Preparation of scutellarin solid dispersion based on deep eutectic solvents
10.16438/j.0513-4870.2024-0433
- VernacularTitle:基于低共熔溶剂的灯盏花素固体分散体的制备
- Author:
Yong-jing LIU
;
Li LOU
;
Dong-ting HUANG
;
Li-rong CHEN
;
Xiao-ying WANG
- Publication Type:Research Article
- Keywords:
eep eutectic solvent;
scutellarin;
solid dispersion;
issolution;
pharmacokinetic study
- From:
Acta Pharmaceutica Sinica
2024;59(9):2665-2672
- CountryChina
- Language:Chinese
-
Abstract:
In this study, deep eutectic solvents (DESs) were used as excipients to prepare solid dispersion (SD) of scutellarin. The SD of scutellarin were prepared by melting method with cumulative dissolution rate as the index of investigation. The preparation conditions of SD of scutellarin were optimized by single factor experiment, which investigated the type of the carrier material, the type of DESs, and the ratio of the drug to the carrier. The optimum preparation conditions of DESs-SD were as follows: using Poloxamer 407 as the carrier material, PEG 200/urea (2∶1) as the DESs system, and the ratio of carrier, DESs, and drug was 6∶1∶1. The drug loading capacity of scutellarin in SD was 12.53% under the optimum preparation conditions. Differential scanning calorimetry, Fourier transform infrared spectroscopy, X-ray powder diffraction and scanning electron microscope exhibited that scutellarin was amorphous form in the SD system. Furthermore, the stability of the DESs-based SD of scutellarin was evaluated by high temperature, high humidity, and strong light tests, which showed that the cumulative dissolution rate and scutellarin content of SD decreased with time under these conditions. Finally, the result of pharmacokinetic studies indicated that the oral absorption of the scutellarin could be increased using DESs as an excipient in the preparation of SD. The animal experiment was approved by the Experimental Animal Ethics Committee of Fujian University of Traditional Chinese Medicine (approval number: FJTCMIACUC 2023048). Consequently, this research offers a novel and effective approach for using DESs to enhance the oral bioavailability of active substances with low water solubility.
