Skin penetration of topical formulations of ibuprofen 5%: an in vitro comparative study

Autor: Jonathan Hadgraft, P.H. Rosher, M. Whitefield
Rok vydání: 2002
Předmět:
Zdroj: Skin pharmacology and applied skin physiology. 16(3)
ISSN: 1422-2868
Popis: An in vitro isolated human skin technique with known reliable predictive value for in vivo performance was used to compare the skin penetration of the proprietary ibuprofen gel formulation, IbugelTM, with five other commercially available topical formulations containing ibuprofen 5%: IbusprayTM, IbumousseTM, Proflex CreamTM, Fenbid GelTM and Deep Relief GelTM. There was a marked difference between some formulations in the percentage of applied ibuprofen penetrating the skin samples, with IbusprayTM, IbugelTM and IbumousseTM showing the most efficient penetration. The percentage of applied ibuprofen penetrating the skin samples from these formulations was significantly greater (p < 0.05) at all sampling intervals when compared with Proflex CreamTM, Fenbid GelTM or Deep Relief GelTM. By 48 h, the percentage of applied ibuprofen that had penetrated through the skin samples from IbusprayTM, IbugelTM and IbumousseTM was approximately 2.5 times greater than that from Deep Relief GelTM, 3 times greater than that from Proflex CreamTM and 5 times greater than that from Fenbid GelTM. The data demonstrate that, with topically applied preparations, the composition of the vehicle can have a significant impact on the percutaneous penetration of the active medicament. The possible reasons for this are discussed in terms of partition and diffusion phenomena. Different topical presentations of the same drug substance – especially agents like ibuprofen which are intended for subcutaneous action – cannot be assumed to be pharmaceutically and clinically equivalent or indeed interchangeable.
Databáze: OpenAIRE