Department of Pharmaceutical Physics and Informatics .
Pharm Dev Technol. 2014 Mar;19(2):194-9. doi: 10.3109/10837450.2013.763265. Epub 2013 Jan 30.
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.
两种 1%和一种 0.75%甲硝唑乳膏产品被批准为生物等效产品。这些产品通过皮肤药代动力学（DPK）和皮肤微透析（DMD）采样方法学来评估其体内皮肤穿透特性。这三种产品还评估了其流变学和体外药物释放（IVR）特性。在得到的流动曲线中观察到了结构差异。然而，含有 1%甲硝唑的两种局部半固体制剂得到了相似的 IVR 曲线。对于低强度产品，更高的 IVR 速率与更低的 DPK 曲线相关。当通过 DMD 进行研究时，所有三种产品的曲线下面积值均相似。这种体外评估证实了使用体内方法学发现的不同的穿透特性。
