Study On Formulation Experiment And Preparation Of Meloxicam Nanosuspension

It is estimated that about 40% of pharmaceutically active compounds are currently insoluble in water,which problem has hindered the further development and utilization of these active substances.Therefore,more and more methods to solve this problem have appeared,such as adding a cosolvent to form a solid.Dispersions,emulsions,nanoparticle carriers,etc,but these methods require the addition of a large amount of co-solvent or organic solvent,which can cause serious toxic side effects to the human body.The nanosuspension technique is a submicron colloidal dispersion that is formed by mechanical force or precipitation to reduce the drug particles to the nanometer scale and stabilized by a surfactant.The technology does not need to add too much excipient or carrier matrix,and has the advantages of good solubility,high drug loading,low cost and wide range of drug use.Meloxicam(MLX)is not only an anti-inflammatory and analgesic drug,but also has been reported that MLX can also be used as a candidate for anticancer drugs,but the poor water solubility at physiological pH hinders the wide application of MLX.This topic model drug is MLX.The subject mainly uses the grinding method,high pressure homogenization method and precipitation method to prepare MLX nanosuspension.In the experiment,the single factor experiment was carried out on the concentration of the surfactant,the amount of grinding medium and the concentration of the drug in the grinding method to determine the optimal range.On the basis of the response surface design,the particle size was used as the reference index,and the final analysis was obtained.The optimum condition is that the ratio of grinding ball to water is 1:2(volume ratio),the drug concentration is 1%,the surfactant concentration is 0.5%,and the suspension prepared according to this condition has a particle size of 443 nm;high pressure homogenization method,single factor experiment Determine the optimal range of cycle pressure,number of cycles and drug concentration.On this basis,the optimal conditions for the response surface design are 1300 bar,the number of cycles is 20,the drug concentration is 1%,and the obtained particle size is 374 nm.The influencing factors of Ultrasound-precipitation method mainly consider the ultrasonic power,the concentration of the drug in the organic solvent,the comparison of the organic phase with the water and the dosing mode.The single factor determines the optimal range of the main factors,and the response surface design determines the optimal preparation condition as the ultrasonic-precipitation.The conditions were as follows: ultrasonic power was 600 W,the concentration of the drug in the organic solvent was 4%,the ratio of DMSO to water was 1:4,and the obtained suspension had a particle size of 339 nm.This subject mainly uses two methods to prepare capsules,one is the traditional two-step method(first freeze-dried into powder and then prepared),and the nanosuspension is dried into powder,which is often complicated;the other method is creative in this experiment.The nanosuspension was directly used as a wetting agent for the preparation of capsules.This method eliminated the freeze-drying step,and at the same time,the capsules prepared by the two methods were eluted and found that the new method showed an advantage in dissolution rate compared with the two-step method.In this experiment,different excipients were used in the preparation of capsules.It was found that lactose capsules were more advantageous in the final drug release than starch capsules.In this experiment,the lyophilized powders prepared by different methods were tested for redispersion.The lyophilized powder of the high pressure homogenization method has good redispersibility,but the lyophilized powder obtained by the precipitation method cannot be redispersed,and the capsule prepared by the lyophilized powder is relatively low in dissolution,which proves for the first time that organic.The solvent affects the freeze-drying process,which in turn affects the redispersion of the lyophilized powder and the dissolution of the capsule,which may be the reason why the precipitation method has not been widely used.Finally,the subject is compared by comparing nanosuspension,MLX bulk drug,nanosuspension capsule and raw material capsule,which proves that the preparation of nanosuspension has advantages in improving the dissolution rate and bioavailability of MLX drug.