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KMID : 0043320130360010069
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Archives of Pharmacal Research
2013 Volume.36 No. 1 p.69 ~ p.78
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Enhanced dissolution of celecoxib by supersaturating self-emulsifying drug delivery system (S-SEDDS) formulation
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Song Woo-Heon
Park Jong-Hyeok
Yeom Dong-Woo
Ahn Byeong-Kil
Lee Kyung-Min
Lee Sang-Gon
Woo Hye-Seung
Choi Young-Wook
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Abstract
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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.
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KEYWORD
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Celecoxib, Self-emulsification, S-SEDDS, Soluplus, Solubilization, Supersaturation
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