Comparison of the Dissolution Rate of Ceftriaxone Sodium Preparations for Injection

摘要

This study aimed to compare the dissolution rate of eight different formulations of ceftriaxone sodium preparation for injection, the original product and seven generic versions. The dissolution time was measured precisely as the point at which the freeze-dried ceftriaxone sodium preparation became a transparent solution on the addition of 0.9% sodium chloride solution. To investigate whether differences in the crystalline structure may explain the differences in dissolution rates, the eight products were subjected to X-ray diffraction (XRD) and differential scanning calorimetry (DSC). Powder surface characteristics were examined, including surface area, amount of water adsorbed, water interactions and morphology. The measurement of near-infrared spectroscopy of powder preparations was conducted, and we predicted dissolution time by partial least squares (PLS). The dissolution time of the eight products were different. There were no differences in XRD and DSC findings between the original and generic products, surface characteristics, i.e. , surface area, morphology etc. , were different between preparations. On near-infrared (NIR) spectroscopy, a good relationship was demonstrated between the actual and predicted dissolution time for each ceftriaxone preparation. The difference in dissolution time between the eight products was due to differences in powder surface characteristics, such as water interaction and crystal shape. Finally, it was shown that the dissolution rates of the products could be predicted by NIR analysis.