| Objective:Bauhinia championii(Benth.) Benth. is the plant from leguminous of the genus sheep hoof nail, its medicinal part is the dry stem. Bauhinia championii(Benth.)Benth. mainly distributed at Guang Dong, Guang Xi, Fu Jian provinces and so on. It has good function of dispelling theumatism and promoting flow of qi-blood circulation.According to plenty of researches, the main efficacy components of Bauhinia championii(Benth.) Benth. were flavonoids, saponins and carbohydrate components. Total flavonoids from Bauhinia championii(Benth.)Benth. has good function on anti-inflammatory analgesic. The study aim at determining the equilibrium solubility and apparent oil-water partition coefficient of total flavonoids from Bauhinia championii(Benth.)Benth. and5,7,3’,4’,5’-pentamethoxyflavon in different pH phosphate buffer solution; investigating the pharmacokinetic behavior which were orally treated with total flavonoids from Bauhinia championii(Benth.)Benth. and 5,7,3’,4’,5’-pentamethoxyflavon. In order to study the equilibrium solubility and the liposolubility, the absorption in rats and provide a basis for new formulations designing of 5,7,3’,4’,5’-pentamethoxyflavon, so as to provide a basis for further research of Bauhinia championii(Benth.)Benth..Methods:(1) The ethyl acetate extracts of Bauhinia championii(Benth.)Benth. was used the 70% ethanol to extract Bauhinia championii(Benth.)Benth. and then the total flavonoids from Bauhinia championii(Benth.)Benth. and 5,7,3’,4’,5’-pentamethoxyflavon were separated by silica gel column chromatography and gel column chromatography.(2) A high performance liquid chromatography method was established and used to detect the concentration in water and different pH phosphate buffer solution of 5,7,3’,4’,5’-pentame-thoxyflavon and 5,7,3’,4’,5’- pentamethoxyflavon at total flavonoids; the oil-water partition coefficient for the n-octanol-water/buffer solution systems of 5,7,3’,4’,5’-pentamethoxyflavon and 5,7,3’,4’,5’-pentamethoxyflavon at total flavonoids were determined by shaking flask method.(3) Qualified SD rats were used as experimental animals, which were orally treated with total flavonoids from Bauhinia championii(Benth.)Benth.(the dose was 60mg/kg) and 5,7,3’,4’,5’- pentamethoxyflavon(the dose was 113 mg/kg,). The concentration of 5,7,3’,4’,5’-pentamethoxyflavon in plasma was determined by HPLC. The pharmacokinetic parameters were calculated with DAS 2.0 program.Results:(1) The total flavonoids from Bauhinia championii(Benth.)Benth.(The quality fraction of 5,7,3’,4’,5’-pentamethoxyflavon was 24.0 %, The quality fraction of 5,6,7,5′-tetramethoxy- 3′,4′-methylendioxyflavone was 14.6%, The quality fraction of 5,6,7,3′,4′,5′-hexamethoxyflavone was 28.0%, The quality fraction of the three flavonoids was66.6%) and 5,7,3’,4’,5’- pentamethoxyflavon( determining by area normalization, The quality fraction of 5,7,3’,4’,5’-pentamethoxyflavon was 97.0%) after extracted.(2) The equilibrium solubility of 5,7,3’,4’,5’-pentamethoxyflavon was 0.603 μg/mL in water at 37℃and the pH of buffer solution had no influence on its equilibrium solubility. The oil-water partition coefficient of the total flavonoids from Bauhinia championii(Benth.)Benth. was77.678 μg/mL in water at 37℃. The oil-water partition coefficient of 5,7,3’,4’,5’-pentamethoxyflavon was 246.24( lg Papp = 2.39) and 5,7,3’,4’,5’-pentamethoxyflavon at total flavonoids was 257.51( lg Papp = 2.41). The pH of buffer solution and other ingredients in total flavoniods had no influence on its oil-water partition coefficient.(3) Metabolic processes of total flavonoids from Bauhinia championii(Benth.)Benth. and 5,7,3’,4’,5’-pentamethoxyflavon were fit with single compartment model after intragastric administration.The main pharmacokinetic parameters of 5,7,3’,4’,5’-pentamethoxyflavon were: Cmax=Conclusions:(1) Gain total flavonoids from Bauhinia championii(Benth.)Benth. and5,7,3’,4’,5’-pentamethoxyflavon by extraction and separation.(2)The studies showed that5,7,3’,4’,5’-pentamethoxyflavon was almost insoluble and the other ingredients in total flavonoids could increase the solubility of 5,7,3’,4’,5’-pentamethoxyflavon in water. The logarithm of oil-water partition coefficient of 5,7,3’,4’,5’-pentamethoxyflavon and 5,7,3’,4’,5’-pentamethoxyflavon in total flavonoids from Bauhinia Championii(Benth.) Benth.were between 1 and 3, which prompt that 5,7,3’,4’,5’-pentamethoxyflavon could get a good absorption in gastrointestinal system.(3) The Cmax was higher; the absorption rate constant was bigger; the Tmax was shorter when administered small dose of total flavonoids from Bauhinia championii(Benth.)Benth. was compared with administered big dose of monomer.Other ingredients of total flavonoids from Bauhinia championii(Benth.)Benth. can promote the absorption and change the distribution of 5,7,3’,4’,5’-pentamethoxyflavon. |
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