目的:研究千金子制霜前后提取物中主要二萜酯类化学成分千金子素L1、千金子素L2、千金子素L3在大鼠肠道的吸收特性差异。方法:用大鼠在体肠灌流模型,采用高效液相色谱法分别测定千金子制霜前后提取物中主要二萜酯类成分的浓度。结果:千金子素L1、千金子素L2和千金子素L3在大鼠各肠段的吸收速率常数(Ka)依次分别为千金子生品提取物中(19.81±0.24)-(26.89±1.01)、(15.79±1.70)-(24.03±2.60)、(19.37±2.14)-(26.66±1.33),千金子霜品提取物中(15.38±1.27)-(21.92±3.74)、(9.67±1.01)-(17.51±2.35)、(14.56±0.93)-(22.31±2.29);千金子素L1、千金子素L2和千金子素L3在大鼠各肠段的药物表观渗透系数(Papp)依次分别为在千金子生品提取物中(2.36±0.23)-(3.10±0.11)、(1.84±0.30)-(2.51±0.35)、(2.32±0.20)-(2.87±0.24),千金子霜品提取物中(1.74±0.18)-(2.55±0.51)、(0.99±0.22)-(1.58±0.14)、(1.62±0.20)-(2.15±0.14)。千金子生品提取物中上述3成分的Ka、Papp值大于千金子霜品提取物的相应成分的Ka、Papp值。结论:千金子制霜前后提取物中主要二萜醇酯类成分千金子素L1、千金子素L2、千金子素L3在整个肠段吸收均较好,制霜可以显著减少千金子素L1、千金子素L2、千金子素L3的吸收,进一步揭示了千金子制霜减毒的作用机理。
Objective : To study the differences of rat intestinal absorption trait of the main diterpenoid ester components Euphorbia factor Ll, Euphorbia factor L2, Euphorbia factor L3 in Semen Euphorbiae and Semen Euphorbiae Pulveratun extract. Methods : The absorption of Euphorbia factor LI, Euphorbia factor L2, Euphorbia factor L3 in small intestine ( duodenum, jejunum and ileum ) and colon of rats were investigated using in situ single-pass perfusion method and the drug content was measured by HPLC. Results : The absorption rate constants ( Ka ) of Euphorbia factor Lj, Euphorbia factor L2, Euphorbia factor L3 in Semen Euphorbiae extract were at the range of ( 19.81 ± 0.24 ) - ( 26.89 ± 1.01 ), ( 15.79 ± 1.70 ) - ( 24.03 ± 2.60 ), ( 19.37 ± 2.14 ) - ( 26.66 ± 1.33 ); K,, of Euphorbia factor Li, Euphorbia factor L2, Euphorbia factor L3 in Semen Euphorbiae Pulveratun extract were at the range of( 15.38 ± 1.27 )-( 21.92 ± 3.74 ), ( 9.67 ± 1.01 ) - ( 17.51 ± 2.35 ), ( 14.56 ± 0.93 ) - ( 22.31 ± 2.29 ); and apparent permeability coefficient ( Paw ) of Euphorbia factor LI, Euphorbia factor L2, Euphorbia factor L3 in Semen Euphorbiae extract were at the range of ( 2.36 ± 0.23 )- ( 3.10 ± 0.11 ), ( 1.84± 0.30 )- ( 2.51 ± 0.35 ), ( 2.32 ± 0.20 ) - ( 2.87 ± 0.24 ); Pavp of Euphorbia factor LI, Euphorbia factor L2, Euphorbia factor L3 in Semen Euphorbiae Pulveratun extract were at the range of( 1.74 ± 0.18 )-( 2.55 ± 0.51 ),( 0.99 ± 0.22 )- ( 1.58 ± 0.14 ), ( 1.62 ± 0.20 ) - ( 2.15 ± 0.14 ). Ka and Papp of these three constituents in Semen Euphorbiae extract were more than Semen Euphorbiae Pulveratun extract. Conclusion : These three constituents in raw and processed Semen Euphorbiae extract can be absorbed in the whole intestinal segments and they absorbed are less in Semen Euphorbiae Pulveratun extract. The paper is to further reveal mechanism of the attenuation after processing of Semen Eup