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 Cmax decreased, and the tmax 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.
Keywords: Binder, In vivo pharmacokinetics, Pore-former, Sustained-release pellets, Topiramate.
Current Drug Delivery
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 Cmax decreased, and the tmax 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.
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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
DOI https://dx.doi.org/10.2174/1567201813666151113122433 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
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