Study On Scopolamine Hydrobromide Orally Disintegrating Tablets Based On NiMS

Objective:To prepare Scopolamine Hydrobromide orally disintegrating tablets (ODTs)based on nanoparticles-in-microsphere system (SH-NiMS) optimize the formulation of nanospheres and orally disintegrating tablets,and evaluate its drug release characteristics in vitro.To complete the sale-up of the preparation technology and the experiment on stability and provide the basis for industrial production.Method:SH nanospheres were prepared by ionic crosslinking method with tripolyphosphate (TPP) as crosslinker and chitosan as carrier, and sprayed to microspheres which encapsuled SH nanospheres by spray drying technique. The orthogonal design was used to optimize the formulation of SH nanospheres,which took the property of encapsulation efficiency and drug loading as evaluation parameters. Adjusted the parameters of spray drying technique.SH-NiMS release characteristics in vitro were evaluated.Mixed SH-NiMS with auxiliary materials and prepared SH-NiMS orally disintegrating tablets according to the optimized pormulation. Evaluated its pharmaceutical characteristics in vitro. Adjusted the parameters of spray drying technique in scale-up.Completed the sale-up of the preparation technology (about 100000 pieces of SH-NiMS ODTs) and the experiment on stability of the first 3 months.Result:The optimized formulation of SH nanospheres was TPP:CS 1:3,HPMC 0.3%,SH 0.2%.The encapsulation efficiency,drug loading and particle sizes were 94.2%,20.4%,1256.5nm respectively. The optimized formulation of SH ODTs was composed of mannitol 40%, MCC 35%, lactose 0%, CMS-Na 10%.SH-NiMS orally disintegrating tablets prepared by optimized formulation had glabrous and well-proportioned appearace, nice taste, uniformitarian content,and released completely in 360min.After the scale-up,the temperature of the spray drying technique were adjusted to 110℃/53.5℃,the thickness of ODTS was 1.8±0.2,the depth of ODTs was 5.8±0.3,the race of compresing is 20 rpm.The characteristics were steady after sale-up 3months.Conclution:NiMS could be an available carrier for drugs. SH-NiMS orally disintegrating tablets prepared had the characteristics of rapid disintegration and slow release.The preparation technique were steady,conquered the inconvenience of travelling outside and short of water conditions, decreased the frequency of administration and the side reaction,provided the basis for industrial production.