Study On Baicalin Solid Dispersion Drop Pills

Baicalin (C₂₁H₁₈O₁₁) is the active ingredients of Labiatae Scutellaria Scutellaria species contained in flavonoids. Pharmacology Experimental studies confirm that baicalin has antibacterial, anti-inflammatory, anti-oxidation, inhibit aldose reductase, control diabetes and chronic complications of cardiovascular and brain injury in rats and other pharmacological effect. In this paper, PVP_K30 as a carrier, was used to prepare pills by the technology of solid dispersions. It improved baicalin solubility and dissolution rate, and reached the purpose of increasing its pharmacodynamics.According to the literature, UV spectrophotometry was developed for in vitro assay of solubility, dissolution, the determination of content and the study of stability of baicalin-PVP_K30 solid dispersion in different pH conditions, different times.The solid dispersion were prepared by solvent volatilization method .The influence of dosage of PVP_K30 on the solubility and dissolution of baicalin was examined. It can be concluded from the result that the solid dispersion could apparently increase the solubility and dissolution degree of baicalin. The infrared spectrum, DSC and X-Ray powder diffraction analysis exhibit that the solid dispersion of baicalin- PVP_K30 exists in an amorphous form of solid dispersion system.Single-factor optimization methods were applied for assessing the pills preparation process : the weight ratio of baicalin solid dispersion and matrix PEG6000 1:5, melting temperature 80℃to 90℃, drop temperature 85℃to 90℃, liquid paraffin: vegetable oil （condensing agent） 1:1.The difference of absorption in vivo between baicalin and drop pills was forecasted by using the Caco-2 cell model. The Papp value of the drop pills and baicalin is 4.462×10^-6±1.1cm·s^-1 and 0.2213×10^-6±0.3 c·s^-1, Whether there is a ratio of about 20 times. It can predict that baicalin pills are better in oral absorption than baicalin.The research of pharmacokinetics in Beagle dogs verified that the AUC_0-12, C_max and T_max of the baicalin drop pill and the capsule were 5.797μg·h/mL, 1.563μg/mL, 3.0h or 5.031μg·h/mL, 1.106μg/mL, 2.0h, respectively and the relative bioavailability was 115.23 percent.