Preparation and In Vivo Pharmacokinetics of the Tongshu Suppository

Abstract EN

Astragalus polysaccharide (APS) (used for intestinal protection) was added to formulate the Tongshu suppository to improve the pharmacokinetics of Aceclofenac, which were assessed in New Zealand rabbits using an orthogonal experimental design.

The single-agent Aceclofenac was taken as the control formulation.

The concentration-time and drug release curves were drawn, and Tmax (min), Cmax (μg·mL−1), AUC0→∞, and MRT were compared using a pharmacokinetic systems program.

The formulated Tongshu suppository had moderate hardness, a smooth surface with uniform color, and theoretical drug-loading rate of 8%.

Its release rate was in accordance with the drug preparation requirements.

The concentration-time curves and drug release curves revealed that the maximum concentrations (Cmax) were 4.18±1.03 μg·mL−1 and 3.34±0.41 μg·mL−1 for the Tongshu and Aceclofenac suppositories, respectively, showing statistically insignificant difference, while the peak times were 34.87±4.69 min and 34.76±6.34 min, respectively, also showing statistically insignificant difference.

Compared with the Aceclofenac suppository, the relative bioavailability of the Tongshu suppository was 104.4%, and the difference between them was statistically insignificant.

In this experiment, the Tongshu suppository was prepared using the hot-melt method.

In vivo pharmacokinetic studies confirmed it had higher bioavailability than the Aceclofenac suppository.