Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
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57 巻, 10 号
選択された号の論文の33件中1～33を表示しています
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Review
Regular Articles
  • Improvement of Dissolution Property of Poorly Water-Soluble Drug by Supercritical Freeze Granulation
    Ryoichi Sonoda, Yuko Hara, Tomohiro Iwasaki, Satoru Watano
    原稿種別: Regular Article
    2009 年 57 巻 10 号 p. 1040-1044
    発行日: 2009/10/01
    公開日: 2009/10/03
    DOIhttps://doi.org/10.1248/cpb.57.1040
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    The dissolution property of the poorly water-soluble drug, flurbiprofen (FP) was improved by a novel supercritical freeze granulation using supercritical carbon dioxide. Supercritical freeze granulation was defined as a production method of the granulated substances by using the dry ice to generate intentionally for the rapid atomization of the supercritical carbon dioxide to the atmospheric pressure. This process utilized a rapid expansion of supercritical solutions (RESS) process with the mixture of the drug and lactose. In the supercritical freeze granulation, needle-like FP fine particles were obtained which adhered to the surface of lactose particles, which did not dissolve in supercritical carbon dioxide. The number of FP particles that adhered to the surface of particles decreased with an increase in the ratio of lactose added, leading to markedly improve the dissolution rate. This improvement was caused not only by the increase in the specific surface area but also the improvement of the dispersibility of FP in water. It is thus concluded that the supercritical freeze granulation is a useful technique to improve the dissolution property of the poorly water-soluble flurbiprofen.
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  • Anchoring of Ulex Europaeus Agglutinin to Chitosan Nanoparticles-in-Microparticles and Their in Vitro Binding Activity to Bovine Submaxillary Gland Mucin
    Feng-Qian Li, Yi-Bo Fei, Xu Chen, Xian-Ju Qin, Ji-Yong Liu, Quan-Gang ...
    原稿種別: Regular Article
    2009 年 57 巻 10 号 p. 1045-1049
    発行日: 2009/10/01
    公開日: 2009/10/03
    DOIhttps://doi.org/10.1248/cpb.57.1045
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    Focused on the natural biodegradable material of chitosan (CS), this investigation concerned its spray-dried nanoparticles-in-microparticles (NiMPs) modified with ulex europaeus agglutinin (UEA). Chitosan nanoparticles were obtained by ionotropic gelation process with pentasodium tripolyphosphate as gelatinizer. Then UEA lectin was bound onto the CS nanoparticles activated by glutaraldehyde. The conjugated spherical UEA-CS-NiMPs, prepared by spray drying method, exhibited 12—85% coupling efficiency of UEA depending upon the amount of activator glutaraldehyde. And the UEA-grafted particles showed additional higher binding tendency with bovine submaxillary gland mucin as compared to the plain chitosan microparticles. Furthermore, the activity and intrinsic fucose-specificity of UEA were still maintained after the covalent modification. It is thus evident that the UEA anchored CS-NiMPs might be used as a potential drug delivery system targeted to the specific regions of gastrointestinal tract.
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  • Nanoparticulation of Poorly Water Soluble Drugs Using a Wet-Mill Process and Physicochemical Properties of the Nanopowders
    Yusuke Tanaka, Mitsugi Inkyo, Ryoko Yumoto, Junya Nagai, Mikihisa Taka ...
    原稿種別: Regular Article
    2009 年 57 巻 10 号 p. 1050-1057
    発行日: 2009/10/01
    公開日: 2009/10/03
    DOIhttps://doi.org/10.1248/cpb.57.1050
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    In order to improve the dissolution and oral absorption properties of poorly water soluble drugs such as omeprazole, albendazole and danazol, various dispersing agents were added to prepare nanopowder formulations using an ULTRA APEX MILL, which is a wet-mill instrument, and their physicochemical properties were evaluated. Using Pluronic F-108 or F-68 as dispersing agents, slurries containing drug particles having nanometer size were obtained for all model drugs tested. Omeprazole, a heat labile drug, was not degraded by wet-milling and the omeprazole nanoparticles in a milled slurry did not aggregate for 24 h after wet-milling. After lyophilization of these milled slurries containing drug nanoparticles, fine solid white nanopowders were obtained. Scanning electron microscopy (SEM) suggested that the model drugs were milled into nanometer size. X-ray powder diffraction (XRPD) patterns and Differential Scanning Calorimetry (DSC) curves confirmed that all milled drug nanopowders were crystalline, although milling of albendazole nanopowder transformed it to another crystal form. Wet-milling using an ULTRA APEX MILL offers a highly effective approach to produce stable drug nanopowders and is a very useful tool for bioavailability enhancement of poorly water soluble and heat labile drugs.
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  • Preparation and Evaluation of Medicinal Carbon Tablets with Different Saccharides as Binders
    Kenta Yamamoto, Akihiko Ito, Yoshiharu Machida
    原稿種別: Regular Article
    2009 年 57 巻 10 号 p. 1058-1060
    発行日: 2009/10/01
    公開日: 2009/10/03
    DOIhttps://doi.org/10.1248/cpb.57.1058
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    Medicinal carbon (MC) tablets were prepared with several saccharides to improve the formability and absorption ability of MC tablets made with maltitol (MT). The MC tablets were made by the wet granule compression method, in which maltitol, xylitol (XYL), mannitol (MAN), and sorbitol (SOR) were used as binders. Granule and tablet formability, tablet strength, disintegration, and MC adsorption potential were evaluated for each formulation. Acetaminophen (AA) was used in checking effect of binders on adsorption. Due to low water solubility, MAN was added only up to 30% (w/w) of MC; in greater concentrations, the tablet could not be formed. However, tablets formed easily when using XYL or SOR at 120% (w/w) of the MC amount. This result was similar for MT. The XYL, SOR, and MT tablets displayed sufficient hardness and rapid disintegration. The tensile strength of the SOR tablets exceeded that of the MT tablets, which in turn had greater tensile strength than the XYL tablets. In addition, the XYL tablets disintegrated more quickly than the MT tablets, which disintegrated more quickly than the SOR tablets. The MC adsorption capacity was slightly decreased by XYL and SOR, but to a lesser extent than the decrease caused by MT. Overall, XYL and SOR were superior to MT as binding agents for preparation of MC tablets. Therefore, we recommend preparing the tablets with XYL or SOR as a binder using the wet granule compression method to produce a compact dosage form of MC.
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  • Nanosizing of Poorly Water Soluble Compounds Using Rotation/Revolution Mixer
    Takayuki Takatsuka, Tomoko Endo, Yao Jianguo, Kayo Yuminoki, Naofumi H ...
    原稿種別: Regular Article
    2009 年 57 巻 10 号 p. 1061-1067
    発行日: 2009/10/01
    公開日: 2009/10/03
    DOIhttps://doi.org/10.1248/cpb.57.1061
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    In this study, nanoparticles of various poorly water soluble compounds were prepared by wet milling that was carried out using a rotation/revolution mixer and zirconia balls. To be compared with Beads mill, rotation/revolution mixer has superior in very quick process (5 min) and needs very few amounts of zirconia balls (2.4 g) for pulverizing drugs to nanometer range. Phenytoin, indomethacin, nifedipine, danazol, and naproxen were selected as the standard poorly water soluble compounds. Various parameters of the rotation/revolution mixer were studied to decide the optimal pulverization conditions for the production of nanoparticles of the abovementioned compounds. The rotation/revolution speed, shape of the mixing vessel, amount of zirconia balls, and volume of the vehicle (methylcellulose solution) mainly affected the pulverization of the compounds. Using the mixer, phenytoin could be pulverized to nanoparticles within a few minutes. The particle size was confirmed by using a scanning electron microscope and a particle size analyzer. The crystallinity of the pulverized phenytoin particles was confirmed by X-ray diffractometry (XRD) and differential scanning calorimetry (DSC). It was observed that the pulverized phenytoin particles retained their crystallinity, and amorphous phenytoin was not detected. Particles of other poorly water soluble compounds were also reduced to the nanometer range by using this method.
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  • Stomach-Site Specific Drug Delivery System of Clarithromycin for Eradication of Helicobacter pylori
    Paruvathanahalli Siddalingam Rajinikanth, Brahmeshwar Mishra
    原稿種別: Regular Article
    2009 年 57 巻 10 号 p. 1068-1075
    発行日: 2009/10/01
    公開日: 2009/10/03
    DOIhttps://doi.org/10.1248/cpb.57.1068
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    Gellan gum based floating beads containing clarithromycin (FBC) were prepared by iontotropic gelation method for stomach-specific drug delivery against Helicobacter pylori. The scanning electron microscope photograph indicated that prepared beads were spherical in shape with rough outer surface. Formulation variables such as concentrations of gellan, calcium carbonate and drug loading influenced the in vitro drug release characteristics of prepared beads. In vitro release rate of clarithromycin was corrected using first order degradation rate constant which is degraded significantly during the release study in simulated gastric fluid pH 2.0. Further, the absence of interactions between drug and polymer was confirmed by differential scanning calorimetry analysis. Kinetic treatment of the in vitro drug release data with different kinetic equations revealed matrix diffusion mechanism. Prepared beads showed good anti-microbial activity against isolated H. pylori strain. The prepared beads have shown good in vivo floating efficiency in rabbit stomach. The stability studies of beads did not show any significant changes after storage of beads at 40 °C/75% relative humidity for 6 months. The preliminary results from this study suggest that floating beads of gellan can be used to incorporate antibiotics like clarithromycin and may be effective when administered locally in the stomach against H. pylori.
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  • Anti-human Immunodeficiency Virus-1 Protease Activity of New Lanostane-Type Triterpenoids from Ganoderma sinense
    Naoto Sato, Qun Zhang, Chao-Mei Ma, Masao Hattori
    原稿種別: Regular Article
    2009 年 57 巻 10 号 p. 1076-1080
    発行日: 2009/10/01
    公開日: 2009/10/03
    DOIhttps://doi.org/10.1248/cpb.57.1076
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    Five new highly oxygenated lanostane-type triterpenoids [ganoderic acid GS-1 (1), ganoderic acid GS-2 (2), ganoderic acid GS-3 (3), 20(21)-dehydrolucidenic acid N (4) and 20-hydroxylucidenic acid A (5)] were isolated from the fruiting body of Ganoderma sinense, together with known compounds including 6 triterpenoids and 3 sterols. The structures of the new triterpenoids determined by spectroscopic means including 2D NMR were 7β-hydroxy-3,11,15-trioxo-lanosta-8,24(E)-dien-26-oic acid (1), 7β,15α-dihydroxy-3,11-dioxo-lanosta-8,24(E)-dien-26-oic acid (2), 12β-acetoxy-3β,7β-dihydroxy-11,15-dioxo-lanosta-8,24(E)-dien-26-oic acid (3), 3β,7β-dihydroxy-11,15-dioxo-25,26,27-trinorlanosta-8,20-dien-24-oic acid (4), and 7β,20ξ-dihydroxy-3,11,15-trioxo-25,26,27-trinorlanost-8-en-24-oic acid (5), respectively. Among these, ganoderic acid GS-2, 20-hydroxylucidenic acid N, 20(21)-dehydrolucidenic acid N and ganoderiol F inhibited human immunodeficiency virus-1 protease with IC50 values of 20—40 μM.
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  • Syntheses of Glycoclusters Containing a Phosphocholine Residue Related to a Glycosphingolipid from the Earthworm Pheretima hilgendorfi
    Noriyasu Hada, Yukihiko Shida, Natsuko Negishi, Frank Schweizer, Tadah ...
    原稿種別: Regular Article
    2009 年 57 巻 10 号 p. 1081-1088
    発行日: 2009/10/01
    公開日: 2009/10/03
    DOIhttps://doi.org/10.1248/cpb.57.1081
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    Three types of glycoclusters related to an amphoteric glycosphingolipid found in the earthworm Pheretima hilgendorfi were synthesized. The glycoclusters were prepared from a common precursor and a simple approach for the rational design of a glycocluster was developed.
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  • Structures of New Flavonoids and Benzofuran-Type Stilbene and Degranulation Inhibitors of Rat Basophilic Leukemia Cells from the Brazilian Herbal Medicine Cissus sicyoides
    Fengming Xu, Hisashi Matsuda, Hiroki Hata, Kaoru Sugawara, Seikou Naka ...
    原稿種別: Regular Article
    2009 年 57 巻 10 号 p. 1089-1095
    発行日: 2009/10/01
    公開日: 2009/10/03
    DOIhttps://doi.org/10.1248/cpb.57.1089
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    Three new flavonoid glycosides (cissosides I, II, and III) and a new benzofuran-type stilbene (cissusin) were isolated from the methanolic extract of the aerial parts of Cissus sicyoides cultivated in Brazil. Their structures were elucidated on the basis of chemical and physicochemical evidence. The inhibitory effects of the isolated constituents on the release of β-hexosaminidase as a marker of degranulation in rat basophilic leukemia (RBL-2H3) cells were examined. Cissusin, flavonols (kaempferol, quercetin), flavones (7,3′,4′-trihydroxyflavone, lanceolatin B), pterocarpanes (homopterocarpin), chalcones (isoliquiritigenin, E-7-O-methylpongamol), and tryptanthrin markedly inhibited the release of β-hexosaminidase.
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  • Generation of Formaldehyde by Pharmaceutical Excipients and Its Absorption by Meglumine
    Megumi Fujita, Tomohiko Ueda, Tetsurou Handa
    原稿種別: Regular Article
    2009 年 57 巻 10 号 p. 1096-1099
    発行日: 2009/10/01
    公開日: 2009/10/03
    DOIhttps://doi.org/10.1248/cpb.57.1096
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    Formaldehyde is a well-known air impurity. The possibility was investigated in this study that pharmaceutical excipients commonly used in oral solid dosage forms might also be sources of formaldehyde. The results showed that formaldehyde is generated by the excipients lactose, D-mannitol, microcrystalline cellulose, low-substituted hydroxypropylcellulose, magnesium stearate and light anhydrous silicic acid. Since the quality and safety of pharmaceutical products can be significantly affected by the presence of formaldehyde, various amines were then investigated for their ability to decrease levels of formaldehyde using an aqueous solution system. Of the four amines investigated, only meglumine proved capable of reducing formaldehyde levels. The reaction product between formaldehyde and meglumine was obtained by fractionation using the preparative HPLC system and the structure was clarified by 1H-, 13C-NMR, various types of two-dimensional NMR and mass spectroscopy. The reaction product was determined to be a compound with a 1,3-oxazinane skeleton and containing one more carbon than meglumine. It was presumed that formaldehyde reacted with the secondary amino group in meglumine to form the reaction product via an iminium salt intermediate by cyclization. As meglumine is permitted to be used as a pharmaceutical excipient in both oral and parenteral dosage forms by regulations worldwide, the addition of meglumine to pharmaceutical products can be expected to contribute to the stabilization of many drug substances.
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  • Lactone Derivatives from the Marine-Derived Fungus Penicillium sp. PSU-F44
    Kongkiat Trisuwan, Vatcharin Rukachaisirikul, Yaowapa Sukpondma, Souwa ...
    原稿種別: Regular Article
    2009 年 57 巻 10 号 p. 1100-1102
    発行日: 2009/10/01
    公開日: 2009/10/03
    DOIhttps://doi.org/10.1248/cpb.57.1100
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    Two new fungal metabolites, penicipyrone (1), and penicilactone (2), were isolated from the marine-derived fungus Penicillium sp. PSU-F44 along with three known macrolides, (+)-brefeldin A (3), (+)-brefeldin C (4), and 7-oxobrefeldin A (5). Their antimicrobial activities against methicillin-resistant Staphylococcus aureus SK1 and Microsporum gypseum SH-MU-4 were examined.
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  • First Syntheses of (−)-Tauranin and Antibiotic (−)-BE-40644 Based on Lipase-Catalyzed Optical Resolution of Albicanol
    Sadayuki Ishii, Mikio Fujii, Hiroyuki Akita
    原稿種別: Regular Article
    2009 年 57 巻 10 号 p. 1103-1106
    発行日: 2009/10/01
    公開日: 2009/10/03
    DOIhttps://doi.org/10.1248/cpb.57.1103
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    First syntheses of sesquiterpene quinones (−)-tauranin and (−)-BE-40644 which exhibited strong cytotoxicity against several cancer cell lines, were achieved from (8aS)-albicanol obtained by enzymatic optical resolution. By comparison of the sign of specific rotation between synthetic (12bS)-BE-40644 and natural (−)-BE-40644, the absolute configurations of natural (−)-BE-40644 were determined to be 4aS, 6aS, 12aR, 12bS.
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Notes
Communicatins to the Editor
  • Role of Excipients on N-Oxide Raloxifene Generation from Raloxifene–Excipients Binary Mixtures
    Sanjeeva Yarkala, Sivakumar Amaravadi, Vinay U. Rao, Vijaykumar V, Sam ...
    原稿種別: Communications to the Editor
    2009 年 57 巻 10 号 p. 1174-1177
    発行日: 2009/10/01
    公開日: 2009/10/03
    DOIhttps://doi.org/10.1248/cpb.57.1174
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    Raloxifene HCl (RHCl) is known to be susceptible to oxidation and forms the corresponding N-oxide derivative as the primary degradation product. The purpose of this study was to evaluate the role of excipients on the generation of the N-oxide derivative from the corresponding RHCl–excipient binary mixtures. Binary mixtures of RHCl with crospovidone, povidone, magnesium stearate, Tween 80 and anhydrous lactose in drug: excipients ratio of 1 : 1 (crospovidone and povidone); 10 : 1 (Tween 80 and magnesium stearate) and 1 : 5 (anhydrous lactose) were prepared by both dry blending (trituration) and wet blending (to improve contact between drug and excipients). The prepared binary mixtures were then stored at 25, 40, 75 and 125 °C and generation of the N-oxide derivative was monitored over six months using a validated HPLC method. Pure drug and excipients stored similarly acted as controls. Further, all the individual excipients (used as control) were monitored for peroxide impurity generation using an in-house colorimetric method. The results showed that N-oxide generation was observed from all binary mixtures and the amount of N-oxide derivative formed were always higher from the mixtures prepared by wet blending and the amount of N-oxide derivative formed was dependent on storage temperature. This study thus shows that the presence of peroxide in the excipient and its role in oxidative degradation of drug substance calls for monitoring of the peroxide impurity present in the excipients used for formulating of drug sensitive to oxidation as used herein.
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Errata
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