In vitro and in vivo evaluation of three metronidazole topical products.
Two 1% and one 0.75% metronidazole cream products were approved as bioequivalent products. These products were evaluated for their in vivo cutaneous penetration characteristics by dermatopharmacokinetic (DPK) and dermal microdialysis (DMD) sampling methodologies. The same three products were also evaluated for their rheological and in vitro drug release (IVR) properties. Structural differences were observed in the resulting flow curves. However, similar IVR profiles were obtained for the two topical semisolid dosage forms containing 1% metronidazole. For the lower strength product, a higher IVR rate was associated with the lower DPK profile. All three products exhibited similar values of area under the curve when investigated by DMD. This in vitro evaluation corroborated the divergent penetration characteristics found using in vivo methodologies.
Department of Pharmaceutical Physics and Informatics .
Dalia Simona
DS
Miron
Flavian Stefan
FS
Rădulescu
Eva
E
Benfeldt
Vinod P
VP
Shah
Victor A
VA
Voicu
D000279:Administration, Cutaneous; D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D008795:Metronidazole / Q000008:administration & dosage / Q000493:pharmacokinetics*; D014677:Pharmaceutical Vehicles / Q000737:chemistry / Q000378:metabolism; D012212:Rheology; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption
D000890:Anti-Infective Agents; D014677:Pharmaceutical Vehicles; D008795:Metronidazole