Rice spouted bed for manufacturing inclusion complexes of Endopleura uchi L extracts in β-cyclodextrin--颗粒学报PARTICUOLOGY

Freitas, L. V. D., Montes, A. C. R., Campos, E. I. A., Conceição, E. C., Tacon, L. A., Lanchote, A. D., & Freitas, L. A. P. (2019). Rice spouted bed for manufacturing inclusion complexes of Endopleura uchi L extracts in β-cyclodextrin. Particuology, 42, 208-215. https://doi.org/10.1016/j.partic.2018.03.014

Rice spouted bed for manufacturing inclusion complexes of Endopleura uchi L extracts in β-cyclodextrin

L.V.D. Freitas, A.C.R. Montes, E.I.A. Campos, E.C. Conceição, L.A. Tacon, A.D. Lanchote, L.A.P. Freitas ^*

Faculdade de Ciências Farmacêuticas de Ribeirão Preto, University of São Paulo, Via do Café s/n, 14040-903, Ribeirão Preto, SP, Brazil

10.1016/j.partic.2018.03.014

Volume 42, February 2019, Pages 208-215

Received 30 November 2017, Revised 26 February 2018, Accepted 25 March 2018, Available online 11 September 2018, Version of Record 21 January 2019.

E-mail: lapdfrei@usp.br; lapdfrei@fcfrp.usp.br

Highlights

• β-cyclodextrin/bergenin inclusion complexes were incorporated on cooked rice in spouted bed.

• Multivariate approach was used to determine optimum conditions for improving product quality.

• Water solubility of bergenin in the product was almost twice that of pure bergenin.

Abstract

Uxi (Endopleura uchi) is a plant from the Brazilian Amazon. It has many biological activities that are attributed to its main active component, bergenin (BG), which has low water solubility. The aim of this work was to obtain β-cyclodextrin (β-CD) inclusion complexes of uxi using lyophilized cooked rice as the solid substrate. The process was studied using a Box–Behnken design with the solution feed rate, molar ratio of β-CD to BG, and rice bed load as factors. These factors greatly affected the product bulk density, angle of repose, water content, and BG content, loss, and water solubility. The optimum process conditions determined using a desirability functions methodology were an extract feed rate of 1 mL/min, a ratio of β-CD to BG of 3:1, and a substrate load of 100 g. The predicted values under the optimum conditions were close to the experimental results of a water content of 5.8% ± 0.2%, BG content of 985.7 ± 15.4 μg/g, BG water solubility of 2230.2 ± 21.1 μg/mL, and BG loss of 1.2% ± 0.1%. These results confirm that spouted beds are an important tool for rapid, one-step preparation of pharmaceutical β-CD inclusion complexes in a solid form.

Graphical abstract

Keywords

Bergenin; Chromatography; Yield; Active loss; Solubility

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