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Open AccessArticle

Development and In Vitro-In Vivo Evaluation of a Novel Sustained-Release Loxoprofen Pellet with Double Coating Layer

1
College of Pharmacy, China Pharmaceutical University, No. 639 Longmian Road, Nanjing 211100, China
2
College of Pharmacy, China Pharmaceutical University, Xuanwumen Campus, No. 24 Tongjiaxiang, Nanjing 210009, China
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(6), 260; https://doi.org/10.3390/pharmaceutics11060260
Received: 7 May 2019 / Revised: 28 May 2019 / Accepted: 3 June 2019 / Published: 5 June 2019
This study aimed to develop a novel sustained release pellet of loxoprofen sodium (LXP) by coating a dissolution-rate controlling sub-layer containing hydroxypropyl methyl cellulose (HPMC) and citric acid, and a second diffusion-rate controlling layer containing aqueous dispersion of ethyl cellulose (ADEC) on the surface of a LXP conventional pellet, and to compare its performance in vivo with an immediate release tablet (Loxinon®). A three-level, three-factor Box-Behnken design and the response surface model (RSM) were used to investigate and optimize the effects of the citric acid content in the sub-layer, the sub-layer coating level, and the outer ADEC coating level on the in vitro release profiles of LXP sustained release pellets. The pharmacokinetic studies of the optimal sustained release pellets were performed in fasted beagle dogs using an immediate release tablet as a reference. The results illustrated that both the citric acid (CA) and ADEC as the dissolution- and diffusion-rate controlling materials significantly decreased the drug release rate. The optimal formulation showed a pH-independent drug release in media at pH above 4.5 and a slightly slow release in acid medium. The pharmacokinetic studies revealed that a more stable and prolonged plasma drug concentration profile of the optimal pellets was achieved, with a relative bioavaibility of 87.16% compared with the conventional tablets. This article provided a novel concept of two-step control of the release rate of LXP, which showed a sustained release both in vitro and in vivo. View Full-Text
Keywords: sustained release pellets; double coating layer; loxoprofen; citric acid; pharmacokinetic studies sustained release pellets; double coating layer; loxoprofen; citric acid; pharmacokinetic studies
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MDPI and ACS Style

Wan, D.; Zhao, M.; Zhang, J.; Luan, L. Development and In Vitro-In Vivo Evaluation of a Novel Sustained-Release Loxoprofen Pellet with Double Coating Layer. Pharmaceutics 2019, 11, 260.

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