,Redispersible, dry emulsion of Iovastatin protects against intestinal metabolism and improves bioav

来源 :中国药理学报(英文版) | 被引量 : 0次 | 上传用户:yichunyang
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Aim: To prepare a redispersible, dry emulsion (DE) and investigate whether it can improve intestinal stability and oral absorptive efficiency of the poorly water- soluble lovastatin (Lov). Methods: Phosa153 MCT, Tween 80, and starch sodium octenyl succinate were employed as the oil phase, emulsifying agent, and matrix material, respectively. The redispersible, DE of Lov (Lov-DE) was prepared by spray drying the submicron emulsion of Lov. The characteristics of DE and the in vitro drug release were studied. The protective effects on the metabolism of Lov- DE and reference formulations, including the Lov suspension and the hydroxypropyl-β-cyclodextrin (CD) complex were investigated in microsomes and the gut wall of male Sprague-Dawley (SD) rats. The bioavailability in SD rats was evaluated simultaneously. Results: Lov-DE in distilled water was reconstituted compared with the submicron emulsion of Lov before spray drying, and remained almost unchanged after 3 months’ storage at room temperature. Compared with the Lov suspension, the in vitro Lov dissolution of both the redispersible, DE and CD complex increased obviously. Compared with control formulations, the me- tabolism studies carried out in vitro and in vivo confirmed that the redispersible, DE presented remarkable protective effects as indicated by the decreased metabo- lism rate of Lov. Lov-DE showed a 1.83-fold and 1.44-fold higher the area under the curve(AUC0-8h)of Lov compared with that of the Lov suspension and CD complex in SD rats, respectively. Conclusion: Lov-DE reduced the metabolism of Lov in the small intestine and improved its oral absorption in SD rats.
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