Dixit Rahul P, Nagarsenker M S
Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (East), Mumbai, India.
Drug Dev Ind Pharm. 2008 Dec;34(12):1285-96. doi: 10.1080/03639040802071570.
Self-nanoemulsifying granules were formulated with the objective of improving the bioavailability of the ezetimibe and simvastatin when administered together. Composition of self-nanoemulsifying system (SNS) was optimized using various modified oils, surfactant, and cosurfactant mixtures. SNSs were mixed with water and resultant emulsions were characterized for mean globule size and stability. SNSs were adsorbed on hydrophilic colloidal silicon dioxide to give free-flowing self-nanoemulsifying granules. Self-nanoemulsifying granules were characterized by X-ray diffraction pattern, scanning electron microscopy, dissolution profile, and for in vivo performance in hypercholesterolemic rats. X-ray diffraction studies and scanning electron microscopy indicated loss of crystallinity and/or solubilization of both drugs in the self-nanoemulsifying granules. Self-nanoemulsifying granules effected substantial increase in dissolution of the drugs as compared with pure powder of drugs. In vivo evaluation in rats showed significant decrease in the total cholesterol levels and triglyceride levels in rats as compared with positive control confirming potential of self-nanoemulsifying granules as a drug delivery system for the poorly water-soluble drugs.
自纳米乳化颗粒的制备目的是提高依折麦布和辛伐他汀联合给药时的生物利用度。使用各种改性油、表面活性剂和助表面活性剂混合物优化自纳米乳化系统（SNS）的组成。将SNS与水混合，并对所得乳液的平均粒径和稳定性进行表征。将SNS吸附在亲水性胶体二氧化硅上，得到自由流动的自纳米乳化颗粒。通过X射线衍射图谱、扫描电子显微镜、溶出曲线以及在高胆固醇血症大鼠体内的性能对自纳米乳化颗粒进行表征。X射线衍射研究和扫描电子显微镜表明，两种药物在自纳米乳化颗粒中结晶度降低和/或溶解。与药物纯粉末相比，自纳米乳化颗粒使药物溶出度大幅增加。大鼠体内评价显示，与阳性对照相比，大鼠的总胆固醇水平和甘油三酯水平显著降低，证实了自纳米乳化颗粒作为难溶性药物给药系统的潜力。
