Study Of Duloxetine Hydrochloride Enteric-coated Tablets

Duloxetine hydrochloride is a new generation of antidepressants,belongs to serotonin and norepinephrine reuptake inhibitors.It is mainly used for the treatment of severe depression,generalized anxiety disorder.Currently,the types of Duloxetine hydrochloride are mainly enteric-coated tablets and enteric-coated capsules,enteric-type solution can effectively avoid the stimulation of gastric epithelial cells and injury,with delayed release effect.Because of good safety and well tolerated,effective and less side effects,Duloxetine hydrochloride has great potential in the market.In this study,Duloxetine hydrochloride enteric-coated tablets were prepared by wet granulation and tablet coating.Base on In vitro release curve similarity factor of commercial preparation and homemade preparation as the evaluation index,To carry out experimental exploration and optimization.The optimized prescription: main drug content in Duloxetine hydrochloride was 20 mg,the average particle size of the drug substance was 50 μm,fillers Lactose consumption was 71.32 %,microcrystalline cellulose dosage was 15.02 %,the percentage of povidone 90 F as adhesive was 1.50 %,the percentage of cross-linked povidone as disintegrants was3.00 %,the percentage of magnesium stearate as lubricant was 0.75 %,isolation layer coating weight gained 5 %,enteric coating layer gained 8 %.Preparation Process: 20 mins of raw material premix time,60 mins of particle drying time,drying temperature: 55 ℃,20 mins of total mixing time,7~9kg of tablet hardness,isolation layer coating temperature:32±2 ℃,enteric coating temperature: 28±2 ℃.The content of duloxetine hydrochloride enteric-coated tablets was determined by high performance liquid chromatography,result showed that the concentration of duloxetine hydrochloride was linear in the range of 2.24 μg / mL ~ 13.44 μg / mL;RSD of precision,repeatability,accuracy,stability,durability test were less than 2.0 %,chromatographic conditions: Agela ODS-2 Chromatography Column(4.6×250 mm,5 μm),Detection wavelength 230 nm,using Acetonitrile(58:42),Phosphate buffer solution,with ph5.5 as mobile phase,column temperature:40 ℃,Flow rate: 1.2 mL/min,volume of sample injection: 20 μL,The method can effectively control the product content.A method of ultraviolet-visible spectrophotometry was used to determine the dissolution of Duloxetine hydrochloride enteric-coated tablets,result showed that the concentration of duloxetine hydrochloride was linear in the range of 2 μg/mL~7 μg/mL,RSD of precision,stability and accuracy were less than 2.0 %,which can be used for the detection of dissolution.The result of quality test of homemade Duloxetine hydrochloride enteric-coated tablets showed that tablet appearance,tablet weight difference,hardness,fragility,moisture and other indicators all meet the requirements listed in "Chinese Pharmacopoeia"(2015 Edition).The content of Duloxetine hydrochloride,content uniformity,dissolution,results of relevant substances test in homemade tablets all meet requirements of Duloxetine hydrochloride enteric-coated tablets(YBH25082O06).The f2 similarity factor reachs 75 between the comparison with commercial preparations,Duloxetine hydrochloride enteric-coated tablets,produced by Shanghai Chinese and Western Pharmaceutical Co.,Ltd in In vitro release curve,showing a good In vitro release characteristic.