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The Relationship Between Pharmcokinetics And Pharmacodynamics Of The Water-soluble

Posted on:2002-05-18Degree:MasterType:Thesis
Country:ChinaCandidate:Z F YangFull Text:PDF
GTID:2144360032452384Subject:Journal of Clinical Pharmacology
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Using safflor yellow(SY) as the quantiative index, the pharmacokinetical character of the water-soluble of safflower in the normal and blood-stasis animal was studied, We conjugate PK with pharmacodynamics(PD) to study the relationship and inquire the effective substance of safflower.1 The extraction of the water-soluble of safflowerUsing SY as the quantiative index, the effect of different solvents and extraction on the content SY from carthamus tinctorius L. was measured through UV. It was suggested that we could obtain satisfying SY with water and 70 % methanol, while the production would be reduced significantly if using 80 % acetone.2 The PK of the water-soluble extraction of safflower (1) The PK of the water-soluble extraction of safflower in mice Using SY as the quantiative index, we measured theconcentration of SY in the serum at different times after iv the water-soluble extraction of safflower (264. 89 mg ?kg"1 and 26. 84 mg ?kg-1). The concentration-time profiles in mice after iv and both dosages of the water-soluble extraction of safflower were shown to fit a single-compartment open model .Higher dosage.- AUC was 57862. 17 u g ?min ?ml-1, t1/2 was 41. 62 min, ke was 0. 02 rain"1; lower dosage: AUC was 7842. 40 n g ?min ?ml"1, t,/2 was 27. 90 min, ke was 0. 02 min-1. In the higher dosage, the highest level of SY was found in the liver and kidney, while the lesser SY was found in the heart, lung and spleen . The level of SY in brain was hardly found.(2) The PK of the water-soluble extraction of safflower in the normal rats and the acute model rats with blood stasis syndrome. Using SY as the quantiative index, we measured the concentration of SY in the serum at different times after iv the water-soluble extraction of safflower (37. 08 mg ?kg"1) in normal rats and the acute model rats with blood stasis syndrome. The concentration-time data of SY in normal rats was shown to fit a single-compartment open model . ti/2was 66.27 min, AUC was 42266.86n g ?min ?ml/-1. But the concentration-time data of SY in acute model rats with blood stasis syndrome was shown to fit a double-compartment open model . t1/2a was 1. 43 min, ti/Zp was 95. 65 min, AUC was 49632.90 ug ?min ?mL"1. The metabolism of SY was evidently longer in acute model rats with blood stasis syndrome than that of the normal rats.3 The PD of the water-soluble extraction of safflower(1) The effect of the water-soluble extraction of safflower on the torsion times in the menorrhalgia miceSixty female mice weighted 18?2 g. They were sensitized by using diethylstibestro 12 mg ?kg-1 during 12 d(ig).They were randomed into six groups. The water-soluble extraction of safflower (26. 49 mg ?kg-1, 52. 98 mg ?kg-1, 264. 90 mg ?kg"1) , pethidine (50. 00 mg ?kg-1 ) and NS (same bulk) in lld(iv), menorrhalgia model induced by oxytocin in 12 d, and recorded the torsion times in menorrhalgia mice after iv oxytocin in the 30 min. The result showed that compared with the model group, there was markedly different between the model and the animals which were treated with the water-soluble extraction of safflower (26.49 mg ?kg"1; 52. 98 mg ?kg"1) (P<0. 05), There was very markedly different between the model and the animals which were treated with the water-soluble extraction of safflower (264.90 mg ?kg"1 ) (P<0.01). The water-soluble extraction of safflower can inhibit the autonomic contractive activities of mouse uterus .(2) The effects of the water-soluble extraction of safflower on hemorheology and microcirculation in the normal rats and the acute model rats with blood stasis syndromeWe;observed the microcirculation of mesentery and measured the index of hemorheology at appropriate times ( 5, 10, 30, 60, 120, 180,320,480 min ) after iv safflor yellow (37. 08 mg ?kg"1) in control group and the model group. The results showed that it markedlyincreased on the number of net dot and the caliber of arteria, vein in microcirculation and decreased on the n^ r\Pand n f in the normal rats (p<0. 05,vs co...
Keywords/Search Tags:the water-soluble extraction of safflower, safflor yellow, pharmacodynamics, pharmcokinetics, blood stasis syndrome, hemorheology, micocirculation
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