Physical properties of pharmaceutical pellets

Šibanc, Rok; Kitak, Teja; Govedarica, Biljana; Srčič, Stanko; Dreu, Rok

doi:10.1016/j.ces.2012.04.037

Cited by 16 publications

(4 citation statements)

References 40 publications

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“…b = l are round pellets, b ˂ l are elliptical pellets having an aspect ratio 1.2–1.5. The limiting value is 1.1 for aspect ratio, whereas, the acceptable lower limit value for e R is 0.6 [27, 28]. …”

Section: Methodsmentioning

confidence: 99%

Lipids bearing extruded-spheronized pellets for extended release of poorly soluble antiemetic agent—Meclizine HCl

et al. 2017

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BackgroundAntiemetic agent Meclizine HCl, widely prescribed in vertigo, is available only in immediate release dosage forms. The approved therapeutic dose and shorter elimination half-life make Meclizine HCl a potential candidate to be formulated in extended release dosage form. This study was aimed to develop extended release Meclizine HCl pellets by extrusion spheronization using natural and synthetic lipids. Influence of lipid type, drug/lipid ratio and combinations of different lipids on drug release and sphericity of pellets were evaluated.MethodsThirty two formulations were prepared with four different lipids, Glyceryl monostearate (Geleol®), Glyceryl palmitostearate (Precirol®), Glyceryl behenate (Compritol®) and Carnauba wax, utilized either alone or in combinations of drug/lipid ratio of 1:0.5–1:3. Dissolution studies were performed at variable pH and release kinetics were analyzed. Fourier transform infrared spectroscopy was conducted and no drug lipid interaction was found.ResultsSphericity indicated by shape factor (eR) varied with type and concentration of lipids: Geleol® (eR = 0.891–0.997), Precirol® (eR = 0.611–0.743), Compritol® (eR = 0.665–0.729) and Carnauba wax (eR = 0.499-0.551). Highly spherical pellets were obtained with Geleol® (Aspect ratio = 1.005–1.052) whereas irregularly shaped pellets were formed using Carnauba wax (Aspect ratio = 1.153–1.309). Drug release was effectively controlled by three different combinations of lipids: (i) Geleol® and Compritol®, (ii) Geleol® and Carnauba wax and (iii) Geleol®, Compritol® and Carnauba wax. Scanning electron microscopy of Compritol® pellets showed smooth surface with pores, whereas, irregular rough surface with hollow depressions was observed in Carnauba wax pellets. Energy dispersive spectroscopy indicated elemental composition of lipid matrix pellets. Kinetics of (i) Geleol® and Compritol® pellets, explained by Korsmeyer-Peppas (R2 = 0.978–0.993) indicated non-Fickian diffusion (n = 0.519-0.597). Combinations of (ii) Geleol® and Carnauba wax and (iii) Geleol®, Compritol® and Carnauba wax pellets followed Zero-order (R2 = 0.991–0.995). Similarity test was performed using combination of Geleol® and Compritol® (i) as a reference.ConclusionsMatrices for the extended release of Meclizine HCl from extruded-spheronized pellets were successfully formed by using three lipids (Geleol®, Compritol® and Carnauba wax) in different combinations. The encapsulated pellets of Meclizine HCl can be effectively used for treatment of motion sickness, nausea and vertigo for extended period of time.

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Section: Methodsmentioning

confidence: 99%

Lipids bearing extruded-spheronized pellets for extended release of poorly soluble antiemetic agent—Meclizine HCl

et al. 2017

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“…Most of the literature presents the coefficient of restitution of spherical and cylindrical particles through experimental tests using various materials, including metal [12], microcrystalline cellulose [13], glass [14] and rubber [15]. Šibanc also determined Young's modulus, the tensile strength and the stiffness of pellets [13].…”

Section: Introductionmentioning

confidence: 99%

Experimental determination of parameter effects on the coefficient of restitution of differently shaped maize in three-dimensions

et al. 2015

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“…For granules and pellets, tensile strength (Equation 4) and Young's elastic modulus, related to the stiffness and crushing strength (hardness) of the material, are the most frequently determined. For this purpose, a strain chart can be obtained by using a texture analyzer device, in which the material is exposed to a given load against time (Santos et al, 2006;Šibanc et al, 2013;Yeung, Rein, 2015). Equation 4δ = tensile strength; F = intensity of the force required to break; r 2 = radius of the particle obtained by Feret´s diameter For friability, different adjustments are performed (Table IX), typically using glass or steel balls, in order to increase the material´s abrasion and improve the sensitivity of the method (Chopra, Venkatesan, Betageri, 2013;Issa et al, 2012b;Santos et al, 2006).…”

Section: Mechanical Strengthmentioning

confidence: 99%

“…The study of Issa et al (2012b) reported an alternative in which the mass loss is measured by comparing the amounts retained in the sieves, where the particle size distribution is carried out before and after the assay. Bialleck, Rein, 2011;Podczeck, Newton, 2014;Santos et al, 2005 Pellets Hardness, tensile strength and relaxation module Cespi et al, 2007Pellets Hardness Costa, Pais, Sousa, 2004Ghanam, Hassan, Kleinebudde, 2010;Hamedelniel, Bajdik, Pintye-Hódi, 2010;Rabišková et al, 2012;Rahmaniam, Naji, Ghadiri, 2011 Pellets Tensile strength and elastic modulus Šibanc et al, 2013Minitablets Hardness Aleksovski et al, 2015Lopes et al, 2006;Stoltenberg, Breitkreutz, 2011;Tomuta, Leucuta, 2007;Weyenberg et al, 2006 Minitablets Tensile strength Tissen et al, 2011 *Hot melt extrusion…”

Section: Mechanical Strengthmentioning

confidence: 99%

Physical characterization of multiparticulate systems

Issa

Souza

Duque

et al. 2018

Braz. J. Pharm. Sci.

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The search for new pharmaceutical dosage forms and different drug delivery systems already used in therapeutics is a global trend, serving as an opportunity to expand the portfolio for the pharmaceutical industry. In this context, multiparticulate systems, such as pellets, granules, and minitablets, represent an attractive alternative, given the range of possibilities they provide. Among the methods used in the production of these systems, we highlight the process of extrusion-spheronization for pellet manufacture, wet granulation and hot-melt extrusion for the obtention of granules, and direct compression for minitablets. Although highly versatile, depending on the technology chosen, many processes and formulation variables can influence the ensuing stages of manufacture, as well as the final product. Therefore, the characterization of these small units is of fundamental importance for achieving batch homogeneity and optimal product performance. Analyses, including particle size distribution, morphology, density, porosity, mechanical strength and disintegration, are example tests used in this characterization. The objective of this review was to address the most widely used tests for the physical evaluation of multiparticulate systems.

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Physical properties of pharmaceutical pellets

Cited by 16 publications

References 40 publications

Lipids bearing extruded-spheronized pellets for extended release of poorly soluble antiemetic agent—Meclizine HCl

Lipids bearing extruded-spheronized pellets for extended release of poorly soluble antiemetic agent—Meclizine HCl

Experimental determination of parameter effects on the coefficient of restitution of differently shaped maize in three-dimensions

Physical characterization of multiparticulate systems

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