Pharmacokinetic Studies On Lamivudine And Protocatechuic Acid And The Study Of Tablet Prescription

Lamivudine is a nucleoside drug for anti-HBV treatment. It has a rapid and marked inhibition to HBV DNA,and has a significant improvement to liver function. Protocatechuic acid is a water-soluble phenolic constituents. It has a obvious effect on anti-hepatitis B virus. After the study of pharmacodynamics and pharmacology for amivudine and protocatechuic acid,Our laboratory found that protocatechuic acid and lamivudine have obvious pharmacodynamics synergy on anti-DHBV when combined with each other, and it has greater protection on liver cells injured by HBV.Based on Earlier research of the lab, pharmacokinetic study and tablet formulation technology of his drug combination was researched in this paper:After giving a oral administration of different doses of lamivudine and protocatechuic respectively acid, blood was collected at different time points,The content of lamivudine and protcatechuic acid in rat plasma was determined by HPLC method. The results indicated:lamivudine and protocatechuic acid is linear dynamic in the dose within 40 mg/kg and 80 mg/kg. When the dosage is too high, PA absorption half-life extended.By the detection of dissolution curves and other different properties, we filter out the best types of prescription materials:Microcrystalline cellulose as diluen, CMS-NA as disintegrants,pvp as adhesives,Magnesium stearate as lubricants. Crumbling degrees as the index, the dosage of excipien was optimized through orthogonal design,the preparation procedure of the tablet was established finally:mix 3TC(22.5g) with PA (22.5g),MCC (48g),CMS-NA (7%) and PVP (6%), stir it with 90% ethanol(1%pvp).Dry it and then add Magnesium stearate 0.45g and mix it,and then tablet was pressed.The tablet disintegrates rapidly.It has moderate hardnes,accuracy dose and good dissolution uniformity.The preparation is simple and feasible.