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伊潘立酮片剂的制备

         

摘要

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.%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.

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