目的 优化广 藿 香油胃漂浮缓释微粒(Gastro-floating sustained release particles of patchouli oil，PO-GFSRP)的缓释材料处方，并初步评价制剂质量。方法 采用挤出-滚圆法制备了胃漂浮缓释微粒。以PO体外累积释放率为考察指标，对主要缓释材料种类、含量及不同缓释材料间比例进行单因素考察，结合星点设计-效应面法优化缓释材料处方，考察缓释材料乙基纤维素(EC)和羧丙甲基纤维素(HPMC)总量及其质量比对PO累积释放率的影响;通过PO-GFSRP物理性质、体外8 h漂浮率、体外释放度以及加速稳定性实验进行制剂质量的初步评价。结果 优化的缓释材料处方为EC 22。5％、HPMC 27。5％;PO-GFSRP 的收率 72。70％、休止角 37。63 °、松密度 0。60 g/mL、脆碎度 0。84％、体外 8 h 漂浮率87。67％;12 h PO累积释放率达到96％以上;在温度25℃、相对湿度60％条件下6个月药物损失量在10％以内。结论 基于EC/HPMC缓释材料的PO-GFSRP具有良好的缓释效果，PO累积释放率及微粒漂浮性能良好。
Formulation optimization and Preparation evaluation for Gastro-floating sustained re-lease particles of Pachouli oil
Objective To optimize the formulation for gastro-floating sustained release particles of Pachouli oil(PO-GFSRP),and to primarily evaluate their quality.Methods The PO-GFSRP were fabricated by the extrusion-spheronization method.The type,ratio and total amount of sustained-release polymers in formulation were screened by single factor experiments using in vitro drug release as the index.Furthermore,the central composite design-response surface methodology was adopted to optimize the ratio and total amount of ethyl celulose(EC)and hydroxypropyl methyl cellulose(HPMC)according to their influences on accu-mulative drug release.The obtained microparticles were evaluated on their physiochemical properties,in vitro floating rate at 8h and drug release,accelerate stabilitys.Results The optimized formulation contained 22.5％EC and 27.5％HPMC as sustained-release materials.The yield,repose angle,bulk density,friability and floating rate of particles were 72.70％,37.63°,0.60 g·mL-1,0.84％and 87.67％respectively.The particles released over 96％PO after 12 hours,and drug loss was within 10％after storage for 6 months at 25 ℃ and 60％relative humidity.Conclusion PO-GFSRP showed a preferable sustained-re-lease pattern with acceptable release and floating rates.
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