Dissolution And Pharmacokinetics Study Of The Components In Ultramicro-Pulverised Powder Of Andrographis Paniculata

Objective:To study the effects of dissolution contents and Pharmacokinetics parameters and the bioavailability in rabbits of the components in ultramicro pulverization of Andrographis paniculata.Pharmacokinetics characteristics in rabbits and piglets were compared after they were administered with ultramicro-pulverised powder to provide useful reference and scientific testify for the clinical application of the ultramicro-pulverised powder of Andrographis paniculata in rabbits and piglets.Metheds:1.The Andrographis paniculata was made into ordinary powder and ultramicro-pulverised powder.High performance liquid chromatography(HPLC)was applied to determine the contents of Andrographalide and Dehydroandrographolide from ordinary powder and ultramicro-pulverised powder treated with water and methanol to compare the dissolution differences.2.The plasma concentration of Andrographalide and Dehydroandrographolide was determined by HPLC in two groups of rabbits after they were administered with ultramicro-pulverised powder and with ordinary powder of Andrographis paniculata 2g·Kg^-1·BW dosage by gastrogavage,respectively.The plasma concentration-time data of Andrographalide and Dehydroandrographolide was analyzed by Pharmaceutical Kinetics Software(PKS).Pharmacokinetic parameters and the bioavailabilities in both groups were compared.3.HPLC was applied to determine the plamsa concentrations in rabbits and piglets after they were administered with ultramicro-pulverised powder of Andrographis paniculata 4g·Kg^-1·BW dosage by gastrogavage,respectively. Pharmacokineties parameters and the bioavailabilities in both groups were compared. Results:1.Compared with ordinary powder,the contents of Andrographalide from ultramicro-pulverised powder of Andrographis paniculata raised 30.30%and 92.45% after treated with water and methanol,while the contents of Dehydroandrographolide raised 31.00%and 125.00%.2.Both the concentration-time curves of Andrographalide and Dehydroandrographolide were Confirmed to two compartment model after the rabbits were administered with.the ordinary powder and ultramicro-pulverised powder of Andrographis paniculata 2g·Kg^-1·BW dosage by gastrogavage,respectively. Compared with taking ordinary powder,the Andrographalide's area under concentration-time(AUC)raised 59.86%,the tisne reach the maximum consistency (T_peak)was 7.14 minutes premature,and the maximum consistency(C_max)enlarged 0.60%after the rabbits were administered with ultramicro-pulverised powde;the Dehydrographolide's AUC raised 124.64%,T_peakwas 1.433 minutes premature,and C_maxenlarged 88.34%.3.Both the concentration-time curves of Andrographalide and Dehydroandrographolide were confirmed to two compartment model after the rabbits were administered with ultramicro-pulverised powder of Andrographis paniculata 4g·Kg^-1·BW dosage by gastrogavage,while the two components above were confirmed to one compartment model after the piglets were administered with ultramicro-pulverised powder 4g·Kg^-1·Bw dosage by gastrogavage,respectively. Compared with piglets,the Andrographolide's AUC raised 19.74%,T_peakwas 26 minutes premature,and C_maxenlarged 12.47%after the rabbits were administered with ultramicro-pulverised powder;the Dehydrographolide's AUC raised 2651.10%, T_peakwas 10 minutes premature,and C(max)enlarged 2174.42%. Conclusion:1.The technique of ultromicro-pulverization promotes the dissolution contents of Andrographalide and Dehydroandrographolide of Andrographis paniculata.2.Compared with ordinary powder,the bioavailabilites of Andrographalide and Dehydroandrographolide were higher after the rabbits were administered with ultramicro-pulverised powder of Andrographis paniculata,especially,the bioavailability of Dehydroandrographolide raised obviously.3.The bioavailabilities of Andrographalide and Dehydroandrographolide after the rabbits were administered with ultramicro-pulverised powder were higher than piglet,especially,the bioavailability of Dehydroandrographolide raised obviously.