Abstract
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.
Keywords
Full Text:
References
Clewell A, Hirka G, Glavits R, Palmer PA, Endres JR, Murbach TS, et al. . A 90-day oral toxicological evaluation of the methylurate purine alkaloid theacrine. J Toxicol. (2016) 2016:6206859. doi:10.1155/2016/6206859.
Zheng XQ, Ye CX, Kato M, Crozier A, Ashihara H. Theacrine (1,3,7,9-tetramethyluric acid) synthesis in leaves of a Chinese tea, kucha (Camellia assamica var. kucha). Phytochemistry. 2002 May;60(2):129-34. doi: 10.1016/s0031-9422(02)00086-9. [PubMed]
Cappelletti S, Piacentino D, Sani G, Aromatario M. Caffeine: cognitive and physical performance enhancer or psychoactive drug? Curr Neuropharmacol. 2015 Jan;13(1):71-88. doi: 10.2174/1570159X13666141210215655. Erratum in: Curr Neuropharmacol. 2015;13(4):554. Daria, Piacentino [corrected to Piacentino, Daria].
Qiao H, Ye X, Bai X, He J, Li T, Zhang J, Zhang W, Xu J. Theacrine: A purine alkaloid from Camellia assamica var. kucha with a hypnotic property via the adenosine system. Neurosci Lett. 2017 Oct 17;659:48-53. doi: 10.1016/j.neulet.2017.08.063.
Xu JK, Kurihara H, Zhao L, Yao XS. Theacrine, a special purine alkaloid with sedative and hypnotic properties from Cammelia assamica var. kucha in mice. J Asian Nat Prod Res. 2007 Sep-Dec;9(6-8):665-72. doi: 10.1080/10286020601103155.
Wang GE, Li YF, Zhai YJ, Gong L, Tian JY, Hong M, Yao N, Wu YP, Kurihara H, He RR. Theacrine protects against nonalcoholic fatty liver disease by regulating acylcarnitine metabolism. Metabolism. 2018 Aug;85:227-239. doi: 10.1016/j.metabol.2018.04.011.
Li WX, Li YF, Zhai YJ, Chen WM, Kurihara H, He RR. Theacrine, a purine alkaloid obtained from Camellia assamica var. kucha, attenuates restraint stress-provoked liver damage in mice. J Agric Food Chem. 2013 Jul 3;61(26):6328-35. doi: 10.1021/jf400982c.
Wang Y, Yang X, Zheng X, Li J, Ye C, Song X. Theacrine, a purine alkaloid with anti-inflammatory and analgesic activities. Fitoterapia. 2010 Sep;81(6):627-31. doi: 10.1016/j.fitote.2010.03.008.
Gao M, Zheng J, Zheng C, Huang Z, Huang Q. Theacrine alleviates chronic inflammation by enhancing TGF-?-mediated shifts via TGF-?/SMAD pathway in Freund's incomplete adjuvant-induced rats. Biochem Biophys Res Commun. 2020 Feb 12;522(3):743-748. doi: 10.1016/j.bbrc.2019.11.126.
Sheng YY, Xiang J, Wang ZS, Jin J, Wang YQ, Li QS, Li D, Fang ZT, Lu JL, Ye JH, Liang YR, Zheng XQ. Theacrine From Camellia kucha and Its Health Beneficial Effects. Front Nutr. 2020 Dec 17;7:596823. doi: 10.3389/fnut.2020.596823.
Ko JH, Yang MH, Baek SH, Nam D, Jung SH, Ahn KS. Theacrine attenuates epithelial mesenchymal transition in human breast cancer MDA-MB-231 cells. Phytother Res. 2019 Jul;33(7):1934-1942. doi: 10.1002/ptr.6389.
Nardi-Ricart A, Nofrerias-Roig I, Suñé-Pou M, Pérez-Lozano P, Miñarro-Carmona M, García-Montoya E, Ticó-Grau JR, Insa Boronat R, Suñé-Negre JM. Formulation of Sustained Release Hydrophilic Matrix Tablets of Tolcapone with the Application of Sedem Diagram: Influence of Tolcapone's Particle Size on Sustained Release. Pharmaceutics. 2020 Jul 17;12(7):674. doi: 10.3390/pharmaceutics12070674.
Liu C, Li J, Li K, Xie C, Liu J. Oxidized konjac glucomannan-cassava starch and sucrose esters as novel excipients for sustained-release matrix tablets. Int J Biol Macromol. 2020 Aug 1;156:1045-1052. doi: 10.1016/j.ijbiomac.2019.11.146. [PubMed]
Mathur V, Nagpal K, Singh SK, Mishra DN. Comparative release profile of sustained release matrix tablets of verapamil HCl. Int J Pharm Investig. 2013 Jan;3(1):60-5. doi: 10.4103/2230-973X.108965.
Malakar J, Das K, Nayak AK. In situ cross-linked matrix tablets for sustained salbutamol sulfate release - formulation development by statistical optimization. Polim Med. 2014 Oct-Dec;44(4):221-30.
Lu Jiang, Dandan Chen, Minjie Sun, Qineng Ping, Can Zhang. Advances of wax matrix tablets. Journal of China Pharmaceutical University. 2016;47(04):497-502.
Kaleemullah M, Jiyauddin K, Thiban E, Rasha S, Al-Dhalli S, Budiasih S, Gamal OE, Fadli A, Eddy Y. Development and evaluation of Ketoprofen sustained release matrix tablet using Hibiscus rosa-sinensis leaves mucilage. Saudi Pharm J. 2017 Jul;25(5):770-779. doi: 10.1016/j.jsps.2016.10.006.
Udeni Gunathilake TMS, Ching YC, Chuah CH. Enhancement of Curcumin Bioavailability Using Nanocellulose Reinforced Chitosan Hydrogel. Polymers (Basel). 2017 Feb 15;9(2):64. doi: 10.3390/polym9020064.
Yan G, Sun W, Pei Y, Yang Z, Wang X, Sun Y, Yang S, Pan J. A novel release kinetics evaluation of Chinese compound medicine: Application of the xCELLigence RTCA system to determine the release characteristics of Sedum sarmentosum compound sustained-release pellets. Saudi Pharm J. 2018 Mar;26(3):445-451. doi: 10.1016/j.jsps.2017.07.007.
Yin JQ, Wang WJ, Xu XL, Li HX, Cong MY, Zhao X, et al. Preparation, characterization and pharmacokinetics of extended-release tablets of marine polysaccharide drug. Journal of Drug Delivery Science and Technology. 2018;43:353-61.
Refbacks
- There are currently no refbacks.
Copyright (c) 2021 Journal of Pharmaceutical and Biomedical Sciences
This work is licensed under a Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.