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Wongmekiat, Arpansiree; Tozuka, Yuichi; Oguchi, Tamio; Yamamoto, Keiji

doi:10.1023/a:1021401826554

Cited by 36 publications

(15 citation statements)

References 17 publications

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“…[10][11][12] We also found that moisture content in the co-grinding process was an important factor and a suitable moisture condition during co-grinding was indispensable for nanoparticle formation.…”

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confidence: 82%

“…In the past few years, there are many publications focusing on the preparation of drug particles at the nanometer level by co-grinding with additives. [7][8][9][10][11][12][13][14] In previous studies, we have reported the formation of pranlukast nanoparticle with mean particle size around 200 nm by co-grinding with CDs.10) Co-grinding with CDs could be applied as a nanoparticle preparation method for various kinds of poorly water-soluble drugs. [10][11][12] We also found that moisture content in the co-grinding process was an important factor and a suitable moisture condition during co-grinding was indispensable for nanoparticle formation.…”

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Preparation of Drug Nanoparticles by Co-grinding with Cyclodextrin: Formation Mechanism and Factors Affecting Nanoparticle Formation

Wongmekiat

Tozuka

Moribe

et al. 2007

CHEMICAL & PHARMACEUTICAL BULLETIN

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Several techniques have been widely applied to enhance the bioavailability of poorly water-soluble drug, for examples, inclusion complex formation, 1,2) polymeric nanoparticle, 3) solid dispersion, 4) and particle size reduction by grinding. 5,6) Micron-sized particles can be produced by grinding but particles at the nanometer level are difficult to obtain by the dry milling method. In the past few years, there are many publications focusing on the preparation of drug particles at the nanometer level by co-grinding with additives. [7][8][9][10][11][12][13][14] In previous studies, we have reported the formation of pranlukast nanoparticle with mean particle size around 200 nm by co-grinding with CDs.10) Co-grinding with CDs could be applied as a nanoparticle preparation method for various kinds of poorly water-soluble drugs. [10][11][12] We also found that moisture content in the co-grinding process was an important factor and a suitable moisture condition during co-grinding was indispensable for nanoparticle formation. 13)Pranlukast is a cysteinyl leukotriene receptor antagonist which is chemically described as (4-oxo-8-[4-(4-phenylbutoxy)benzoylamino]-2-(tetrazol-5-yl)-4H-1-benzopyran). Pranlukast is practically insoluble (1.2 mg/ml H 2 O at 25°C), resulting in poor absorption after oral administration.Environmental scanning electron microscopy (ESEM) can be used to observe samples in a moist condition by controlling water vapor pressure in the microscope specimen chamber. The observation of wet organic samples by ESEM has been reported recently. 14,15) In this study, the effects of grinding time, moisture content and CD content on the nanoparticle formation were evaluated by means of UV quantitative determination and particle size analysis. High-resolution scanning electron microscope was employed to observe the surfaces of the ground mixtures prepared under various conditions. Moreover, ESEM was used to observe the drug particles after dispersal into water.The mechanism for nanoparticle formation was discussed. ExperimentalMaterials Pranlukast hemihydrate was received from Ono Pharmaceutical Co., Ltd., Japan as jet-milled material. b-Cyclodextrin (b-CD) was kindly supplied by Nihon Shokuhin Kako Co., Ltd., Japan as a hydrate form (b-CD · 10.5H 2 O). The water content of b-CD was measured by the Karl-Fischer method and was found to be 14.2 w/w%. The anhydrous form of b-CD was obtained by drying b-CD · 10.5H 2 O in vacuum at 110°C for 3 h and the water content was limited to less than 1%. All chemicals used were of reagent grade. Preparation of Ground MixturesThe physical mixture of anhydrous b-CD and pranlukast was prepared at molar ratios of 1 : 2, 1 : 1, and 2 : 1 (b-CD : pranlukast) in a glass vial using a vortex mixer. To control the moisture content during the co-grinding process, the required amount of distilled water was added to the physical mixture and mixed homogeneously. The ground mixture was obtained by grinding the physical mixture in a vibrational rod mill (TI-200, Heiko Seisakusho, Japan) with ...

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Preparation of Drug Nanoparticles by Co-grinding with Cyclodextrin: Formation Mechanism and Factors Affecting Nanoparticle Formation

Wongmekiat

Tozuka

Moribe

et al. 2007

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Improved dissolution by co-grinding has been described in many reports regarding dry milling, 18),20),22), [25][26][27][28][29][30][31][32][33][34][35][36][37][38][39][40] although some studies utilized the formation of amorphous particles by co-grinding. 18), [25][26][27][28][29][30][31][32][33][34] The unintentional formation of amorphous particles is undesirable because the quality of the powder can easily change during storage. Therefore, the present study demonstrates that co-grinding with PVP by LN2 milling is a powerful tool for improving the dissolution of poorly water-soluble phenytoin without the formation of amorphous particles.…”

Section: Dissolution Of Co-ground Mixturesmentioning

confidence: 99%

Novel Ultra-Cryo Milling and Co-grinding Technique in Liquid Nitrogen to Produce Dissolution-Enhanced Nanoparticles for Poorly Water-Soluble Drugs

Sugimoto

Niwa

Nakanishi³

et al. 2012

CHEMICAL & PHARMACEUTICAL BULLETIN

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A novel ultra-cryo milling micronization technique for pharmaceutical powders using liquid nitrogen (LN2 milling) was used to grind phenytoin, a poorly water-soluble drug, to improve its dissolution rate. LN2 milling produced particles that were much finer and more uniform in size and shape than particles produced by jet milling. However, the dissolution rate of LN2-milled phenytoin was the same as that of unground phenytoin due to agglomeration of the submicron particles. To overcome this, phenytoin was co-ground with polyvinylpyrrolidone (PVP). The dissolution rate of co-ground phenytoin was much higher than that of original phenytoin, single-ground phenytoin, a physical mixture of phenytoin and PVP, or jet-milled phenytoin. X-Ray diffraction showed that the crystalline state of mixtures co-ground by LN2 milling remained unchanged. The equivalent improvement in dissolution, whether phenytoin was co-ground or separately ground and then mixed with PVP, suggested that even when co-ground, the grinding of PVP and phenytoin occurs essentially independently. Mixing original PVP with ground phenytoin provided a slight improvement in dissolution, indicating that the particle size of PVP is important for improving dissolution. When mixed with ground phenytoin, PVP ground by LN2 milling aided the wettability and dispersion of phenytoin, enhancing utilization of the large surface area of ground phenytoin. Co-grinding phenytoin with other excipients such as Eudragit L100, hypromellose, hypromellose acetate-succinate, microcrystalline cellulose, hydroxypropylcellulose and carboxymethyl cellulose also improved the dissolution profile, indicating an ultra-cryo milling and co-grinding technique in liquid nitrogen has a broad applicability of the dissolution enhancement of phenytoin.Key words cryo-milling; media milling; liquid nitrogen; submicron; zirconia bead; co-grinding Combinatorial chemistry and high throughput screening have contributed to an increase in the number of poorly watersoluble drug candidates emerging from the discovery pipeline.1) Many technologies for reducing the particle size of drug substances have been developed and applied in pharmaceutical research in order to enhance the gastrointestinal dissolution and absorption of poorly water-soluble drug substances 2,3) or to reduce variations in uptake between fed and fasted conditions.4) Mechanical milling of dry drug substances by ball milling, hammer milling and jet milling has been traditionally used in pharmaceutical manufacturing because of its widespread application and the simplicity of the process. However, this approach can only reduce particle size to approximately 2-3 μm due to secondary co-aggregation between particles caused by van der Waals interactions and electrostatic forces. 5)In the past decade, the "1-micron limitation" in particle size has been overcome by micronization and nanonization strategies 6) by employing media milling and high pressure homogenization techniques conducted on aqueous suspensions. The resulting nanometer-sized drug ...

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“…[2][3][4] It is clinically used in the treatment of gastroeosophageal reflux disease (GERD), gastric and duodenal ulcers and ZollingerEllison syndrome. [5] Formation of cyclodextrin inclusion complex is of immense application in improving the physical [6] , chemical [7] and thermal stability [8] of drugs. Cyclodextrins are toroidal shaped presenting hydroxyl groups to the external environment and hydrophobic functionality lining interior of the cavity.…”

Section: Introductionmentioning

confidence: 99%

Physicochemical Investigation of Engineered Nanosuspensions Containing Model Drug, Lansoprazole

Shende

Chaphalkar

Deshmukh

et al. 2015

Journal of Dispersion Science and Technology

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Lansoprazole is a proton-pump inhibitor used in treatment of gastric ulcers, gastroesophageal reflux disease (GERD) and Zollinger-Ellison syndrome. The objective of the study was physicochemical investigation and comparatively characterization nanosuspensions of lansoprazole by complexing with β-cyclodextrin and β-cyclodextrin based nanosponges to enhance its solubility and stability. Inclusion complexes of lansoprazole with β-cyclodextrin and nanosponges were prepared by physical method and polymer condensation method respectively. Particle size, zeta potential, encapsulation efficiency, in-vitro release, FTIR and DSC studies were used as characterization parameters. The average particle size of lasoprazole nanoparticles was found to be in the range of 178.7 ± 6.39 nm to 204.9 ± 2.91 nm. The high zeta potential values attained to ensure a high-energy barrier and favour a good stability of nanosuspensions. In-vitro release study showed the controlled release of lansoprazole which was more satisfactory than individual drug. FTIR spectroscopy showed that there was interaction of cyclodextrin and its nanosponges with drug. DSC study revealed that drug was involved in complexion with cyclodextrin and nanosponges. Solubility and stability of Downloaded by [New York University] at 02:29 10 June 2015 2 lansoprazole were remarkably improved by inclusion complexation. Based on these findings, it can be concluded that engineered nanosuspension of lansoprazole is promising carrier for nanoparticulate drug delivery in gastric ulcer.

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Abstract: Cogrinding with a beta-CD of higher water content can be an effective method to prepare fine drug particles at the submicron level.

Cited by 36 publications

References 17 publications

Preparation of Drug Nanoparticles by Co-grinding with Cyclodextrin: Formation Mechanism and Factors Affecting Nanoparticle Formation

Preparation of Drug Nanoparticles by Co-grinding with Cyclodextrin: Formation Mechanism and Factors Affecting Nanoparticle Formation

Novel Ultra-Cryo Milling and Co-grinding Technique in Liquid Nitrogen to Produce Dissolution-Enhanced Nanoparticles for Poorly Water-Soluble Drugs

Physicochemical Investigation of Engineered Nanosuspensions Containing Model Drug, Lansoprazole

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