Studies on Sustained Release Tablets of Theacrine with Erodible Matrix Material

Background Theacrine is a purine alkaloid with sedative, hypnotic and liver protection effects, which was investigated in treatment of insomnia, liver damage and hepatic steatosis. These are generally chronic diseases needing long-term medication. Sustained release preparations have good effect and compliance in prolonged treatment. Aim This study aimed to develop theacrine sustained release tablets using wax matrix material with simple preparing process. Methods: The content assay method of theacrine was developed using UV-visible spectrophotometry, and the method was fully validated. Wax matrix materials were used to prepare theacrine sustained release tablets by melting-granulation tableting process. The formulation was optimized by single-factor experiments with drug release behavior as evaluation index. The parameter f2 was used to compare the similarity of the drug release behavior of theacrine tablets prepared by different formulations. Weight variation and friability was also used to control the quality of theacrine tablets. Results The established UV analysis method had good specificity, linearity and precision. The results of single factor experiments showed that theacrine tablets of good sustained release effect were prepared with glycerol monostearate as matrix material and microcrystalline cellulose (MCC) as filler, and the ratio of glycerol monostearate to MCC was 1:2. The accumulative drug release percentage of theacrine sustained release tablets was 18.33% at 2 h and more than 95% within 12 h. Conclusion In this work, theacrine tablets were successfully prepared with wax matrix material and the tablets exerted a slow complete sustained release effect within 12 h without burst effect. The theacrine sustained release tablets were expected to be used as a long-acting preparation for chronic disease.