ABSTRACT
Objective: To prepare the sustained-release solid dispersion of tripterin (SRSDT) with the intention of improving drug dissolution, meanwhile, the drug release was slowed down so as to make the toxicity diminished. Methods: SRSDT was prepared by the solvent method with colloidal silica dioxide (CSD) as carrier. The physical characteristics and in vitro release rate were further evaluated. Results: The ideal SRSDT was prepared by mixing tripterin and colloidal silica dioxide with the weight ratio of 1:12; The release rate of drug could keep moderate and controllable. In vitro cumulative release of SRSDT was up to more than 90% after 8 h. The results of differential scanning calorimetry, scanning electron microscopy, and X-ray powder diffraction could prove that the tripterin existed as amorphous form in the carrier. Conclusion: The SRSDT carried by CSD could control the release rate of drug and keep moderate and controllable, and the preparation process is simple, which has potential applications.
ABSTRACT
Objective: To prepare the Tripterin Sustained-release Dropping Pills (TSRDPs), investigate the disperse state and in vitro release, and optimize the preparation technology. Methods: The TSRDPs were prepared by solid dispersion method with PEG 4000 and glycerol monostearate (GM) as carrier materials. Orthogonal design was conducted to explore the influencing factors of the preparation technology by evaluating the indexes of roundness and weight difference. Results: The ideal condition of TSRDPs: the ratio of tripterin-GM-PEG 4000 was 1:3:7; the temperature of drug mixture was 80 °C; dropping speed was 20 d/min; dropping distance was 5 cm; and the condensate temperature was 15 °C. Tripterin existed as amorphous state in carriers. The maximum cumulative release amount of tripterin was 91.2% at 12 h. Conclusion: The prepared TSRDPs have a good sustained-release effect.