Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
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ISSN-L : 0009-2363
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56 巻, 12 号
選択された号の論文の22件中1～22を表示しています
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Regular Articles
  • A New Spectrophotometric Method for the Determination of Tianeptine in Tablets Using Ion-Pair Reagents
    Sevgi Tatar Ulu, Zeynep Aydogmus
    原稿種別: Regular Article
    2008 年 56 巻 12 号 p. 1635-1638
    発行日: 2008/12/01
    公開日: 2008/12/01
    DOIhttps://doi.org/10.1248/cpb.56.1635
    ジャーナル フリー
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    A new rapid and sensitive procedure assay is proposed for the spectrophotometric determination of tianeptine. The developed method involves formation of colored chloroform extractable ion-pair complexes of tianeptine with bromophenol blue (BPB), bromocresol green (BCG), bromothymol blue (BTB) and methyl orange (MO) in acidic medium. Beer's law is obeyed in the concentration ranges 3.0—12.0, 4.0—16.0, 4.0—14.0 and 2.0—10.0 μg ml−1 with BPB, BCG, BTB and MO, respectively. The detection limit of tianeptine was found to be 1.8 μg ml−1 for BPB, 2.0 for BCG, 2.0 μg ml−1 for BTB and 1.0 μg ml−1 for MO. Validation of the method was performed in terms of linearity, limit of detection (LOD), quantification (LOQ), accuracy and precision. Common excipients used as additives in pharmaceutical preparations do not interfere in the proposed method. The proposed method has been applied to determination of the examined drugs in pharmaceutical formulations and the results demonstrated that the method is equally accurate, precise, and reproducible as the official method. The t-test showed no significant difference at 95% confidence level.
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  • Analysis of Oseltamivir in Tamiflu® Capsules Using Micellar Electrokinetic Chromatography
    Farnaz Jabbaribar, Alireza Mortazavi, Reza Jalali-Milani, Abolghasem J ...
    原稿種別: Regular Article
    2008 年 56 巻 12 号 p. 1639-1644
    発行日: 2008/12/01
    公開日: 2008/12/01
    DOIhttps://doi.org/10.1248/cpb.56.1639
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    A simple and rapid micellar electrokinetic chromatography (MEKC) method was developed for the analysis of an antiviral drug, oseltamivir, and its hydrolyzed product in Tamiflu® capsules. Background electrolytes consisted of boric acid 10 mM, pH 10, and sodium dodecyl sulphate (SDS) 40 mM. The limit of detection (LOD) and limit of quantification (LOQ) of oseltamivir were 1.7 and 8.0 μg/ml, respectively. MEKC sweeping in a high electroosmotic flow environment for neutral analytes was also utilized to improve the sensitivity of the assay. In MEKC-sweeping mode, a buffer comprising boric acid 30 mM, pH 10, and SDS 50 mM was used. A 17-fold increase in detection sensitivity was achieved with the MEKC-sweeping method compared with the MEKC mode. Unlike in MEKC, the LOD and LOQ for oseltamivir were 0.1 and 0.3 μg/ml, respectively, using the MEKC-sweeping method. Both methods were successful in determining oseltamivir concentration in its capsule formulation, and the MEKC-sweeping method was capable of determination of the drug at lower concentrations. The hydrolyzed product of oseltamivir (oseltamivir carboxylate) was also detected using the MEKC method. Our observations revealed that the prodrug could be hydrolyzed to the active compound at alkaline pH within ca. 60 min.
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  • Preparation of a Dispersible PEGylate Nanostructured Lipid Carriers (NLC) Loaded with 10-Hydroxycamptothecin by Spray-Drying
    Xinxin Zhang, Weisan Pan, Li Gan, Chunliu Zhu, Yong Gan, Shufang Nie
    原稿種別: Regular Article
    2008 年 56 巻 12 号 p. 1645-1650
    発行日: 2008/12/01
    公開日: 2008/12/01
    DOIhttps://doi.org/10.1248/cpb.56.1645
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    Nanostructured lipid carriers (NLC) are based on mixture of solid lipids with spatially incompatible liquid lipids, which offer advantages of improving drug loading capacity and release properties. In the present study, hydroxycamptothecin (HCPT) loaded polyethylene glycol (PEG) modified NLC (PEG-NLC) was prepared by high pressure homogenize and spray drying method. PEG-NLC showed spherical particle with smooth surface in scanning electron microscopic (SEM) analysis. The crystallinity of lipid matrix within PEG-NLC was evaluated by powder X-ray diffraction and differential scanning calorimetry (DSC). The less ordered crystals or amorphous state of matrix were found in nanoparticles. A small, homogeneous particle size and high drug loading with fine entrapment efficiency of HCPT was obtained in PEG-NLC system. HCPT releasing from PEG-NLC showed a sustained release trend, and no significantly difference was found between two release curves of PEG-NLC before or after spray drying. After storage for 6 months, PEG-NLC powder after spray drying showed no significantly changes in particle size, drug loading and entrapment efficiency, crystal form and in vitro release. PEG modification statistically decreased the phagocytosis of NLC by RAW 264.7 cells, and spray drying process did not influence the cellular uptake of PEG-NLC. These results suggest that PEG-NLC prepared by spray drying is a stable and high-performance delivery system for HCPT.
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  • Development and Validation of an Adsorptive Stripping Voltammetric Method for the Quantification of Vincamine in Its Formulations and Human Serum Using a Nujol-Based Carbon Paste Electrode
    Amr Mohamed Beltagi
    原稿種別: Regular Article
    2008 年 56 巻 12 号 p. 1651-1657
    発行日: 2008/12/01
    公開日: 2008/12/01
    DOIhttps://doi.org/10.1248/cpb.56.1651
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    An easy, rapid and selective adsorptive stripping voltammetry (AdSV) method for the determination of vincamine in its formulation and human serum was developed and validated. It was based on the oxidation of the drug onto a Nujol-based carbon paste electrode. The stripping step was carried out by using a square-wave (SW) potential-time voltammetric excitation signal. The optimal experimental variables as well as accumulation parameters were investigated as; frequency f=120 Hz, scan increment ΔEi=10 mV, pulse-amplitude ΔEa=25 mV and an accumulation potential Eacc of 0.0 V using a Britton–Robinson (B-R) universal buffer of pH 5 as a supporting electrolyte. After validation of the described method, it was applied for determination of vincamine in its formulation and human serum. Mean recovery of 100.41±0.74 (n=5) was achieved for assay of vincamine in Oxybral® capsules. Limits of detection and quantitation of 6.0×10−9 M (2.20 ng ml−1) and 2×10−8 M (7.33 ng ml−1) vincamine were achieved in human serum with a mean recovery of 99.5±1.79%, without prior extraction of the drug. No interferences were observed in formulation and/or human serum. Due to high sensitivity and specificity of the developed method, it was successfully applied for evaluating some pharmacokinetic parameters of two healthy volunteers after administration of a single oral Oxybral® capsule.
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  • Formulation and Evaluation of Clarithromycin Microspheres for Eradication of Helicobacter pylori
    Paruvathanahalli Siddalingam Rajinikanth, Lakshmi Narayanan Karunagara ...
    原稿種別: Regular Article
    2008 年 56 巻 12 号 p. 1658-1664
    発行日: 2008/12/01
    公開日: 2008/12/01
    DOIhttps://doi.org/10.1248/cpb.56.1658
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    The objective of the study was to develop a stomach-specific drug delivery system for controlled release of clarithromycin for eradication of Helicobacter pylori (H. pylori). Floating-bioadhesive microspheres of clarithromycin (FBMC) were prepared by emulsification-solvent evaporation method using ethylcellulose as matrix polymer and Carbopol 934P as mucoadhesive polymer. The prepared microspheres were subjected to evaluation for particle size, incorporation efficiency, in vitro buoyancy, in vitro mucoadhesion and in vitro drug release characteristics. The prepared microspheres showed a strong mucoadhesive property with good buoyancy. The formulation variables like polymer concentration and drug concentration influenced the in vitro drug release significantly in simulated gastric fluid (pH. 2.0). The in vivo H. pylori clearance efficiency of prepared FBMC in reference to clarithromycin suspension following repeated oral administration to H. pylori infected Mongolian gerbils was examined by polymerase chain reaction (PCR) technique and by a microbial culture method. The FBMC showed a significant anti-H. pylori effect in the in vivo gerbil model. It was also noted that the required amount of clarithromycin for eradication of H. pylori was significantly less in FBMC than from corresponding clarithromycin suspension. The results further substantiated that FBMC improved the gastric stability of clarithromycin (due to entrapment within the microsphere) and eradicated H. pylori from the gastrointestinal tract more effectively than clarithromycin suspension because of the prolonged gastrointestinal residence time of the formulation.
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  • A Polymer Film Modified Sensor for Voltammetric Determination of Uric Acid in the Presence of Ascorbic Acid and Its Application in Urine
    Ailin Liu, Wei Chen, Liying Huang, Xinhua Lin
    原稿種別: Regular Article
    2008 年 56 巻 12 号 p. 1665-1669
    発行日: 2008/12/01
    公開日: 2008/12/01
    DOIhttps://doi.org/10.1248/cpb.56.1665
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    A novel uric acid electrochemical sensor was fabricated by electropolymerization on glassy carbon electrode (GCE) with 4-(2-pyridylazo)-resorcinol (PAR) and its electrochemical property was investigated through cyclic voltammetry. The effect of film thickness on the oxidation response was also studied by electropolymerized scan times. The voltammetric behavior of uric acid (UA) was studied with the poly PAR modified GCE. The modified GCE was used to electrochemically detect the individual of UA and the mixture of UA and ascorbic acid (AA) by cyclic voltammetry (CV) or differential pulse voltammetry (DPV) method. For the ternary mixture containing UA and AA, the two compounds can well be separated from each other at a scan rate of 100 mV s−1 with a potential difference of 345 mV in DPV between UA and AA. The peak currents of UA oxidation increase linearly with the concentration in ranges of 1.0×10−8—5.0×10−5 mol l−1, and the detection limits (S/N=3) was 1.0×10−9 mol l−1. This method was successfully applied to the determination of uric acid in human urine samples.
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  • Three New Pentasaccharide Resin Glycosides from the Roots of Sweet Potato (Ipomoea batatas)
    Yong-Qin Yin, Xue-Feng Huang, Ling-Yi Kong, Masatake Niwa
    原稿種別: Regular Article
    2008 年 56 巻 12 号 p. 1670-1674
    発行日: 2008/12/01
    公開日: 2008/12/01
    DOIhttps://doi.org/10.1248/cpb.56.1670
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    Three new pentasaccharide resin glycosides, batatosides III—V (1—3), were isolated from the roots of Sweet potato (Ipomoea batatas). Saponification of the crude resin glycoside mixture yielded substituents and simonic acid B. The structures of the isolated compounds (1—3) were established through spectroscopic analyses, including high field NMR spectroscopy and HR-ESI-MS, and chemical correlation. The major characteristics of 3 are the presence of three different substituents, especially the substituent of cinnamic acid was seldom. The monosaccharides of 1—3 were proved by GC-MS and the absolute configuration of aglycone was further established as S by Mosher's method with R-methyloxyphenylacetic acid (MPA) and S-MPA.
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  • Synthesis and Cytotoxicity of Novel 3-Aryl-1-(3′-dibenzylaminomethyl-4′-hydroxyphenyl)-propenones and Related Compounds
    Halise Inci Gul, Kadir Ozden Yerdelen, Umashankar Das, Mustafa Gul, Bu ...
    原稿種別: Regular Article
    2008 年 56 巻 12 号 p. 1675-1681
    発行日: 2008/12/01
    公開日: 2008/12/01
    DOIhttps://doi.org/10.1248/cpb.56.1675
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    The reaction of various 4′-hydroxychalcones (1a—e) with paraformaldehyde and dibenzylamine led to the formation of a novel series of 4′-hydroxy-3′-dibenzylaminomethyl chalcones (7a—e) instead of 4′-hydroxy-3′,5′-bis-(dibenzylaminomethyl)chalcones 4. In order to rationalise the formation of monoadduct 7, energy minimized model structures of 4a and 7a were compared. The in vitro cytotoxic activities of 7a—e were tested against PC-3 cell lines for the first time in this study and compared with the precursor 4′-hydroxychalcones (1a—e). Except for compound 7a (IC50: 19.85 μM), insertion of dibenzylaminomethyl function into 4′-hydroxychalcones resulted in complete loss of cytotoxic activity. The results suggested that it is not only the pKa but also the shape and size of the amine that is critical in governing the cytotoxic activity.
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  • Rheological Behavior of Worm-Like Micelles in a Mixed Nonionic Surfactant System of a Polyoxyethylene Phytosterol and a Glycerin Fatty Acid Monoester
    Kaname Hashizaki, Nao Tamaki, Hiroyuki Taguchi, Yoshihiro Saito, Koji ...
    原稿種別: Regular Article
    2008 年 56 巻 12 号 p. 1682-1686
    発行日: 2008/12/01
    公開日: 2008/12/01
    DOIhttps://doi.org/10.1248/cpb.56.1682
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    In the present study, we examine a worm-like micelle consisting of a nonionic surfactant system of polyoxyethylene phytosterol (PhyEOm)/glycerin fatty acid monoester (GFA-Cn)/Water (m=10, 20, 30; n=8, 10, 12) using rheological measurements looking towards potential application of the system as a gel base. Phase diagrams in the dilute region of the PhyEOm/GFA-Cn/Water systems show the formation of worm-like micelles in some of the surfactant combinations. It is thought that the worm-like micelles form with the GFA-Cn solubilized in the palisade layer of a spherical or rod-like micelle consisting of PhyEOm, resulting in a decrease in the interfacial curvature of the molecular assembly. The rheological properties of micellar solutions were examined while changing the ratio of GFA-Cn (R) with the total concentration of the surfactants (wt%) fixed. Steady-flow viscosity measurements in the region of worm-like micelle formation showed Newtonian flow in the low shear rate region and non-Newtonian flow at higher shear rates. This result shows that the network structure of worm-like micelles does not break in the low shear rate region, but does break in the high shear rate region. The zero-shear viscosity (η0) was calculated from the steady-flow viscosity curve and was found to change dramatically with changing R value, increasing to a value 10000 times that of other values at the maximum. Thus, there is an optimal composition of surfactants which leads to the greatest entanglement of the worm-like micelles. To consider the change in η0 in detail, dynamic viscoelasticity measurements were carried out. Consequently, the viscoelastic behavior of the worm-like micelles was found to be similar to the Maxwell model, which represents the most basic model for a viscoelastic body, and it was shown that this worm-like micelle had a single relaxation time. Moreover, it was found that the change in η0 of a worm-like micelle was influenced by its mechanical strength.
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  • Hydronaphthalenones and a Dihydroramulosin from the Endophytic Fungus PSU-N24
    Ubonta Sommart, Vatcharin Rukachaisirikul, Yaowapa Sukpondma, Souwalak ...
    原稿種別: Regular Article
    2008 年 56 巻 12 号 p. 1687-1690
    発行日: 2008/12/01
    公開日: 2008/12/01
    DOIhttps://doi.org/10.1248/cpb.56.1687
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    Three new hydronaphthalenone derivatives (1—3) and one new dihydroramulosin derivative (4), were isolated from the endophytic fungus PSU-N24 together with eight known compounds. Their structures were elucidated by spectroscopic methods. Griseofulvin (9) displayed strong antifungal activity against Microsporum gypseum SH-MU-4 with a minimum inhibitory concentration (MIC) value of 2 μg/ml while all metabolites exhibited very weak antibacterial activity (MIC value≥128 μg/ml) against Staphylococcus aureus, both standard and methicillin-resistant strains. 3-(2-Hydroxypropyl)benzene-1,2-diol (10) showed moderate antimalarial activity against Plasmodiun falciparum with an IC50 value of 6.68 μg/ml. For antimycobacterial activity against Mycobacterium tuberculosis, compound 3 gave the best activity with the MIC value of 12.50 μg/ml.
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  • Antibacterial Novel Phenolic Diterpenes from Podocarpus macrophyllus D. DON
    Kimihiko Sato, Keito Sugawara, Hirono Takeuchi, Hyun-Sun Park, Toshiyu ...
    原稿種別: Regular Article
    2008 年 56 巻 12 号 p. 1691-1697
    発行日: 2008/12/01
    公開日: 2008/12/01
    DOIhttps://doi.org/10.1248/cpb.56.1691
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    Two new sempervirol type diterpenes, inumakiols A, B, and six new totarol type diterpenes, inumakiols C—H, were isolated from a methanolic extract of bark of Podocarpus macrophyllus (Podocarpaceae), along with one known abietane, two known totarol type diterpenes, and one known totarol type diterpene dimer. The structures of the new compounds were elucidated by the spectroscopic methods. Some of them possessed antibacterial activity against oral pathogenic microorganisms with minimum inhibitory concentration (MIC) values ranging from 3.1 to 25 ppm.
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  • Phosphorylation of Nucleosides and Nucleotides with Inorganic Monoimido-cyclo-Triphosphate
    Hideko Maeda, Takeshi Chiba, Mitsutomo Tsuhako, Hirokazu Nakayama
    原稿種別: Regular Article
    2008 年 56 巻 12 号 p. 1698-1703
    発行日: 2008/12/01
    公開日: 2008/12/01
    DOIhttps://doi.org/10.1248/cpb.56.1698
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    The phosphorylation of nucleosides (adenosine, guanosine, cytidine, and uridine) and nucleotides (adenosine 5′-monophosphate, guanosine 5′-monophosphate, cytidine 5′-monophosphate and uridine 5′-monophosphate) has been achieved using inorganic monoimido-cyclo-triphosphate (MCTP, Na3P3O8NH) in aqueous solution. In this reaction, the 2′-OH or 3′-OH group of the β-D-ribofuranose unit was phosphorylated and the total yield was more than 30% and 14%, respectively. The main products were 2′-diphosphoramidophosphononucleoside and 2′-diphosphoramidophosphononucleoside 5′-monophosphate.
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  • Medicinal Flowers. XXIV. Chemical Structures and Hepatoprotective Effects of Constituents from Flowers of Hedychium coronarium
    Seikou Nakamura, Yoshie Okazaki, Kiyofumi Ninomiya, Toshio Morikawa, H ...
    原稿種別: Regular Article
    2008 年 56 巻 12 号 p. 1704-1709
    発行日: 2008/12/01
    公開日: 2008/12/01
    DOIhttps://doi.org/10.1248/cpb.56.1704
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    The 80% aqueous acetone extract from the flowers of Hedychium coronarium was found to show a protective effect on D-galactosamine-induced cytotoxicity in primary cultured mouse hepatocytes. On the other hand, two new labdane-type diterpene glycosides, coronalactosides I (1) and II (2), and a new labdane-type trinorditerpene, coronadiene (3), were isolated together with 8 known compounds from the extracts, which were obtained with chloroform and 80% aqueous acetone from the flowers of H. coronarium. The structures of new constituents were elucidated on the basis of chemical and physicochemical evidence. In addition, the principal constituents, coronaririn C and 15-hydroxylabda-8(17),11,13-trien-16,15-olide, displayed hepatoprotective effects, which were stronger than that of the hepatoprotective agent, silybin.
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  • Structures of New Sesquiterpenes from Curcuma comosa
    Fengming Xu, Seikou Nakamura, Yang Qu, Hisashi Matsuda, Yutana Pongpir ...
    原稿種別: Regular Article
    2008 年 56 巻 12 号 p. 1710-1716
    発行日: 2008/12/01
    公開日: 2008/12/01
    DOIhttps://doi.org/10.1248/cpb.56.1710
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    From the methanolic extract of the rhizomes of Curcuma comosa cultivated in Thailand, six new sesquiterpenes, (+)- and (−)-comosols (1, 2), comosones I (3), II (4), and III (5), and dimethoxycurcumenone (6), were isolated. Their structures were elucidated on the basis of chemical and physicochemical evidence.
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