Design and <i>in Vitro</i>Evaluation of Eudragit^®S100/Lipid Based Simvastatin Chronotherapeutic Drug Delivery System  

作　　者：Ehab I. Taha 

机构地区：[2]Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt [2]Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia

出　　处：《Pharmacology & Pharmacy》2014年第13期1157-1162,共6页药理与制药（英文）

摘　　要：The present study was undertaken to 1) formulate a pulsatile colonic delivery of simvastatin (SIM) as chronotherapy for treatment of hypercholesterolemia, and 2) enhance the dissolution profile of the prepared SIM chronotherapeutic system. Lipid based formulations were utilized to formulate SIM in capsule dosage form coated with Eudragit&reg S100. SIM was formulated using different percentages of Cremophor EL40, Capmul MCM EP and PEG 400. SIM coated capsules (SIMcc) were evaluated for drug release in different pH media. The results showed that SIMcc were able to withstand the acidic pH for 2 hours. Drug release rate was higher (88%) from SIMcc containing 10% polyethylene glycol (PEG) 400. In conclusion, Eudragit&reg S100 as time-dependent and site specific polymer retards SIM release from coated capsules;hence SIMcc could be considered as successful pulsatile treatment of hypercholesterolemia. Also, dissolution profile of lipid based SIMcc was enhanced in comparison with that of SIM filled capsules.The present study was undertaken to 1) formulate a pulsatile colonic delivery of simvastatin (SIM) as chronotherapy for treatment of hypercholesterolemia, and 2) enhance the dissolution profile of the prepared SIM chronotherapeutic system. Lipid based formulations were utilized to formulate SIM in capsule dosage form coated with Eudragit&reg S100. SIM was formulated using different percentages of Cremophor EL40, Capmul MCM EP and PEG 400. SIM coated capsules (SIMcc) were evaluated for drug release in different pH media. The results showed that SIMcc were able to withstand the acidic pH for 2 hours. Drug release rate was higher (88%) from SIMcc containing 10% polyethylene glycol (PEG) 400. In conclusion, Eudragit&reg S100 as time-dependent and site specific polymer retards SIM release from coated capsules;hence SIMcc could be considered as successful pulsatile treatment of hypercholesterolemia. Also, dissolution profile of lipid based SIMcc was enhanced in comparison with that of SIM filled capsules.

关 键 词：CHRONOTHERAPY Circadian Rhythms Colon Delivery Dissolution Profile LIPID BASED Formulation 

分 类 号：R73[医药卫生—肿瘤]