Different Material Properties Of Traditional Chinese Medicine (TCM) Effect On The Dissolution Of Baicalin And Rhein In Vivo And In Vitro Studies

Objective:Design the prescription and study the dissolution rate of baicalin and rhein in vitro and in vivo release rate,Determine the different properties of traditional Chinese medicine material effect on the dissolution of effective components from the pills,provide the basis for Chinese medicine materials science database established,through adjusting the variety and dosage of traditional Chinese medicine(TCM)for the next step change to pills of dissolution of the preparation of Chinese herbal medicine used to lay the foundation.Methods :1.The prescription design and the model of pill preparation.By early Chinese medicine materials classification select cassia twig,yam,tuckahoe,frankincense,almonds,stiff silkworm,gypsum,seven different material properties of traditional Chinese medicine as auxiliary materials,using the uniform design method to the material properties of different seven kind of traditional Chinese medicine as the seven factors,with all kinds of traditional Chinese medicine(TCM)in the prescription dosage of different ratio of level 12 prescription design,the relative contents of each prescription to join the same baicalin,rhein extract after extensive in the preparation of 14 batches of pills,and make sure the relative content is the same and check the general principles of the pills in each batch of model.2.the content determination of baicalin and rhein in model pills stripping liquid.Choose oar method of dissolution determination method to 900 ml of pure water as dissolution medium,set the dissolution speed of 100 r/min,37 plus or minus 0.5 ?,temperature keeping insulation 30 min before the start of the experiment,after the input model pills at different time points of sampling,remove the dissolution of liquid by high performance liquid chromatograph after 0.45?m head filtration in the sample.Chromatographic conditions for: Agilent SB-AQ C18 chromatographic column(5?m,4.6 mm * 250 mm).Mobile phase:acetonitrile – 0.1%phosphate water gradient elution,and the flow rate of 1 ml/min,column temperature 30 ?,detection wavelength:254 nm.3.The content determination of baicalin in rat plasma.Choose the representative model of the pills and grind into small particles and prepared into suspension solution,lavage the rats,0.5 ml blood was sampled from rat eyes on different time points after lavage,make the blood centrifuge tubed,precision measuring 200?l after centrifugal plasma,and precision measuring 50?l methanol mixed with plasma,add 1:1 ratio methanol mixture of acetonitrile 0.4 ml protein deposition,vortex learned after centrifugal clear liquid,with nitrogen gas blowing dry samples,residue with 1:1 ratio of 0.2% formic acid water mixed with methanol solvent in high performance liquid sample analysis.Chromatographic conditions:Agilent SB-AQ C18 chromatographic column(5?m,4.6 mm * 250 mm).Mobile phase: acetonitrile-0.1% phosphoric acid(30:70),water flow rate of 1 ml/min,column temperature 30 ?,detection wavelength:278 nm,determinate the content of baicalin in rat plasma.Results :1.Pellet as excipients cassia twig,yam,tuckahoe,frankincense,almonds,stiff silkworm,gypsum,the target component in vitro dissolution rate of baicalin,the equation for Y20 min = 0.427X1-0.967X4-0.693X5,(Y20min on behalf of the cumulative release rate of baicalin in each prescription after added the pills 20 min later,the X1 said poria cocos proportion in the material prescription,X4 said frankincense proportion in the material prescription,the X5 said almond proportion in the material prescription),poria cocos accelerate the dissolution of baicalin,frankincense and almond hold-up the dissolution of baicalin,the size relationship of the effect on the dissolution of baicalin is poria cocos> almond > frankincense,other auxiliary materials is not obvious influence on dissolution of baicalin.2.Pellet as excipients cassia twig,yam,tuckahoe,frankincense,almonds,stiff silkworm,gypsum,the target component in vitro dissolution rate of rhein,the equation for Y30min=0.282X1-0.674X5-0.431X6,(Y30min on behalf of the cumulative release rate of rhein in each prescription after added the pills 30 min later,the X1 said cassia twig proportion in the material prescription,X4 said almonds proportion in the material prescription,the X5 said stiff silkworm proportion in the material prescription),cassia twig accelerate the dissolution of rhein,stiff silkworm and almond hold-up the dissolution of rhein,the size relationship of the effect on the dissolution of rhein is stiff silkworm > almond > cassia twig,other auxiliary materials is not obvious influence on dissolution of rhein.3.the process of model pills in vitro dissolution experiment,can be seen from the curve of cumulative dissolution percentage of baicalin ingredients dissolution speed order also in the order:12> 9>1.Of three groups of rats maximum blood drug concentration time lavage prescription of 12 groups of rats predated lavage prescription 9 groups of rats,gastric prescription 9 groups of rats and earlier than lavage prescription 1 in rats.Conclusion :1.Fiber,starch,fat,protein,polysaccharide,resin,mineral materials with different properties such as pills certain quantitative relationship exists between the dissolution parameters,including polysaccharide has obvious promoting effect to baicalin dissolution,grease,resin has inhibition;Protein has obvious inhibition to the rhein dissolution,oil also has inhibitory effect,stimulates fiber class;The grease of baicalin and rhein has inhibitory effect.2.The dissolution rate in vitro and in vivo absorption of baicalin speed consistent.3.In traditional Chinese medicinal materials as auxiliary materials in the preparation of pills,the dissolution of effective components from the material properties of pills velocity have obvious effect...