Research On The Pharmacokinetics Of Loureirin A Of Sanguis Draconis

Sanguis Draconis is mainly made of the ethanol extractive of resin or fruits from deamonorops draco BL. and Dracaena Cochinchinensis (Lour.)S. C. Chen, originated from more than 20 kinds of plants which belong to 4 branches 5 categories. It has more than 1500 years in its application as precious traditional herb. Sanguis Draconis made in China developed from 1971. It establishes the foundation of nationalization of traditional Chinese herb, Sanguis Draconis. Domestic and import Sanguis Draconis distinguish in chemical constituents, but their medical activities are similar, including quickening the blood and transforming stasis, detumenscen and relieving pain, constringency and stanch bleeding. At present, Sanguis Draconis made in China makes better healing efficacy in angiocardiopathy.Study on pharmacokinetics of Loureirin A f Sanguis Draconis. The metabolism of Loureirin A in rats after oral administration,with the parameters of pharmacokinetics calculated with DAS pharmacokinetics program. After ig. Loureirin A in rats, the concentration in tissues was determined by HPLC.The main contents can be summarized as follows:1 IntroductionSummarized advances in studies on pharmacognosy, chemical constituents, pharmacological action and pharmacokinetics of Loureirin A of Sanguis Draconis.2 Determination of blood protein binding rate of Loureirin AThe blood protein binding rate of Loureirin A of rats and human were determined. The equilibrium dialysis combined with HPLC to determine the blood concentration and blood protein binding rate of Loureirin A was carried out. The blood protein binding rates of Loureirin A at low, middle and high concentration were 79.5%, 80.7% and 80.3% respectively.3 Research on the pharmacokinetics of Loureirin A in rats To establish a RP—HPLC method for the determination of Loureirin A in rat blood for pharmacokinetics study after a single dose of Dracaena cochinehinesis(Lour.)S.C.Chen in rats. The samples were mixed with acetonitrile and ethyl acetate. The organic layer separated was blown to dry and dissolved reconstituted in methanol.The HPLC separation was perform ed on a Cl8 column and the UV detector wavelength was set at 280 nm.The blood samples were analyzed after an oral administration of Dracaena cochinehinesis(Lour.)S.C.Chen to rats (2.5g·kg^-1 ),the pharmacokinetic parameters were valuated by DAS software.Good linearities of Loureirin A was obtained over the range of 0.051～4.836μg·mL^-1 in blood.The recoveries of Loureirin A was over 80%.The precisions of intra-day and inter—day were all less than 8%.The main pharmacokinetics parameters were as follows:Ka of Loureirin A was 2.09h^-1; t_1/2(Ka) 0.33h and Ke was 0.32h-1 t_1/2(Ke) 2.19h;tmax was 2.06h;Cmax 0.64μg·mL^-1 and AUC 2.08μg·mL^-1·h. The method is sensitive,accurate and reproducible,and can be applied to the Loureirin A in blood.The sharmacokinetics characteristics showed Loureirin A was absorbed rapidly and eliminated soon.Study on the tissue distribution of Loureirin A in rats. After ig. administration of Loureirin A at does of 250mg/100g in rats, the tissue concentrations at different time points were determined by HPLC.After ig. administration, the main tissue distribution of Loureirin A concentrations in the liver and kidney were the highest and those in the spleen,heart,lung,brain,stomach,fat and muscle decreased sequentially.4 Research on the pharmacokinetics of Loureirin A in dogs To establish a RP—HPLC method for the determination of Loureirin A in dogs'blood for pharmacokinetics study after a single dose of Dracaena cochinehinesis(Lour.)S.C.Chen . The samples were mixed with acetonitrile and ethyl acetate. The organic layer separated was blown to dry and dissolved reconstituted in methanol.The HPLC separation was performed on a C₁₈ column and the UV detector wavelength was set at 280 nm. The blood samples were analyzed after an oral administration of Dracaena cochinehinesis(Lour.)S.C.Chen to dogs (0.25g·kg^-1 ),the pharmacokinetic parameters were valuated by DAS software.Good linearities of Loureirin A was obtained over the range of Good linearities of Loureirin A was obtained over the range of 0.025～2.05μg·mL^-1 in blood.The recoveries of Loureirin A was over 80%.The precisions of intra-day and inter—day were all less than 10%.The main pharmacokinetics parameters were as follows Ka of Loureirin A was0.47h^-1; t_1/2(Ka) was 1.49h and t_1/2(Ke) was 1.86h; Ke was 0.37 h^-1;tmax was 3.00h;Cmax 0.18μg·mL^-1 and AUC 1.07μg·mL^-1h. CONCLUSION The method is sensitive,accurate and reproducible,and can be applied to the Loureirin A in blood.The sharmacokinetics characteristics showed Loureirin A was absorbed and eliminated slowly in dogs.