Transport Study of Andrographolide Sulfonate on Cell Models / 中国药学杂志

ABSTRACT

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 μg•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.