Influence of process conditions on drug release from pellets

Sousa, João; Sousa, Ana M. L.; Podczeck, Fridrun; Newton, JM

doi:10.1016/s0378-5173(96)04745-x

Cited by 30 publications

(20 citation statements)

References 11 publications

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“…8) show that the drying conditions had a dramatic impact that may be due to (a) polymorphic transitions of ibuprofen during pellet preparation (38), (b) differences in the ibuprofen profile (18), and/ or (c) differences in the pellet micro-structure (7,11,14,15). Via SWAXS analysis, it was confirmed that no polymorphic transition occurred during any of the preparation processes.…”

Section: Discussionmentioning

confidence: 91%

“…Drying conditions were also shown to affect the final pellet size and the corresponding size distribution (1,(4)(5)(6)(7)9,11), as well as the pellet micro-structure (3,(6)(7)(8)(9)(10)(11). Drying-induced differences in the micro-structure significantly influence the pellet's compaction behavior (7)(8)(9)12,13) and the active pharmaceutical ingredient (API) release (dissolution) characteristics (7,11,14,15). Additionally, the spatial API distribution, which is expected to vary with the drying conditions (16), may affect the dissolution behavior.…”

Section: Introductionmentioning

confidence: 99%

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Ibuprofen-Loaded Calcium Stearate Pellets: Drying-Induced Variations in Dosage Form Properties

et al. 2012

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Abstract. Pellets intended for oral dosing are frequently produced via extrusion/spheronization followed by drying. Typically, the last active process step, i.e., drying, is assumed to have little effect on the final dosage form properties (e.g., dissolution characteristics). Thus, there exist only a few studies of this subject. In the present study, calcium stearate/ibuprofen pellets were used as model system to investigate the impact of the drying conditions. Lipophilic calcium stearate matrix pellets containing 20% ibuprofen were prepared via wet extrusion/spheronization. Subsequently, desiccation, fluid-bed drying, and lyophilization were applied for granulation liquid removal. The impact of these drying techniques on the final pellet properties was evaluated. The in vitro dissolution behavior was dramatically altered by the drying techniques that were considered. The investigated pellets showed drug release rates that varied as much as 100%. As no polymorphic transitions occurred during drying, we focused on two possible explanations: (a) a change in the drug distribution within the pellets and (b) a change in pellet micro-structure (porosity, pore size). The ibuprofen distribution proved to be homogeneous regardless of the drying conditions. Pellet porosity and pore sizes, however, were modified by the drying process. Our results clearly demonstrate that a single process step, such as drying, can play a crucial role in achieving desired pellet properties and release profiles.

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Section: Discussionmentioning

confidence: 91%

Section: Introductionmentioning

confidence: 99%

Ibuprofen-Loaded Calcium Stearate Pellets: Drying-Induced Variations in Dosage Form Properties

et al. 2012

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“…A certificação da distribuição homogênea do líquido pode ser conseguida através do armazenamento da massa umidificada em bolsas plásticas devidamente seladas em condições ideais para evitar perdas por evaporação ou deterioração até o prosseguimento do processo de extrusão (Bains et al, 1991;Fielden et al, 1989;Fielden et al 1992a;Fielden et al, 1992b;Fielden et al, 1993;Pinto et al, 1993;Sousa et al, 1996).…”

Section: Processo De Extrusão -Esferonização Malaxagemunclassified

“…Normalmente a água é utilizada como líquido de granulação (Iyer et al, 1996;Sousa et al, 1996;Varshosaz et al, 1997b), contudo, soluções hidroalcoólicas ou apenas álcool podem ser utilizados com o mesmo propósito (Goodhart et al, 1973;Briquet et al, 1986;Millili, Schwartz, 1990;Elbers et al, 1992;Santos et al, 2002).…”

Section: Líquido De Granulação E Umidade Da Massa De Extrusãounclassified

Obtenção de pellets por extrusão e esferonização farmacêutica: parte I. avaliação das variáveis tecnológicas e de formulação

Santos¹,

Veiga²,

Pina³

et al. 2004

Rev. Bras. Cienc. Farm.

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INTRODUÇÃOA administração oral de uma forma farmacêutica é a via mais usual, confortável e conveniente para a liberação de uma substância ativa no organismo.Dentre as diversas formas farmacêutica para a via oral em que os sistemas de liberação de uma substância ativa podem ser concebidos, os pellets têm despertado crescente interesse devido às diversas vantagens tecnológicas e terapêuticas apresentadas (Reynolds, 1970;Bechgaard, Hegermann Nielsen, 1978;Eskilson 1985;Dietrich, 1989). Salientam-se as suas ótimas propriedades de escoamento, devido, principalmente, à forma esférica, estreita distribuição de tamanho de partículas, superfície suscetível ao revestimento por película com interesse à proteção entérica ou à liberação controlada ou sustentada, incorporação de grande quantidade de substância ativa e de substâncias ativas incompatíveis numa mesma forma farmacêutica, grande dispersão no trato gastrintestinal e conseqüente redução da irritação do trato por fármacos gastro-irritantes e baixo risco de efeitos adversos por superdosagem.O processo de produção de pellets, denominado peletização, consiste na aglomeração de pós finos de substância ativa e excipientes em pequenas unidades esféricas, assim denominadas pellets. Estas unidades esféricas diferenciam-se do produto obtido no processo de granulação clássica não apenas no que respeita ao processo pelo qual são produzidas, mas também pelas características físicas apresentadas.O interesse pela utilização de pellets como forma farmacêutica remonta à segunda metade da década de 1940. Em 1952, a Smith Kline & French (SKF) lançou no mercado uma nova forma farmacêutica, o Spansule, que consistia em cápsulas cheias com pellets revestidos que dissolveriam a tempos diferentes. Os pellets eram produzidos por revestimento em camadas a partir de núcleos de açúcar por uma técnica até então não empregada na in-*Correspondência:

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“…The influence of process and formulation variables upon the quality (e.g., size, shape, drug release rate) of produced pellets has extensively been investigated (Bashaiwoldu et al, 2004;Hasznos et al, 1992;Hellén and Yliruusi, 1993;Hellén et al, 1993a;Hellén et al, 1993b;Newton et al, 1995;Sonaglio et al, 1995;Sousa et al, 1996;Vervaet and Remon, 1996;Wan et al, 1993). Due to the large amount of liquid in the granulated mass, the interaction with water can induce phase transformations altering the pharmaceutical and biopharmaceutical performance of the drug.…”

Section: Introductionmentioning

confidence: 99%

Real-time image-based investigation of spheronization and drying phenomena using different pellet formulations

Burggraeve¹,

Sandler²,

Heinämäki³

et al. 2011

European Journal of Pharmaceutical Sciences

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Extrusion-spheronization (ES) is a frequently used agglomeration process in the pharmaceutical industry to manufacture spherical solid units or pellets with a narrow size and shape distribution. In this study, photometric stereo imaging was applied in real-time during the final steps of the ES process, being spheronization and drying. In addition to the pellet size distribution of undispersed (wet) samples, the imaging technique captures visual information on pellet shape and surface brightness. Pellet samples were taken at 20 time points during spheronization and were imaged atline (during spheronization) and off-line (after spheronization). Particle size distributions and visual image information were both used to characterize the spheronization behaviour of different formulations. Next, particle size distributions and surface brightness values calculated from the atline obtained images during fluid bed drying of pellets were analysed. The particle size distribution and brightness value changes occurring during pellet drying were explained both by the reduction in residual moisture content and drug solid-state transition. Due to the rapidness of the technique with regard to sample preparation, sample measurement and the acquisition of results in combination with the possibility to measure undispersed (wet) samples, valuable information on spheronization and drying characteristics of different formulations was obtained in real-time. KeywordsPhotometric stereo imaging -extrusion-spheronization -fluid bed drying -particle size and shape (distribution) -brightness -visualization

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Influence of process conditions on drug release from pellets

Cited by 30 publications

References 11 publications

Ibuprofen-Loaded Calcium Stearate Pellets: Drying-Induced Variations in Dosage Form Properties

Ibuprofen-Loaded Calcium Stearate Pellets: Drying-Induced Variations in Dosage Form Properties

Obtenção de pellets por extrusão e esferonização farmacêutica: parte I. avaliação das variáveis tecnológicas e de formulação

Real-time image-based investigation of spheronization and drying phenomena using different pellet formulations

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