Atorvastatin has low aqueous solubility resulting in low oral bioavailability(12%)and thus presents a challenge in formulating a suitable dosage form.To improve the aqueous solubility,a solid dispersion formulation of...Atorvastatin has low aqueous solubility resulting in low oral bioavailability(12%)and thus presents a challenge in formulating a suitable dosage form.To improve the aqueous solubility,a solid dispersion formulation of atorvasta tin was prepared by lyophilization utilising skimmed milk as a carrier.Six different formulations were prepared with varying ratios of drug and carrier and the corresponding physical mixtures were also prepared.The formation of a solid dispersion formulation was confirmed by differential scanning ca lorimetry and X-ray diffraction studies.The optimum drug-to-carrier ratio of 1:9 en hanced solubility nearly 33-fold as compared to pure drug.In vitro drug release studies exhibited a cumulative release of 83.69% as compared to 22.7% for the pure drug.Additionally,scanning electron microscopy studies suggested the conversion of crystalline atorvastatin to an amorphous form.In a Triton-induced hyperlipidemia model,a 3-fold increase in the lipid lowering potential was obtained with the reformulated drug as compared to pure drug.These results suggest that solid dispersion of atorvastatin using skimmed milk as carrier is a promising approach for oral delivery of atorvastatin.展开更多
文摘Atorvastatin has low aqueous solubility resulting in low oral bioavailability(12%)and thus presents a challenge in formulating a suitable dosage form.To improve the aqueous solubility,a solid dispersion formulation of atorvasta tin was prepared by lyophilization utilising skimmed milk as a carrier.Six different formulations were prepared with varying ratios of drug and carrier and the corresponding physical mixtures were also prepared.The formation of a solid dispersion formulation was confirmed by differential scanning ca lorimetry and X-ray diffraction studies.The optimum drug-to-carrier ratio of 1:9 en hanced solubility nearly 33-fold as compared to pure drug.In vitro drug release studies exhibited a cumulative release of 83.69% as compared to 22.7% for the pure drug.Additionally,scanning electron microscopy studies suggested the conversion of crystalline atorvastatin to an amorphous form.In a Triton-induced hyperlipidemia model,a 3-fold increase in the lipid lowering potential was obtained with the reformulated drug as compared to pure drug.These results suggest that solid dispersion of atorvastatin using skimmed milk as carrier is a promising approach for oral delivery of atorvastatin.
