Comparison of the Dissolution Rate of Ceftriaxone Sodium Preparations for Injection

Abstract

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.Key words dissolution rate; near-infrared spectroscopy; X-ray diffraction; differential scanning calorimetry; generic drug; powder property Dissolution properties are important in the formulation design of pharmaceutical preparations, and improvement in dissolution rate is a critical issue in drug development for nonparenteral preparations. There are a number of mathematical models for dissolution profile.

PBPK modelling of ceftriaxone Na-loaded starch-sodium alginate polymeric blend prepared by water-in-oil emulsification for oral delivery

“…Thermal analysis of sodium alginate indicates that 1st endothermic peak at approximately 100 °C was due to the evaporation of moisture (figure 2(a)). The second and third exothermic peaks at 238.1 °C and 368.3 °C to 394.8 °C belong to the degradation of the biopolymer and the formation of the corresponding carbonates (Devi & Kakati, 2013) [36]. DSC curve of pure starch is demonstrated in figure 2(b) where the first endothermic peak at around 27.21 °C is attributed to moisture discharge, then weight loss (25 to 50% of the original weight) occurs in the second step within the temperature range of 317.26 °C to 331.35 °C, which is an indicator of the start of starch decomposition.…”

“…The endothermic peak at 335 °C was attributed to the polymorphism and melting of ceftriaxone sodium. Additionally, this matrix remained stable up to 534 °C with a total loss of weight of approximately 73.6% (Devi & Kakati, 2013; Fontes et al, 2013) [31,36].…”