Studies On The Development Of Naoshuan Kangfu Pills And Alkaloid Extracts In The Leaves Of Uncaria Rhynchophylla (Miq.) Jacks

For the purpose to develop the 8th kinds of new drugs Naoshuan Kangfu Pills on the basis of Chinese preparation ofNaoshuan Kangfu Capsules which can cure cerebral thrombus included in standards compiled by SFDA. For the purpose to offer the evidence of exploitation on the leaves of Uncaria spp, the chemical constituents of the leaves of Uncaria rhynchophylla (Miq.) Jacks were investigated, the preparation technology and Determination of the alkaloid extracts of leaves of Uncaria rhynchophylla (Miq.)Jacks were studied.1. Researched the preparing technology of Naoshuan Kangfu Pills. Equal comparing design was used to study the speed and volume of solvent in percolating technology. The optimal process was studied by orthogonal design and contrast experiment with yield of extract and contents of puerarin as indexes. Four factors were selected in this experiment, including the volume of water, soak time, the duration of extraction and times of extraction. Methods of granulating were studied, excipients were selected, stable and feasible processing technology of Naoshuan Kangfu pill was established.2. Established the quality criterion of Naoshuan Kangfu Pills. On the basis of original standard, improved the identification methods of Sanguis Draconis, Radix Curcumae, Radix Paeoniae, established TLC methods to identify Radix et Rhizoma Notoginseng, Rhizoma Chuanxiong, Flos Carthami. The employed methods were simple and reliable, the spots of TLC chromatograms were clear. A method of HPLC gradient elution determination was established for the assay of deleterious compounds (notoginsenoside R₁, ginsenoside Rg₁ and ginsenoside Rb₁). The solvent system [CH₃CN—H₂O] and Kromasil-C₁₈ column (4.6×200mm, 5μm)were used in the quantitative analysis of notoginsenoside R₁, ginsenoside Rg₁ and Rb₁. The linear ranges were at 0.0126～0.1260mg·mL^-1, 0.0500～0.5000mg·mL^-1 and 0.0392～0.3920mg·mL^-1 respectively (r≥0.9997). This thesis improved the method that determined the content of ginsenoside Rg₁ and added the method which detected notoginsenoside R₁ and ginsenoside Rb₁. The methods employed were accurate, and reliable, they provided modern quality criteria for Naoshuan Kangfu Pills.3. A reversed-phase high performance liquid chromatography(RP-HPLC) method was developed for the assay of rhynchophylline,isorhynchophylline,corynoxeine and isocorynoxeine) and vincoside lactam in extracts of Uncaria spp. The gradient solvent system with 0.05 mol·L^-1 ammonium acetate buffer (pH=5.20) and acetonitrile and ODS reversed-phase column of Kromasil C₁₈ (4.6mm×200mm, 5μm) were used in the quantitative analysis of the 5 marker components. The eluate was monitored at 245nm. The linear ranges of rhynchophylline, corynoxeine, Vincoside lactam, isorhynchophylline and isocorynoxeine were 0.84～13.50 mg·mL^-1, 0.86～27.00 mg·mL^-1, 1.58～50.50 mg·mL^-1, 1.63～52.00 mg·mL^-1 and 1.47～47.00 mg·mL^-1 (r＞0.9995) respectively. The results indicated that the assay methods were rapid and with good reproducibility.4. The preparation technology of the extracts of the leaves of Uncaria rhynchophylla (Miq.) Jacks was studies. with the yield of extract, the contents of marker components and the availability as the review indexes. The 75%EtOH extracts were preparated by percoalting and macraporous adsorption resin were introduced to refine the extracts.