The use of beta-cyclodextrin in the manufacturing of disintegrating pellets with improved dissolution performances.
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 (betaCD) was therefore explored for the manufacturing of pellets with a potential for effective disintegration and immediate release of poorly soluble active ingredients. MCC/betaCD 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% betaCD. Based on dissolution testing results, the suitability of betaCD for the preparation of disintegrating MCC-containing pellets with improved dissolution performance was finally demonstrated.
Istituto di Chimica Farmaceutica e Tossicologica "P. Pratesi", Università degli Studi di Milano, viale Abruzzi 42, 20131 Milan, Italy.
Lucia
L
Zema
Luca
L
Palugan
Alessandra
A
Maroni
Anastasia
A
Foppoli
Maria Edvige
ME
Sangalli
Andrea
A
Gazzaniga
D000082:Acetaminophen / Q000737:chemistry; D002482:Cellulose / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D004304:Dosage Forms; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry*; D007660:Ketoprofen / Q000737:chemistry; D007700:Kinetics; D015233:Models, Statistical; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods; D047392:beta-Cyclodextrins / Q000737:chemistry*
D004304:Dosage Forms; D005079:Excipients; D047392:beta-Cyclodextrins; D000082:Acetaminophen; D002482:Cellulose; D007660:Ketoprofen; C109691:microcrystalline cellulose