Study On The Formulation Optimization And Quality Standard For The Dispersible Tablets Of Total Flavones From Bauhinia Championii(Benth.) Benth.

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. has the function of dispelling theumatism and promoting flow of qi-blood circulation. It is usually used to treat rheumatism injury, stroke hemiplegia, the diagnosis pain, injuries, ect. A large number of studies have shown that the flavones are the active ingredients for anti-inflammatory analgesic and the treatment of rheumatoid arthritis from Bauhinia championii(Benth.) Benth. herb. The dispersible tablets of total flavones from Bauhinia championii(Benth.) Benth. were combined the total flavones from Bauhinia championii(Benth.) Benth. with some appropriate auxiliary materials. The study aim at reducing the drug dose, improve drug bioavailability, which could provide experimental basis for quality standard of the total flavones from Bauhinia Chaampionii(Benth.) Benth. dispersible tablet. Methods:① The knee osteoarthritis model was setd up by qualified SD rats, with inflammatory biomarkers such as joint diameter, digit volume as the basis of anti-inflammatory effects. Studied the anti-inflammatory effects of different concentrations of ethanol extractfrom from Bauhinia chaampionii(Benth.) Benth. on knee osteoarthritis model in rats and determined the optimum concentration of ethanol extract by pharmacodynamics tracking test. Separated Bauhinia chaampionii(Benth.) Benth. herbs by silica gel column chromatography to get the total flavones. ② The content of 3’,4’-methy Lenedioxy-5’,5,6,7-tetramethoxyflavone and 3’,4’,5’,5,7-pentamethoxyf Lavone in total flavones from Bauhinia chaampionii(Benth.) Benth. was measured by RP-HPLC method. ③ By using single-factor test, investigating the accessories for the dispersible tablets of the total flavones from Bauhinia championii(Benth.) Benth. can be pressed, molding, the influence of the dispersion uniformity and disintegration time limit, selecting appropriate filler, disintegratnts, join way of disintegratnts, wetting agent, lubricant. Choosing the influential factors for investigation, using disintegration time and dispersion uniformity as index, through central composite design and response surface methoclology to optimize prescription craft of the total flavones from Bauhinia championii(Benth.) Benth. dispersible tablets. ④ The quality standard was developed according to Chinese pharmacopoeia 2010 edition of the general principles of the preparation of dispersible tablets under(appendixⅠD). TLC was carried out to identify the true and false of dispersible tablets. To determinate the content of two known components as 3’,4’-methy Lenedioxy-5’,5,6,7-tetramethoxyflavone and 3’,4’,5’,5,7-pentamethoxyf Lavone by RP- HPLC method. To develop the quality standard for the dispersible tablets of total flavones from Bauhinia championii(Benth.) Benth.. Results: ① The knee osteoarthritis model was setd up by rats whose knee joint cavity injection concentration of 1 mg/m L iodine sodium acetate solution, and the injection volume of 0.1 m L/only. This method was simple and the inflammation index change significantly, which was convenient for observation. The 70 % ethanol extract of Bauhinia chaampionii(Benth.) Benth. had the best anti-inflammatory effect, and the method used the solvent system in dichloromethane / ethyl acetate(8/1 to 4/1) gradient to isolate the total flavones from Bauhinia chaampionii(Benth.) Benth. herbs was feasible. ② The content of 3’,4’-methy Lenedioxy-5’,5,6,7-tetramethoxyflavone was 21.3 % and the content of 3’,4’,5’,5,7-pentamethoxyf Lavone was 46.7 % in the total flavones from Bauhinia chaampionii(Benth.) Benth. herb. ③ The formulation technology for the dispersible tablet of total flavones from Bauhinia Chaampionii(Benth.) Benth. was optimized by single factor experiment and central composite design and response surface method, with the appearance of the character, tablets differences or disintegration time as index, and the optimal formulation technology consisted of total flavones 6.6 %, Lactose 18.4 %, MCC 64.0 %, CMS-Na 10.0 %, talcum powder 1 %, disintegrant to join in addition, wetting agent of 90 % ethanol. ④ The assessments of weight difference, disperse uniformity, disintegration time and accumulative dissolution were within the rules. The disintegration time was 31.2 s, and the accumulative dissolution in vitro was 30 min reaching 70 % and meet the requirements of quick release. The TLC test was positive. The content of 3’,4’-methy Lenedioxy-5’,5,6,7-tetramethoxyflavone in each tablet was 4.23 mg and the content of 3’,4’,5’,5,7-pentamethoxyf Lavone in each tablet was 8.89 mg. Conclusions: ① The total flavones from Bauhinia championii Bauhinia championii(Benth.) Benth. have strong anti-inflammatory effect on the knee osteoarthritis model of rats, which have good prospects for clinical application.② The optimal technology optimized by single factor experiment and central composite design and response surface method was stable and feasible, which could reach the requirement of rapid disintegration. ③ Established the quality standards for the dispersible tablets of total flavones from Bauhinia championii(Benth.) Benth., which could provide experimental basis for quality standard of the dispersible tablets of total flavones from Bauhinia championii(Benth.) Benth..