孟鲁司特钠口腔崩解片的制备及比格犬体内生物等效性研究

Preparation of Montelukast Sodium Orally Disintegrating Tablets and Study on the Bioequivalence in Beagle Dogs

目的制备孟鲁司特钠口腔崩解片,进行比格犬体内生物等效性研究。方法粉末直接压片法制备口腔崩解片,通过正交试验结果确定最优处方。采用HPLC-荧光检测法测定比格犬体内血药浓度。结果口腔崩解片的优化处方为孟鲁司特钠10.4 g,微晶纤维素60 g,交联聚维酮30 g,甘露醇15 g,硬脂酸镁2 g,微粉硅胶1 g,阿司帕坦1 g,香精0.6 g,制成1 000片。结论优化处方制备的口腔崩解片崩解迅速,相对生物利用度为90.7%。

OBJECTIVE To prepare montelukast sodium orally disintegrating tablets and investigate the bioequivalence in Beagle dogs.METHODS The orally disintegrating tablets were prepared by direct compression method,and the optimal formulation was screened by orthogonal test.HPLC-fluorescence method was developed for determination of montelukast sodium plasma concentration in Beagle dogs.RESULTS The optimized formulation（1 000 tablets） was montelukast sodium 10.4 g, microcrystalline cellulose 60 g, cross linked povidone 30 g, mannitol 15 g, magnesium stearate 2 g, aerosil 1 g, aspartame 1 g, flavor 0.6 g.CONCLUSION Montelukast sodium orally disintegrating tablets made of the optimized formulation could disintegrate rapidly. Relatively bioavailability of montelukast sodium orally disintegrating tablets is 90.7%.