Drug Delivery Research Laboratory, College of Pharmacy, Chung-Ang University, 221 Heuksuk-dong, Dongjak-gu, Seoul 156-756, South Korea.
Arch Pharm Res. 2013 Jan;36(1):69-78. doi: 10.1007/s12272-013-0011-z.
A supersaturating self-emulsifying drug delivery system (S-SEDDS) was prepared and evaluated for enhanced dissolution of celecoxib (CXB), a poorly water-soluble drug. The selected CXB-dissolved SEDDS formulation consisting 10 % Capryol 90 (oil), 45 % Tween 20 (surfactant), and 45 % Tetraglycol (cosurfactant) had the characteristics of small droplet size and great solubility as 208 nm and 556.7 mg/mL in average, respectively. CXB dissolution from SEDDS in simulated gastric fluid was increased to about 20 % for the initial period of 5 min, but decreased to a half level as time elapsed. Thus, precipitation inhibitors were screened to stabilize the supersaturation. The stabilizing effect of Soluplus, an amphiphilic copolymer, was concentration-dependent, revealing the greatest dissolution of approximately 90 % level with delayed drug crystallization by the addition of the copolymer. CXB dissolution from S-SEDDS was pH-independent. We concluded that S-SEDDS formulation would be very useful in the future for developing oral delivery product of poorly water-soluble drugs.
制备了超饱和自乳化药物传递系统（S-SEDDS）并对其进行了评价，以提高难溶性药物塞来昔布（CXB）的溶解度。所选的 CXB 溶解的 SEDDS 制剂由 10%的 Capryol 90（油）、45%的 Tween 20（表面活性剂）和 45%的 Tetraglycol（助表面活性剂）组成，具有小的平均粒径和高的溶解度，分别为 208nm 和 556.7mg/mL。SEDDS 中的 CXB 在模拟胃液中的溶解度在最初的 5 分钟内增加到约 20%，但随着时间的推移，溶解度降低到一半。因此，筛选沉淀抑制剂以稳定过饱和度。两亲性共聚物 Soluplus 的稳定作用具有浓度依赖性，表明共聚物的加入可最大程度地提高约 90%的溶解度并延迟药物结晶。S-SEDDS 中的 CXB 溶解度与 pH 无关。我们得出结论，S-SEDDS 制剂在未来对于开发难溶性药物的口服递送产品将非常有用。
