Preparation of sustained-release tablets of tilianin nanosuspension lyophilized powder / 中草药

ABSTRACT

Objective: To prepare sustained-release tablets of tilianin nanosuspension lyophilized powder. The factors that might influence drug release and release mechanism were studied in present study. Methods: High pressure homogenization method was used to prepare tilianin nanosuspension. Lactose and mannitol (31) were employed as freeze-drying protective agent to prepare lyophilized powder. HPMC was used as framework material to prepare sustained-release tablets of tilianin nanosuspension lyophilized powder. Based on single factor test, the effects of proportion and amounts of HPMC K4M and HPMC K15, amounts of PEG 4000 and magnesium stearate on in vitro drug release of sustained-release tablets were investigated. Orthogonal test was designed to gain the optimum prescription. Results: The particle size and zeta potential of tilianin nanosuspension were (164.41 ± 9.72) nm and (-37.21 ± 2.38) mV, respectively. The particle size and zeta potential of re-dispersed freeze-drying products were (211.83 ± 11.26) nm and (-31.66 ± 2.92) mV, respectively. The optimum prescription was as follow the proportion and amounts of HPMC K4M and HPMC K15 were 21 and 40 mg, amounts of PEG 4000 was 20 mg, and amounts of magnesium stearate were 0.5%. Sustained release tablets of tilianin nanosuspension were well accorded with Higuchi kinetics model. The equation was Mt/M∞ = 0.286 8 t1/2-0.073 8, r2 = 0.981 4. And the cumulative release could achieve 92.36% in 12 h. The drug release from the tablets was controlled by diffusion and degradation of the matrix. Conclusion: The preparation technology of sustained release tablets of tilianin nanosuspension lyophilized powder has good reproducibility. This sustained release tablets could control the release of tilianin