Preparation and Evaluation of Ibuprofen Solid Dispersion Systems with Kollidon Particles Using a Pulse Combustion Dryer System

Xu, Lu; Li, San Ming; Sunada, Hisakazu

doi:10.1248/cpb.55.1545

Cited by 30 publications

(27 citation statements)

References 18 publications

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“…2), indicating that this methodology can prepare fine granules regardless of the drug properties (wettability and primary PSD). However, the yields of the granules were in the range of 68-78%, indicating that raw drug materials would have flied and adhered more readily to 10) the walls of upper part of the equipment at the early stage of granulation. However, IBU and ETZ granules were found to show a higher sphericity (>0.72) compared with APAP granules (Fig.…”

Section: Resultsmentioning

confidence: 99%

Investigation of Physicochemical Drug Properties to Prepare Fine Globular Granules Composed of Only Drug Substance in Fluidized Bed Rotor Granulation

Mise

Iwao

Kimura

et al. 2015

CHEMICAL & PHARMACEUTICAL BULLETIN

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The effect of some drug properties (wettability and particle size distribution) on granule properties (mean particle size, particle size distribution, sphericity, and granule strength) were investigated in a high (>97%) drug-loading formulation using fluidized bed rotor granulation. Three drugs: acetaminophen (APAP); ibuprofen (IBU); and ethenzamide (ETZ) were used as model drugs based on their differences in wettability and particle size distribution. Granules with mean particle sizes of 100-200 µm and a narrow particle size distribution (PSD) could be prepared regardless of the drug used. IBU and ETZ granules showed a higher sphericity than APAP granules, while APAP and ETZ granules exhibited higher granule strength than IBU. The relationship between drug and granule properties suggested that the wettability and the PSD of the drugs were critical parameters affecting sphericity and granule strength, respectively. Furthermore, the dissolution profiles of granules prepared with poorly water-soluble drugs (IBU and ETZ) showed a rapid release (80% release in 20 min) because of the improved wettability with granulation. The present study demonstrated for the first time that fluidized bed rotor granulation can prepare high drugloaded (>97%) globular granules with a mean particle size of less than 200 µm and the relationship between physicochemical drug properties and the properties of the granules obtained could be readily determined, indicating the potential for further application of this methodology to various drugs.Key words high drug-loading; globular fine granule; fluidized bed rotor granulation; wettability Wet granulation is a technique to enlarge particle size by the coalescence of primary particles with the binder liquid and contributes to improved powder flowability, compaction behavior, and uniformity of drug content. In particular, high drug-loading wet granulation has recently gathered special interest as it can enhance patient compliance through reduction of dosage size, save manufacturing costs, and simplify the granulation process. In addition, if the particle size is less than 200 µm, improvements in the taste and texture of the powders would also be expected. Alternatively, if the particle size is too small, especially if it is less than 100 µm, uniform coating is difficult because of the aggregation of smaller particles via static electrical charge. Therefore, manufacturing high drug-loaded granules with a narrow particle size distribution of approximately 100-200 µm is critically important. To date, there have been many reports of drug-loaded granules prepared using high shear mixing and surfactants 1) ; however, the particle sizes of these granules were mostly over 200 µm, and it would be technically quite difficult to prepare high drugloaded fine granules using just a basic granulation technique.In the present study, we tried to investigate whether fluidized bed rotor granulation using the multi-functional rotor processor "Granurex ® (GX)" can prepare fine granules of a high (> 97%) drug-loadi...

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Section: Resultsmentioning

confidence: 99%

Investigation of Physicochemical Drug Properties to Prepare Fine Globular Granules Composed of Only Drug Substance in Fluidized Bed Rotor Granulation

Mise

Iwao

Kimura

et al. 2015

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…IBU also has a short half-life, 2.0 ± 0.5 hours. Because of its low solubility and short half-life, IBU is difficult to be absorbed into the blood circulation system hence IBU has relatively low bioavailability [1][2][3]. Thus, the dissolution rate is required to achieve high bioavaibility of IBU.…”

Section: Introductionmentioning

confidence: 99%

“…Pyo et al, Kim et al, and Puri et al were using spray drying to control the amorphous states of the drugs because this state are often desired in order to achieve fast dissolution rates and high bioavailability [15,19,[20][21][22][23]. Xu et al, Li et al, and Shen et al improved solubility and dissolution of IBU by spray drying technique with using various polymer [1,21,24]. At previous research, microparticle was prepared by spray drying using nozzle or rotary atomizer which produced particle size 2-30 μm [9,[25][26][27].…”

Section: Introductionmentioning

confidence: 99%

“…Therefore, to prevent those, stabilizer is necessary. Mauludin et al and Xu et al applied polyvinyl alcohol (PVA) as a stabilizer for hesperidin and celecoxib respectively [1,6]. In addition, an anionic surfactant such as sodium lauryl sulphate (SLS) was employed to prevent microcapsules from attaching to the inner wall of spray-drying chamber and to produce freeflowing powder.…”

Section: Introductionmentioning

confidence: 99%

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Enhancement of solubility and dissolution of ibuprofen microparticle prepared by ultrasonic spray drying

Rachmaniar¹,

Panatarani²,

Joni³

et al. 2017

mpj

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Ibuprofen (IBU) is one of the most commonly used nonsteroidal anti-inflammatory drugs with high permeability and low solubility. The aims of this research is to improve the solubility and dissolution of the IBU by reducing particle size using ultrasonic spray drying method and utilizing watersoluble polymer (polyvinyl alcohol (PVA)) and surfactant (sodium lauryl sulphate (SLS)) for particles formulation. The results showed that increasing amount of PVA, smaller particle size of as-prepared IBU-PVA-SLS was obtained, 6.3-fold smaller than untreated IBU. The in vitro drug release study for simulated gastric fluid without enzymes (0.1 N HCl or Buffer pH 1.2) shows the dissolution of prepared IBU-PVA-SLS significantly increase 2.4-fold higher than untreated IBU for dissolution time of 30 minutes. While the solubility of the IBU-PVA-SLS was increased 4.7-fold compare to untreated IBU. In general, IBU possessing relatively high dissolution in intestinal fluid. In contrast, the finding of recent investigation on dissolution of IBU-PVA-SLS is significantly increase in gastric fluid, either due to smaller particles size or PVA-SLS. Thus, despite the PVA and SLS determine the particles formation during polymerization yielding smaller particle size, they also responsible for effective drug delivery system. It was concluded that PVA and SLS in ultrasonic spray drying technique for IBU preparation successfully reduces the particle size and effectively enhances the solubility and dissolution rate of poorly water-soluble IBU in 0.1 N HCl.

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“…Previous literature had discussed various preparations of IBU/ SDs for improving its dissolution using different carriers (Dabbagh and Taghipour, 2007;Esnaashari et al, 2005;Islam et al, 2010;Newa et al, 2007;Newa et al, 2008a;Newa et al, 2008b;Newa et al, 2008c;Park et al, 2009;Xu et al, 2007). SDs prepared by fusion method was used to enhance the solubility, dissolution rate and absorption of IBU using PEG 6000 (Gawai et al, 2013), mixture of tween 80 & span 80 (Shahrin and Huq, 2012) and polyethylene glycol (PEG) 8000 (Ofokansi et al, 2016).…”

Section: Introductionmentioning

confidence: 99%

Hot melt extrusion method for preparation of ibuprofen/sucroester WE15 solid dispersions: evaluation and stability assessment

2017

J App Pharm Sci

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Low melting points Sucroesters (SEs) are used in hot-melt extrusion technology (HME). However, there are few literatures studying the effect of SEs on drug release and their storage stability. In this study, SE  WE15 was proposed to prepare sustained-release solid dispersions with Iburpofen (IBU), containing 60 & 30% w/w, by HME, fusion method and compared to physical mixtures. The fresh and stored samples were evaluated by a well-established release rate study (USP Apparatus IV), DSC and XRD. Results revealed that HME technique succeeded to produce sustained-release patterns for IBU. Stored samples (6 months at 40C / 75 % RH) were unstable and showed gradual decrease in IBU release rate for both IBU loadings. HME formula (60% w/w IBU) showed an increase in the amount of drug released. Long term stability, one year at room temperature, showed a marked increase in IBU release rate for both drug loadings. Only HME containing 30% w/w IBU gave stable form among others. DSC and XRD suggested that increase of SE content led to almost complete IBU dissolved in this carrier, and considerable decrease in IBU release rate. This has been proven by DSC and XRD data analysis for IBU and SE (enthalpy and counts).

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Preparation and Evaluation of Ibuprofen Solid Dispersion Systems with Kollidon Particles Using a Pulse Combustion Dryer System

Cited by 30 publications

References 18 publications

Investigation of Physicochemical Drug Properties to Prepare Fine Globular Granules Composed of Only Drug Substance in Fluidized Bed Rotor Granulation

Investigation of Physicochemical Drug Properties to Prepare Fine Globular Granules Composed of Only Drug Substance in Fluidized Bed Rotor Granulation

Enhancement of solubility and dissolution of ibuprofen microparticle prepared by ultrasonic spray drying

Hot melt extrusion method for preparation of ibuprofen/sucroester WE15 solid dispersions: evaluation and stability assessment

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