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Reported in the literature tanshinone Ⅱ A (Tanshinone Ⅱ A, TS) has significant anti-anoxia, anti-tumor, anti-ischemic and antithrombotic pharmacological effects and low toxicity. However, because of its poor water solubility, low bioavailability, limiting its widespread application. Improve its efficacy in order to improve its solubility, sulfonated made of a water-soluble derivative of tanshinone Ⅱ A sulfonate (Sodium tanshinone Ⅱ A sulfonate, STS), the current clinical application of STS injection. However, due to the impact of today's eating habits, the average high intake of sodium ions, lead to high blood pressure, then induced cardiovascular and cerebrovascular diseases, the appropriate supplemental potassium can help prevent high blood pressure, beneficial to human health, therefore, this The papers were synthesized by chemical means Tanshinone Ⅱ A sulfonic acid potassium (Potassium Tanshinone Ⅱ A Sulfonate, PTS), to play the dual role of the TS and potassium ions to provide a new drug for treatment of heart cerebrovascular disease clinical. First, using the semi-synthetic method, TS is the precursor, by sulfonation reaction, the synthesis can be obtained PTS crude purified by recrystallization method using methanol a PTS the crude product, obtained with a purity> 98% of a red needle-like crystals, yield about 10% Second, the establishment of the PTS in vitro analysis (UV and HPLC) method, the precision of the method, the recovery rate of compliance; examine some of its physical and chemical properties and stability among the different media; The results showed that the PTS solubility in methanol to 8.11 mg / ml, PTS decrease in stability in the medium of pH greater than 6. To mannitol as Lyoprotectant, prepared by freeze-drying injection PTS formability, good complex insoluble; drug with 5% glucose compatibility is more stable; stored in the dark at room temperature under the conditions of the basic stability of 3 months. IV hypoxia tolerance in mice with acute cerebral ischemia and rat cortical neurons against hypoxia model, examine the pharmacological effects of PTS-injection against cerebral ischemia and hypoxia, also investigated the drug dose and the dose the toxic effects of the drug on mice; research results show that PTS cerebral ischemia and hypoxia and hypoxia-induced rat cortical neurons have a protective effect, no toxic effects of the drug in the maximum dose. 5, three different doses by intravenous injection using the PTS and the injection of the reference formulation STS, while orally administered high doses of PTS and STS The results show that the PTS in vivo metabolism and elimination are very rapid, in the 10mg/kg and 20mg / kg dose range, eliminating the linear kinetics, non-linear dynamics in the high dose of 50mg/kg. The rats orally administered PTS and STS (50mg/kg dose), was not detected in the plasma drug, indicating that the poor bioavailability of drugs orally. After intravenous PTS in rats mainly unchanged drug metabolites. The clinical treatment after the study is to provide the basis for a new drug for treatment of heart cerebrovascular disease clinical.
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