NGHIÊN CỨU BÀO CHẾ PELLET CHỨA PARACETAMOL 80% BẰNG TIẾP CẬN THIẾT KẾ THỰC NGHIỆM 

Summary

In recent years, pellets with high drug loading ratios have received more and more research attention. However, up to now, data on the simultaneous influence of formulation ingredients (especially spherical – aid excipients, moisture content) and preparation process parameters on the properties of resultant pellets are incomplete. The current study was carried out to determine the effect of formulation and process parameters on the properties of pellets containing paracetamol 80 %. The influence of factors is considered simultaneously through experimental design before optimization using Design – Expert v12.0 software. Pellets properties were evaluated considering sphericity, density, and mass ratio in the range of 0.85 – 1.18 mm.
The results show that five factors: Type of spherical – aid excipients, moisture content, extrusion mesh, residence time, and spheronization speed, have statistically significant effects on all three properties of the studied pellets. Pellets prepared according to the optimized conditions have a sphericity of 0.9 and tapped density of 0.65; more than 70 % of resultant pellets are sized in the range 0.85 – 1.18 mm. Regarding the dissolution test, the in vitro release of paracetamol after 45 minutes is greater than 95 %. The behavior of pellets during their formation is also clarified. The results provide more valuable data on the preparation of pellets with a high loading rate of active ingredients in Vietnam.

Keywords: Pellet, high drug loading, experimental design, extrusion spheronization.

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