A decrease in the drug release rate over time typically affects the performance of hydrophilic matrices for oral prolonged release. To address such an issue, a Non-Uniform Drug Distribution Matrix (NUDDMat) based on hypromellose was proposed and demonstrated to yield zero-order release. The system consisted of 5 overlaid layers, applied by powder layering, having drug concentration decreasing from the inside towards the outside of the matrix according to a descending staircase function. In the present study, manufacturing and performance of the described delivery platform were evaluated using drug tracers having different water solubility. Lansoprazole, acetaminophen and losartan potassium were selected as slightly (SST), moderately (MST) and highly (HST) soluble tracers. By halving the thickness of the external layer, which contained no drug, linear release of HST and MST was obtained. The release behavior of the NUDDMat system loaded with a drug having pH-independent solubility was shown to be consistent in pH 1.2, 4.5 and 6.8 media. Based on these results, feasibility of the NUDDMat platform by powder layering was demonstrated using drugs having different physico-technological characteristics. Moreover, its ability to generate zero-order release was proved in the case of drugs with water solubility in a relatively wide range.

Non-uniform drug distribution matrix system (NUDDMat) for zero-order release of drugs with different solubility / M. Cerea, A. Foppoli, L. Palugan, A. Melocchi, L. Zema, A. Maroni, A. Gazzaniga. - In: INTERNATIONAL JOURNAL OF PHARMACEUTICS. - ISSN 0378-5173. - 581(2020 May 15). [10.1016/j.ijpharm.2020.119217]

Non-uniform drug distribution matrix system (NUDDMat) for zero-order release of drugs with different solubility

M. Cerea
Primo
;
A. Foppoli
Secondo
;
L. Palugan;A. Melocchi;L. Zema;A. Maroni
Penultimo
;
A. Gazzaniga
Ultimo
2020-05-15

Abstract

A decrease in the drug release rate over time typically affects the performance of hydrophilic matrices for oral prolonged release. To address such an issue, a Non-Uniform Drug Distribution Matrix (NUDDMat) based on hypromellose was proposed and demonstrated to yield zero-order release. The system consisted of 5 overlaid layers, applied by powder layering, having drug concentration decreasing from the inside towards the outside of the matrix according to a descending staircase function. In the present study, manufacturing and performance of the described delivery platform were evaluated using drug tracers having different water solubility. Lansoprazole, acetaminophen and losartan potassium were selected as slightly (SST), moderately (MST) and highly (HST) soluble tracers. By halving the thickness of the external layer, which contained no drug, linear release of HST and MST was obtained. The release behavior of the NUDDMat system loaded with a drug having pH-independent solubility was shown to be consistent in pH 1.2, 4.5 and 6.8 media. Based on these results, feasibility of the NUDDMat platform by powder layering was demonstrated using drugs having different physico-technological characteristics. Moreover, its ability to generate zero-order release was proved in the case of drugs with water solubility in a relatively wide range.
Gradient concentration; Hydrophilic matrices; Oral prolonged release; Powder layering; Tangential-spray rotary fluid bed; Zero-order kinetics
Settore CHIM/09 - Farmaceutico Tecnologico Applicativo
9-mar-2020
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/729914
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