Preparation and in vitro quality evaluation of self-microemulsion co-loaded with tenuifolin and β-asarone / 中国中药杂志

To prepare and optimize the self-microemulsion co-loaded with tenuifolin and β-asarone(TF/ASA-SMEDDS) and evaluate its quality. The prescription compositions of TF/ASA-SMEDDS were screened by solubility test, single factor test and pseudo-tern-ary phase diagram, and the prescriptions were further optimized by Box-Behnken response surface method, with the drug loading and particle size as the evaluation indexes. Then the optimized TF/ASA-SMEDDS was evaluated for emulsified appearance, particle size, morphology and drug release in vitro. The optimized prescription for TF/ASA-SMEDDS was as follows: caprylic citrate triglyceride polyoxyethylene castor oil-glycerol(10.8∶39.2∶50), drug loading of(5.563±0.065) mg·g~(-1) for tenuifolin and(5.526±0.022) mg·g~(-1) for β-asarone; uniform and transparent pan-blue nanoemulsion can be formed after emulsification, with particle size of(28.84±0.44) nm. TEM showed that TF/ASA-SMEDDS can form spherical droplets with a uniform particle size after emulsification; In vitro release test results showed that the drug release rate and cumulative release of tenuifolin and β-asarone were significantly improved. The preparation process of TF/ASA-SMEDDS was simple and can effectively improve in vitro release of tenuifolin and β-asarone.

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

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 (10:67.5:22.5:2). 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.