The Research Of Sustained Release Delivery System Of Sanao

Objective:First studying on the extraction are investigated.Through the study of the compatibility of the drug found compound fried is better.Methods:(1)Single factor experiment of compound fried and single herb decoction points comparative is studied.Single factor test studys different extraction solvent on the extraction rate of the active ingredients.In the amount of water,extraction time and extraction times investigated factors by L9(34)orthogonal test,preferably optimum extraction parameters.(2)By macroporous resin adsorption separation technology extract refined soup.Single factor experiment of macroporous resin types(D-101、HPD 100、HPD 300、AB-8、XAD-7、ADS-17、HPD 500、HPD 600),resin column diameter to height ratio,loading conditions(liquid concentration,sample flow rate and pH value),impurity elution conditions(kind and amount of elution solvent,the elution flow rate),the active ingredient elution conditions(kind and amount of elution solvent,the elution flow rate)were optimized.(3)BY LC method and HPLC-based method fort and determination of quality standards established three local soup refined intermediates.The purified intermediate carry physicochemical properties and pharmacokinetic studies which clear the main active ingredient in the intermediate half-life in vivo pharmacokinetic basic parameters for the design and preparation of sustained release tablets Sanao basis.(4)Single factor test and design-response surface methodology for the preparation of sustained-release tablets prescription Sanao optimization.Single factor test method for the preparation of particles and tableting methods of preparation molding process parameters were optimized.(5)By TLC on Sanao sustained release tablets of ephedrine,licorice and bitter almond identification.HPLC method for simultaneous determination of S anao sustained-release tablets of ephedrine,pseudoephedrine,licorice acid and amygdalin.Sustained performance using the in vitro release test evaluated Sanao sustained-release tablets which establish the quality of standards Sanao sustained release tablets.(6)To study stability of sustained-release tablets of Sanao initially by high temperature,humidity,light and acceleration testResults:(1)Extraction method has great influence on the rate of extraction of ephedrine and other four index components.Ephedrine and extraction transfer rate of glycyrrhizin in the compound are fried in greater than points decoctions,extracts transfer rate of pseudoephedrine is highest in ephedra and bitter almond compatibility extracted transfer rate of amygdalin in ephedra and bitter almond Combinations highest.This extraction method for the preparation of water as co-solvent compound mention.Orthogonal test shows that:the number of ephedrine extract on the extraction rate and other four ingredients have significant,and the impact of water extraction and processing time on the extraction rate is no significant.The optimum extraction parameters are A2B1C3,ten times the amount that is added to boiling water three times an hour.(2)Macroporous resin HPD 300 had the best adsorption and desorption properties.In the course of adsorption,the optimum concentration of the sample liquid was 1.67 g crude drugs of per milliliter,the resin column size ratio was 1:7,the concentration of sample solution was 0.6 g/mL crude drug,the sample flow rate was 4.0 BV/h.In the course of elution,2 BV deionized water was used and the resin column chromatography was eluted with 5 BV of 70%EtOH by flow rate of 4 BV/h.(3)Sanao soup refined intermediates gavage rat that the pharmacokinetic results showed that:ephedrine hydrochloride and pseudoephedrine hydrochloride AUC(0-t)is 746.03 and 415.634 respectively;MRT(0-t)is 138.066 and 115.355 min respectively;Cmax is 5.564 and 3.898 mg/L respectively,t1/2 is 110.93 and 83.189 min respectively.Since nearly half of ephedrine hydrochloride 2 h,pseudoephedrine hydrochloride close 1.5 h,in order to avoid frequent dosing,the soup made from sustained release drug delivery system is feasible and reasonable.(4)To optimize prescription by single factor experiment and central composite design-response surface which the best prescription is HPMCK4M 160 mg,MCC 90 mg,the main drug 250 mg,magnesium stearate 1%.Optimum molding conditions are:weigh prescriptions intermediates and accessories,by 100 mesh sieve,using the same amount of incremental approach to make it fully mixed with anhydrous ethanol and made soft material,through a 24-mesh sieve granulating at 60℃,granulated particles are passed through a 24 mesh screen,add 1%magnesium stearate,and mix with a diameter of 1 mm dimple die in tableting on single punch tablet press,tablet weight control is 0.50g.(5)The method of a sustained release tablets Sanao ephedra about almonds and licorice TLC is established.HPLC method for simultaneous determination of Sanao sustained release tablets of ephedrine and other ingredients.Sanao sustained-release tablets of ephedrine,pseudo-ephedrine,amygdalin glycyrrhizin content are 2.00%,1.41%,6.68%and 4.95%.The results show that in vitro release:2 hours cumulative release of 25%,60%cumulative 6 hours,12 hours accumulated release more than 90%,indicating that the phenomenon of sudden release of its release and has no obvious sustained release properties.Fitting model on release curve found that it met higuchi equation which explain the release mechanism is diffusion of the drug and dissolution in the regulation.(6)Sanao sustained-release tablets in the high-temperature test,humidity test,light test and accelerated test conditions are not significantly change.In the choice of packaging materials need to choose to avoid moisture absorption and should be sealed.Conclusion:Preparation process and quality standards Sanao Sustained Release Tablets is scientific and reasonable and feasible.