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采用o/w型乳化-溶剂挥发法制备了洛伐他汀聚乳酸微球。优化后微球的平均粒径为(2.54±0.37)μm,粒度分布较窄,包封率为(90.93±0.94)%。SEM观察表明制品外观形态较圆整、平滑,红外和X射线衍射分析提示药物的化学结构未发生改变,但结晶衍射峰消失,药物可能以无定形状态分布于微球中。体外释放试验显示药物释放重现性良好。大鼠体内试验表明,肌注洛伐他汀微球与口服市售片剂相比,cmax由(15.8±0.8)ng/ml提高到(21.7±1.0)ng/ml,tmax由(1.7±0.1)h延长为(91.5±3.0)h,且t1/2、AUC0→∞和MRT均显著增加(P<0.05),说明自制微球肌注能够延长药物在大鼠体内的滞留时间,改善药物的吸收。
Lovastatin polylactic acid microspheres were prepared by o / w emulsion-solvent evaporation method. The average diameter of the microspheres was (2.54 ± 0.37) μm. The particle size distribution was narrow and the entrapment efficiency was (90.93 ± 0.94)%. The SEM observation showed that the appearance of the product was round and smooth. The infrared and X-ray diffraction analysis showed that the chemical structure of the drug did not change, but the crystal diffraction peak disappeared and the drug could be distributed in the amorphous state in the microsphere. In vitro release tests showed good reproducibility of drug release. Rat in vivo tests showed that cmax increased from (15.8 ± 0.8) ng / ml to (21.7 ± 1.0) ng / ml vs (1.7 ± 0.1) ng / ml vs h prolonged to (91.5 ± 3.0) h, and t1 / 2, AUC0 → ∞ and MRT increased significantly (P <0.05), indicating that homemade microspheres intramuscular injection can prolong drug residence time in rats to improve drug absorption .