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KMID : 1146920230530020323
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Journal of Pharmaceutical Investigation
2023 Volume.53 No. 2 p.323 ~ p.331
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Formulation development and pharmacokinetic evaluation of enteric-coated dexrabeprazole tablets
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Lee Tae-Jin
Kim Do-Hyun
Kim Jae-Cheon
Ro Si-Won
Na Dong-Hee
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Abstract
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Purpose : This study investigated the development of an enteric-coated tablet of dexrabeprazole, the R(+)-isomer of rabeprazole, and evaluated the stability and pharmacokinetic properties in beagle dogs.
Methods : The optimal alkaline excipient was investigated for stabilizing dexrabeprazole through drug-excipient compatibility test. The enteric-coated tablets were prepared comprising a core containing dexrabeprazole and the optimal stabilizer, an enteric-coat surface layer, and an intervening thin seal coat. Dissolution test of the enteric-coated dexrabeprazole tablets was performed in various buffer settings, and the dissolution pattern was compared with that of commercial rabeprazole tablets. The optimized dexrabeprazole tablet was characterized by accelerated stability testing for 6 months and pharmacokinetic study in beagle dogs.
Results : The enteric-coated dexrabeprazole tablets were successfully prepared using magnesium oxide as an alkaline stabilizer. In the dissolution study, all dexrabeprazole tablets exhibited delayed-drug-release properties; the optimal formulation indicated similar dissolution behavior to the commercial rabeprazole product. A dose-proportional pharmacokinetic profile was observed in beagle dogs for the optimized formulation, which achieved higher stability compared to the commercial rabeprazole, as proved by the 6-month accelerated stability testing.
Conclusion : The novel dexrabeprazole enteric-coated tablet that was developed showed superior stability and similar dissolution as the commercial rabeprazole product with dose-proportional pharmacokinetics. These findings suggest that the dexrabeprazole tablet has a high potential for commercialization.
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KEYWORD
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Dexrabeprazole, Enteric-coated tablet, Pharmacokinetics, Rabeprazole isomer, Stability
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