Pharmaceutical Reserach Of Ligusticum Chuanxiong Oil Microcapsule Gel Paste

The microcapsule gel paste of Chuanxiong oil was prepared with the volatile oil of Lligusticum chuanxiong as the main medicinal component,it had the effect of invigorating blood circulation and activating pneuma,removing wind and relieving pain.It was applied in the syndrome of blood stasis and pneuma stagnation pain,headache,rheumatic arthralgia,it was an important medicine for treating headache.Currently,Chinese patent medicines for migraine on the market were mainly oral preparations.Gel paste had the advantages of avoiding"first pass effect"and easy to carry,but because the volatile oil had the character of unstable to heat,light and easy oxidation,it applied to the cataplasm was easy to produce the phenomenon such as oil bleeding.Therefore,through the preparation of the microcapsule as intermediates to improve its stability,in order to provide references for the application of volatile oil to cataplasm preparation.This study mainly included the following four aspects.1.In the resrach of Chuanxiong volatile oil extraction processBy using steam distillation and the yield of volatile oil was taken as the evaluation index,The optimum extraction process was determined by single factor investigation and orthogonal test,the optimal extraction technology of Chuanxiong volatile oil was the coarsest powder of chuanxiong addded 8 times water for 2 h and the extraction time was 10 h.2.In the resrach of chuanxiong oil microcapsule preparation technologyThe preparation was carried out by complex condensation method.Taking sedimentation rate,drug-loading capacity and encapsulation rate as evaluation indexes,The optimal range of process parameters was screened by single factor and the factors with significant influence on microcapsules were optimized by plackett-burman design,Furthermore,the interaction between gelatin concentration,gum Arabic concentration and capsule core:capsule material ratio was investigated.The moisture,solubility,sedimentation rate,drug-loading capacity,encapsulation rate,particle size and ZETA potential of microcapsule samples were comprehensively analyzed.The optimal process was wall material concentration was 3%,core-wall ratio was 50%,emulsifying speed was 15000 rpm,stirring time was 1h,and complex coacervation p H was 4.1.The quality of microcapsules prepared by the optimal process was evaluated.The appearance was exquisite and uniformity powder.Optical micrograph analysis,differential scanning calorimetry and infrared spectrum all showed that chuanxiong oil were encapsulated in the wall material,the average particle size was 252.4 nm,ZETA potential was 15.0 mv,PDI value was 0.190,The particle size distribution range was concentrated and the system was stable.Release degree in vitro showed that the microcapsule had no sudden release effect,The cumulative release rate of 12 h was65.45%.The stability test results showed that the microcapsule can effectively improve the humidity and heat stability,but the light has a big effect on it.So in the process of production,transportation and storage should avoid light as far as possible.3.In the forming process of Chuanxiong oil microcapsule gel pasteThe matrix’s initial viscosity,uniformity,spreadability,skin pursuance,residual amount,backing layer exudation degree,the number of bubbles were taken as the comprehensive score,Single factor was used to screen excipients and their optimal application range,and the formulation was optimized by D-optimal mixture design.Taking the comprehensive score of initial viscosity,adhesion force and peel strength as indicators,The optimal preparation process was obtained as NP700:1.25 g,glycerol:5g,kaolin:0.25 g,glyoxyaluminum:0.025 g as phase I.Microcapsules:0.5 g,pure water:5 ml and tartaric acid:0.025 g were used as phase II.0.3%kapom 940:7 g as phase III.Phase II was heated to 50℃to dissolve the microcapsules,phase I was slowly added and stirred evenly.Phase III was added.then it was Stirred until uniform and immediately applied to nonwoven fabric.Relevant inspection of gel paste were carried according to the 2015 edition of the Chinese pharmacopoeia.Chuanxiong oil microcapsule gel paste was pale yellow,The TLC identification method of chuanxiong volatile oil were established,the gel paste content was 15.577 g/cm~2,the Ligustilide content of each patch was not less than 25.00 mg,The initial viscosity was no less than9 ball,the adhesion force was no less than 30 min,peel strength was not lower than 0.2kgf,shape forming ability,heat resistance,cold resistance,content uniformity are in line with the provisions,The application of Ligusticum chuanxiong oil microcapsule to gel paste has significantly improved the unstable properties of Ligusticum chuanxiong oil.4.In the study of mechanism and irritant of treating migraine with Chuanxiong oil microcapsule gel pasteThe migraine model rats were replicated by subcutaneous injection of nitroglycerin into the neck.Compared with the positive drug compound bauhinia wound removing cataplasm and indomethacin cataplasm,medium and high dose chuanxiong oil microcapsule gel paste could significantly reduce the behavior characteristics of ear red and head scratching,reduce the CGRP and 5-HT content in plasma,It meant that could significantly improve the symptoms of migraine rats.And the guinea pigs skin irritation test was investigated,the results showed that each gel paste had no irritation.