Hot Melt Pressure Sensitive Adhesive Wet As The Injury Acetanilide Experimental Research

Objective:In order to develop an new type of SIS Hot-melt pressure sensitive adhesive patch, to find a substitute of the traditional rubber patch, and to solve the problem in life and clinical use that the traditional rubber patch had large excitability and easy to cause allergys; we compered the preparation process of two different stroma of ShangShi ZhiTong Gao Patch;And then drafting quality standards of Hot melt pressure sensitive adhesive ShangShi ZhiTong Gao patch, which is not only have a nice stability and a well adhesion to skin.; Finally conducting a test on the release regularity and the in-vitro transdermal, then contrasted drug release property of two different kinds of ShangShi ZhiTong Gao Patch, the result provide information for the development of hot melt pressure sensitive adhesive patch.Methods::1The study on process:comprehended the original rubber stromal technology:The new technology used comprehensive adhesion (initial tack, holding tack, peel degree) and comprehensive physical properties (formability, flexibility, toughness, comfort, glide) of pressure-sensitive adhesive as indicators, in order to study on raw material selection> dosage screening test and optimization of the preparation technology, and then examining the drug carrier for pressure sensitive adhesive; Contrasting the rubber stromal and the hot melt pressure sensitive adhesive stromal through the relevant literature.2The study on the quality standards for the Preparation:The Atropine Sulfate fluid extract in The New ShangShi ZhiTong Gao Patch were identified by TLC. The weight variation of the preparation were tested according to the method described for adhesive ointment in2010China Pharmacopeia below the relative volumes of appendix I I. The content of atropine sulfate^Strychnine> Brucine in the ShangShi ZhiTong Gao Patch was determined by HPLC. The chromatography conditions were that the Agilent SB-C18(250mmx4.6mm,5μm) column was used; that mobile phase was composed of Acetonitrile-O.Olmol/L sodium1-heptanesulfonate and0.02mol/L KH2PO4equivalent mixture(used10%phosphoric acid regulating PH value to2.8)(21:79); the flow rate was1mL/min with UV detection at260nm, and that the column temperature was30℃3The study on the release rate and the in vitro percutaneous absorption rate:The equipment of release and aptitude percutaneous absorption were used to carry out the experiments of two different stroma of ShangShi ZhiTong Gao Patch. The content of Strychnine、Brucine、 Atropine Sulfate released and in vitro permeated from ShangShi ZhiTong Gao Patch were determined by HPLC. Calculated the release rate and the in vitro percutaneous absorption rate of rubber ShangShi ZhiTong Gao Patch and hot melt pressure sensitive adhesive ShangShi ZhiTong Gao Patch, contrasting the drug release property between two different stroma of ShangShi ZhiTong Gao Results:1Through the experiment selection that determined raw material of Hot melt pressure sensitive adhesive choose SIS1105as skeleton material, rosin derivatives as tackifier, liquid paraffin as plasticizer. And the prescription ratio of raw material was SIS1105:Rosin derivatives:liquid paraffin (100:120:50); The preparation conditions:reaction temperature wasl20℃, reaction time was30min, coating temperature was90℃; and the optimum temperature of medicine mixed in stromal was105℃. Compared to rubber stromal, hot melt pressure sensitive adhesive stromal had obviously superiority. New hot melt pressure sensitive adhesive patch will replace tradition rubber patch.2The study on the quality standards:TLC was used to identify Belladonna in Hot melt pressure sensitive adhesive ShangSh ZhiTong Gao Patch preparation. The examination of the weight variation of the patch preparation were right to the regulation. Determined the content by HPLC:the determination of Strychnine and Brucine had shown that retention time of the chromate graphy were16.8min and14.0min, the measured peaks and other peaks well separated; Raw Strychnos negative reference substance sample solution without interference; the liner rang were0.53-53.0μg-g-’and0.5-50.0μg.g-1(R2=0.9995), and the precision RSD were0.50%and0.81%; The Stability RSD were0.75%and2.69%, sample solution was stable within16h; The redupplicate RSD were4.90%and2.63%; And the average recovery were90.68%and100.10%, with RSD were2.94%and1.18%; Three batches of Hot melt pressure sensitive adhesive ShangShi ZhiTong Gao Patch in which the content of Strychnine were22.12μg.g-1,22.56μg.g-1、22.93μg.g-1、 and content of Brucine were15.52μg.g-1、15.07μg.g-1、15.84μg.g-1、3The study on the release rate and the in vitro percutaneous rate:The cumulative permeation rate of strychnine. Strychnine, Atropine sulfate from Rubber ShangShi ZhiTong Gao Patch within72hours were54.90%.50.24%,46.54%;and the release rate in the30%ethanol saline were92.29%,81.77%.53.28%in24hours;And the cumulative permeation rate of strychnine, Strychnine, Atropine sulfate from Hot-melt pressure sensitive adhesive ShangShi ZhiTong Gao Patch within72hours were53.25%,74.52%.34.32%;and the release rate in the30%ethanol saline were49.62%,82.25%,25.76%in24hours,Conclusion:prepared of Hot-melt pressure sensitive adhesive ShangShi ZhiTong Gao have well skin-adhesive, release rate and skin permeability. Through the preparation of technology, studying on in-vitro permeated and release rate of the regularity, drawing up the quality standards, laid a good foundation for development of pressure-sensitive adhesive matrix for Plaster preparations.