The preparation and characterization of sustained-release solid dispersion of resveratrol by hot-melt extrusion technology

doi:10.5246/jcps.2023.03.014

Abstract

Abstract:

In the present study, we aimed to prepare, characterize, and evaluate the capability of solid dispersion (SD) for resveratrol (RES) with low solubility and high melting points. A sustained-release solid dispersion (SRSD) was prepared by hot melt extrusion (HME). The release of RES was controlled using a hydrophobic-hydrophilic polymer mixture (Eudragit RS and Poloxamer 188). The effects of formula and process parameters were systematically studied by univariate analysis. Then the Box-Behnken design (three factors, three levels) was used to optimize the preparation process of SRSD. Differential scanning calorimetry and X-ray diffraction were adopted to determine the physical state of SD. Scanning electron microscopy was used to observe its surface properties, and Fourier transform infrared spectroscopy was used to explore chemical interactions between excipients. Dissolution studies were carried out to investigate the kinetics and drug release time. In vitro studies showed that RES release followed the Weibull model kinetic. RES SRSD (RESRS P188-SRSD) was successfully prepared using HME, in which the mass ratio of the drug to the carrier was 1:3, the release regulator was P188, and the dosage was 10%. The stability of the preparation was good, and the dissolution was increased by 10 times.

Key words: Sustained-release solid dispersion, Resveratrol, Hot-melt extrusion, Box-Behnken design

Supporting:

Meiqi Gao, Jiali Wu, Wenjing Zhu, Xiaotong Zhang, Wenling Fan. The preparation and characterization of sustained-release solid dispersion of resveratrol by hot-melt extrusion technology[J]. Journal of Chinese Pharmaceutical Sciences, 2023, 32(3): 165-179.

Figures/Tables 30

Table 1. Single-factor experiment programs.

Table 2. The factors and responses of the BBD.

Table 3. Release model equations.

Table 4. The solubility parameter values for drugs and carriers.

Table 5. Results of BBD.

Table 6. Variance analysis of regression model.

Table 7. Equilibrium solubility of RES and RES-SD.

Table 8. The release pattern of RES/RS/P188-SRSD.

Table 9. The result of the long-term retention test.

Table 10. Pharmacokinetic parameters of raw RES and SRSD in rats after oral administration.

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