Affiliations: [a] Chongqing Academy of Chinese Materia Medica, Chongqing, China | [b] Chongqing Centre for Drug Evaluation and Certification, Chongqing, China
Correspondence:
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Corresponding author: Yong Yang, Chongqing Academy of Chinese Materia Medica, No. 34 of Nanshan Street, Nan’an District, Chongqing 400065, China. Tel.: +86 23 89029198; Fax: +86 23 89029008; E-mail: yangyong_259@163.com.
Note: [1] These authors contributed equally to this study.
Abstract: OBJECTIVE: In this study we explore the method to prepare tanshinone self-microemulsifying sustained-release microcapsules using tanshinone self-microemulsion as the core material, and chitosan and alginate as capsule materials. METHODS: The optimal preparation technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules was determined by using the orthogonal design experiment and single-factor analysis. The drug loading and entrapment rate were used as evaluation indexes to assess the quality of the drug, and the in vitro release rate was used to evaluate the drug release performance. RESULTS: The best technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules is as follows: the concentration of alginate is 1.5%, the ratio of tanshinone self-microemulsion volume to alginate volume to chitosan mass is 1:1:0.5 (ml: ml: g), and the best concentration of calcium chloride is 2.0%. To prepare the microcapsules using this technology, the drug loading will be 0.046%, the entrapment rate will be 80.23%, and the 24-hour in vitro cumulative release rate will be 97.4%. CONCLUSION: The release of the microcapsules conforms to the Higuchi equation and the first-order drug release model and has a good sustained-release performance.
Keywords: Tanshinone, chitosan-alginate, self-microemulsifying sustained-release microcapsules, preparation, in vitro release
