSN:00092363)

巻号頁・発行日

vol.19, no.1, pp.72-79, 1971

被引用文献数

25

---

A number of N-acyl and N-nitroso-3-dialkylaminosydnonimines (II) were synthesized by various acylating methods. In some cases, the acylation with activated esters, mixed anhydrides or dicyclohexylcarbodiimide was found to be more favorable. The reactivities of these derivatives towards acids and alkalis were investigated. Trifluoroacetyl (II-6) and formyl (II-1) compounds were easily deacylated in varuous conditions. Methylation took place at the acylated imino nitrogen of N-ethoxycarbonyl compound to give the quaternary salt (II-18). N-Acetyl compound (II-2) was compared with its 3-alkyl analog in the physicochemical properties ; its pK<SUB>a</SUB> values reveals that the morpholino group has little effect on the basicity of the compound.

著者

Gul Halise Inci Gul Mustafa Vespalainen Jouko ERCIYAS Ercin HANNINEN Osmo

出版者

公益社団法人日本薬学会

雑誌

Biological & pharmaceutical bulletin (ISSN:09186158)

巻号頁・発行日

vol.26, no.5, pp.631-637, 2003-05-01

参考文献数

38

被引用文献数

2 23

---

Acetophenone derived mono-Mannich bases (Ig1&mdash;Ig4), 1-aryl-3-amino-1-propanone hydrochlorides, which are known to have cytotoxicity in Jurkat cells, were synthesized. Then, they were converted to corresponding azine derivatives (D1&mdash;D4), <i>N</i>, <i>N</i>&prime;-bis(3-amino-1-aryl-propylidene)hydrazine dihydrochlorides, which are bifunctional agents. The aryl part was replaced by phenyl in Ig1, Ig2, Ig3, D1, D2, and D3, and by <i>p</i>-hydroxyphenyl in Ig4 and D4. The amine part was replaced by dimethylamine in Ig1, D1, Ig4 and D4, by piperidine in Ig2 and D2, and by morpholine in Ig3 and D3. The aim of this study was to investigate whether the modification in chemical structure, converting the mono-Mannich base to a corresponding azine derivative, improves the cytotoxicity. In addition, the effect of the representative compound, D3, <i>N</i>, <i>N</i>&prime;-bis(3-morpholine-4-yl-1-phenylpropylidene)hydrazine dihydrochloride, on cellular glutathione level after 1 h exposure in phosphate buffer at 37 &deg;C was also determined to provide information on a possible mechanism of cytotoxic action. Compounds D2&mdash;D4 are reported for the first time in this study. Except for Ig2 and D2, the cytotoxicity of mono-Mannich bases, Ig1, Ig3 and Ig4 and corresponding azine derivatives, D1, D3 and D4 were higher than the reference compound 5-FU. Azine derivatives D1 and D4 had almost equal cytotoxic potency with corresponding mono-Mannich bases Ig1 and Ig4, respectively. On the other hand, azine derivatives D2 and D3, had 1.28 and 1.90-times less cytotoxicity in Jurkat cells compared with the mono-Mannich bases, Ig2 and Ig3, respectively, from which they are derived. Azine derivative D3 dose-dependently decreased the total cellular glutathione level, suggesting that azine derivatives may exert cytotoxicity by thiol alkylation. Azine derivatives with equal or less cytotoxic potency compared to the mono-Mannich bases they are derived from seemed to be less suitable derivatives for the development of new cytotoxic compounds.

著者

Makino Yukiko Tanaka Satoshi Kurobane Shingo NAKAUCHI Masato TERASAKI Takahiro OHTA Shigeru

出版者

公益社団法人日本薬学会

雑誌

Journal of health science (ISSN:13449702)

巻号頁・発行日

vol.49, no.2, pp.129-137, 2003-04-01

参考文献数

7

被引用文献数

4 23

---

We have investigated 100 illegal amphetamine-type stimulant (ATS) tablets seized in Japan to obtain information about the nature of these tablets abused in Japan. For physical characterization, 15 items (logo, vertical view, colour, diameter, weight, smell, <I>etc</I>.) were measured and a photograph was taken. For chemical characterization, the components in the tablet were identified by GC-MS and HPLC, and quantified by HPLC using an ODS-type column. The maximum content of <I>N</I>-methyl-3,4-methylenedioxyamphetamine (MDMA) was 189 mg/tablet and that of 3,4-methylenedioxyamphetamine (MDA) was 87 mg/tablet. The detected components, other than MDMA and MDA, were <I>N</I>-ethyl-3,4-methylenedioxyamphetamine (MDEA), ephedrine, caffeine, ketamine, and methamphetamine. In this report, we propose a method for profiling ATS tablets.

著者

森田 直賢 清水 岑夫 竹崎 孝行

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.88, no.10, pp.1277-1280, 1968-10

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A new glycoside (I), C_<24>H_<26>O_<18>・11/2H_2O, mp 274-275°, was isolated from Chrysosplenium grayanum MAXIM. (Japanese name"Nekonomeso"), and a glycoside (II), C_<24>H_<26>O_<12>・2H_2O, mp 175-176°, from C. flagelliferum FR. SCHM. (Japanese name"Tsurunekonomeso"). I was determined as oxyayanin-A (5,2', 5'-trihydroxy-3,7,4'-trimethoxyflavone)-2'-glucoside, and was named chrysosplenoside-A , and II as pendulin (5,4'-dihydroxy-3,6,7-trimethoxyflavone-4'-glucoside).

著者

萩庭丈寿 坂井 進一郎 相見 則郎 山中 悦二 新間 信夫

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.93, no.4, pp.448-452, 1973-04

被引用文献数

2

---

In the reinvestigation of the constituents of Uncaria rhynchophylla MIQ. (Japanese name "kagikazura"), the presence of two oxindole alkaloids, corynoxeine and isocorynoxeine, was demonstrated, besides the reported rhynchophylline and isorhynchophylline.^<3)> Furthermore, four indole alkaloids were newly isolated ; hirsutine, hirsuteine, dihydrocorynantheine, and corynantheine. A chemical structural evidence of hirsutine was obtained from its epimerization to dihydrocorynantheine with acetic acid catalysis.

著者

古川

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.104, pp.698-705, 1890-10-26

著者

本間 克明 酒井 律子 武島 晶子 島森 美光 早瀬 幸俊

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 = Journal of the Pharmaceutical Society of Japan (ISSN:00316903)

巻号頁・発行日

vol.124, no.10, pp.693-697, 2004-10-01

参考文献数

5

被引用文献数

1

---

生活環境の改善や医学の進歩等により, わが国の平均寿命は平成13年では男性78.07年, 女性84.93年となり, 1)世界有数の長寿国となっている. そして, 65歳以上の高齢者人口は平成12年でおよそ2200万人と総人口の17.4%を占めており, 平成27年には26%台となり, さらに平成42年には29.6%, 平成62年には35.7%に達すると推計されている. 2)このような急速な高齢化の進展や疾病構造の変化等によりわが国の医療をとりまく環境は大きく変化しており, それに伴い国民医療費は年々増大し, 平成11年度には約30兆円に到達した. 年齢階級別国民医療費を平成12年度で見ると, 65歳以上の医療費が約12兆円で, 実に50%を占めるに至っており, これを1人当たりの医療費で見ると, 15歳から44歳が約7万円, 45歳から64歳が約19万円であるのに対して, 65歳以上では約54万円, 70歳以上では約63万円, 75歳以上では約70万円と15歳から44歳及び45歳から64歳の医療費に比べて, それぞれ約3倍から10倍高くなっている. 3)この原因としては高齢者は受診率が高く, また重症化し易く, かつ治療には長期間かかることなどが考えられている.

著者

樫原 宏 末宗 洋 常広 菜穂美 酒井 浄

出版者

公益社団法人日本薬学会

雑誌

Chemical & pharmaceutical bulletin (ISSN:00092363)

巻号頁・発行日

vol.38, no.9, pp.2581-2582, 1990-09-25

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The enones (II), which were obtained from dimethyl 4,5-isopropylidenedioxy-2-oxopentylphosphonate (Ia) and various aldehydes, were easily converted to 2-alkenylfurans (III) by treatment with p-TsOH in MeOH. In a similar manner, the furfuryl phosphonate (IVa) and the 3-methylfurfuryl phosphonate (IVb) were obtained from Ia and its 3-methylated analogue (Ib), respectively.

著者

渡部 恵 杉浦 宗敏 清野 敏一 光永 義治 中村 均 山田 安彦 土屋 文人 大江 和彦 伊賀 立二

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 = Journal of the Pharmaceutical Society of Japan (ISSN:00316903)

巻号頁・発行日

vol.122, no.10, pp.841-847, 2002-10-01

参考文献数

4

被引用文献数

4 4

---

In the computerized prescription order entry system, it has been pointed out that a physician's input mischoice for medicine is one of the causes of medication errors. We therefore investigated the input mischoices by physicians at the time of writing prescriptions. Subsequently, the number of input characters in a prescription order was changed to three characters from two characters. Furthermore, 105 items of high-alert medications, which are likely to result in injury if errors occur, were established. A warning screen display system that requests reconfirmation of the effect, name, usage, and dosage of those medicines was also built. It was found that 70% of input mistakes were caused by choosing the medicine displayed immediately above or below the desired drug. By changing the number of input characters of a prescription order to three characters from two characters, the rate of specification of a trademark improved sharply from 36% to 85%. Consequently, the rate of choice of a drug with another trademark decreased significantly from 0.028% to 0.0047%. In 5% of cases when the warning screen was displayed for a high-alert medicine, the prescription was stopped, and 25% were changed to other medicines. The above results show that the system that requires the input of three or more characters for the physician order entry and displays a warning screen for high-alert medicines is useful in preventing mischoices at the time of prescription input.<br>

著者

Fortin Helene Tomasi Sophie Jaccard Philippe ROBIN Valerie BOUSTIE Joel

出版者

公益社団法人日本薬学会

雑誌

Chemical & pharmaceutical bulletin (ISSN:00092363)

巻号頁・発行日

vol.49, no.5, pp.619-621, 2001-05-01

参考文献数

18

被引用文献数

19

---

A new coumarin identified as 5-hydroxy-6-methoxy-7-(3-methyl-but-2-enyloxy)-2H-1-benzopyran-2-one (isoobtusitin) was isolated from Psiadia dentata. This compound showed, in vitro, a moderate inhibitory activity against poliovirus and a very weak activity against (HIV), whereas it was inactive against (HSV1), (VSV), and murine tumoral cell lines (3LL, L1210).

著者

Jiang Saho Jun Zhou Xiao Jun

出版者

公益社団法人日本薬学会

雑誌

Biological & pharmaceutical bulletin (ISSN:09186158)

巻号頁・発行日

vol.26, no.1, pp.66-68, 2003-01-01

参考文献数

16

被引用文献数

1 39

---

The epidermal permeability barrier appears to be regulated primarily by the lamellar arrangement of lipid bilayers between coneocytes of the stratum corneum and presents a significant barrier to the transdermal delivery of drugs. The aim of the present study was to investigate the effects of oleic acid on the ultrastructure of stratum corneum lipids in rat skin. Wistar rats were treated topically with 10% oleic acid/propylene glycol for 2 h, the structure of stratum corneum was examined by electron microscopy using osmium tetroxide or ruthenium tetroxide postfixation, and the epidermal barrier function was evaluated in a lanthanum tracer study. Ultrastructural examination revealed that there was a marked alteration in the stratum corneum and the tracer penetrated into the intercellular spaces of the stratum corneum after application of oleic acid. These results suggest that ruthenium tetroxide postfixation is a powerful tool for the study of the stratum corneum lipid structure. Oleic acid might increase the epidermal permeability through a mechanism involving the perturbation of stratum corneum lipid bilayers and lacunae formation to enhance transdermal drug delivery.

著者

柴田 丸 吉田 玲子 本橋 幸子 福島 正子

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.93, no.12, pp.1660-1667, 1973-12

被引用文献数

8

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Crude saikosides did not affect the LD_<50> value of sodium hexobarbital in mice. It also exerted a protective effect on the pylorus-ligated ulcer of the rat with inhibiting gastric secretion. The cure of chronic ulcer produced by the injection of dilute acetic acid into the rat gastric wall was promoted by crude saikosides. Saikogenin A showed a potent effect of decreasing spontaneous motor activities of the mice treated with methamohetamine hydrochloride. It had a significant antitussive, hypothermic, and antipyretic effect, and inhibition of acetic acid-induced writhing responses. In addition, salikogenin A strongly reduced a carrageenin-induced rat paw edema, without any local irritaition by topical application. On the contrary, only analgesic effect was found in the syrupy residue. The significance of these pharmacological results was discussed.

著者

Sun Nan Hao Lili Xue Jian Jin Hongyu Tian Jingai Lin Ruichao

出版者

公益社団法人日本薬学会

雑誌

Journal of health science (ISSN:13449702)

巻号頁・発行日

vol.53, no.4, pp.464-469, 2007-08-01

被引用文献数

17

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A rapid and simple method for the simultaneous analysis of 18 pesticides (α-(C_6H_6Cl_6)-Benzene hexachloride, β-BHC, γ-BHC, δ-BHC, heptachlor, heptachlor epoxide, tecnazene, pentachloronitrobenzene (PCNB), hexachlorobenzene, aldrin, methyl pentachlorophenyl sulphide (MPCPS), α-endosulfan, trans-chlorodane, cis-chlorodane, p,p'-(C_<14>H_8Cl_4)-Dichlorodiphenyl dichloroethylene, o,p'-(C_<14>H_9Cl_5)-Dichlorodiphenyl trichloroethane, p,p'-(C_<14>H_<10>Cl_4)-Dichlorodiphenyl dichloeoethane, p,p'-DDT) by gas chromatography (GC) in 10 Traditional Chinese Medicines (TCMs) has been developed. The limit of detection was found to be 1.2×10^<13> to 9.0×10^<13>g with the recoveries ranging from 72.9 to 114.5% and Relative Standard Deviation being less than 17.5%. In addition, the assay was applied to monitor the residues in 10 TCMs, amongst which at least one of the above pesticides were found in 67 samples. The results showed that α-BHC was the most frequently detected with a presence of 44.6% in the tested samples, whilst heptachlor epoxide, trans-chlorodane, cis-chlorodane and p,p'-DDD were not detected at all. Nonetheless, none of pesticides in all samples appeared to exceed the maximum residue limits (MRLs) seen in the Chinese regulations.

著者

山崎 正利 池並 通裕 来生 淳 油井 聡 安部 茂 水野 伝一

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.104, no.7, pp.p769-774, 1984-07

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The present study shows that some selected anti-cancer drugs induce tumor lysis in vitro in cooperation with phagocytic cells (drug-dependent cellular cytotoxicity ; DDCC) and that chemotherapeutic drugs augment the mediator-dependent killing activity of macrophages. Tumor cells pretreated with the drugs were susceptible to phagocytemediated killing. Tumor necrosis serum can also cooperate with some drugs in killing tumor cells. Moreover, some selected drugs can induce cytotoxic macrophages and the quantitative changes of phagocytes such as polymorphonuclear leukocytes. These results suggest that some anti-cancer drugs have the activities of inactivation of tumor cells and/or activation of host cells. Thus, tumor cells may be killed effectively in vivo by anti-cancer drugs through these mechanisms.