Study Of The Breviscapine Solid Dispersions Sustained-released Capsule

Brevescapine was a kind of flavone, extracted from Erigeron breviscapus (Van.)H.-M. of feverfew. Brevescapine possessed the efficacy of promoting blood circulation, dispersing blood stasis, and dredging collateral to stop pain. Brevescapine was a weak acid with low oil/ water distribution coefficient, short half-life, soluble in alkaline solution and insoluble in water nor organic solvent. Therefore, it was necessary to develop a sustained-release dosage form with good bioavailability and stable efficacy to permit reduction in the frequency of brevescapine administration. Sustained release solid dispersions capsule have been investigated using ethylcellulose(EC) as carriers and sparingly water-soluble breviscapine as a model drug.The physicochemical properties of breviscapin were investigated, which were connected closely with pharmacertic form design. The study on solubility showed that the equilibrium solubility in distilled water, phosphate buffer in different pH respectively. apparent oil-water partition coefficient in the system of n-octyl alcohol and water was relatively was relatively highe in acid environment.Methods of content assay and in-vitro release test (spectrophotography) and relative substances detection (HPLC) were respectively carried out. All methods had good linearity, sufficient recovery and good accuracy . Brevescapine sustained-release capsule contain enhancer was prepared. and the drugrelease behavior and characteristic were investigated. Single factor experiment design was employed to optimize the best formulation using the drug-releasing rate from sustained-release capsule as target parameter. The curve of cumulative drug release was accorded with the Higuchi equation.With the best formulation selected, we made some batches of Brevescapine and carried out the accelerated testing and long-term testing. Results showed that those batches didn't make conspicuous changes in 6 months.A reversed-phase HPLC method was developed for determination of breviscapine in Beagle dog's plasma. Breviscapine conventional capsule was used as a comparison to study...