Innovation Application Of Powder Modification Technology In Traditional Chinese Dispersible Tablets

Objective:The nature of intermediate is an important factor affecting the nature of the formulation.The problems of compliance and dissolution in GanKeShuangQing preparation are taken aspect, the form of raw materials is viewed as a starting point, the dosage of dispersible tablet is regarded as the carrier, the practicability of liquid dispersion technology and particle composite method used to mask bitterness and improve dissolution is investigated.GanKeShuangQing dispersible tablets prepared according to the above conditions are yellow, bitter, and its size is about 5mm,hardness is between 50～60N.Methods and results:With the disintegration time as the index, the auxiliary materials of GanKeShuangQing dispersible tablets are determined by single factor experimental design, Calcium sulfate or MCC, L-HPC,2% PVP in 60% ethanol, micro-silica gel.On this basis, the proportion of baicalin, andrographolide, calcium sulfate or MCC, L-HPC is determined as follows,50%,12.5%,22.5%,10%,5%; 50%,12.5%, 21%,11%,5.5%. It can significantly promote the disintegration that micro-silica gel is mixed with drugs before other accessories.The design method micro-silica gel loading baicalin and andrographolide is used, corresponding intermediates substitute drugs to improve the dissolution of raw dispersible tablets.The solubility of sbaicalin and andrographolide are measured through flask shaking method, solubility in methanol solvent are respectively 2601.13.13667.35μg/mL. It can be seen from the data, that both are poorly soluble drugs.The methanol is choosed as the solvent of liquid dispersion technology, the powder properties of micro-silica gel from different manufacturers are examined, the specification is initially identified, micro-silica gel prepared by gel method is suitable for dispersant; the dissolution is used as marker, the type of micro-silica gel is further preferred and the ratio of the carrier and the drugs is explored, the micro-silica gel from C manufacturer is screened as the dispersant, the proportion of baicalin, andrographolide and micro-silica gel is identified as 4:2:1.Drugs. carrier.corresponding liquid dispersed intermediate and mixture are characterized from the micro-structure, X-ray diffraction and the surface area and porosity.The results show the dissolution of liquid dispersion intermediate has a significant increase; micro structure differs from that of mix. the surface of intermediate is covered massive micro-silica gel; the specific surface area and porosity are between the drug and the micro-silica gel.The study shows that liquid dispersion technique can be used to improve the vitro solubility of dispersible tablets, and thus enhance the possibility of improving the bioavailability.Particle design principle is refered, and mechanical particle composite technology is applied, baicalin-andrographolide composite particles are builded, without additional accessories, the premise of suppressing bitterness can be achieved.The crushed law of baicalin is investigated, baicalin of appropriate particle size is selected as "shell particles", the results show baicalin powder smashed for 6min is appropriate, tasting evaluation criteria is established, the coating time of baicalin-andrographolide intermediate powder is screened, the bitterness of 6-min composite particles is the lightest;Drugs, carrier,corresponding particle composite intermediate and mixture are characterized from wetting, microstructure, IR spectra, X-ray diffraction areas.The study shows that the composite particle technology can be used to mask the bitter formulation and improve the compliance.The intermediate powders of liquid dispersion technology and particle composite method are made into corresponding dispersible tablets, the appearance shape and internal quality of three dispersible tablets are compared. The active ingredient content and dispersion uniformity of three dispersible tablets are little different,the difference is mainly reflected in the color, taste and dissolution.Compared with the other two groups, Gan Ke Shuang Qing dispersible tablets based on particle composite technology are more yellow and less bitter, the dissolution of Gan Ke Shuang Qing dispersible tablets bsaed on liquid dispersion technology is higher than the other two groups.The feasibility and scientific of liquid dispersion technology and particle composite technology used to improve the dissolution rate and mask the bitter taste of the drug are proved.Conclusions:The vitro dissolution of baicalin and andrographolide can be improved by liquid dispersion technology; the feasibility of particle composite technology used to relieve drug bitterness is explored, and the mechanism is explained.The scientificity of liquid dispersion technology and particle composite technology used for traditional Chinese medicine research is demonstrated.The full text provides new research ideas and technical reference for improving the bioavailability of insoluble drugs and covering bitterness of drugs and has certain theoretical value and practical significance for the enrichment and development of particle design technology.