Romanian Society of Pharmaceutical Sciences
 

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THE IMPACT OF THE LUBRICATION STEP WITH MAGNESIUM STEARATE ON THE QUALITY TARGET PRODUCT PROFILE OF A MODIFIED RELEASE ORAL DOSAGE FORM CONTAINING A BCS CLASS II ACTIVE PHARMACEUTICAL INGREDIENT

PAUL ANCU DUMITRAȘCU 1,2, CRISTINA GABRIELA STECOZA 2,3, MARILENA GAVRILESCU 2, CARMEN ALECSANDRESCU 2, ALINA IVANCENCU 2, VALENTINA ANUȚA 1*, LACRĂMIOARA POPA 1, MIHAELA VIOLETA GHICA 1, CRISTINA ELENA DINU-PÎRVU 1

1.“Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Physical and Colloidal Chemistry, 6 Traian Vuia Street, 020956, Bucharest, Romania
2.Zentiva S.A., Portofolio Strategy and Investment Department, 50 Theodor Pallady Boulevard, 032266, Bucharest, Romania
3.“Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, Center for Drug Sciences, 6 Traian Vuia Street, 020956, Bucharest, Romania

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Magnesium stearate is an excipient widely used in the pharmaceutical industry, due to its lubrication proprieties. The aim of the study is to evaluate the impact of the lubrication step with magnesium stearate on the Quality Target Product Profile of a modified release oral dosage form containing a BCS Class II active pharmaceutical ingredient and to determine the critical process parameters correlated to the lubrication step. In this context, experimental batches at industrial scale and pilot scale batches were manufactured with two different sorts of magnesium stearate in concentration of approximately 0.5% (w/w). Based on the experimental results, the over-lubrication phenomena was observed only during the manufacturing of batches with magnesium stearate with lower particle size distribution (~ 1 µm) and higher surface area. The over-lubrication had an higher impact on the physical parameters of the core tablets, such as resistance to crushing. Furthermore, the direct proportionality between the compressing settings and the resistance to crushing parameter was observed to be altered by the lubrication process. Due to the fact the over lubrication phenomena is dependent to the functional-related characteristics of magnesium stearate it can be concluded that the two magnesium stearate sorts cannot be interchangeable, for a tablet matrix with a majority plastic character during compression step.