ABSTRACT
Objective: To prepare hydrogel matrix sustained-release tablets of resveratrol solid lipid nanoparticles, and the factors that might influence drug release and in vitro release models were also investigated in present study. Methods: The resveratrol-solid lipid nanoparticles (Res-SLN) were prepared by thin-film ultrasonic dispersion method, and then the hydrogel matrix was prepared by dispersed in excipients of hydrogel matrix sustained-release tablets. Single factor analysis was used to study the effects of varieties of adhesives, PEG, HPMC, and the amounts of HPMC K15 on drug release. Then the orthogonal design was used to gain the optimum formulation. Zero-order, first-order, Higuchi, and Ritger-Pappas models were used for the model fitting of drug release. Results: Hydrogel matrix sustained-release tablet of Res-SLN was better accorded with Zero-order kinetics model. The equation was Mt/M∞ = 0.078 7 t + 0.003 6 (r = 0.998 0). In vitro release behavior was in line with Ritger-Peppas equation, and the drug release from the tablets was controlled by degradation of the matrix. Conclusion: Prescription of hydrogel matrix sustained-release tablet of Res-SLN is reasonable; The preparation technology is feasible and exhibits perfect sustained-release characteristics in vitro in 12 h.
ABSTRACT
OBJECTIVE:To prepare Zuojin gastric-mucoadhesive tablets and evaluate their drug release properties in vitro. METHODS:Zuojin gastric-mucoadhesive tablets were prepared with hydroxypropyl methyl cellulose K15M(HPMC-K15M),car-bomer 934P and HPMC-E50 as the bioadhesive and matrix materials,and basic magnesium carbonate(foaming material),95% al-cohol solution(adhesive)and aerosil(glidant and lubricant)as the adjuvants. With the accumulative release of total alkaloids from Coptis chinensis Franch. at 2,6 and 10 h(Q2 h,Q6 h and Q10 h)as the indexes,orthogonal design test was conducted to optimize the amounts of HPMC-K15M,carbomer 934P,HPMC-E50 and basic magnesium carbonate,and verification was carried out. Drug re-lease properties in vitro of the preparation and Zuojin conventional tablets were observed and in vitro adhesion thereof determined. RESULTS:The optimal formulation was as follows as that for 50 tablets,HPMC-K15M of 0.7 g,carbomer 934P of 0.2 g, HPMC-E50 of 3.5 g and basic magnesium carbonate of 0.4 g. The Q2 h,Q6 h and Q10 h of three batches of prepared samples were 24.32%,56.10% and 77.04% respectively. 1-12 h drug release in vitro of prepared samples was in conformity with Ritger-Peppas equation. The Q2 h of Zuojin conventional tablets and Zuojin gastric-mucoadhesive tablets were 80.46% and 24.04%,Q12 h thereof 92.15% and 95.83% and gastric adhesion thereof 24.2 and 74.0 g/cm2,respectively. CONCLUSIONS:Zuojin gastric-mucoadhesive tablets which have sustained-release effect and adhesive property have been prepared successfully.