Ocular pharmacokinetics of puerarin in anesthetic rabbits by microdialysis / 中国中药杂志

<p><b>OBJECTIVE</b>To establish the model of microdialysis, and study the ocular pharmacokinetics of puerarin in anesthetic rabbits.</p><p><b>METHOD</b>Implanted the probe into anterior chamber of anesthetic rabbit by surgery. After balanced for 2 h, 1% puerarin eye drop (100 microL) was applied into the cul-de-sac with micropipette. Immediately the dialysate was collected at different time and detected by HPLC with the detection wavelength of 249 nm. The mobile phase was methanol and 0.1% citric acid solution (30:70); the flow rate was 1.0 mL x min(-1).</p><p><b>RESULT</b>After the administration, puerarin can be absorbed into aqueous humor quickly. The peak concentration of puerarin appeared at about 1 h and then reduced gradually. The peak concentration(C(max)) is (2.52 +/- 0.31) mg x L(-1). The other lower peak was shown at 3.5 h during the eliminate phase. This might be attributed to the inhibition of aqueous humor production by the puerarin and resulted in a high drug concentration. The area under concentration-time curve (AUC(0-t)) is (5.04 +/- 0.21) mg x h x L(-1) and the eliminate half life (t1/2) is (0.38 +/- 0.13) h.</p><p><b>CONCLUSION</b>The microdialysis technique can be used to detect the ocular pharmacokinetics of puerarin, and support the valuable pharmacokinetics parameter for the clinical applications of puerarin eye drop.</p>

Corneal penetration of PAMAM dendrimers-coated puerarin liposomes / 中国中药杂志

<p><b>OBJECTIVE</b>To study the corneal penetration of PAMAM dendrimers-coated puerarin liposomes in rabbits.</p><p><b>METHOD</b>Evaluated PAMAM (G2, G3) dendrimers-coated puerarin liposomes were prepared and the in vitro transcorneal penetration were compared to puerarin drop solution and uncoated liposomes. The effect of different proportion of PAMAM to phospholipids in formulation on corneal penetration and the penetration parameters were investigated.</p><p><b>RESULT</b>The steady state fluxes and permeability coefficients of puerarin by PAMAM G2 (1.0%) and PAMAM G3 (0.5%) coated puerarin liposomes were greater than that by puerarin drop solution and uncoated liposomess (P < 0.01), meanwhile the PAMAM G2 (1.0%) and PAMAM G3 (0.5%) coated liposomes were better than other ratios of coated liposomes for improvement of corneal penetration (P < 0.01).</p><p><b>CONCLUSION</b>The PAMAM coated liposomes is able to enhance the corneal penetration of puerarin and promising as an ocular drug carriers.</p>

Preparation and dissolution characteristics of solid dispersion of ginsenoside Rg_3 / 中草药

Objective To prepare the solid dispersion of ginsenoside Rg3 with different carriers and measure their solubility and dissolution characterisitics. Methods The solid dispersion of ginsenoside Rg3 was prepared by the melted and dissolved methods with Poloxamer 188(F68), PVP k29/32, and PEG 6000 as carriers, respectively. The equilibrium solubility and dissolution characteristics of the solid dispersion in vitro were measured by HPLC. The existing state of ginsenoside Rg3 in the solid dispersion was identified by the differential scanning calorimetery. Results The ginsenoside Rg3 was completely dispersed in carrier and formed a mixture with carriers. The solubility and dissolution rates of all solid dispersion were increased obviously. Conclusion The solid dispersion of ginsenoside Rg3 with Poloxamer 188 as carriers is better on improving dissolution and solubility than those with PVP and PEG 6000 as carriers.