Preparation And Quality Evaluation Of Vitamin D₃ Microcapsule And Calcium Tablets

Purpose As a calcium supplement,vitamin D₃ can promote the absorption and utilization of calcium.However,the stability of vitamin D₃ is poor.Compound calcium carbonate/vitamin D₃ tablets sold in the market are usually coated with thin film to improve their stability.Organic solvents are often used in the manufacturing and coating process of calcium supplement tablets,resulting in residual organic solvents,which can not guarantee the safety of production and use.Microencapsulation has the advantages of improving drug stability and increasing drug absorption.In this paper,vitamin D₃ microcapsules were used as intermediates to prepare compound vitamin D₃/calcium carbonate tablets.The formulation and process of vitamin D₃ microcapsules calcium tablets were optimized by computer mathematical model.The prepared vitamin D₃ microcapsule calcium tablets can not only improve the safety of production and use,but also increase the stability of vitamin D₃,and expect to have better calcium supplementation effect.Methods In the preparation of vitamin D₃ microcapsules,the homogenization temperature,solid content,shell-to-shell ratio and core-to-shell ratio were taken as independent variables,and the total evaluation normalization values of drug loading,encapsulation rate and yield were dependent variables.In the preparation of vitamin D₃ calcium tablets,the prescription dosage of polyvinyl ketone K30,microcrystalline cellulose 101 and microcrystalline cellulose 102 were taken as independent variables,and the total evaluation normalization values of drug loading,tablet hardness and tablet weight differences were taken as independent variables.It is a dependent variable.BBD-RSM and CCD-RSM,which are more suitable for each experimental model,were used to design the experiment and optimize the prescription.Finally,it is validated according to their optimal prescriptions.The quality evaluation of vitamin D₃ includes drug loading,encapsulation efficiency,yield,morphological characterization,particle size analysis and stability evaluation.The quality evaluation of vitamin D₃ tablets includes drug loading,hardness,tablet weight difference,content determination,dissolution determination,content uniformity determination and stability evaluation.Results According to single factor investigation and star design-response surface methodology,the optimum formulation of vitamin D₃ microcapsules was determined as follows: homogenization temperature 70 ?,solid content 26%,shell material ratio 1:1,core-shell ratio 1:4.The optimum prescription of vitamin D₃ calcium tablets was 4.92 g for polyvinyl ketone,1.73 g for MCC101 and 4.22 g for MCC102.The results of the optimum formulation and process validation and stability test showed that the prepared vitamin D₃ microcapsules and vitamin D₃ microcapsules calcium tablets were better.Conclusions The preparation of vitamin D₃ microcapsules and vitamin D₃ calcium tablets is feasible,and the optimized process and formulation are proved to be feasible in practice by validation experiments.The mathematical model established by Box-Behnken Design and Central Composite Design-response surface method has accurate predictability.The quality of vitamin D₃ microcapsules and vitamin D₃ tablets showed that the self-made vitamin D₃ microcapsules and vitamin D₃ calcium tablets had high quality.Vitamin D₃ microcapsules can be used as intermediates or products directly.It not only achieves the purpose of experiment,but also provides a reference for industrial production.