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Volume 113, Issue 5
Displaying 1-8 of 8 articles from this issue
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Atsushi SUGII1993 Volume 113 Issue 5 Pages 343-355
Published: May 25, 1993
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe versatility of 4-vinylpyridinium (4VP-EG-Q) and quaternized dimethylaminomethylstyrene (PDAMS-Q) polymers synthesized by suspension copolymerization as column packings for high performance ion-exchange chromatography was described. The proposed polymer columns afforded resolution of human/bovine serum albumin components, such as mercaptalbumin and nonmercaptalbumin. It was suggested that the physicochemical structure on the external surface of the ion-exchangers was very important in the resolution. The characteristics of 4VP-EG-Q column were effectively applied to the investigation of the metal-albumin complexes, whereas a rapid analysis of mercaptalbumin in the human serum using the PDAMS-Q column was performed by isocratic elution.View full abstractDownload PDF (1043K) -
Yoshiharu MACHIDA1993 Volume 113 Issue 5 Pages 356-368
Published: May 25, 1993
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSTopical drug delivery is important from the view points of improvement of therapeutic effect and reduction of systemic side effects. Utilization of polymeric materials seemed to be as a key for the development of new topical dosage forms including targeting drug delivery ststems. Adriamycin ointment for local chemotherapy to breast cancer prepared using polyethylene glycol, ammonium polyacrylate and hydroxypropyl cellulose (HPC) according to an optimum formulation showed an excellent clinical effect in spite of a decreased drug content. Double-layered mucoadhesive sticks for the treatment of uterine cervix cancer were prepared by direct compression of powder mixture of bleomycin, HPC and carboxyvinyl polymer (CP). Drug release property of the sticks could be controlled by the weight of outer layer, drug combining ratio to each layer and coating of core layer. The results suggested a possibility of a "once-a-week"treatment that is preferable for the patients. Magnetic granules for the treatment of esophageal cancer were prepared using ferrite, HPC and CP. Magnetic guidance and retainment of the granules on esophageal mucosa were confirmed using rabbits in vivo. Buoyant sustained release preparations were prepared using chitosan, soybean protein, HPC and other polymers. Usefulness of the buoyant preparations was suggested from the results in vitro and in vivo. Insulin microspheres (IMS) for targeting delivery to the small intestine were prepared by the newly developed method. Employment of enteric coating material (Eudragit) and combination of protease inhibitor protected insulin from enzymatic attack and gave decreased levels of blood glucose by oral administration.View full abstractDownload PDF (1300K) -
Shigeo KUBO, Tetsuya UEDA, Itaru NAKANISHI, Katsuko HOSODA, Mamoru NOG ...1993 Volume 113 Issue 5 Pages 369-375
Published: May 25, 1993
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSFor the purpose of investigating the effect of soil microflora on the growth of Bupleurum falcatum (B. falcatum), colony forming units (CFU) of bacteria, gram-negative bacteria, fluorescent Pseudomonas species, actinomycetes, facultative anaerobes, fungi and yeast in the non-rhizosphere soil, rhizosphere soil and rhizoplane of B. falcatum cultivated under 3 kinds of soils with and without ventilation were assayed. Although the conditions of cultivation were different among each experimental field, CFU of fluorescent Pseudomonas species and actinomycetes had a highly positive correlation with the growth of B. falcatum. A negative correlation between CFU of fungi and the growth of B. falcatum was also observed. These results suggested that populations of these microorganisms are closely related to the growth of B. falcatum.View full abstractDownload PDF (683K) -
Tamaki MIYAZAKI, Chikako YOMOTA, Satoshi OKADA1993 Volume 113 Issue 5 Pages 376-384
Published: May 25, 1993
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe partition behavior of tropane alkaloids (TrA) between organic solvent and water was studied under various conditions. The apparent partition coefficient, log P', increases with pH with a slope of +1 in the acidic to neutral pH range, then tends to approach to a constant value in the alkaline region. Thus the partition of TrA to the organic phase is based on the neutral form of TrA. From the pH dependency of the partition and pH titration of TrA, the intrinsic partition coefficients log P0 and pKa values for each TrA were estimated. Values of pKa and log P0 for scopolamine were smaller than those for atropine or homatropine. It was considered that the presence of the epoxide ring in scopolamine molecule reduces the log P0 and pKa because of its polar and electro-inductive effect. It was also expected from the results of pH-dependent partition behavior that in the low pH region some portion of TrA cations is transferred to the organic phase by forming an ion-pair complex with an anion, in the aqueous phase. The log P'of TrA was measured in the presence of various kinds of anions (halides and alkyl sulfonates, C5-C8) at about pH 2, where almost all TrA are present as a protonated form. The relations between the log P'and the logarithmic concentration of anions is linear at low concentrations of anions as expected from the ion-pair partition equation. The ion-pair partition coefficient Pi and the ion-pair formation constant Ki for each ion-pair of TrA/anion were obtained separately from the reciprocal plot of 1/[X-]w versus 1/P'. The differences of Pi, Ki and the product Pi·Ki between anions and/or TrAs were discussed in detail.View full abstractDownload PDF (873K) -
Shuji YAMAUCHI, Noriyuki NIMURA, Toshio KINOSHITA1993 Volume 113 Issue 5 Pages 385-390
Published: May 25, 1993
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSProtamine was found to stabilize ascorbic acid (AsA) in aqueous solution. The concentration of AsA (50 μmol/l) dissolved in 0.05 M phosphate buffer, pH 7, decreased by 57% after standing for 90 min at 30°C, whereas 91% of AsA remained under the same conditions in the presence of 60 μmol/l protamine. When 0.5 μmol/l of copper ion (II) was added to the above AsA solution (0.05 M phosphate buffer, pH 7) in the absence of protamine, AsA decreased by 5% after standing for 15 min at 30°C. On the other hand, 91% of AsA remained after 15 min and 52% of AsA remained after 90 min under the same conditions in the presence of 60 μmol/l protamine. Furthermore, the effect of protamine on the stability of AsA in various pH solutions (pH 1-10) was examined after standing for 90 min at 30°C. Degradation of AsA was accelerated by increasing the pH from 1 to 10. On the other hand, the effect of protamine (60 μmol/l) on the stabilization of AsA was recognizable above pH 5 and degradation of AsA was controlled at higher pH. When 0.5 μmol/l of copper ion (II) was added to the above solutions in the absence of protamine, degradation of AsA was greatly accelerated above pH 5. When 60 μmol/l of protamine was added to the solutions, the effect of protamine on the stabilization of AsA was observed above pH 5 and degradation of AsA was controlled at higher pH.View full abstractDownload PDF (624K) -
Hiroyuki FUJINO, Ikuyo UENO, Shujiro GOYA1993 Volume 113 Issue 5 Pages 391-395
Published: May 25, 1993
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESS3-(7'-Methoxycoumarin-3'-carbonyl)-benzoxazoline-2-thione (MCBT) was synthesized as a precolumn fluorescent labeling reagent for amantadine for use in high-performance liquid chromatography (HPLC). Amantadine was derivatized quantitatively into a fluorescent compound through the amino group by treatment with MCBT at room temperature for 5 min in aqueous 95% acetonitrile solution in the presence of 4-dimethylaminopyridine. The derivative was subjected to HPLC on TSK gel ODS-80TM (250×4.6 mm i.d.) with methanol-water (10 : 1) as the mobile phase and monitored with an excitation wavelength of 355 nm and an emission wavelength of 405 nm. The limit of detection was 2.0 μg/ml in the urine. This method was satisfactory with respect to simplicity and precision to quantify amantadine spiked in the urine.View full abstractDownload PDF (568K) -
Kazutomo OHASI, Katsuhito SATONAKA, Tetsuro YAMAMOTO, Masatoshi YAMAZA ...1993 Volume 113 Issue 5 Pages 396-399
Published: May 25, 1993
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe antitumor activity of a preparation of heat-killed cells of Enterococcus faecalis, FK-23. Intraperitoneal injection of the preparation prolonged the lifespan of C3H/He N mice which were intraperitoneally inoculated with MM46 mammary carcinoma. Not only intraperitoneal but also oral administration of the FK-23 preparation inhibited the growth of these carcinomas inoculated intradermally. The tumor-bearing mice produced tumor necrosis factor (TNF) in their sera 2 h after intravenous injection of OK432. This TNF level increased after the mice were fed with food supplemented with the FK-23 preparation. Additionally, the FK-23 preparation inhibited the growth of Meth A fibrosarcoma in cyclophosphamide-treated BALB/c mice.View full abstractDownload PDF (464K) -
Takafumi IMAMURA, Atsuko NODA, Shigenobu SHIBATA, Shigenori WATANABE, ...1993 Volume 113 Issue 5 Pages 400-405
Published: May 25, 1993
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSA series of pentanthrene type heterocyclic compounds were synthesized and evaluated for anxiolytic activities by three kinds of behavioral pharmacological tests. Several compounds showed anxiolytic activities. In particular, s-triazolo [3, 4-a] phthalazine (Tri-P) and 3-propyl derivatives of Tri-P (PTP) showed remarkable activities, although the activities were slightly lower than those of diazepam. The results suggested that Tri-P or PTP is a useful lead compound for the development of the antianxietic agents. The relationship between the structure and anxiolytic activity, and the inducing mechanism of the activity was discussed.View full abstractDownload PDF (681K)
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