Biowaiver extension potential and IVIVC for BCS class II drugs by formulation design: Case study for cyclosporine self-microemulsifying formulation

Su Geun Yang

doi:10.1007/s12272-010-1116-2

Biowaiver extension potential and IVIVC for BCS class II drugs by formulation design: Case study for cyclosporine self-microemulsifying formulation

Su Geun Yang

Research output: Contribution to journal › Article › peer-review

33 Scopus citations

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 AUC_0→24h, C_max and T_max, 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.

Original language	English
Pages (from-to)	1835-1842
Number of pages	8
Journal	Archives of Pharmacal Research
Volume	33
Issue number	11
DOIs	https://doi.org/10.1007/s12272-010-1116-2
State	Published - Dec 2010

Bibliographical note

Funding Information:
This work was supported by the Korea Research Foundation Grant funded by the Korean Government (MOEHRD, KRF-2006-214-E00039), and International R&D Center START-UP FUND Program funded by Incheon Free Economic Zone Authority(IFEZA) and Ministry of Knowledge and Economy (MKE).

Keywords

Biopharmaceutics classification system (BCS)
Biowaiver
Cyclosporine
In vitro-in vivo correlation (IVIVC)
Self-microemulsifying drug delivery systems (SMEDDS)

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10.1007/s12272-010-1116-2

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title = "Biowaiver extension potential and IVIVC for BCS class II drugs by formulation design: Case study for cyclosporine self-microemulsifying formulation",

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.",

keywords = "Biopharmaceutics classification system (BCS), Biowaiver, Cyclosporine, In vitro-in vivo correlation (IVIVC), Self-microemulsifying drug delivery systems (SMEDDS)",

author = "Yang, {Su Geun}",

note = "Funding Information: This work was supported by the Korea Research Foundation Grant funded by the Korean Government (MOEHRD, KRF-2006-214-E00039), and International R&D Center START-UP FUND Program funded by Incheon Free Economic Zone Authority(IFEZA) and Ministry of Knowledge and Economy (MKE).",

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AB - 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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Biowaiver extension potential and IVIVC for BCS class II drugs by formulation design: Case study for cyclosporine self-microemulsifying formulation

Abstract

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Keywords

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