Preparation And Evaluation On The Solubility And Absorption Of Albendazole Nanometer Powder

Objective:the preparation techniques and evaluation on the solubility and absorption of Albendazole nanometer powder are studied to enhance its bioavailability and lay the foundation for the research and application of nanoparticle preparation.Methods:the average particle size and the distribution of particle size in Albendazole nanoparticle suspension,the average particle size and the distribution of Albendazole nanometer powder,the Albendazole concentration after the centrifugation of the suspension and the water solubility of Albendazole nanometer powder as taken as the indicators.In this way,the paper aims at selecting and screening the categories and concentration of dispersant for preparing the Albendazole nanometer powder.Firstly,the high-speed shearing technology is adopted to prepare the initial suspension of Albendazole and the comprehensive score for average particle size of initial suspension of Albendazole and Albendazole concentration in supernatant after centrifugation is taken as the indicator.The best technical parameters of high-speed cutting process are screened by carrying out the single factor experiment and orthogonal experiment;Secondly,the high-pressure homogenization is adopted to prepare the Albendazole nanometer suspension.The average size of the Albendazole nanometer suspension is taken as the indicator.The best technical parameters of high-speed cutting process are screened by carrying out the single factor experiment and the quality evaluation of the Albendazole nanometer suspension is also carried out;then 4 drying processes as atmospheric-pressure drying,vacuum drying,spray drying and freeze drying are used to Albendazole nanometer powder.After that,the yielding rate of the nanometer powder,repose angle of the powder,the rate of recovery of Albendazole,the average size of the nanometer powder after hydration and water solubility of Albendazole nanometer powder are taken as the indicators.The best drying process,the corresponding technical parameters and the categories and concentration of drying protective agents are screened by single factor experiment.The qu ality evaluation of the Albendazole nanometer powder is also carried out;finally,the equilibrium solubility,oil-water partition coefficient and dissolution rate in vitro and Ussing Chamber test are measured,its solubility and water absorption performance is evaluated by comparing to the Albendazole material.Results:the two dispersants of Albendazole nanometer powder to be prepared are Poloxamer 407 and Twain 80.Their mass ratios to the Albendazole are respectively 1:1 and 1:2.The high-speed shearing technology is the optimum process for preparing the primary suspension of Albendazole:shearing speed is:24000 r/min,shearing time is 10min,the shearing temperature is 20?;The high-speed shearing technology is the optimum process for preparing the pri mary suspension of Albendazole:the sample concentration of Albendazole is 2%,the homogenization pressure and times are respectively 15000Psi15 and 20000Psi15 in combination,the homogenization temperature is 20?.The average particle sizes of Albendazole suspension prepared by the two kinds of dispersants are respectively 336.52nm±8.36nm and 272.36±7.56nm.They have good stablity within 72 hours;the spray drying is used as the drying technique,the drying protective agent is hydroxypropyl beta cyclodextr in with the concentration being 10%,it is the optimum process for preparing the Albendazole nanometer powder;the inlet temperature is 180?,the inlet speed is20mL·min^-1,the spray velocity is 5000ml/h,the prepared Albendazole nanometer powder is the white powder with the repose angle being smaller than 30°,the particles are dispersed uniformly after 30 seconds of hydrationand the particl es are small and highly dispersed under transmission electron microscope.The average particle sizes of Albendazole nanometer powder made by the two different dispersants are respectively362.43nm±3.98nm and 359.92±0.94nm.The equilibrium solubility,oil-water partition coefficient,dissolution rate in vitro and absorption rate constant and apparent permeability coefficient of Albendazole nanometer powder are all improved compared to that of the Albendazole raw material.Conclusion:the process of preparing Albendazole nanometer powder by adopting high-speed shearing and high-pressure homogenization spray drying technology is stable and good in reproduction.The appearance,the fluidity and dispersion after hydration of the prepared Albendazole nanometer powder are good,the average particle size of Albendazole after hydration meets the standards required by“Guidelines for Particle Preparation”of“Chinese Pharmacopoeia”.The particle size is also uniform.After the nanocrystallization of Albendazole raw mat erial,its solubility and absorption are improved significantly,which has laid a certain experimental basis for the research and development of Albendazole nanoparticle preparation in the future.