Physico-chemical product effects on the behavior of clotrimazole vaginal tablets

Objective In addition to the nature and level of the active material for treating fungal vaginal conditions, the physico-chemical properties and other ingredients in the formulation are also important factors in determining the product performance. Two vaginal tablets (CanestenGYN 3-Tage Kombi and KadeFungin3 Kombi) each containing 200mg Clotrimazole have been compared for surface roughness and dissolution behavior, to help better understand their reported in-vitro anti-fungal activity.

Materials/methods Surface roughness of the tablets was performed using scanning electron microscopy (SEM, FEI Quanta 250 FEG Microscope equipped with a SDD Brucker detector) and optical profilometry (Sensofar Neox 3D optical profilometer). Clotrimazole release rate during dissolution was measured in a pH4.5 buffered acetate solution over up to 6 hours (temperature of 37°C±0.5°C).

Results SEM observations show that tablets surface both show roughness on the micron scale. Specifically on KadeFungin®​3, there was an agglomeration of grains (plates) to form larger structures. Optical profilometry highlighted a significant difference in the Sa (average surface roughness) and Sz (maximum height of features) between the samples, with CanestenGYN having the smoother surface (Sa – 1.7µm±0.1µm vs 2.2µm±0.1µm, Sz – 37.4µm±2.5µm vs 45.0µm±1.9µm). Clotrimazole was released at faster rates from the CanestenGYN tablet vs Kadefungin3 (99% release vs 70% release at 10 mins).

Summary Significant differences were demonstrated between the test products in terms of surface roughness and dissolution characteristics. CanestenGYN had a smoother surface texture and showed faster release of Clotrimazole during dissolution.

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Artikel online veröffentlicht:
11. Oktober 2022