Use of fine particle ethylcellulose as the diluent in the production of pellets by extrusion-spheronization

Mallipeddi, Rama; Saripella, Kalyan K.; Neau, Steven H.

doi:10.1016/j.jsps.2013.11.001

Cited by 16 publications

(9 citation statements)

References 17 publications

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“…Also, in the coating context, its important feature is insolubility at any physiological pH. However, the polymer exhibits swelling in the presence of gastric juice, making it permeable for water and permitting extended modified drug release [4,17,18,19,20,21,22]. EC-coated beads have also demonstrated the ability to absorb pressure and hence protect the coating from fracture during compression.…”

Section: Pharmaceutical Characteristics Of Ecmentioning

confidence: 99%

Ethylcellulose–A Pharmaceutical Excipient with Multidirectional Application in Drug Dosage Forms Development

2019

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Polymers constitute the most important group of excipients utilized in modern pharmaceutical technology, playing an essential role in the development of drug dosage forms. Synthetic, semisynthetic, and natural polymeric materials offer opportunities to overcome different formulative challenges and to design novel dosage forms for controlled release or for site-specific drug delivery. They are extensively used to design therapeutic systems, modify drug release, or mask unpleasant drug taste. Cellulose derivatives are characterized by different physicochemical properties, such as swellability, viscosity, biodegradability, pH dependency, or mucoadhesion, which determine their use in industry. One cellulose derivative with widespread application is ethylcellulose. Ethylcellulose is used in pharmaceutical technology as a coating agent, flavoring fixative, binder, filler, film-former, drug carrier, or stabilizer. The aim of this article is to provide a broad overview of ethylcellulose utilization for pharmaceutical purposes, with particular emphasis on its multidirectional role in the development of oral and topical drug dosage forms.

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Section: Pharmaceutical Characteristics Of Ecmentioning

confidence: 99%

Ethylcellulose–A Pharmaceutical Excipient with Multidirectional Application in Drug Dosage Forms Development

2019

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“…EC is also utilized in modified-release tablets as an excipient creating a matrix structure. Commercially, it is available in a wide range of viscosity grades as well as in the form of aqueous dispersions, giving a good range of possibilities for the formulators [11,12,13,14,15,16]. Examples of solid organic forms are Ethocel ® and Aqualon ™, and of aqueous dispersions Aquacoat ® ECD, Surelease ® , Aquarius ™ Control ECD, or AshaKote ® [17,18,19,20,21].…”

Section: Introductionmentioning

confidence: 99%

“…Despite widespread utilization of EC in the pharmaceutical technology [6,11,12,13,14,15,16,25], there are only a few papers concerning its application for obtaining microparticles by the spray drying technique. The aim of this work was to compare the characteristics of microparticles made using EC in organic or aqueous form.…”

Section: Introductionmentioning

confidence: 99%

Ethylcellulose in Organic Solution or Aqueous Dispersion Form in Designing Taste-Masked Microparticles by the Spray Drying Technique with a Model Bitter Drug: Rupatadine Fumarate

et al. 2019

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The taste of drugs is an important factor affecting pharmacotherapy effectiveness, and obtaining formulations with acceptable organoleptic properties is still an ongoing issue in pharmaceutical technology. One of the innovative methods of taste masking is preparation of microparticles by the spray drying technique, utilizing polymers with different physicochemical properties. Rupatadine fumarate (RUP) is one of the newest antihistamines, with an innovative and multidirectional mechanism of action, and an extremely bitter taste. The aim of this work was to investigate the feasibility of utilizing organic or aqueous forms of ethylcellulose (EC) for the preparation of microparticles with RUP by the spray drying technique. Spray dried samples at different drug:polymer ratios were prepared using organic solution (Ethocel®) or aqueous dispersions of EC (Surelease®, Aquacoat® ECD). Evaluation of the taste masking efficacy was performed in vivo in human taste panel, in vitro based on dissolution test, and by self-constructed electronic tongue. It was shown that microparticles obtained from aqueous dispersions of EC have superior pharmaceutical properties in terms of both morphology and taste masking efficacy in comparison to those obtained from organic solution.

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“…While the sphericity might describe the circular nature of the pellet images more clearly, the aspect ratio proved to be more discriminating regarding the influences of the different factors on the response, as observed by Mallipeddi et al [33] with pellets where fine particle ethyl cellulose was the diluent. ANOVA of the sphericity data does not reveal the influences of the factors because the sphericity for the center point batches almost covers the breadth of the sphericity values for the entire study (Table III).…”

Section: Sphericity and Aspect Ratiomentioning

confidence: 86%

A Quality by Experimental Design Approach to Assess the Effect of Formulation and Process Variables on the Extrusion and Spheronization of Drug-Loaded Pellets Containing Polyplasdone® XL-10

et al. 2015

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Abstract. Successful pellet production has been reported in literature with cross-linked poly(vinylpyrrolidone), Polyplasdone ® XL-10 and INF-10. In the present study, a quality by experimental design approach was used to assess several formulation and process parameter effects on the characteristics of Polyplasdone ® XL-10 pellets, including pellet size, shape, yield, usable yield, friability, and number of fines. The hypothesis is that design of experiments and appropriate data analysis allow optimization of the Polyplasdone product. High drug loading was achieved using caffeine, a moderately soluble drug to allow in vitro release studies. A five-factor, two-level, half-fractional factorial design (Resolution V) with center point batches allowed mathematical modeling of the influence of the factors and their two-factor interactions on five of the responses. The five factors were Polyplasdone ® level in the powder blend, volume of water in the wet massing step, wet mixing time, spheronizer speed, and spheronization time. Each factor and/or its two-factor interaction with another factor influenced pellet characteristics. The behavior of these materials under various processing conditions and component levels during extrusionspheronization have been assessed, discussed, and explained based on the results. Numerical optimization with a desirability of 0.974 was possible because curvature and lack of fit were not significant with any of the model equations. The values predicted by the optimization described well the observed responses. The hypothesis was thus supported.

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Use of fine particle ethylcellulose as the diluent in the production of pellets by extrusion-spheronization

Cited by 16 publications

References 17 publications

Ethylcellulose–A Pharmaceutical Excipient with Multidirectional Application in Drug Dosage Forms Development

Ethylcellulose–A Pharmaceutical Excipient with Multidirectional Application in Drug Dosage Forms Development

Ethylcellulose in Organic Solution or Aqueous Dispersion Form in Designing Taste-Masked Microparticles by the Spray Drying Technique with a Model Bitter Drug: Rupatadine Fumarate

A Quality by Experimental Design Approach to Assess the Effect of Formulation and Process Variables on the Extrusion and Spheronization of Drug-Loaded Pellets Containing Polyplasdone® XL-10

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