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Formulation design of granules prepared by wet granulation method using a multi-functional single-punch tablet press to avoid tableting failures

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Asian Journal of Pharmaceutical Sciences 2018年第2期13卷 113-119页

作者： Takashi Osamura Yoshiko Takeuchi risako onodera Masahiro Kitamura Yoshiteru Takahashi Kohei Tahara Hirofumi Takeuchi Laboratory of Pharmaceutical Engineering Gifu Pharmaceutical University Pharmaceutical Technology Department Sawai Pharmaceutical Co.Ltd

We previously determined "Tableting properties" by using a multi-functional single-punch tablet press(GTP-1). We plotted "Compactability" on the x-axis against "Manufacturability"on the y-axis to allow visual evaluation of "Tableting properties". Here, we examined whether this evaluation method can be used in the formulation design of tablets prepared by wet granulation. We used the GTP-1 to measure "Tableting properties" with different amounts of binder, disintegrant, and lubricant, and compared the results with those of tableting on a commercial rotary tableting machine. Tableting failures(capping and binding in particular) occurred when samples that had been evaluated as having poor "Compactability" or"Manufacturability" on the GTP-1 were compressed on the rotary tableting machine. Thus,our evaluation method predicted tableting failure at the commercial scale. The method will prove useful for scaling up production.

关键词： tableting formulation design wet granulation capping binding single-punch tablet press

Prediction of effects of punch shapes on tableting failure by using a multi-functional single-punch tablet press

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Asian Journal of Pharmaceutical Sciences 2017年第5期12卷 412-417页

作者： Takashi Osamura Yoshiko Takeuchi risako onodera Masahiro Kitamura Yoshiteru Takahashi Kohei Tahara Hirofumi Takeuchi Laboratory of Pharmaceutical Engineering Gifu Pharmaceutical University1-25-4Daigaku-NishiGifu501-1196Japan Pharmaceutical Technology Department Sawai Pharmaceutical Co.Ltd12-34HiroshibachoSuita-ShiOsaka564-0052Japan

We previously determined 'Tableting properties' by using a multi-functional single-punch tablet press(GTP-1). We proposed plotting 'Compactability' on the x-axis against'Manufacturability' on the y-axis to allow visual evaluation of 'Tableting properties'. Various types of tableting failure occur in commercial drug production and are influenced by the amount of lubricant used and the shape of the punch. We used the GTP-1 to measure'Tableting properties' with different amounts of lubricant and compared the results with those of tableting on a commercial rotary tableting machine. Tablets compressed with a small amount of lubricant showed bad 'Manufacturability', leading to sticking of powder on punches.We also tested various punch shapes. The GTP-1 correctly predicted the actual tableting results for all punch shapes. With punches that were more likely to cause tableting failure, our system predicted the effects of lubricant quantity in the tablet formulation and the occurrence of sticking in the rotary tableting machine.

关键词： Tableting Formulation design Lubricant Punch shape Single-punch tablet press Losartan potassium

Recent advances in particulate drug delivery systems: Oral, pulmonary, and ophthalmic administrations

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Asian Journal of Pharmaceutical Sciences 2016年第1期11卷 3-4页

作者： Hirofumi Takeuchi Kohei Tahara risako onodera Gifu Pharmaceutical University

Colloidal drug carriers such as liposomes,lipid emulsions,and polymeric nanoparticles have great potential to deliver drugs effectively.Preparation of nano-crystals of API has also received much attention to design dosage forms to complete effective drug delivery.A variety of investigations have been carried out toward the design of an optimal particulate system.

关键词： Drug delivery systems Liposomes Administration routes Absorption

Novel approaches for posterior segment ocular drug delivery with folate-modified liposomal formulation

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Asian Journal of Pharmaceutical Sciences 2016年第1期11卷 201-202页

作者： Toshiki Hayashi risako onodera Kohei Tahara Hirofumi Takeuchi Gifu Pharmaceutical University

The leading causes of vision impairment and blindness are posterior segment-related diseases including age-related macular degeneration,diabetic macular edema and endophthalmitis.Recently,pharmaceutical approaches to these diseases have used steroids and oligonucleotides.These drugs are usually administered via invasive injection because noninvasive delivery method such as eye drop administration of drugs is not available.However,repeated injections are associated with potential risks of complications.Moreover,patients may not comply with such regimens.

关键词： Liposome Retina Eyedrop Active targeting

Inhalation properties of water-soluble drug loaded liposomes atomized by nebulizer

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Asian Journal of Pharmaceutical Sciences 2016年第1期11卷 205-206页

作者： Shinshu Unida Yosuke Ito risako onodera Kohei Tahara Hirofumi Takeuchi Gifu Pharmaceutical University

The pulmonary route presents several advantages in designing drug delivery systems in both systemic and topical administration.The use of particulate carriers is an attractive method for designing pulmonary drug delivery systems,because such carriers could control drug release and selective drug targeting when the carriers reach the target site in the lung.The prevention of local irritation,reduced drug toxicity,and improved drug stability are also preferable results of utilizing such carrier systems.Among a number of particulate carriers,liposomes have an advantage in safety,because they consist of phospholipids,which are bio-components.

关键词： Liposome Nebulizer Inhalation property Pulmonary drug delivery

Preparation of silymarin nanocrystals using a novel high pressure crystallization technique and evaluation of its dissolution and absorption properties

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Asian Journal of Pharmaceutical Sciences 2016年第1期11卷 211-212页

作者： risako onodera Tomohiro Hayashi Tatsuo Nakamura Kaori Aibeb Kohei Tahara Hirofumi Takeuchi Gifu Pharmaceutical University 1-25-4 Daigaku-nishiGifu 501-1196Japan FANCL Corporation 12-13 Kamisinano Totsuka-kuYokohamaKanagawa 244-0806Japan

Oral bioavailability of drug is limited by the factors such as the membrane permeability, the solubility, the dissolution rate and so on (1)In case of a poorly water-soluble drug, its solubility and dissolution rate is a critical factor for its oral bioavailability.Among various techniques for enhancing solubility or dissolution properties, physical modification of drug products such as reducing the particle size is one of common approaches [2].

关键词： PureNano^(■) Silymarin Hydroxypropyl cyclodextrin Crystallization

The Cross-ratio Compactification of the Configuration Space of Ordered Points on 

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Acta Mathematica Sinica,English Series 2012年第10期28卷 2129-2138页

作者： risako FUNAHASHI Masahiko TANIGUCHI Department of Mathematics Graduate School of Humanities and SciencesNara Women’s University Department of Mathematics Faculty of Science Nara Women’s University

A natural compactification of the virtual configuration space of N points on the Riemann sphere C is constructed by using cross-ratios. We show that this compactification is homeomorphic to the Bers＇ compactification of the virtual moduli space of a punctured Riemann sphere of type N. In particular, the system of global and explicit coordinates of this standard compactification is given by cross-ratios.

关键词： Cross-ratios configuration space planar domains with nodes

Extract of Yokukansan improves anxiety-like behavior and increases serum brain-derived neurotrophic factor in rats with cerebral ischemia combined with amyloid-β42 peptide

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Journal of Traditional Chinese Medicine 2019年第1期39卷 50-58页

作者： Ai Nogami-Hara Kaori Kubota Kotaro Takasaki Takuya Watanabe Nobuaki Egahira Hikari Iba risako Fujikawa Shutaro Katsurabayashi Funda Bolukbasi Hatip Izzettin Hatip-Al-Khatib Katsunori Iwasaki Department of Neuropharmacology Faculty of Pharmaceutical ScienceFukuoka UniversityFukuoka 814-0180Japan Institute for Aging and Brain Sciences Fukuoka UniversityFukuoka 814-0180Japan Department of Pharmacy Kyushu University HospitalFukuoka 812-8582Japan Department of Medical Pharmacology Faculty of MedicinePamukkale UniversityDenizli 20070Turkey

OBJECTIVE: To examine the effects of Yokukansan(YKS) extract on two endogenous modulators of anxiety, brain-derived neurotrophic factor(BDNF)and serotonin (5-HT)_(2A) receptors pharmacologically, in the ischemic rat model of dementia.METHODS: The cerebral ischemia(CI) was induced by bilateral occlusion of the vertebral and common carotid arteries(4-vessel occlusion ischemia). The CI was combined with the amyloid-β42 peptide(A42) injected intracerebroventricularly, and referreβdto as CI+Aβ. Anxiety-like behaviors were assessed by elevated plus maze(enclosed arm), light/dark transition test(dark chamber), and open-field test.Wet-dog shakes were induced by the 5-HT_(2A) receptor agonist 2, 5-dimethoxy-4-iodoamphetamine(DOI). The concentration of BDNF in serum was determined by enzyme-linked immuno sorbent assay.RESULTS: CI + Aβ increased anxiety, as demonstrated by the increase of time spent in the enclosed arms and dark chambers, and locomotion in the outer zone of the open field(thigmotaxis). CI + Adecreased the serum concentration of BDNF. YKS reβ-duced the anxiety-like behaviors, suppressed the DOI-induced wet-dog shakes and increased serum BDNF concentrations.CONCLUSION: Our findings suggest that YKS extract improves CI + Aβ-induced anxiety by antagonizing 5-HT_(2A) receptors and increasing BDNF.

关键词： Brain ischemia Amyloid beta-peptides Anxiety brain-derived neurotrophic factor Receptor serotonin 5-HT2A Yokukansan

Glutathione Production by <i>Yarrowia lipolytica</i>Showing Both Methyglyoxal Resistance and a High Activity of Glutathione Synthetase

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Advances in Microbiology 2012年第2期2卷 171-180页

作者： Naofumi Shiomi Emi Harada risako Nabeshima Graduate School of Human Sciences Kobe College Kobe Japan

Although Yarrowia lipolytica is an important host strain, there have so far been few studies on the production of glutathione by the strain. We therefore performed a study to obtain an improved strain of Y. lipolytica ATCC20688, which could produce a high yield of glutathione. First, the capability of glutathione production in the ATCC20688 strain was estimated. In comparison with other yeasts, the yield of this strain was higher than those in Pichia strains. Furthermore, this strain could produce glutathione by assimilating sodium oleate. We next performed mutation and gene cloning to improve the yield. After the yield of glutathione was improved in the isolated methylglyoxal-resistant mutant (MGR3), the glutathione synthetase gene was cloned into the MGR3 strain. By using this recombinant strain, we could reach the maximum yield and intracellular content of glutathione of 54 mg/L-medium and 30 mg/g-dry cell weight, respectively.

关键词： Glutathione Yarrowia lipolytica Glutathione Synthetase GSH2 Methylglyoxal