Preparation and in vitro quality evaluation of silybin supersaturated self-microemulsion drug delivery system / 中草药

ABSTRACT

Objective: To develop and optimize the silybin supersaturated self-microemulsion drug delivery system (SLB-SSMEDDS) and improve the oral bioavailability of SLB in the biological medium. Methods: The formulation of SLB-SMEDDS was selected by solubility test, emulsifying ability of emulsifier and pseudo-ternary phase diagram. The analytic hierarchy process (AHP) was used to evaluate the performance of each prescription to screen the optimal ratio. The type and dosage of precipitation inhibitors (PPIs) was optimized to maintain the supersaturation and duration of drugs in biological media in vitro; Finally, the emulsification effect, emulsion size and surface morphology of SLB-SSMEDDS was comprehensively evaluated in terms of in vitro release and in vitro supersaturation. Results: The SLB-SSMEDDS prescription was Capryol 90-Cremophor RH-Transcutol HP-HPMC-AS MF (1067.522.52). The self-microemulsion with a drug loading of 50.19 mg/g was uniform and the emulsion droplets were spherical in shape and uniform in size. And the emulsification time was (30.67 ± 4.16) s, the average particle size was (11.67 ± 0.81) nm, and the PDI was (0.15 ± 0.04). The dissolution rate of SLB-SSMEDDS in FaSSGF and FaSSIF-V2 was significantly increased. And the in vitro dilution and supersaturation could be maintained above 10 within 120 min. Conclusion: SLB-SSMEDDS has a simple preparation process and can improve the stability of traditional SMEDDS, maintain supersaturation effectively and enhance the dissolution of SLB in vitro.