Preparation, Characterization and in vivo Evaluation of Simple Monolithic Ethylcellulose-coated Pellets Containing Topiramate with Biphasic Release Characteristics

Title:Preparation, Characterization and in vivo Evaluation of Simple Monolithic Ethylcellulose-coated Pellets Containing Topiramate with Biphasic Release Characteristics

Volume: 13 Issue: 2

Author(s): Wei Gong, Yuli Wang, Shuai Shao, Si Xie, Li Shan, Meiyan Yang, Chunsheng Gao and Wu Zhong

Affiliation:

Keywords: Binder, In vivo pharmacokinetics, Pore-former, Sustained-release pellets, Topiramate.

Abstract: In our previous study, polyvinylpyrrolidone (PVP) was used both as a binder and a pore-former to prepare ethylcellulose (EC)-coated pellets to deliver topiramate (TPM) for a controlled release profile. The objective of this work was to further optimize the formulation and evaluate the in vivo profiles of TPM sustained-release pellets. Similar to the previous formulation with no binder, the in vitro drug release of TPM sustained-release pellets with 50% PVP binder in drug layer was sensitive to pore-former PVP level ranged from 27.0% to 29.0%. The higher the level of PVP was, the quicker release rate in vitro was. Moreover, when the proportion of poreformer PVP decreased, the C_max decreased, and the t_max and mean residence time of TPM coated pellets were both prolonged. The in vitro release profile of optimal formulation showed biphasic release characteristics similar to reference formulation Trokendi XR^®, i.e., involving immediate release of TPM in initial release stage followed by a sustained release up to 24 h. Moreover, the impact of the pH of release medium on the drug release rate of TPM sustained-release pellets was not significant. The release mechanism of TPM from the sustained-release pellets might be the interaction of diffusion (coating-film) and corrosion (drug layer). The in vivo pharmacokinetics results showed the TPM sustained-release pellets had the similar in vivo pattern compared with Trokendi XR^®. These studies provide valuable basis for further development of TPM sustained-release pellets.

Cite this article as:

Gong Wei, Wang Yuli, Shao Shuai, Xie Si, Shan Li, Yang Meiyan, Gao Chunsheng and Zhong Wu, Preparation, Characterization and in vivo Evaluation of Simple Monolithic Ethylcellulose-coated Pellets Containing Topiramate with Biphasic Release Characteristics, Current Drug Delivery 2016; 13 (2) . https://dx.doi.org/10.2174/1567201813666151113122433