| Wet granulation is an important process in the pharmaceutical industry.It is a method to prepare particles by means of the bridge or bonding effect of adhesive or wetting agent.However,there is no scientific basis for the selection of excipients and binder types and amounts in granulation,and the influence of the types and amounts on the quality properties of the particles is unknown.This topic is aimed at the selection of excipients and adhesives in the process of wet granulation,with four kinds of commonly used excipients(lactose,starch,microcrystalline cellulose,dextrin)and two kinds of commonly used adhesives(PVP and HPMC)as the research object,the properties of excipients,binding properties between adhesives and excipient.To find the internal relationship between them,in order to establish the relationship between materials and the type and amount of adhesion,to provide a theoretical basis for the scientific realization of granulation process,the main results of this research are as follows:(1)The bulk density of lactose powder of different specifications is G-70 > G-140 > G-200,and the vibration density has the same law,and the Carr index is G-70 < G-140 < G-200.The bulk density of MCC is 0.298 g/ m L,the vibration density is 0.496 g/ m L,and the Carr index is 0.399.The bulk density,vibration density and Karl index of starch were 0.417 g/ m L,0.603 g/ m L and 0.335 respectively.The bulk density,vibration density and index of dextrin were 0.385 g/ m L,0.706 g/ m L and 0.454 respectively.The hygroscopicity of lactose was G-70 < G-140 < G-200.The hygroscopicity of MCC,starch and dextrin was 7.83 %,11.69 % and 2.26 % respectively.The angle of rerest of lactose excipients with different particle sizes was G-70 < G-140 <G-200,and the powder flow time had the same law.The angle of repose of MCC is 45.2 °,and the flow time is 14.38 s.The angle of rerest of starch was 44.3° and the flow time was 13.14 s.The Angle of rerest of dextrin was 48.2 ° and the flow time was 16.52 s.(2)In the experiment of saturated powder absorption of different adhesives to different excipients,we found that with the increase of time,the saturated liquid absorption of lactose increased,and the powder absorption rate of lactose decreased.The saturated powder absorption of lactose G-70 was: water > 0.5% > 1.5% > 3.0%,and the saturated powder absorption decreased with the increase of adhesive concentration.G-140 saturated powder absorption is: water > 3.0% = 1.5% > 0.5%,G-200 saturated powder absorption is: water >3.0% > 1.5% > 0.5%,G-140,G-200 saturated powder absorption increases with the increase of adhesive concentration,the law is just the opposite with G-70.The influence of adhesive PVP K30 on the absorbance of MCC powder was not affected by the amount of adhesive,and the influence of adhesive concentration on the absorbance was not significant.With the increase of time,the fluctuation range of adhesive PVP K30 powder absorption is not large,but the change trend of powder absorption rate is the same,both of them decrease with the increase of time,and finally constant at a certain value.(3)In the process of wet granulation of four excipients,the amount of lactose is the least when selecting the amount of adhesive.Lactose particles of the three specifications are mainly concentrated between 80 mesh and 120 mesh screens.The proportion of lactose particles of three different sizes in 80-mesh screen was in the order of 1.5% > 3.0% > 0.5%,and decreased with the smaller particle size,that is,G-70 > G-140 > G-200.With the decrease of lactose particle size,the proportion of fine powder increased after the whole grain,and it could be found that the proportion of fine powder was G-200 > G-140 > G-70.The yield of lactose G-70 and G-140 was 1.5%>3.0%>0.5%,and that of G200 was 0.5% > 1.5% > 3.0%.Among them,1.5% PVP K30 and G-70 achieved the highest rate of 66.26%.This indicates that the particle size of the material and the concentration of the binder will affect it.With the increase of adhesive concentration,there was no significant change in the proportion of large particles in MCC particle size distribution after wet granularization.It should be that the type and concentration of adhesive did not increase the cohesive force of MCC,and the relative homogeneity index of particles of different adhesives did not change significantly.The particle size distribution after granulating is relatively obvious from the table,with most particles concentrated in 40 mesh to 80 mesh.However,the particle yield is not significantly affected,and the particle yield is about 60%,which is not affected by the type and concentration of adhesive,and the yield is good and stable.Most of the particles produced by adhesives with different concentrations are concentrated between 40-80 mesh,and the particle size distribution is relatively concentrated,and the distribution of particles with more than 200 mesh is less.No matter what kind of concentration of adhesive,particle yield is basically more than 70%,except for 1.5%PVP yield is slightly smaller,other concentration yield is general,among which 0.5%PVP yield is the largest,reaching 83.5%. |
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