Study On Self-Microemulsifying Enteric Beads Of Berberine

In recent years.increasing attention has been focused on self-microemulsifying drug delivery system (SMEDDS), which has shown great success in improving oral bioavailability of poorly soluble drugs and become a potential drug delivery system. In this research, for the merits of self-microemulsifyingdrug delivery system, the traditional berberine was recasted by using the solid-self-microemulsifying enteric bead as a new carrier. The formulation was selected by determining the solubility of berberine and drawing pseudo-ternary phase diagram; The ion gelation was used to preparation solid-self-microemulsifying enteric bead of berberine, and the release properties in viro, encapsulation efficiency and pharmacokinetics were studied. The abstracts are as follows:(1) The establishment of HPLC analytical method of berberine.To establish the HPLC analytical method for content determining of berberine The good linear range of the blood plasma was 3～250μg/mL, The mean recovery was 96.1% and RSD of the recovery was 6.55%. The accuracies with-day and between-day were lesss than 6%.The analysis method we established in this study had high recovery and accuracy,which could used in quality control and dynamics research.(2) The prescription screening of liquid self-microemulsifyingdrug delivery system.The formulation was selected by determining the solubility of berberine and drawing pseudo-ternary phase diagram; The results showed that the formulation optimal proportion was berberine:CapmulMCMC8:SolutolHS15:PEG400.(3) The preparation and in vitro evaluation on solid-self-microemulsifying enteric bead of berberine.The SMEDDS of berberine were optimized by studying the pseudoternary phase diagram, and using sodium alginate and CaCl2(0.1 mol/L) as solid carriers. The preparation of solid-self-microemulsifying enteric bead of berberine by high speed emulsifying machine.The preparation method was optimized by entrapment efficiency and drug loading as evaluation standard. The results show that drug loading was 1.78 % and entrapment efficiency was 77.72 %, The quality of berberine S-SMEDDS enteric beads was stable.use artificial gastric fluid(PH=1.0) and artificial intestinal liquid (PH=6.8) as medium disssolve the beads,and use the Drug Solution Instrument determine the ralease of enteric beads.the result is that in artificial gastric liquid is 18.09 % and artificial intestinal liquid is 94.62%,the formulation have a good ralease rate in intestinal. the mechanism were studied.(4) The pharmacokinetics study of berbeine S-SMEDDS enteric beadsCollection the blood of rats which was administered the enteric beads, determine berberine which in plasma with HPLC.and draw the curve of pharmacy and time. And then the pharmacokinematicsparameter was calculated by 3P87 pharmacokinematics calculation program.