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Transport Study of Andrographolide Sulfonate on Cell Models

??OBJECTIVE To establish a method for determination of the total content of andrographolide sulfonate, transport of two kinds of main components in the injection in Calu-3 and Caco-2 cell model, can be applied to the assessment of lung and oral administration to the safety and effectiveness of drugs. METHODS Screening of safe concentration of drugs by cytotoxicity test. Injection of andrographolide total sulfonate in safe concentrationwere applied to Calu-3 and Caco-2 cell models. Samples were taken for a certain period of time to determine the influence of concentration and time on the transport, and the apparent osmotic coefficients of the principal components were calculated. RESULTS When the concentration of the drug was less than 500 ??g??mL^-1, the survival rate of Calu-3 and Caco-2 cells was close to 100%.The established cell model showed excellent compactness and integrity.In the Calu-3 cell model, the apparent permeability coefficients of andrographolide sulfate C and 9-dehydro-17-hydro-andrographolide were 1??10^-5 orders of magnitude.In the Caco-2 cell model, both were 1??10^-6 orders of magnitude.On two cell models, the efflux ratios were less than 2. CONCLUSION The principal component of andrographolide total sulfonate injection is not the substrate for P glycoproteins, it has moderate absorption in the intestine, and has good absorption in the respiratory tract. Pulmonary administration is safer and more effective.