Preparation and evaluation of cefditoren bioadhesive sustained-release dry suspension in vitro and in vivo studies

doi:10.5246/jcps.2026.01.004

Abstract

Abstract:

In the present study, cefditoren sodium (CT-Na), the sodium salt form of cefditoren (CT), was selected as the model compound, and cholestyramine resin was employed as the drug carrier to formulate CT-Na-resin complexes. The interaction mechanism between CT-Na and cholestyramine resin was elucidated using scanning electron microscopy (SEM), fourier-transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC). Bioadhesive, sustained-release microcapsules were subsequently developed via an emulsification–solvent evaporation technique. Comprehensive characterization of the formulation was conducted, with key quality indices systematically evaluated. Notably, the formulation exhibited minimal leakage (0.07%) after 7 d of storage and retained 94.59% of its drug content over a 6-month period. Pharmacokinetic studies comparing the CT-Na active pharmaceutical ingredient (API) solution and the self-developed dry suspension revealed a marked extension in drug release for the latter. The dry suspension displayed a delayed T_max (3 h vs. 2 h), an extended half-life (t_1/2) (12.44 h vs. 4 h), and a moderately reduced peak concentration (C_max) (3.99 μg/mL vs. 4.82 μg/mL), while achieving a significantly higher overall drug exposure (AUC_{0–24 h}: 50.868 μg·h/mL vs. 30.281 μg·h/mL). These findings indicated that relative to the API solution, the optimized dry suspension provided sustained drug release with improved bioavailability.

Key words: Cefditoren, Ion-exchange resin, Sustained-release dry suspension

Supporting:

Yuanrong Xin, Chi Zhang, Jintong Dai, Kailun Yang, Haibing He, Hongfei Liu. Preparation and evaluation of cefditoren bioadhesive sustained-release dry suspension in vitro and in vivo studies[J]. Journal of Chinese Pharmaceutical Sciences, 2026, 35(1): 54-70.

Figures/Tables 17

Table 1. Effects of different coating prescriptions on retention test and sustained-release weighted score of CT-Na–CM in isolated animals (n = 3).

Table 2. Similarity analysis of different coating prescriptions on the in vitro release of CT-Na–CM.

Table 3. Room temperature retention test data for self-made CT-Na dry suspension.

Table 4. Pharmacokinetic parameters of CT-Na API and self-prepared CT-Na bioadhesive sustained-release suspension (n = 6).

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