甲氧氯普胺口腔速溶膜剂的制备与体外评价

Preparation and in vitro Evaluation of Metoclopramide Oral Fast Dissolving Films

甲氧氯普胺是市场占有率较高的一类镇吐药,然而上市剂型少、顺应性差,难以契合呕吐患者的给药特点。本研究将甲氧氯普胺制成口腔速溶膜剂,有助于解决现有剂型的缺陷。通过正交设计和单因素考察法对甲氧氯普胺口腔速溶膜剂进行处方工艺研究,采用溶剂浇铸法制备甲氧氯普胺口腔速溶膜剂,并对最终制剂进行质量评价。结果表明,本处方工艺重现性高,所得制剂均匀稳定,口味良好,可以在(56±9)s内完全崩解,10 min左右完全溶出,有望成为1种前景良好的止吐制剂。

Metoclopramide is the antiemetic drug with high market share. However, the approved dosage form is not a better choice for patients with vomiting, resulting in poor drug compliance. In this study, metoclopramide was formulated in the oral fast dissolving film to overcome the dilemma of the existed preparations and increased the bioavailability. The formulation process of the films was studied by orthogonal design and single factor investigation. The solvent casting method was applied to preparing metoclopramide oral fast dissolving films, and the quality of the final preparation was evaluated. The results demonstrated that the films from the optimal formulations were uniform, stable and had good taste. Moreover, the films could be completely disintegrated within(56±9)s, and dissolved the drug in approximately 10 min, which was expected to be a promising antiemetic preparation.