College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea.
Int J Pharm. 2011 Nov 28;420(2):412-8. doi: 10.1016/j.ijpharm.2011.09.007. Epub 2011 Sep 16.
In order to compare the effects of hydrophilic and hydrophobic solid carrier on the formation of solid self-microemulsifying drug delivery system (SMEDDS), two solid SMEDDS formulations were prepared by spray-drying the solutions containing liquid SMEDDS and solid carriers. Colloidal silica and dextran were used as a hydrophobic and a hydrophilic carrier, respectively. The liquid SMEDDS, composed of Labrafil M 1944 CS/Labrasol/Trasncutol HP (12.5/80/7.5%) with 2% w/v flurbiprofen, gave a z-average diameter of about 100 nm. Colloidal silica produced an excellent conventional solid SMEDDS in which the liquid SMEDDS was absorbed onto its surfaces. It gave a microemulsion droplet size similar to that of the liquid SMEDDS (about 100 nm) which was smaller than the other solid SMEDDS formulation. In the solid SMEDDS prepared with dextran, liquid SMEDDS was not absorbed onto the surfaces of carrier but formed a kind of nano-sized microcapsule with carrier. However, the drug was in an amorphous state in two solid SMEDDS formulations. Similarly, they greatly improved the dissolution rate and oral bioavailability of flurbiprofen in rats due to the fast spontaneous emulsion formation and the decreased droplet size. Thus, except appearance, hydrophilic carrier (dextran) and hydrophobic carrier (colloidal silica) hardly affected the formation of solid SMEDDS such as crystalline properties, dissolution and oral bioavailability.
为了比较亲水性和疏水性固体载体对固体自微乳药物传递系统(SMEDDS)形成的影响,通过喷雾干燥含有液体 SMEDDS 和固体载体的溶液制备了两种固体 SMEDDS 制剂。胶体二氧化硅和葡聚糖分别用作疏水性和亲水性载体。液体 SMEDDS 由 Labrafil M 1944 CS/Labrasol/Trasncutol HP(12.5/80/7.5%)与 2%w/v 氟比洛芬组成,粒径约为 100nm。胶体二氧化硅产生了一种极好的常规固体 SMEDDS,其中液体 SMEDDS 被吸收到其表面上。它给出了与液体 SMEDDS 相似的微乳液液滴尺寸(约 100nm),小于其他固体 SMEDDS 制剂。在使用葡聚糖制备的固体 SMEDDS 中,液体 SMEDDS 没有被载体吸收到表面上,而是与载体形成了一种纳米级微胶囊。然而,两种固体 SMEDDS 制剂中的药物均处于无定形状态。同样,由于快速自发乳化形成和液滴尺寸减小,它们大大提高了氟比洛芬在大鼠中的溶解速率和口服生物利用度。因此,除了外观外,亲水性载体(葡聚糖)和疏水性载体(胶体二氧化硅)几乎不会影响固体 SMEDDS 的形成,如结晶性质、溶解和口服生物利用度。