Study On Technology Of Increasing Solubility Of Paeonol And Preparation And Quality Evaluaticn Of Roses Buccal Tablets

Paeonol is the main effective components of peony from Paeonia in Ranunculaceae, and cynanchum paniculatum from Asclepiadaceae. But for its insoluble in the water, it’s hard to be made into preparations. Rose is the dry flower bud of rose from Rosaceae; it’s called KIZIL GUL in Uyghur. Whereas rose has wide range of pharmacological activity, its dosage form is relatively single on the market. In this paper, we improved paeonol’s Solubility to ameliorate the problem of druggability by changed its size; Made rose to be drug directly, and made the relative quality evaluation to enrich its dosage form.HPLC method was used to test the equilibrium solubility and dissolving characteristic of Paeonol, and to investigate the relations between the solubility of paeonol and solute, grain size, solubilization and pH value. Paeonol was proved to belong to the category of very slightly soluble in the water, and its dissolve characteristics in the water was a process of rise, reduce and rise again with time. Particle size reduction can significantly speed up the dissolution rate. With the reduced of the pH value, the solubility of paeonol was increased. Paeonol is soluble very slightly in the water, and it needs about12hours to get dissolve balance for its slowly dissolution velocity. pH value can be adjusted to improve the solubility of paeonol. The dissolution velocity of paeonol has a distinct increase after made into Nano micro powder. As a technology of increasing dissolution rate, the micronization of Paeonol can be used in new dosage form design.We prepare paeonol nanoparticles by hydro method preparation, and then determine its micro morphology, particle size and distribute and pharmacokinetic in miceits of paeonol nanoparticles. The average size of paeonol nanoparticles particles is reduced to281.3nm, which smaller than phenol raw materials. It states by pharmacokinetics:The Tmax of ig paeonol, ig nanoparticles were180min and15min, AUC0-∞of ig paeonol, ig nanoparticles were177809.76mg·L-1·min-1and615859.449mg·L-1-min-1. The paeonol dissolution rate and bioavailability in rats can be effectively increased with nano-grinding technology.To assess the method to determine total polyphenol content of Roses with UV and the contrast of different varieties of total polyphenol of Roses. We use Gallic acid as reference to draw the standard curve, and then to determination repeatability, precision, stability, plus sample recovery. The order of the total polyphenol content (from higher to lower) was Pingyin roses (56.80mg·g-1), Miaofengshan roses (41.09mg·g-1), Kushui roses (40.03mg·g-1), Hetian roses(24.51mg·g-1), Hei Longjiang Yichun(22.40mg·g-1). The method of UV-visible spectrophotometry to determine total polyphenol content of rose is simple, accurate, reproducible, and it can be widely used.Determine the Rose buccal tablet formulation design and do related quality evaluation.