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| Preparation and in vitro evaluation of berberrubine solid dispersion |
| Hits 1660 Download times 897 Received:June 10, 2019 |
| View Full Text View/Add Comment Download reader |
| DOI
10.11656/j.issn.1673-9043.2019.05.21 |
| Key Words
hot-melt extrusion;berberrubine;solid dispersion;in vitro release behavior |
| Author Name | Affiliation | E-mail | | MA Li | Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-Established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | | LI Xiyue | Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-Established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | | LIANG Chunxia | Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-Established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | | ZHANG Bing | Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-Established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | | LIU Jingjing | Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-Established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | | QI Dongli | Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-Established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | qidongli2013@163.com | | LIU Zhidong | Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-Established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | lonerliuzd@163.com |
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| Abstract
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| [Objective] To prepare a solid dispersion of the sparingly soluble drug berberrubine by hot melt extrusion to increase its solubility and delay its in vitro release behavior.[Methods] A solid dispersion of berberrubine was prepared by homo twin-screw extrusion using Soluplus® as the carrier. The prepared solid dispersion was characterized by differential scanning calorimetry (DSC) analysis,powder X-ray diffraction (XRD) analysis, scanning electron microscopy (SEM) observation and Fourier transform infrared spectroscopy (FT-IR) analysis. The solubility and in vitro dissolution of the solid dispersion were investigated in different media.[Results] The results of DSC and XRD analysis showed that the main characteristic peaks of berberrubine in the solid dispersion weakened or even partially disappeared,and the SEM results showed that the solid dispersion was irregular. The FT-IR results indicate that there is hydrogen bonding between the berberrubine and Soluplus®. The prepared solid dispersion of berberrubine had a solubility of 2.59 times that of the drug substance in a phosphate buffer of pH 6.8. The results of dissolution in vitro showed that berberrubine solid dispersion had an obvious sustained release effect.[Conclusion] The solid dispersion of berberrubine was successfully prepared,and its solubility was significantly improved,and its release behavior in vitro was delayed. |
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