Optimization of extrusion spheronization process and gamma scintigraphy of coated rifaximin pellets
DOI:
https://doi.org/10.1590/s2175-97902026e25034Keywords:
Pellets, Colon targeting, Rifaximin, Extrusion-spheronization, Optimization, Gamma scintigraphyAbstract
This study aims to optimize the process of extrusion spheronization for the development of rifaximin pellets and target them to the colon. Microcrystalline cellulose (MCC) is used to spheronizing aid in formulating pellets. MCC concentration, water content, spheronization speed, and time were optimized against roundness and % usable yield using Box-Behnken design. Coating levels of both the polymers were optimized using central composite design for drug release at 2, 4, 7, and 12 h at pH levels of 1.2, 6.8, 7.4, and 6.8 respectively. A gamma scintigraphy study helps in identifying transit pattern of coated pellets in GIT. Optimal conditions for rifaximin pellets with the desired pellet characteristics were identified as 34.19% MCC, 8.6% water, 1004 rpm, and 5.12 minutes. The observed values for drug release at 2, 4, 7, and 12 h at the aforesaid pH conditions were 0.17±0.00%, 3.08±0.13%, 39.01±1.17%, and 99.37±2.73%, respectively. This shows strong concordance between the observed and predicted values. The average durations for colon arrival, small intestine transit, and stomach emptying were 6.26±0.142 h, 5.72±0.408 h, and 0.70±0.265 h, respectively. This shows that the higher number of pellets reaches the colon in the desired time period. The study concluded with the development of optimized pellets and gamma scintigraphy confirms that the coating improves colonic rifaximin delivery.
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Data Availability Statement
The raw/processed data required to reproduce these findings are available on request from the corresponding author. The data are not publicly available at this time as the data also forms part of an ongoing study.
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