Compressibility of Gastroretentive Pellets Coated with Eudragit NE Using a Single-Stroke and a Rotary Tablet Press

Łunio, Rafał; Sawicki, Wiesław; Skoczen, Przemyslaw; Walentynowicz, Olga; Kubasik-Juraniec, Jolanta

doi:10.1080/10837450802089206

Cited by 15 publications

(8 citation statements)

References 11 publications

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“…During the production of verapamil solid foam, the foam cell temperature was higher by 2 • C than that previously described with the BaSO 4 composition due to the higher melting point of the verapamil mixture [3,24]. Three compositions were produced with 15% verapamil-HCl, containing 80-120 mg of verapamil per capsule, which corresponds to the active substance content available in the literature and to the marketed preparations [20,34,35]. An increase in the stearic acid content from 10% (V1) to 12.5% (V2) helped to form the foam structure, as described previously by Vasvári et al [3], but it is important to mention that the excessive stearic acid content reduced foaming.…”

Section: Discussionmentioning

confidence: 99%

In Vitro and In Vivo Studies of a Verapamil-Containing Gastroretentive Solid Foam Capsule

et al. 2022

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Gastroretentive systems may overcome problems associated with incomplete drug absorption by localized release of the API in the stomach. Low-density drug delivery systems can float in the gastric content and improve the bioavailability of small molecules. The current publication presents verapamil–HCl-containing solid foam prepared by continuous manufacturing. Production runs were validated, and the foam structure was characterized by micro-CT scans and SEM. Dissolution properties, texture changes during dissolution, and floating forces were analyzed. An optimized formulation was chosen and given orally to Beagle dogs to determine the pharmacokinetic parameters of the solid foam capsules. As a result, a 12.5 m/m% stearic acid content was found to be the most effective to reduce the apparent density of capsules. Drug release can be described by the first-order model, where 70% of verapamil dissolved after 10 h from the optimized formulation. The texture analysis proved that the structures of the solid foams are resistant. Additionally, the floating forces of the samples remained constant during their dissolution in acidic media. An in vivo study confirmed the prolonged release of the API, and gastroscopic images verified the retention of the capsule in the stomach.

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Section: Discussionmentioning

confidence: 99%

In Vitro and In Vivo Studies of a Verapamil-Containing Gastroretentive Solid Foam Capsule

et al. 2022

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“…Data for the analysis describing the parameters of pellets tableting process, tablet mass composition and tablet properties come from the research of Sawicki's team [9][10][11][12][13][14]. In these studies, the influence of various excipients and technological parameters on the process of obtaining tablets containing floating pellets with verapamil hydrochloride as API was examined.…”

Section: Data Setmentioning

confidence: 99%

Application of Dominance-Based Rough Set Approach for Optimization of Pellets Tableting Process

et al. 2020

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Multiple-unit pellet systems (MUPS) offer many advantages over conventional solid dosage forms both for the manufacturers and patients. Coated pellets can be efficiently compressed into MUPS in classic tableting process and enable controlled release of active pharmaceutical ingredient (APIs). For patients MUPS are divisible without affecting drug release and convenient to swallow. However, maintaining API release profile during the compression process can be a challenge. The aim of this work was to explore and discover relationships between data describing: composition, properties, process parameters (condition attributes) and quality (decision attribute, expressed as similarity factor f2) of MUPS containing pellets with verapamil hydrochloride as API, by applying a dominance-based rough ret approach (DRSA) mathematical data mining technique. DRSA generated decision rules representing cause–effect relationships between condition attributes and decision attribute. Similar API release profiles from pellets before and after tableting can be ensured by proper polymer coating (Eudragit® NE, absence of ethyl cellulose), compression force higher than 6 kN, microcrystalline cellulose (Avicel® 102) as excipient and tablet hardness ≥42.4 N. DRSA can be useful for analysis of complex technological data. Decision rules with high values of confirmation measures can help technologist in optimal formulation development.

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“…The most common cellulose-based polymer used for sustained release dosage forms is ethyl cellulose (EC) [18]. However, EC is known to be a brittle polymer with inappropriate mechanical properties.…”

Section: Coated Pellets (Reservoir-type Multiparticulate Drug Delimentioning

confidence: 99%

“…The SEM images that were obtained showed a lack of damage to the Eudragit NE 40 D coat as well as to the pellet core when the coated pellets were compressed at 18 kN. Therefore, the Eudragit NE 40 D polymer coat remained intact upon compression, and the pellets deformed rather than fragmented, resulting in a sustained release of VH [18]. The study attributed this to the unsymmetry of the applied force on the pellets using the single-stroke tablet press.…”

Section: Coated Pellets (Reservoir-type Multiparticulate Drug Delimentioning

confidence: 99%

Oral Modified Release Multiple-Unit Particulate Systems: Compressed Pellets, Microparticles and Nanoparticles

et al. 2018

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Oral modified-release multiparticulate dosage forms, which are also referred to as oral multiple-unit particulate systems, are becoming increasingly popular for oral drug delivery applications. The compaction of polymer-coated multiparticulates into tablets to produce a sustained-release dosage form is preferred over hard gelatin capsules. Moreover, multiparticulate tablets are a promising solution to chronic conditions, patients’ adherence, and swallowing difficulties if incorporated into orodispersible matrices. Nonetheless, the compaction of multiparticulates often damages the functional polymer coat, which results in a rapid release of the drug substance and the subsequent loss of sustained-release properties. This review brings to the forefront key formulation variables that are likely to influence the compaction of coated multiparticulates into sustained-release tablets. It focusses on the tabletting of coated drug-loaded pellets, microparticles, and nanoparticles with a designated section on each. Furthermore, it explores the various approaches that are used to evaluate the compaction behaviour of particulate systems.

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Compressibility of Gastroretentive Pellets Coated with Eudragit NE Using a Single-Stroke and a Rotary Tablet Press

Cited by 15 publications

References 11 publications

In Vitro and In Vivo Studies of a Verapamil-Containing Gastroretentive Solid Foam Capsule

In Vitro and In Vivo Studies of a Verapamil-Containing Gastroretentive Solid Foam Capsule

Application of Dominance-Based Rough Set Approach for Optimization of Pellets Tableting Process

Oral Modified Release Multiple-Unit Particulate Systems: Compressed Pellets, Microparticles and Nanoparticles

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