Evaluation of Uniform-Sized Microcapsules Using a Vibration-Nozzle Method

Shimano, Kenjiro; Kondo, Omi; Miwa, Akio; Higashi, Yukihito; Koyama, Ikuko; Yoshida, Tsuguchika; Ito, Yoshinori; Hirose, Jun; Goto, Shigeru

doi:10.3109/03639049509048114

Cited by 13 publications

(6 citation statements)

References 12 publications

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“…The target particle size was set at 150 mm or less, which was based on reference material. 12) Consequently, the target characteristics of taste-masked particles are as follows: 1) Dissolution rate: not more than 30% at D1 min and not less than 85% at D15 min 2) Particle size: not more than 150 mm.…”

Section: Resultsmentioning

confidence: 99%

Formulation Design of Taste-Masked Particles, Including Famotidine, for an Oral Fast-Disintegrating Dosage Form

Mizumoto

Tamura

Kawai

et al. 2008

CHEMICAL & PHARMACEUTICAL BULLETIN

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Many elderly patients often have difficulty swallowing some of the dosage forms (tablets, capsules, and powders) currently used. For this reason, the development of an appropriate dosage form for elderly patients is most desirable. Since the late 1980s, many companies have developed fastdisintegrating dosage forms that disintegrate easily in the mouth and can be taken without water. Cardinal Health marketed a fast-disintegrating, freeze-dried porous wafer known as Zydis 1,2) and CIMA also marketed an effervescent tablet known as OraSolve.3) Eisai developed the EMP tablet, 4) and Ethypharm developed Flashtab.5) A new fast-disintegrating tablet consisting of high-and low-compressibility saccharides was reported in a previous study. 6) Although famotidine was used as a model drug for the new fast-disintegrating tablet, it had an unpleasant taste. In fact, most of the fast-disintegrating technologies described above were not applied to bitter-tasting drugs. Consequently, in this study, attempts have been made to produce a taste-masked, fast-disintegrating tablet using famotidine as a model drug.Various taste-masking technologies, such as the addition of sweeteners and flavors, coating with water insoluble materials, 7) creating a wax matrix by spray congealing, 8) adsorption to ion-exchange resin, 9,10) and complexing with cyclodextrins 11) had been investigated. Water insoluble polymer coating technology was widely employed to control the initial dissolution rate and to suppress the bitter taste. Famotidine bulk powder was coated in a fluidized-bed granulator in an attempt to suppress the bitter taste, but this was not successful. Because the reproducibility of coating operation was not achieved due to the poor flowability of famotidine powder. Therefore, the spray-drying method was selected as an alternative to the powder coating method.The objectives of this study were to determine the optimum formula and manufacturing conditions for producing taste-masked particles using the spray-drying method that could be applied to a fast-disintegrating tablet. If successful, this would result in a novel, taste-masked, fast-disintegrating tablet. ExperimentalMaterials The D-mannitol (Mitsubishi Shoji Foodtech, brand name: Mannit P), maltose (Hayashibara, brand name: Sanmalt), Aquacoat ECD30 (Ethylcellulose Aqueous Dispersion, FMC Corporation), Eudragit NE30D (Ethyl Acrylate Methyl Methacrylate Copolymer Dispersion, Röhm GmbH & Co., KG), triacetin (Yuki Gosei Kogyo), and calcium stearate (Nippon Oil & Fats) were used in this study. Famotidine (Astellas Pharma Inc., JP standard) was used as the model drug.Determination of Bitterness Threshold After mixing famotidine bulk powder and placebo granules consisting of mannitol granulated with 5% maltose in a fluidized-bed granulator, a tablet was prepared by compressing in an hydraulic press (weight of tablet: 170 mg, diameter of tablet: 8.5 mm). The concentrations of famotidine used were 0.5, 1, 2, and 5 mg per tablet. Sensory testing was conducted as follows: each volunteer washed...

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Section: Resultsmentioning

confidence: 99%

Formulation Design of Taste-Masked Particles, Including Famotidine, for an Oral Fast-Disintegrating Dosage Form

Mizumoto

Tamura

Kawai

et al. 2008

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Polyvinylacetal diethylaminoacetate (AEA) is another cationic polymer used in pharmaceutical industry for pH-dependent drug release. AEA has been reported to be insoluble above pH 5.8 [33]. Microspheres of AEA containing trimebutine maleate have been prepared by a water-in-oil-in-water (w/o/w) emulsion solvent evaporation method [26].…”

Section: Ph-sensitive Polymersmentioning

confidence: 99%

pH- and ion-sensitive polymers for drug delivery

Yoshida

Lai

Kwon

et al. 2013

Expert Opinion on Drug Delivery

294

181

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Introduction Drug delivery systems (DDSs) are important for effective, safe, and convenient administration of drugs. pH- and ion-responsive polymers have been widely employed in DDS for site-specific drug release due to their abilities to exploit specific pH- or ion-gradients in the human body. Areas covered Having pH-sensitivity, cationic polymers can mask the taste of drugs and release drugs in the stomach by responding to gastric low pH. Anionic polymers responsive to intestinal high pH are used for preventing gastric degradation of drug, colon drug delivery and achieving high bioavailability of weak basic drugs. Tumor-targeted DDSs have been developed based on polymers with imidazole groups or poly(β-amino ester) responsive to tumoral low pH. Polymers with pH-sensitive chemical linkages, such as hydrazone, acetal, ortho ester and vinyl ester, pH-sensitive cell-penetrating peptides and cationic polymers undergoing pH-dependent protonation have been studied to utilize the pH gradient along the endocytic pathway for intracellular drug delivery. As ion-sensitive polymers, ion-exchange resins are frequently used for taste-masking, counterion-responsive drug release and sustained drug release. Polymers responding to ions in the saliva and gastrointestinal fluids are also used for controlled drug release in oral drug formulations. Expert opinion Stimuli-responsive DDSs are important for achieving site-specific and controlled drug release; however, intraindividual, interindividual and intercellular variations of pH should be considered when designing DDSs or drug products. Combination of polymers and other components, and deeper understanding of human physiology are important for development of pH- and ion-sensitive polymeric DDS products for patients.

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“…This may be achieved using microencapsulation techniques such as spray-drying (Yajima et al, 1999;Wilson et al, 1994), spray-congealing (Shimano et al, 1995;Robson et al, 1999), coacervation (Chukuwu et al 1991;Al-Omranm et al, 2002) or the solvent evaporation method (Hashimoto et al, 2002). Dihydroartemisinin (DHA), a more water-soluble metabolite of artemisinin derivatives, is a safe and highly effective antimalarial analog of artemisinin (Chen et al, 2004).…”

Section: Introductionmentioning

confidence: 99%

The evaluation of coated granules to mask the bitter taste of dihydroartemisinin

Shahzad

Shah

Atique

et al. 2011

Braz. J. Pharm. Sci.

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The purpose of this study was to mask the bitter taste imparted by dihydroartemisinin (DHA) by the use of different coating materials. Trial-1 and trial-2 were conducted to prepare the DHA granules. The granules produced from trial-1 were irregular in shape and smaller in size while the trial-2 granules were more regular and larger in size. The granules obtained from both trials were then coated with two different coating methods, namely A and B, depending upon coating material. The trial-2 granules showed better flow properties than trial-1 granules. In vitro dissolution studies in phosphate buffer at pH 6.8 revealed that granules of trial-2B released only 34% ± 3 DHA in two minutes compared with trial-1A (57% ± 2), trial-1B (48% ± 2) and trial-2A (53% ± 7). The pleasant taste perception (PTP) test also confirmed the taste masking efficacy of trial-2B (P < 0.05). Scanning electron microscopy (SEM) revealed the more regular and smooth surface of trial-2B granules. In addition, the differential thermal and thermogravimetric analysis (TG-DTA) confirmed no interaction between the materials and pure DHA. DHA has shown its characteristic peaks in the x-ray diffraction (XRD) patterns which were also prominent in all the granules. In conclusion, the granules obtained from trial-2B displayed considerable decrease in the bitter taste of DHA thereby fulfilling the purpose of this study.Uniterms: Medicines/coating. Granules/coating. Dihydroartemisinin (DHA)/taste masking. Thermogravimetric analysis/medicines analysis. X-ray diffraction/medicines analysis.O objetivo deste estudo foi o de mascarar o gosto amargo característico da diidroartemisinina (DHA) pelo uso de diferentes materiais de revestimento. Experimento-1 e experimento-2 foram realizados para preparar grânulos de DHA. Os grânulos produzidos pelo experimento-1 mostraram-se irregulares e menores se comparados aos obtidos pelo experimento-2, que foram mais regulares e maiores. Os grânulos obtidos em ambos os experimentos foram, então, revestidos por dois métodos distintos de revestimento, designados como A e B, dependendo do material de revestimento empregado. Os grânulos do experimento-2 mostraram melhor propriedade de fluxo que os obtidos no experimento-1. Estudos de dissolução in vitro em tampão fosfato pH 6,8 revelaram que grânulos do experimento-2B liberaram apenas 34% ± 3 da DHA em dois minutos se comparado com experimento-1A (57% ± 2), experimento-1B (48% ± 2) e experimento-2A (53% ± 7). A Análise Sensorial quanto ao sabor (Pleasant Taste Perception -PTP) também confirmou a eficácia do experimento-2B (P <0,05) em mascarar o gosto amargo da DHA. Microscopia Eletrônica de Varredura (SEM) revelou a superfície mais regular e lisa dos grânulos obtidos pelo experimento-2B. Além disso, Análise Termogravimétrica e Análise Térmica Diferencial (TG-DTA) confirmaram que não há nenhuma interação entre os materiais e a DHA pura. DHA mostrou seus picos característicos na Difração de Raios X (XRD) em padrões que também foram proeminentes em todas as amostras. Em conclusão, o...

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Evaluation of Uniform-Sized Microcapsules Using a Vibration-Nozzle Method

Cited by 13 publications

References 12 publications

Formulation Design of Taste-Masked Particles, Including Famotidine, for an Oral Fast-Disintegrating Dosage Form

Formulation Design of Taste-Masked Particles, Including Famotidine, for an Oral Fast-Disintegrating Dosage Form

pH- and ion-sensitive polymers for drug delivery

The evaluation of coated granules to mask the bitter taste of dihydroartemisinin

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