青蒿素缓释固体分散物的制备及体外溶出研究

Study on the Preparation and Dissolution of the Sustained Release Solid Dispersions of Artemisinin

目的：研制青蒿素缓释固体分散物，提高其制剂的生物利用度。方法：采用固体分散技术制备青蒿素缓释固体分散物，对其进行体外溶出实验，并采用Ｘ－射线衍射方法进行固体分散物的物相分析。结果：固体分散物体外溶出速率随着溶出介质ｐＨ值的增大而明显加快，体外溶出时间明显延长，体外溶出度显著增加，达到原药的５倍以上。固体分散物Ｘ－射线衍射图谱表明，青蒿素以非晶体状态存在；在ＲＨ７５％４０℃条件下放置３个月后，固体分散物Ｘ－射线衍射图谱和体外溶出速率均无明显变化。结论：青蒿素缓释固体分散物稳定，具有增加其制剂生物利用度的作用。

Aim In order to increase bioavailability of Artemisinin'S dosage form, solid dispersion of Artemisinin was prepared.Methods Solid dispersion of Artemisinin was prepared, the dissolution rate was detected. X-ray powder diffraction was used to investigate the nature of the studied forms.Results The results show the drug of solid dispersion existed in amorphous form; when the solid dispersion was exposed to an atmosphere of 75% relative humidity for 3 months at 40℃,dissolution rate and existing state of solid dispersion did not alter much; the dissolution rates and the dissolution release time of dispersion was obviously increased than those of the pure drug.Conclusion Solid dispersion of Artemisinin was stable and could increase bioavailability of Artemisinin'S dosage form.