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Arch Pharm Res ; 36(1): 69-78, 2013 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-23325487

RESUMO

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.


Assuntos
Inibidores de Ciclo-Oxigenase 2/administração & dosagem , Inibidores de Ciclo-Oxigenase 2/química , Sistemas de Liberação de Medicamentos/métodos , Pirazóis/administração & dosagem , Pirazóis/química , Sulfonamidas/administração & dosagem , Sulfonamidas/química , Caprilatos/química , Celecoxib , Química Farmacêutica , Portadores de Fármacos/química , Emulsões , Micelas , Tamanho da Partícula , Transição de Fase , Solubilidade , Tensoativos/química
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