It has recently been highlighted that the release behavior of pellets containing microcystalline cellulose (MCC) as the spheronizing agent may be impaired by the lack of disintegration. Although alternative spheronizing excipients have been proposed, their overall advantages have not thoroughly been assessed. In the present work, the possible use of beta-cyclodextrin (beta CD) was therefore explored for the manufacturing of pellets with a potential for effective disintegration and immediate release of poorly soluble active ingredients. MCC/beta CD powder formulations containing no drug or model drugs with different water solubility, able to form inclusion compounds with the employed cyclodextrin, were pelletized by agglomeration in rotary fluid bed equipment. By applying successive statistical experimental designs, the most critical formulation and operating parameters were identified and optimal manufacturing processes were ultimately set up. High yields of pellets provided with satisfactory physical-technological characteristics were obtained using powder formulations with up to 80% beta CD. Based on dissolution testing results, the suitability of beta CD for the preparation of disintegrating MCC-containing pellets with improved dissolution performance was finally demonstrated.

The use of β-cyclodextrin in the manufacturing of disintegrating pellets with improved dissolution performances / L. Zema, L. Palugan, A. Maroni, A. Foppoli, M.E. Sangalli, A. Gazzaniga. - In: AAPS PHARMSCITECH. - ISSN 1530-9932. - 9:2(2008 Jun), pp. 708-717.

The use of β-cyclodextrin in the manufacturing of disintegrating pellets with improved dissolution performances

L. Zema
Primo
;
L. Palugan
Secondo
;
A. Maroni;A. Foppoli;M.E. Sangalli
Penultimo
;
A. Gazzaniga
Ultimo
2008

Abstract

It has recently been highlighted that the release behavior of pellets containing microcystalline cellulose (MCC) as the spheronizing agent may be impaired by the lack of disintegration. Although alternative spheronizing excipients have been proposed, their overall advantages have not thoroughly been assessed. In the present work, the possible use of beta-cyclodextrin (beta CD) was therefore explored for the manufacturing of pellets with a potential for effective disintegration and immediate release of poorly soluble active ingredients. MCC/beta CD powder formulations containing no drug or model drugs with different water solubility, able to form inclusion compounds with the employed cyclodextrin, were pelletized by agglomeration in rotary fluid bed equipment. By applying successive statistical experimental designs, the most critical formulation and operating parameters were identified and optimal manufacturing processes were ultimately set up. High yields of pellets provided with satisfactory physical-technological characteristics were obtained using powder formulations with up to 80% beta CD. Based on dissolution testing results, the suitability of beta CD for the preparation of disintegrating MCC-containing pellets with improved dissolution performance was finally demonstrated.
β-cyclodextrin; Design of experiments; Microcrystalline cellulose; Pellets; Rotary fluid bed
Settore CHIM/09 - Farmaceutico Tecnologico Applicativo
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/62230
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