| Clarithromycin is a kind of semi-synthetic macrolide antibiotic with broad-spectrum antibacterial activity,which can kill most bacteria and has a certain inhibitory effect on some mycoplasma.Clarithromycin is widely used clinically in various bacterial infections,such as upper and lower respiratory tract infections,skin and soft tissue infections,and genitourinary system infections,especially when treating children,showing good therapeutic effects.However,the oral bioavailability of clarithromycin is low,the taste is extremely bitter,and the injection administration is very irritating to the local area.The purpose of this study is to improve the bioavailability and compliance of the oral preparation of this product,mainly focusing on the formulation screening,process research and Properties evaluation of clarithromycin masking granules.The results show that the prepared clarithromycin taste-masking granules have good in vitro release and excellent taste-masking effect,and the process is easy for industrial production.(1)Pre-prescription research work of clarithromycin granules.With reference to relevant research data at home and abroad,the determination methods of clarithromycin APIs and Granules are studied to investigate their specificity,linearity,repeatability,recovery rate,etc.The experimental results show that the analytical method has good specificity and the linear range of detection concentration is100?g/m L?500?g/m L,linear equation is y=1082.3x+5678.7(R~2=0.9997),precision RSD is less than 4%,repeatability RSD is 1.0%,average recovery rate is 100.1%,using high performance liquid chromatography and sulfuric acid color method Determine the release in different media.(2)Determine the prescription and preparation process of clarithromycin taste-masking granules.The preparation methods were studied by centrifugal spheronization granulation method,swing mechanical granulation method,extrusion spheronization granulation method,sugar core coating method and coating pan method.It was determined that the final preparation process was extrusion spheronization-fluidized bed coating.The specific method is as follows:firstly,the clarithromycin is mixed with the excipients by wet method,then the drug loaded pellets are prepared by extrusion and spheronization equipment,and finally the pellets are coated by the prefabricated resin solution in the fluidized bed.The clarithromycin taste masking granules are obtained after the above samples pass the 30 target quasi sieve,and the drug loading of the pellets is about 30%.In this chapter,through single factor experiment,the dissolution test in vitro,sensory evaluation,sedimentation test were used as the main indicators to screen out the best prescription and the best preparation process.(3)Characterization and Properties evaluation of clarithromycin taste-masking granules.Observe the particle size of the drug through electron microscopy,X-ray powder diffraction to observe the crystal form of the drug,differential scanning calorimetry(DSC)to determine the melting point of the drug and the glass transition temperature of the pharmaceutical excipient,and infrared spectroscopy to determine the bonding relationship between the APIs and the excipient,volunteers made a sensory evaluation of the drug.The results show that the resin has been evenly distributed on the surface of the clarithromycin pellets,forming an effective coating layer.The product has a good taste masking effect and good in vitro release,which has certain reference significance for clinical use and industrial production. |
PDF Full Text Request