伊潘立酮片剂的制备

Preparation of iloperidone tablets

目的:制备伊潘立酮片剂,对影响药物溶出度的处方和工艺进行考察。方法:以羟丙基甲基纤维为载体材料,采用固体分散体技术,以乳糖和微晶纤维素为填充剂,通过单因素考察法对处方进行优化;采用量热差示扫描和X-射线衍射法对片剂中伊潘立酮的存在形式进行鉴定。结果:优选处方为伊潘立酮3.243%、HPMC 6.486%、交联聚维酮11%(内加8%,外加3%)、乳糖52.314%、MCC 26.157%、硬脂酸镁0.5%和微粉硅胶0.3%;量热差示扫描和X-射线衍射结果显示,片剂中伊潘立酮以无定形或分子状态存在。结论:采用该方法可以制备出与市售片剂溶出度相似的伊潘立酮片剂。

Objective： To prepare and characterize the iloperidone tablets. Methods： Hydroxypropyl methyl cellulose （HPMC） was used as carrier of the solid dispersion, and lactose monohydrate and microcrystalline cellulose （MCC） as loading agents. The formulation was optimized via single factor tests. The differential scanning calorimeter （DSC） and powder X-ray diffractometry were used to identify the states of the drug existence in the product. Results： The optimized formulation was composed of 3. 243% iloperidone, 6. 486% HPMC, 11% crospovidone （PVPP, exterior addition 8% and interior addition 3% ） , 52. 314% lactose monohydrate, 26. 157% MCC, 0.5% magnesium stearate （MS） , and 0.3% colloidal silicon dioxide. Iloperidone existed in the product at amorphous forms or solvates according to DSC and X-ray diffractometry. Conclusion： The drug dissolution behavior of obtained iloperidone tablets is similar to commercial products.