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Effect of high-pressure homogenization on stability of emulsions containing zein and pectin

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Asian Journal of Pharmaceutical Sciences 2017年第1期12卷 21-27页

作者： Maneerat Juttulapa Suchada Piriyaprasarth hirofumi takeuchi Pornsak Sriamornsak Department of Pharmaceutical Technology Faculty of PharmacySilpakorn UniversityNakhon Pathom 73000Thailand Pharmaceutical Biopolymer Group(PBiG) Faculty of PharmacySilpakorn UniversityNakhon Pathom 73000Thailand Laboratory of Pharmaceutical Engineering Gifu Pharmaceutical University1-25-4 Daigaku-NishiGifu 501-1196Japan

The aim of this study was to investigate the effect of high-pressure homogenization on the droplet size and physical stability of different formulations of pectin–zein stabilized rice bran oil emulsions. The obtained emulsions, both before and after passing through highpressure homogenizer, were subjected to stability test under environmental stress conditions,that is, temperature cycling at 4 °C/40 °C for 6 cycles and centrifugal test at 3000 rpm for 10 min. Applying high-pressure homogenization after mechanical homogenization caused only a small additional decrease in emulsion droplet size. The droplet size of emulsions was influenced by the type of pectin used;emulsions using high methoxy pectin(HMP) were smaller than that using low methoxy pectin(LMP). This is due to a greater emulsifying property of HMP than LMP. The emulsions stabilized by HMP–zein showed good physical stability with lower percent creaming index than those using LMP, both before and after passing through high-pressure homogenizer. The stability of emulsions after passing through high-pressure homogenizer was slightly higher when using higher zein concentration, resulting from stronger pectin–zein complexes that could rearrange and adsorb onto the emulsion droplets.

关键词： Pectin Zein Emulsions High-pressure homogenization Stability

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

Development of pectin nanoparticles through mechanical homogenization for dissolution enhancement of itraconazole

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Asian Journal of Pharmaceutical Sciences 2016年第3期11卷 365-375页

作者： Kanokporn Burapapadh hirofumi takeuchi Pornsak Sriamornsak Department of Pharmaceutical Technology Faculty of Pharmacy Silpakorn University Pharmaceutical Biopolymer Group (PBiG) Faculty of Pharmacy Silpakorn University Laboratory of Pharmaceutical Engineering Gifu Pharmaceutical University

A simple method to fabricate itraconazole(ITZ)-loaded pectin nanoparticles prepared from nanoemulsion templates is described in this study. Nanoemulsions containing ITZ were prepared by a mechanical homogenization using pectin as emulsifier. After freeze-drying, the morphology, crystallinity state, thermal properties, drug dissolution and stability of the obtained pectin nanoparticles were characterized. The results demonstrated that the morphology of freeze-dried products was different, depending on the type of internal phase; the nanoparticles prepared from chloroform-based nanoemulsions were completely dried and provided a fragile characteristic. The pectin nanoparticles also demonstrated good properties in terms of redispersibility, thermal properties, drug crystallinity and dissolution. The ITZ-loaded pectin nanoparticles showed high percentage of drug dissolved(about 60–80%within 2 h), and maintained their good dissolution properties even after 1-year storage. The results suggested that freeze-dried pectin nanoparticles prepared from nanoemulsions could be used as an effective carrier for enhancement of ITZ dissolution.

关键词： Pectin Poorly water-soluble drug Itraconazole Nanoparticles Stability

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

Preparation of bromfenac-loaded liposomes modified with chitosan for ophthalmic drug delivery and evaluation of physicochemical properties and drug release profile

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Asian Journal of Pharmaceutical Sciences 2013年第2期8卷 104-109页

作者： Toshimasa Tsukamoto Kohei Hironaka Takuya Fujisawa Daiki Yamaguchi Kohei Tahara Yuichi Tozuka hirofumi takeuchi Laboratory of Pharmaceutical Engineering Gifu Pharmaceutical University1-25-4 Daigaku-nishiGifu 501-1196Japan Laboratory of Formulation Design and Pharmaceutical Technology Osaka University of Pharmaceutical SciencesOsakaJapan

The purpose of this study was to design a submicron-sized liposomal non-steroidal antiinflammatory drug(NSAID)preparation that targets the retina via topical instillation of eye drops.Bromfenac(BRF)-loaded liposomes were prepared using the calcium acetate gradient method.Liposome sizes and encapsulation efficiencies were optimized by screening several liposome formulations of lipid,drug concentration,and buffer solution.BRF entrapment efficiency was greater than 90%using this method,and was low using conventional hydration methods.High initial BRF loading using the pH gradient method caused aggregation of liposomes.To circumvent aggregation,the negatively charged lipid dicetylphosphate was incorporated into liposomes,which formed anion layer preventing coalescence.Release of BRF from liposomes was sustained for several hours depending on lipid concentration,inner water phase,initial drug amounts,and surface properties.Surface modification with chitosan(CS),a mucoadhesive cationic polymer,was achieved using electrostatic interactions of negatively charged liposomes.The optimal concentration of CS for evasion of liposome aggregation was 0.15%.

关键词： NSAIDs pH Gradient method Surface modification Chitosan Eye drop

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