| This study on the ultra-fine and fine of Houttuynia cordata Thunb (HCT) powder involved their histomorphology, extractability and pharmacokinetic characteristics. The fingerprint of the ultra-fine HCT powder was obtained and tablets developed. The results provided the fundamental information for further food and medicinal applications of HCT pulverization technology and product development.The HCT powder products were examined under light microscope ((?)), as well as scanning electron microscope (SEM) to compare their histomorphology, particle size, porosity and specific surface area. The results showed that the histological particles in the ultra-fine HCT were spherical in shape, smaller and more uniform in size than its fine powder counterpart. Furthermore, the histomorphological characteristics of the two HCT powder products were remarkably different as observed under the magnifications (i.e., 750X and 1, 000．X). The fine HCT showed a large quantity of cell flocks with the cell wall largely intact, while the ultra-fine product's cell wall broken rate reached 95．61%.The high-performance liquid chromatography (HPLC) was used to determine the extractability of the functional components, such as flavonoids, in the ultra-fine and fine HCT made of HCT harvested at Fujian GAP. (1) HPLC analysis was performed using a Shimadzu C18 (250mm×4．6mm, 5μm). the mobile phase consisted of two components, CH3CN and 1% CH3COOH in the volumetric ratio of 16: 84, the flow-rate was 1．0 ml/min and the detection wavelength 360nm. The results indicated that the ultra-fine pulverization could increase the extraction rates of hyperin and quercitrin. As compared to the conventional fine HCT powder, the extraction rates of hyperin and quercitrin from the ultra-fine powder increased by 35．45% and 40．21%, respectively. (2) The gas chromatography (GC) was used to conduct essential oil extraction comparison tests between the two products. The column used was HP-15 (30m×320μm, 0．25μm), the carrier gas was nitrogen with split ratio of 1: 50, the injector temperature was 200℃, the detector temperature was 250℃, and the column temperature was programmed in the determination. The results showed that the ultra-fine pulverization also increased the extractability of methyl-n-nonylketon by 68．03% over that of the fine powder.The HPLC method was employed to investigate the HCT products' pharmacokineticcal effects on rabbits. Using the PSK Version 1．0 software, the data of plasma concentration-time curves on hyperin and quercitrin for the ultra-fine and fine HCT powder products were compared for their pharmacokinctical characteristics. (1) The best pharmacokinetic models of hyperin for both products were one-compartment open model. The major pharmacokinctical parameters for the ultra-fine powder were: A ( 1．254±0．252) , K (0．020±0．002) , G (1．260±0．247) , Ka( 0．049±0．005) , T1/2k (35．36±4．690) , T1/2ka (14．36±1．300) , CL/F (0．693±0．031) , Vd/F (35．183±2．921) , AUC0-∞(36．140±1．768) , LagTime (0．144±0．232) . Tmax (31．374±0．305) , Cmax (0．383±0．006) . For the fine powder, they were: A (4．528±0．548) , K (2．57E-2±7．55 E-4) , G (4．939±0．544) , Ka (3．31E-2±7．40 E-4) , Tl/2k(27．00±0．08) , Tl/2ka (20．96±0．47) , CL/F (0．945±0．027) , Vd/F (36．767±0．595) , AUC0-∞(26．486±0．757) , LagTime (11．889±0．359) , Tmax (46．116±0．544) , Cmax(0．306±0．002) . The bioavailability of hyperin of the ultra-fine powder was improved 36．45%, as compared with the fine powder. (2) The best pharmacokinetical models of quercitrin for both products were one-compartment open model as well. The major pharmacokinetic parameters for the ultra-fine powder were: A (3．112±0．605) , K (0．012±0．001) , G (3．184±0．614) , Ka (0．034±0．003) , T1/2k (57．480±4．700) , T1/2ka (20．660±1．990) , CL/F (0．126±0．002) , Vd/F (10．474±0．856) , AUC0-∞(158．353±3．106) , LagTime (1．050±0．682) , Tmax (48．482±1．309) , Cmax (1．078±0．040) . The major pharmacokinetic parameters for the fine powder were: A (1．866±0．469) , K( 0．009±0．001 ). G(2．117±0．542) . Ka(0．029±0．005) , Tl/2k (78．380±12．950) , Tl/2ka( 24．230±3．550) , CL/F(0．157±0．008) , Vd/F( 17．579±1．991 ), AUC0-∞(128．034±6．853 ), LagTime ( 6．260±3．122) , Tmax (64．926±2．650) , Cmax (0．678±0．029) . The bioavailability of quercitrin of the ultra-fine powder was improved 23．68% over the fine HCT powder.The HCT fingerprint was established. (1) The fingerprinting of flavonoids in the ultra-fine HCT was established by using HPLC. The chromatographic conditions were as follows: SHIM-PACK VP-C18 column (250mm×4．6mm, 10μm), CHCN-1% HCOOH gradient for the mobile phase, flow rate at 1．0 ml/min and detection wavelength 254nm. The HPLC fingerprint of the ultra-fine HCT had 7 common peaks. (2) The fingerprinting of essential oils in the ultra-fine HCT was established by using HPLC. The chromatographic conditions were: SPDTM-1Capillary Column(30m×0．32mm, 0．25μm), injector temperature at 200℃, flow rate at 1．0 ml/min . nitrogen with split ratio of 50: 1 as carrier gas and column temperature programmed in the determination. The GC fingerprint of the ultra-fine HCTshowed 9 common peaks.By addition of sweetener, acidifier and mallodextrin with the orthogonal experimental design, the ultra-fine HCT powder was made into tablets with an optimized formulation. The tablets were found to have appealing appearance and flavor profile, as well as, uniform composition and long shelf life.
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