Studies have shown that when compressing drugs with low aqueous solubility, the solubility of diluents selected is very crucial as it influences the disintegration, dissolution and bioavailability of such drugs. Based on these reports, the present study was undertaken to investigate the effect of some commonly used hydrophilic tablet diluents (lactose, sucrose, mannitol and dextrose) on the in vitro release properties of griseofulvin from compressed tablets. Griseofulvin granules and tablets were prepared using the wet granulation method. Tablet properties evaluated as a function of the diluents used include, hardness, friability, dissolution profile and dissolution efficiency at 60 min. Results obtained indicated variability in griseofulvin release in the presence of the diluents. The relative enhanced dissolution effects of the four hydrophilic diluents is in the order of dextrose>sucrose>lactose>mannitol. All the griseofulvin tablet batches produced exhibited a better drug release (in terms of rate and extent of release) than a commercially available tablet sample of griseofulvin (Fulcin®). The results of the dissolution efficiency (DE60min) are 91.7, 83.5, 48.7, 35.3 and 15.6% for dextrose, sucrose, lactose, mannitol and fulcin®, respectively. The overall results indicated that dextrose or sucrose can be utilised to improve the in vitro release profile and hence in vivo bioavailability of griseofulvin from compressed tablets. 相似文献
Summary: Molecular weight (MW) effects of atactic polystyrene (aPS) on the morphologies and crystallization kinetics of syndiotactic polystyrene (sPS) blends have been investigated, and miscibility was confirmed for all the sPS/aPS blends. Addition of aPS(M) or aPS(L) leads to a significant increase in the entropy of mixing and gives rise to a pronounced decrease in the equilibrium melting temperature of the blends. On heating from the glassy state, the crystallization peak temperature of the sPS/aPS(H) blend increased with increasing aPS content due to a dilution effect, whereas those of sPS/aPS(M) and sPS/aPS(L) decreased mainly due to enhanced chain mobility. On cooling from the melt state, the crystallization peak temperature decreased with increasing aPS content regardless of the aPS MW. A higher activation energy is required for the sPS component transport from the miscible melt to the growth front in the sPS/aPS(L), suggesting that extra energy is required for the demixing process. Interspherulitic segregation of aPS diluents was evident in the sPS/aPS(L) blends, while interfibrillar segregation morphology was obtained in the sPS/aPS(H) as well as the sPS/aPS(U) blends.
SEM images of sPS/aPS blends 50/50(L) at 230 °C (C) and 70/30(L) at 250 °C (D). 相似文献