Studies On The Preparation Of The Effective Fractions Of Radix Scutellariae And Its Transdermal Drug Release Property

Scutellariae Radix is commonly used traditional Chinese medicine,and its complex c-hemical composition,containing flavonoids,such as baicalin,oroxylin-A-glucoside,wogon oside,baicalein,et al.Current clinical use of the single or compound radix topical formu-lationsis more,including gelatas,patches,cataplasms,ointments,etc.This research studied the preparation of radix scutellariae total flavonoids effective parts and physico-chemical pro perty,compared its relevant preparations(cataplasm,ointment)and its drug release property,the main contents of this paper includes:1 Preparation of EPSR Total flavonoids and its monomer composition baicalin,o roxy-lin-A-glucoside,wogonoside,baicalein,wogonin and oroxyin as the major componen t.Using the single factor and the orthogonal experiment method,study and optimization a nd verify of the extraction process and purif.Finally select the optimum preparation is 10-fold volume of 50%ethanolfor 1 h each time,circumfluence extracting 3 times,merge the filtrate and recycle dethanol;with HPD300 macroporous resin as adsorbent,take 3 BV with a concentration of 100 mg/mL solution,the dynamic adsorption after washing t he sample with 7 BV impurity,and 5BV of 70%ethanol elution,respectively,concentra-ted ofthe alcohol eluention,After decompre-ssion concentration,60 ? vacuum drying,the resulting samples is the scutellariae radix effective parts.2 Study physicochemical properties of EPSR The study on the physicochemical properties of EPSR,the result show that EPSR slightly dissolved in water,and the solu-bility in glyceryl alcohol and 50%ethanol was the best.In the phosphate buffer solution(pH 2.0-6.8),the solubility of total flavonoids scutellaria and their monomer composition increased with the pH value increaseng,and the oil/water distribution value lgP decrease-d as the pH value increaseing.As the pH values were 7.4 and 8,the solubility of baic-alin decreased gradually,the solubility of flavonoids and other compounds increased grad-ually,lgP value ofbaicalin increased gradually,while the lgP values of other ingredients decreased.Compared to phosphate buffer solution of different pH,physiol-ogical saline,40%PSN saline and different concentrations of ethanol normal saline,30%ethanol for sc-utellariae radix effective parts has good solubility,and it is suitable for scutellariae radix effective parts invitro percutaneous penetration fluid.This provides the reference for the f urther development of extemapreparation for EPSR and other pharmaceutical research to provide the reference.3 Preparation of EPSR cataplasm Choose incomplete and polyacrylic acid sodiu-m NP700 as cataplasm skeleton material,povidone PVPK30,sodium carboxymethyl cell-ulose as tackifier,kaolin as the filling agent,hydroxy aluminium as the crosslinking age-nt,citric acid as the crosslinking regulator,glycerol as moisturizing agent.According to s ingle factor and orthogonal test of EPSR cataplasm for the study of prescription and pro cess,finally select the prescription and process as follows:take 2%incomplete poly acry lic acid sodium NP700,0.3%gump hydroxyl aluminum,1.5%sodiumcarboxymethyl cellulos-e,2%kaolin,3%azone,5%propylene glycol di-spersed in 25%glycerin in phase ?;dr-ugs to join the phase ?;take 0.3%citric acid,2.1%PVPK30 and 0.06%phydroxy benz-oic acid ethyl ester,adding suitable amount of water,magnetic stirr-ing until liquid pha-se is clear as phase ?,With the phase ? add in phase ?,stir well,a-pply nonwoven fab-rics.Placed at room temperature,at the air dry natural overnight,covered the polyethyle-ne film.In initial adhesion force,adhesion force,sensory evaluate on,and the permeabil-ity in vitro experiments Q24 cumulants as evaluation index,study drug loading capacity,t he results proved that when the drug was 15%more appropriate.By in vitro permeation test,examines the single transdermal promoter and bi-nary compound transdermal prom-oter on the cataplasm preparation of drug release,The results showed that 3%azone +5%propylene glycol dual accelerator penetration effect isobvious;through the amount of total flavonoids is greater than its monomer composition,the permeability of monomer c o-mposition order:baicalein>wogonin>baicalin>oroxylin>wogonoside>oroxylin-A-glucoside.4 Research about preparation and in vitro permeability of EPSR ointment va-seline as matrix,according to the conventional preparation of EPSR ointment.study by penetration test in vitro,the results showed that the ointment of scutellariae radix perme-ability is greater than excluding transdermal promoter cataplasm,less than 3%azone +5%propylene glycol cataplasm.5 The different method of EPSR pharmacokinetics in vivo Comparison of lava-ge,cataplasm and ointment dosing in SD rats about concentration-time cu-rves and the r elate of permeation kinetic parameters.Results show that the monomer co-mposition were obvious bimodal phenomenon though lavage,but drug percutaneous delivery system is u-nimodal.Transdermal drug delivery preparation relative bioavailability vs oral effect is go-od,relative bioavailability of cataplasm paste is better than ointment,which consistent w-ith the results of in vitro permeation.