硫酸吗啡口腔崩解片的制备及处方工艺研究

Study on Preparation and Formulation Technology of Morphine Sulfate Oral Disintegrating Tablets

目的:制备硫酸吗啡口腔崩解片,优化其处方工艺条件。方法:采用直接压片法制备硫酸吗啡口腔崩解片,以崩解时间和口感为指标采用单因素试验法筛选片剂硬度、硬脂酸镁用量、甜菊苷用量范围等,再以崩解时限为指标采用星点设计法优化微晶纤维素(SMCC)、交联羧甲基纤维素钠(CCMC-Na)、甜菊苷用量,并对最优处方所制制剂进行验证。结果:最优处方组成为(片质量60 mg):硫酸吗啡16.67%、SMCC 35.77%、CCMC-Na 8.94%、甜菊苷2.85%、硬脂酸镁1%、甘露醇34.77%。所制口腔崩解片硬度为3 kg,能在12 s内完全崩解,且味微甜、口感良好。结论:该制剂制备方法简便、可行。

OBJECTIVE： To prepare Morphine sulfate oral disintegrating tablets, and to optimize its formulation technology. METHODS： Morphine sulfate oral disintegrating tablet was prepared with direct compression process. The solidity of tablet, the amount of magnesium stearate and the amount range of stevioside were screened with single factor test using disintegration time and taste as index. The amounts of SMCC, CCMC-Na and stevioside were optimized by central composite design using disintegration time as index. The preparation prepared by optimized formulation was validated. RESULTS： The optimal formulation （60 mg/tablet） was as follows： morphine sulfate 16.67%, SMCC 35.77%, CCMC-Na 8.94%, stevia glycosides 2.85%, magnesium stearate 1%, manmitol 34.77%. The prepared tablets were 3 kg in solidity, and disintegrated completely within 12 s, with desirable taste and a little sweet. CONCLUSIONS： The preparation method is simple and feasible.