Biowaiver extension potential and IVIVC for BCS Class II drugs by formulation design: Case study for cyclosporine self-microemulsifying formulation |
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Authors: | Su-Geun Yang |
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Institution: | (1) Pre-clinical Research Department, Chugai Pharmaceutical Co. Ltd., 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan;(2) Faculty of Pharmaceutical Sciences, Setsunan University, 45-1 Nagaotoge-cho, Hirakata, Osaka 573-0101, Japan;(3) Present address: Global Research & Development, Nagoya Laboratories, Pharmaceutical Sciences, Science & Technology, Pharmaceutical R&D, Pfizer Inc, 5-2 Taketoyo, Aichi 470-2393, Japan |
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Abstract: | The objective of this work was to suggest the biowaiver potential of biopharmaceutical classification system (BCS) Class II
drugs in self-microemulsifying drug delivery systems (SMEDDS) which are known to increase the solubility, dissolution and
oral absorption of water-insoluble drugs. Cyclosporine was selected as a representative BCS Class II drug. New generic candidate
of cyclosporine SMEDDS (test) was applied for the study with brand SMEDDS (reference I) and cyclosporine self-emulsifying
drug delivery systems (SEDDS, reference II). Solubility and dissolution of cyclosporine from SMEDDS were critically enhanced,
which were the similar behaviors with BCS class I drug. The test showed the identical dissolution rate and the equivalent
bioavailability (0.34, 0.42 and 0.68 of p values for AUC0→24h, Cmax and Tmax, respectively) with the reference I. Based on the results, level A in vitro-in vivo correlation (IVIVC) was established from these two SMEDDS formulations. This study serves as a good example for speculating
the biowaiver extension potential of BCS Class II drugs specifically in solubilizing formulation such as SMEDDS. |
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