Mini-tablets as technological strategy for modified release of morphine sulfate

Abstract

This study aimed to use an intelligent formulation design for the development of mini-tablets for the modified release of morphine sulfate. A formulation (F1) was proposed using the Hiperstart® software. Based on the suggested formulation, two other formulations (F2 and F3) were prepared: one for modified and another for immediate drug release. The powders were characterized as bulk and tapped density, Hausner’s factor, and compressibility index analyses. Mini-tablets were directly compressed and characterized by hardness, friability, size, and weight variation. The in vitro drug release profile was carried out according to apparatus 1 of USP. Formulations showed good flow properties, and the mini-tablets displayed characteristics according to the specified. In comparison to F3 (immediate release), F1 and F2 displayed slower drug release time, showing the efficiency of the matrix formed. F3 displayed 90% of drug released up to 10 min, while F1 and F2 required 240 min. The results highlight the importance to use intelligent formulation design for the development of improved mini-tablet matrices. Formulation F1 was found to be suitable for modified morphine sulfate release. Further studies with more formulations are necessary for the production of optimized mini-tablets with suitable prolonged morphine sulfate release.

Keywords:

• Development
• solid dosage form
• drug delivery
• formulation
• analgesics

Authors contributions

Raizza Tafet Carminato e Silva: Conceptualization, Data curation, Formal analysis, Investigation, Methodology, Writing - original draft. Marcos Luciano Bruschi: Conceptualization, Data curation, Methodology, Supervision, Funding acquisition, Project administration, Resources, Writing - original draft, Writing – review & editing.

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

The authors are thankful to the Brazilian funding agencies CAPES (Coordenação de Aperfeiçoamento de Pessoal de Nível Superior/Coordination for the Improvement of Higher Education Personnel; Finance Code 001), CNPq (Conselho Nacional de Desenvolvimento Científico e Tecnológico/National Council for Scientific and Technological Development; Process n° 307695/2020-4) for their support.