Study On Preparation Technology And Quality Standard Of Capsaicin Enteric Sustained-Release Microcapsule Tablets

Capsaicin has many positive effects,such as anti-tumor,anti-inflammatory,promoteing fat oxidation,lowering blood pressure,regulateing endocrine system,protecting cardiovascular,relieving itching,protecting nerves,resisting oxidation,and good analgesic effects.The development of capsaicin as a high-quality oral drug is of great significance,however,its high oral irritability limits the application of capsaicin severely.The purpose of this dissertation is to solve the problem of oral stimulation of capsaicin by using enteric-coated and slow-release microcapsules as a dosage form,and to develop an oral product using capsaicin.The compatibility of sodium alginate with capsaicin was verified by the compatibility test of raw materials and auxiliary materials.The results showed that sodium alginate had good compatibility with capsaicin.What's more,physicochemical method,spray drying method and microcapsule granulator method were all used for preparing microcapsules.The physicochemical method had a low encapsulation rate,the raw material is expensive,and the operation was cumbersome;The spray drying method has serious environmental pollution,microcapsule particle size was extremely uneven;The microcapsule granulator method was easy to operate,encapsulation efficiency was high,microcapsule particle size was controllable,microcapsules had uniform particle size.Therefore,the capsaicin enteric sustained-release microcapsules were prepared by microcapsule granulator method.After determining the preparation method of microcapsules,the optimal experiment of capsaicin microcapsule preparation process was selected out.The caliber of the microcapsule granulator,the ratio of sodium alginate solution and capsaicin,and choice of two capsaicin materials were investigated.The optimal preparation process for the final capsaicin microcapsules was as follows: the capsaicin raw material A was dissolved with a small amount of ethanol,then poured the capsaicin ethanol mixed solution into a 1.5% sodium alginate solution and stir until well mixed.The ratio of capsaicin raw material A to sodium alginate solution was1.3g: 200 mL,and the microcapsules were prepared using a 300 ?m pipette tip.The parameters of the microcapsule granulator were set to a frequency of 770 Hz and a flow rate of 18 mL/min.The results of microcapsule quality evaluation showed that the capsaicin enteric sustained-release microcapsules had uniform particle size,no adhesion,and an average particle size of 200 ?m.In vitro release experiments of microcapsules showed that the microcapsules had enteric and sustained release properties,and the capsaicinwas completely released.Through the screening and optimization experiments of tablet prescriptions,the optimal preparation process of capsaicin enteric-coated slow-release microcapsule tablets was finally determined as follows: Firstly,each accessory material was passed through 100 mesh nylon sieve,and weighed according to the dose in the prescription.Then,the capsaicin microcapsules were thoroughly mixed with polyfructose,mannitol,and crospovidone.The granulation was prepared by a dry granulator,and magnesium stearate was added to the granules according to the formulation amount and then uniformly mixed.Finally,the granules were tableted by a tableting machine.The tablet formulation was as follows: 21.4 g of capsaicin microcapsules,5 g of magnesium stearate,156.2 g of polyfructose,312.4 g of mannitol,and 5 g of crospovidone.In the quality standard study of capsaicin enteric-release microcapsule tablets,the appearance,drug weight difference,content uniformity,tablet hardness,friability,disintegration time limit,and tablet release of the tablets were respectively researched.The results of the study showed that all three batches of tablets met the pharmacopoeia standards and had enteric sustained release properties.The influencing factors of capsaicin microcapsules and the accelerated experiment showed that the tablets had high stability.In summary,the preparation process of capsaicin enteric-release microcapsule tablets is feasible,and the quality control method is scientific and reasonable.