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目的采用小型离心造粒技术制备尼群地平固体分散体微丸。方法以微丸的粉体学性质、收率(Yield)和10min药物累积溶出量(P10)为评价标准,通过处方单因素试验考察可溶性载体、不溶性载体及两者的比例对微丸质量的影响;通过制备工艺单因素试验,考察润湿剂中乙醇的浓度及用量、离心造粒转速及时间对微丸质量的影响;并通过X射线粉末衍射(XRD)和差示扫描量热法(DSC)试验对药物的可能存在状态进行判断。结果尼群地平固体分散体微丸的处方与制备工艺为:可溶性载体采用泊洛沙姆(F68),不溶性载体采用低取代羟丙基纤维素(L-HPC),两者的比例为2:7,润湿剂为70%乙醇,用量25ml,离心造粒转速为300r/min,时间30min,所得微丸P10达86%以上。XRD和DSC实验表明,药物以无定形存在于固体分散体中,但在微丸中有少量晶体析出。结论采用上述方法制备的尼群地平固体分散体微丸,具有固体分散体结构和显著的速释特征。
OBJECTIVE To prepare nitrendipine solid dispersion pellets by small centrifugal granulation technology. Methods The pellet properties, yield and 10min cumulative dissolution (P10) of the pellets were used as the evaluation criteria. The effects of soluble carrier, insoluble carrier and their ratio on pellet quality were investigated by single factor test The effects of ethanol concentration and dosage in wetting agent, centrifugal granulation speed and time on pellet quality were investigated by single factor test of preparation process. The effects of ethanol concentration and dosage on the quality of pellets were investigated by X-ray powder diffraction (XRD) and differential scanning calorimetry ) Test to determine the possible state of the drug. Results The formulation and preparation of nitrendipine solid dispersion pellets were as follows: the soluble carrier was poloxamer (F68), the insoluble carrier was low-substituted hydroxypropyl cellulose (L-HPC), the ratio of the two was 2: 7, wetting agent is 70% ethanol, dosage 25ml, centrifugal granulation speed 300r / min, time 30min, the resulting pellets P10 up to 86%. XRD and DSC experiments showed that the drug was present as amorphous in the solid dispersion, but a small amount of crystals were precipitated in the pellets. Conclusion The nitrendipine solid dispersion pellets prepared by the above method have the characteristics of solid dispersion structure and significant immediate release.