Preparation Of Hesperidin Sustained-Release Pellets And Study On Pharmacodynamicsby

Hesperidin(Hesperidin,HPS)is also called Chuanpisu;dihydroflavonoid glycosides are white or light yellow crystalline powders,insoluble in ethanol or water.Hesperidin is a vitamin drug that can effectively reduce the fragility of capillaries,enhance the toughness of capillaries,prevent capillary rupture and bleeding,and protect capillaries.Therefore,hesperidin can be used in the adjuvant treatment of hypertension.Hesperidin is used as a raw material for pharmacy in the pharmaceutical industry and one of the main components of the Chinese patent medicine Maitong.In this study,used tangerine peel as raw material,using cellulase pretreatment combined with hot reflux extraction to optimize the extraction process of hesperidin,and.discuss the best process parameters for the preparation of hesperidin sustained-release pellets;using ultraviolet The UV absorption value of hesperidin sustained-release pellets under 285nm under simulated artificial gastric juice was detected by a spectrophotometer at different times,and the in vitro release of hesperidin sustained-release pellets was calculated by the measured regression equation.In order to prepare a finished drug product with a relatively uniform in vitro release rate,a blocker research has been conducted on the in vitro release of the drug,and a high efficacy has been achieved.The main results obtained are as follows:(1)In order to explore the best extraction factors for hesperidin from tangerine peel,the cellulase pretreatment of tangerine peel meal combined with ethanol was used to extract hesperidin from tangerine peel.The extraction temperature,material-to-liquid ratio and extraction time were carried out by single factor experiments,and finally the optimal extraction process parameters of hesperidin sustained-release pellets were determined.In an aqueous solution with a pH of 4.8,the pectin and cellulose in the tangerine peel were destroyed after pretreated with cellulase for 1.5 h at a temperature of 45℃,maked the hesperidin in the tangerine peel easier to dissolved when used ethanol as a solvent and thhe hot reflux extraction method was used for dissolution.The results showed that the optimal process conditions for extracting hesperidin from tangerine peel were temperature 85℃,time 3 h,70%ethanol by volume,and the ratio of material to liquid was 1:25.Under this extraction process,the extraction rate of hesperidin was 5.99%.The entire operation process was stable and the cost was low,which was suitable for industrial production.(2)Used tangerine peel as raw material,the hesperidin obtained by cellulase pretreatment combined with hot reflux extraction method was further used to separate and purify the crude hesperidin powder by recrystallization,and the purity was detected by ultraviolet spectrophotometry,and the separation was measured.After purification,its purity was 84.20%-84.29%,and the separation and purification effect was better.(3)The extrusion-spheronization method was used for the preparation of sustained-release pellets of hesperidin.The operation process parameters of extrusion spheronization are as follows:the extruded raw materials were extruded using a 5 mL syringe to ensure that the extruded raw materials were mixed Uniform and dense,the extrusion operation repeated 5 times.The rotary evaporator was used for the spheronization operation for 30 minutes,only the rotary button was turnned on,and the spheronization was performed after drying.At the temperature of 50℃ and treatment time of 12 h,the sustained-release pellets with uniform texture and smooth appearance were obtained.(4)By explored the preparation formula of hesperidin sustained-release pellets,the hydroxy propyl had been added in the formulation of hesperidin sustained-release pellets was fixed after the quality of hesperidin,ethyl cellulose,starch,and polyvinyl pyrrolidone were fixed.Exploring the ratio of methyl cellulose,blocker glyceryl monostearate,and microcrystalline cellulose,through single factor experiment screening,and orthogonal experiment,the results showed that:The addition amount of glycerol monstearate in the formula had the greatest influence on the release rate of hesperidin sustained-release pellets,followed by hydroxypropyl methyl cellulose,and microcrystalline cellulose had the least influence on the release rate of hesperidin sustained-release pellets.The optimal addition amount were hesperidin 2.0 g,ethyl cellulose 1.0g,starch 3.0g,and polyvinyl pyrrolidone 1.0 g,the glycerol monostearate 0.9 g,the hydroxypropyl methylcellulose 2.0 g,and the microcrystalline cellulose 9.0 g.This formula had a relatively uniform drug release rate and a reasonable economic cost.It has certain guiding significance for industrial production.